US20220105070A1 - Topical formulations having cannabinoid - Google Patents
Topical formulations having cannabinoid Download PDFInfo
- Publication number
- US20220105070A1 US20220105070A1 US17/420,335 US202017420335A US2022105070A1 US 20220105070 A1 US20220105070 A1 US 20220105070A1 US 202017420335 A US202017420335 A US 202017420335A US 2022105070 A1 US2022105070 A1 US 2022105070A1
- Authority
- US
- United States
- Prior art keywords
- formulation
- cannabinoid
- cannabinoids
- oil
- phyto
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 229930003827 cannabinoid Natural products 0.000 title claims abstract description 107
- 239000003557 cannabinoid Substances 0.000 title claims abstract description 107
- 239000012049 topical pharmaceutical composition Substances 0.000 title claims description 15
- 239000000203 mixture Substances 0.000 claims abstract description 123
- 238000009472 formulation Methods 0.000 claims abstract description 116
- 235000017807 phytochemicals Nutrition 0.000 claims abstract description 30
- 229930000223 plant secondary metabolite Natural products 0.000 claims abstract description 30
- 238000000034 method Methods 0.000 claims abstract description 29
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 27
- 238000010521 absorption reaction Methods 0.000 claims abstract description 8
- 229940065144 cannabinoids Drugs 0.000 claims description 46
- 229960004242 dronabinol Drugs 0.000 claims description 25
- CYQFCXCEBYINGO-IAGOWNOFSA-N delta1-THC Chemical compound C1=C(C)CC[C@H]2C(C)(C)OC3=CC(CCCCC)=CC(O)=C3[C@@H]21 CYQFCXCEBYINGO-IAGOWNOFSA-N 0.000 claims description 23
- CYQFCXCEBYINGO-UHFFFAOYSA-N THC Natural products C1=C(C)CCC2C(C)(C)OC3=CC(CCCCC)=CC(O)=C3C21 CYQFCXCEBYINGO-UHFFFAOYSA-N 0.000 claims description 22
- QHMBSVQNZZTUGM-UHFFFAOYSA-N Trans-Cannabidiol Natural products OC1=CC(CCCCC)=CC(O)=C1C1C(C(C)=C)CCC(C)=C1 QHMBSVQNZZTUGM-UHFFFAOYSA-N 0.000 claims description 20
- QHMBSVQNZZTUGM-ZWKOTPCHSA-N cannabidiol Chemical compound OC1=CC(CCCCC)=CC(O)=C1[C@H]1[C@H](C(C)=C)CCC(C)=C1 QHMBSVQNZZTUGM-ZWKOTPCHSA-N 0.000 claims description 20
- ZTGXAWYVTLUPDT-UHFFFAOYSA-N cannabidiol Natural products OC1=CC(CCCCC)=CC(O)=C1C1C(C(C)=C)CC=C(C)C1 ZTGXAWYVTLUPDT-UHFFFAOYSA-N 0.000 claims description 20
- 229950011318 cannabidiol Drugs 0.000 claims description 20
- PCXRACLQFPRCBB-ZWKOTPCHSA-N dihydrocannabidiol Natural products OC1=CC(CCCCC)=CC(O)=C1[C@H]1[C@H](C(C)C)CCC(C)=C1 PCXRACLQFPRCBB-ZWKOTPCHSA-N 0.000 claims description 20
- UCONUSSAWGCZMV-HZPDHXFCSA-N Delta(9)-tetrahydrocannabinolic acid Chemical compound C([C@H]1C(C)(C)O2)CC(C)=C[C@H]1C1=C2C=C(CCCCC)C(C(O)=O)=C1O UCONUSSAWGCZMV-HZPDHXFCSA-N 0.000 claims description 14
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 238000002156 mixing Methods 0.000 claims description 13
- AAXZFUQLLRMVOG-UHFFFAOYSA-N 2-methyl-2-(4-methylpent-3-enyl)-7-propylchromen-5-ol Chemical compound C1=CC(C)(CCC=C(C)C)OC2=CC(CCC)=CC(O)=C21 AAXZFUQLLRMVOG-UHFFFAOYSA-N 0.000 claims description 12
- 239000000284 extract Substances 0.000 claims description 12
- WVOLTBSCXRRQFR-DLBZAZTESA-N cannabidiolic acid Chemical compound OC1=C(C(O)=O)C(CCCCC)=CC(O)=C1[C@H]1[C@H](C(C)=C)CCC(C)=C1 WVOLTBSCXRRQFR-DLBZAZTESA-N 0.000 claims description 11
- UAHWPYUMFXYFJY-UHFFFAOYSA-N beta-myrcene group Chemical group C=CC(CCC=C(C)C)=C UAHWPYUMFXYFJY-UHFFFAOYSA-N 0.000 claims description 10
- XMGQYMWWDOXHJM-UHFFFAOYSA-N limonene Chemical compound CC(=C)C1CCC(C)=CC1 XMGQYMWWDOXHJM-UHFFFAOYSA-N 0.000 claims description 10
- CDOSHBSSFJOMGT-UHFFFAOYSA-N linalool Chemical compound CC(C)=CCCC(C)(O)C=C CDOSHBSSFJOMGT-UHFFFAOYSA-N 0.000 claims description 10
- 239000003921 oil Substances 0.000 claims description 10
- 235000019198 oils Nutrition 0.000 claims description 10
- NPNUFJAVOOONJE-ZIAGYGMSSA-N β-(E)-Caryophyllene Chemical compound C1CC(C)=CCCC(=C)[C@H]2CC(C)(C)[C@@H]21 NPNUFJAVOOONJE-ZIAGYGMSSA-N 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 9
- FAMPSKZZVDUYOS-UHFFFAOYSA-N 2,6,6,9-tetramethylcycloundeca-1,4,8-triene Chemical compound CC1=CCC(C)(C)C=CCC(C)=CCC1 FAMPSKZZVDUYOS-UHFFFAOYSA-N 0.000 claims description 8
- WVOLTBSCXRRQFR-SJORKVTESA-N Cannabidiolic acid Natural products OC1=C(C(O)=O)C(CCCCC)=CC(O)=C1[C@@H]1[C@@H](C(C)=C)CCC(C)=C1 WVOLTBSCXRRQFR-SJORKVTESA-N 0.000 claims description 8
- 230000000694 effects Effects 0.000 claims description 8
- 208000002193 Pain Diseases 0.000 claims description 7
- 210000003491 skin Anatomy 0.000 claims description 7
- 208000017520 skin disease Diseases 0.000 claims description 7
- 239000002904 solvent Substances 0.000 claims description 7
- RBEAVAMWZAJWOI-MTOHEIAKSA-N (5as,6s,9r,9ar)-6-methyl-3-pentyl-9-prop-1-en-2-yl-7,8,9,9a-tetrahydro-5ah-dibenzofuran-1,6-diol Chemical compound C1=2C(O)=CC(CCCCC)=CC=2O[C@H]2[C@@H]1[C@H](C(C)=C)CC[C@]2(C)O RBEAVAMWZAJWOI-MTOHEIAKSA-N 0.000 claims description 6
- ZROLHBHDLIHEMS-HUUCEWRRSA-N (6ar,10ar)-6,6,9-trimethyl-3-propyl-6a,7,8,10a-tetrahydrobenzo[c]chromen-1-ol Chemical compound C1=C(C)CC[C@H]2C(C)(C)OC3=CC(CCC)=CC(O)=C3[C@@H]21 ZROLHBHDLIHEMS-HUUCEWRRSA-N 0.000 claims description 6
- YJYIDZLGVYOPGU-XNTDXEJSSA-N 2-[(2e)-3,7-dimethylocta-2,6-dienyl]-5-propylbenzene-1,3-diol Chemical compound CCCC1=CC(O)=C(C\C=C(/C)CCC=C(C)C)C(O)=C1 YJYIDZLGVYOPGU-XNTDXEJSSA-N 0.000 claims description 6
- KASVLYINZPAMNS-UHFFFAOYSA-N Cannabigerol monomethylether Natural products CCCCCC1=CC(O)=C(CC=C(C)CCC=C(C)C)C(OC)=C1 KASVLYINZPAMNS-UHFFFAOYSA-N 0.000 claims description 6
- ZROLHBHDLIHEMS-UHFFFAOYSA-N Delta9 tetrahydrocannabivarin Natural products C1=C(C)CCC2C(C)(C)OC3=CC(CCC)=CC(O)=C3C21 ZROLHBHDLIHEMS-UHFFFAOYSA-N 0.000 claims description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 6
- 229920002472 Starch Polymers 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- YJYIDZLGVYOPGU-UHFFFAOYSA-N cannabigeroldivarin Natural products CCCC1=CC(O)=C(CC=C(C)CCC=C(C)C)C(O)=C1 YJYIDZLGVYOPGU-UHFFFAOYSA-N 0.000 claims description 6
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 claims description 6
- NVEQFIOZRFFVFW-RGCMKSIDSA-N caryophyllene oxide Chemical compound C=C1CC[C@H]2O[C@]2(C)CC[C@H]2C(C)(C)C[C@@H]21 NVEQFIOZRFFVFW-RGCMKSIDSA-N 0.000 claims description 6
- QMVPMAAFGQKVCJ-UHFFFAOYSA-N citronellol Chemical compound OCCC(C)CCC=C(C)C QMVPMAAFGQKVCJ-UHFFFAOYSA-N 0.000 claims description 6
- RRAFCDWBNXTKKO-UHFFFAOYSA-N eugenol Chemical compound COC1=CC(CC=C)=CC=C1O RRAFCDWBNXTKKO-UHFFFAOYSA-N 0.000 claims description 6
- 239000007921 spray Substances 0.000 claims description 6
- 150000003505 terpenes Chemical group 0.000 claims description 6
- 235000007586 terpenes Nutrition 0.000 claims description 6
- 239000000341 volatile oil Substances 0.000 claims description 6
- DTGKSKDOIYIVQL-WEDXCCLWSA-N (+)-borneol Chemical compound C1C[C@@]2(C)[C@@H](O)C[C@@H]1C2(C)C DTGKSKDOIYIVQL-WEDXCCLWSA-N 0.000 claims description 5
- REPVLJRCJUVQFA-UHFFFAOYSA-N (-)-isopinocampheol Natural products C1C(O)C(C)C2C(C)(C)C1C2 REPVLJRCJUVQFA-UHFFFAOYSA-N 0.000 claims description 5
- 239000001490 (3R)-3,7-dimethylocta-1,6-dien-3-ol Substances 0.000 claims description 5
- CDOSHBSSFJOMGT-JTQLQIEISA-N (R)-linalool Natural products CC(C)=CCC[C@@](C)(O)C=C CDOSHBSSFJOMGT-JTQLQIEISA-N 0.000 claims description 5
- WEEGYLXZBRQIMU-UHFFFAOYSA-N 1,8-cineole Natural products C1CC2CCC1(C)OC2(C)C WEEGYLXZBRQIMU-UHFFFAOYSA-N 0.000 claims description 5
- NVEQFIOZRFFVFW-UHFFFAOYSA-N 9-epi-beta-caryophyllene oxide Natural products C=C1CCC2OC2(C)CCC2C(C)(C)CC21 NVEQFIOZRFFVFW-UHFFFAOYSA-N 0.000 claims description 5
- WEEGYLXZBRQIMU-WAAGHKOSSA-N Eucalyptol Chemical compound C1C[C@H]2CC[C@]1(C)OC2(C)C WEEGYLXZBRQIMU-WAAGHKOSSA-N 0.000 claims description 5
- 239000000443 aerosol Substances 0.000 claims description 5
- WUOACPNHFRMFPN-UHFFFAOYSA-N alpha-terpineol Chemical compound CC1=CCC(C(C)(C)O)CC1 WUOACPNHFRMFPN-UHFFFAOYSA-N 0.000 claims description 5
- NPNUFJAVOOONJE-UHFFFAOYSA-N beta-cariophyllene Natural products C1CC(C)=CCCC(=C)C2CC(C)(C)C21 NPNUFJAVOOONJE-UHFFFAOYSA-N 0.000 claims description 5
- CKDOCTFBFTVPSN-UHFFFAOYSA-N borneol Natural products C1CC2(C)C(C)CC1C2(C)C CKDOCTFBFTVPSN-UHFFFAOYSA-N 0.000 claims description 5
- 229940116229 borneol Drugs 0.000 claims description 5
- 239000001506 calcium phosphate Substances 0.000 claims description 5
- NPNUFJAVOOONJE-UONOGXRCSA-N caryophyllene Natural products C1CC(C)=CCCC(=C)[C@@H]2CC(C)(C)[C@@H]21 NPNUFJAVOOONJE-UONOGXRCSA-N 0.000 claims description 5
- 229960005233 cineole Drugs 0.000 claims description 5
- SQIFACVGCPWBQZ-UHFFFAOYSA-N delta-terpineol Natural products CC(C)(O)C1CCC(=C)CC1 SQIFACVGCPWBQZ-UHFFFAOYSA-N 0.000 claims description 5
- DTGKSKDOIYIVQL-UHFFFAOYSA-N dl-isoborneol Natural products C1CC2(C)C(O)CC1C2(C)C DTGKSKDOIYIVQL-UHFFFAOYSA-N 0.000 claims description 5
- 235000001510 limonene Nutrition 0.000 claims description 5
- 229940087305 limonene Drugs 0.000 claims description 5
- 229930007744 linalool Natural products 0.000 claims description 5
- 230000001105 regulatory effect Effects 0.000 claims description 5
- 239000008107 starch Substances 0.000 claims description 5
- 235000019698 starch Nutrition 0.000 claims description 5
- 208000024891 symptom Diseases 0.000 claims description 5
- 229940116411 terpineol Drugs 0.000 claims description 5
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims description 4
- IXJXRDCCQRZSDV-GCKMJXCFSA-N (6ar,9r,10as)-6,6,9-trimethyl-3-pentyl-6a,7,8,9,10,10a-hexahydro-6h-1,9-epoxybenzo[c]chromene Chemical compound C1C[C@@H](C(O2)(C)C)[C@@H]3C[C@]1(C)OC1=C3C2=CC(CCCCC)=C1 IXJXRDCCQRZSDV-GCKMJXCFSA-N 0.000 claims description 4
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 4
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 4
- 229920000881 Modified starch Polymers 0.000 claims description 4
- 208000003251 Pruritus Diseases 0.000 claims description 4
- XCPQUQHBVVXMRQ-UHFFFAOYSA-N alpha-Fenchene Natural products C1CC2C(=C)CC1C2(C)C XCPQUQHBVVXMRQ-UHFFFAOYSA-N 0.000 claims description 4
- CRPUJAZIXJMDBK-UHFFFAOYSA-N camphene Chemical compound C1CC2C(=C)C(C)(C)C1C2 CRPUJAZIXJMDBK-UHFFFAOYSA-N 0.000 claims description 4
- BQOFWKZOCNGFEC-UHFFFAOYSA-N carene Chemical compound C1C(C)=CCC2C(C)(C)C12 BQOFWKZOCNGFEC-UHFFFAOYSA-N 0.000 claims description 4
- 239000006071 cream Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 229940041616 menthol Drugs 0.000 claims description 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 4
- 208000028173 post-traumatic stress disease Diseases 0.000 claims description 4
- 239000003381 stabilizer Substances 0.000 claims description 4
- 238000011200 topical administration Methods 0.000 claims description 4
- GRWFGVWFFZKLTI-UHFFFAOYSA-N α-pinene Chemical compound CC1=CCC2C(C)(C)C1C2 GRWFGVWFFZKLTI-UHFFFAOYSA-N 0.000 claims description 4
- CRDAMVZIKSXKFV-FBXUGWQNSA-N (2-cis,6-cis)-farnesol Chemical compound CC(C)=CCC\C(C)=C/CC\C(C)=C/CO CRDAMVZIKSXKFV-FBXUGWQNSA-N 0.000 claims description 3
- 239000000260 (2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ol Substances 0.000 claims description 3
- QMVPMAAFGQKVCJ-SNVBAGLBSA-N (R)-(+)-citronellol Natural products OCC[C@H](C)CCC=C(C)C QMVPMAAFGQKVCJ-SNVBAGLBSA-N 0.000 claims description 3
- KXKOBIRSQLNUPS-UHFFFAOYSA-N 1-hydroxy-6,6,9-trimethyl-3-pentylbenzo[c]chromene-2-carboxylic acid Chemical compound O1C(C)(C)C2=CC=C(C)C=C2C2=C1C=C(CCCCC)C(C(O)=O)=C2O KXKOBIRSQLNUPS-UHFFFAOYSA-N 0.000 claims description 3
- XZEUYTKSAYNYPK-UHFFFAOYSA-N 3beta-29-Norcycloart-24-en-3-ol Natural products C1CC2(C)C(C(CCC=C(C)C)C)CCC2(C)C2CCC3C(C)C(O)CCC33C21C3 XZEUYTKSAYNYPK-UHFFFAOYSA-N 0.000 claims description 3
- 235000019489 Almond oil Nutrition 0.000 claims description 3
- 241000572565 Alpinia oxyphylla Species 0.000 claims description 3
- UVOLYTDXHDXWJU-UHFFFAOYSA-N Cannabichromene Chemical compound C1=CC(C)(CCC=C(C)C)OC2=CC(CCCCC)=CC(O)=C21 UVOLYTDXHDXWJU-UHFFFAOYSA-N 0.000 claims description 3
- REOZWEGFPHTFEI-JKSUJKDBSA-N Cannabidivarin Chemical compound OC1=CC(CCC)=CC(O)=C1[C@H]1[C@H](C(C)=C)CCC(C)=C1 REOZWEGFPHTFEI-JKSUJKDBSA-N 0.000 claims description 3
- VBGLYOIFKLUMQG-UHFFFAOYSA-N Cannabinol Chemical compound C1=C(C)C=C2C3=C(O)C=C(CCCCC)C=C3OC(C)(C)C2=C1 VBGLYOIFKLUMQG-UHFFFAOYSA-N 0.000 claims description 3
- NPBVQXIMTZKSBA-UHFFFAOYSA-N Chavibetol Natural products COC1=CC=C(CC=C)C=C1O NPBVQXIMTZKSBA-UHFFFAOYSA-N 0.000 claims description 3
- 235000007129 Cuminum cyminum Nutrition 0.000 claims description 3
- 244000304337 Cuminum cyminum Species 0.000 claims description 3
- RRTBTJPVUGMUNR-UHFFFAOYSA-N Cycloartanol Natural products C12CCC(C(C(O)CC3)(C)C)C3C2(CC)CCC2(C)C1(C)CCC2C(C)CCCC(C)C RRTBTJPVUGMUNR-UHFFFAOYSA-N 0.000 claims description 3
- 240000002943 Elettaria cardamomum Species 0.000 claims description 3
- 239000005770 Eugenol Substances 0.000 claims description 3
- 239000001293 FEMA 3089 Substances 0.000 claims description 3
- HVXLSFNCWWWDPA-UHFFFAOYSA-N Isocycloartenol Natural products C1CC(O)C(C)(C)C2C31CC13CCC3(C)C(C(CCCC(C)=C)C)CCC3(C)C1CC2 HVXLSFNCWWWDPA-UHFFFAOYSA-N 0.000 claims description 3
- 244000270834 Myristica fragrans Species 0.000 claims description 3
- 235000009421 Myristica fragrans Nutrition 0.000 claims description 3
- IGHTZQUIFGUJTG-QSMXQIJUSA-N O1C2=CC(CCCCC)=CC(O)=C2[C@H]2C(C)(C)[C@@H]3[C@H]2[C@@]1(C)CC3 Chemical compound O1C2=CC(CCCCC)=CC(O)=C2[C@H]2C(C)(C)[C@@H]3[C@H]2[C@@]1(C)CC3 IGHTZQUIFGUJTG-QSMXQIJUSA-N 0.000 claims description 3
- 108090000526 Papain Proteins 0.000 claims description 3
- HXQRIQXPGMPSRW-UHZRDUGNSA-N Pollinastanol Natural products O[C@@H]1C[C@H]2[C@@]3([C@]4([C@H]([C@@]5(C)[C@@](C)([C@H]([C@H](CCCC(C)C)C)CC5)CC4)CC2)C3)CC1 HXQRIQXPGMPSRW-UHZRDUGNSA-N 0.000 claims description 3
- 239000004365 Protease Substances 0.000 claims description 3
- UVMRYBDEERADNV-UHFFFAOYSA-N Pseudoeugenol Natural products COC1=CC(C(C)=C)=CC=C1O UVMRYBDEERADNV-UHFFFAOYSA-N 0.000 claims description 3
- 239000008168 almond oil Substances 0.000 claims description 3
- FSLPMRQHCOLESF-UHFFFAOYSA-N alpha-amyrenol Natural products C1CC(O)C(C)(C)C2CCC3(C)C4(C)CCC5(C)CCC(C)C(C)C5C4=CCC3C21C FSLPMRQHCOLESF-UHFFFAOYSA-N 0.000 claims description 3
- 239000010619 basil oil Substances 0.000 claims description 3
- 229940018006 basil oil Drugs 0.000 claims description 3
- JFSHUTJDVKUMTJ-QHPUVITPSA-N beta-amyrin Chemical compound C1C[C@H](O)C(C)(C)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C)CCC(C)(C)C[C@H]5C4=CC[C@@H]3[C@]21C JFSHUTJDVKUMTJ-QHPUVITPSA-N 0.000 claims description 3
- QQFMRPIKDLHLKB-UHFFFAOYSA-N beta-amyrin Natural products CC1C2C3=CCC4C5(C)CCC(O)C(C)(C)C5CCC4(C)C3(C)CCC2(C)CCC1(C)C QQFMRPIKDLHLKB-UHFFFAOYSA-N 0.000 claims description 3
- PDNLMONKODEGSE-UHFFFAOYSA-N beta-amyrin acetate Natural products CC(=O)OC1CCC2(C)C(CCC3(C)C4(C)CCC5(C)CCC(C)(C)CC5C4=CCC23C)C1(C)C PDNLMONKODEGSE-UHFFFAOYSA-N 0.000 claims description 3
- JGQFVRIQXUFPAH-UHFFFAOYSA-N beta-citronellol Natural products OCCC(C)CCCC(C)=C JGQFVRIQXUFPAH-UHFFFAOYSA-N 0.000 claims description 3
- HRHJHXJQMNWQTF-UHFFFAOYSA-N cannabichromenic acid Chemical compound O1C(C)(CCC=C(C)C)C=CC2=C1C=C(CCCCC)C(C(O)=O)=C2O HRHJHXJQMNWQTF-UHFFFAOYSA-N 0.000 claims description 3
- QXACEHWTBCFNSA-SFQUDFHCSA-N cannabigerol Chemical compound CCCCCC1=CC(O)=C(C\C=C(/C)CCC=C(C)C)C(O)=C1 QXACEHWTBCFNSA-SFQUDFHCSA-N 0.000 claims description 3
- SEEZIOZEUUMJME-FOWTUZBSSA-N cannabigerolic acid Chemical compound CCCCCC1=CC(O)=C(C\C=C(/C)CCC=C(C)C)C(O)=C1C(O)=O SEEZIOZEUUMJME-FOWTUZBSSA-N 0.000 claims description 3
- SVTKBAIRFMXQQF-UHFFFAOYSA-N cannabivarin Chemical compound C1=C(C)C=C2C3=C(O)C=C(CCC)C=C3OC(C)(C)C2=C1 SVTKBAIRFMXQQF-UHFFFAOYSA-N 0.000 claims description 3
- 235000017663 capsaicin Nutrition 0.000 claims description 3
- 229960002504 capsaicin Drugs 0.000 claims description 3
- 235000005300 cardamomo Nutrition 0.000 claims description 3
- RSYBQKUNBFFNDO-UHFFFAOYSA-N caryophyllene oxide Natural products CC1(C)CC2C(=C)CCC3OC3(C)CCC12C RSYBQKUNBFFNDO-UHFFFAOYSA-N 0.000 claims description 3
- 238000002512 chemotherapy Methods 0.000 claims description 3
- 235000000484 citronellol Nutrition 0.000 claims description 3
- ONQRKEUAIJMULO-YBXTVTTCSA-N cycloartenol Chemical compound CC(C)([C@@H](O)CC1)[C@H]2[C@@]31C[C@@]13CC[C@]3(C)[C@@H]([C@@H](CCC=C(C)C)C)CC[C@@]3(C)[C@@H]1CC2 ONQRKEUAIJMULO-YBXTVTTCSA-N 0.000 claims description 3
- YNBJLDSWFGUFRT-UHFFFAOYSA-N cycloartenol Natural products CC(CCC=C(C)C)C1CCC2(C)C1(C)CCC34CC35CCC(O)C(C)(C)C5CCC24C YNBJLDSWFGUFRT-UHFFFAOYSA-N 0.000 claims description 3
- FODTZLFLDFKIQH-UHFFFAOYSA-N cycloartenol trans-ferulate Natural products C1=C(O)C(OC)=CC(C=CC(=O)OC2C(C3CCC4C5(C)CCC(C5(C)CCC54CC53CC2)C(C)CCC=C(C)C)(C)C)=C1 FODTZLFLDFKIQH-UHFFFAOYSA-N 0.000 claims description 3
- 210000004207 dermis Anatomy 0.000 claims description 3
- 210000002615 epidermis Anatomy 0.000 claims description 3
- 239000010642 eucalyptus oil Substances 0.000 claims description 3
- 229940044949 eucalyptus oil Drugs 0.000 claims description 3
- 229960002217 eugenol Drugs 0.000 claims description 3
- 229940043259 farnesol Drugs 0.000 claims description 3
- 229930002886 farnesol Natural products 0.000 claims description 3
- 239000010643 fennel seed oil Substances 0.000 claims description 3
- BXWQUXUDAGDUOS-UHFFFAOYSA-N gamma-humulene Natural products CC1=CCCC(C)(C)C=CC(=C)CCC1 BXWQUXUDAGDUOS-UHFFFAOYSA-N 0.000 claims description 3
- QBNFBHXQESNSNP-UHFFFAOYSA-N humulene Natural products CC1=CC=CC(C)(C)CC=C(/C)CCC1 QBNFBHXQESNSNP-UHFFFAOYSA-N 0.000 claims description 3
- 239000006210 lotion Substances 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 235000019720 niaouli oil Nutrition 0.000 claims description 3
- 235000019834 papain Nutrition 0.000 claims description 3
- 229940055729 papain Drugs 0.000 claims description 3
- 239000003961 penetration enhancing agent Substances 0.000 claims description 3
- 235000019100 piperine Nutrition 0.000 claims description 3
- MXXWOMGUGJBKIW-YPCIICBESA-N piperine Chemical compound C=1C=C2OCOC2=CC=1/C=C/C=C/C(=O)N1CCCCC1 MXXWOMGUGJBKIW-YPCIICBESA-N 0.000 claims description 3
- 229940075559 piperine Drugs 0.000 claims description 3
- WVWHRXVVAYXKDE-UHFFFAOYSA-N piperine Natural products O=C(C=CC=Cc1ccc2OCOc2c1)C3CCCCN3 WVWHRXVVAYXKDE-UHFFFAOYSA-N 0.000 claims description 3
- 239000010668 rosemary oil Substances 0.000 claims description 3
- 229940058206 rosemary oil Drugs 0.000 claims description 3
- CRDAMVZIKSXKFV-UHFFFAOYSA-N trans-Farnesol Natural products CC(C)=CCCC(C)=CCCC(C)=CCO CRDAMVZIKSXKFV-UHFFFAOYSA-N 0.000 claims description 3
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 3
- WTARULDDTDQWMU-RKDXNWHRSA-N (+)-β-pinene Chemical compound C1[C@H]2C(C)(C)[C@@H]1CCC2=C WTARULDDTDQWMU-RKDXNWHRSA-N 0.000 claims description 2
- WTARULDDTDQWMU-IUCAKERBSA-N (-)-Nopinene Natural products C1[C@@H]2C(C)(C)[C@H]1CCC2=C WTARULDDTDQWMU-IUCAKERBSA-N 0.000 claims description 2
- RGZSQWQPBWRIAQ-CABCVRRESA-N (-)-alpha-Bisabolol Chemical compound CC(C)=CCC[C@](C)(O)[C@H]1CCC(C)=CC1 RGZSQWQPBWRIAQ-CABCVRRESA-N 0.000 claims description 2
- 239000001500 (2R)-6-methyl-2-[(1R)-4-methyl-1-cyclohex-3-enyl]hept-5-en-2-ol Substances 0.000 claims description 2
- GRWFGVWFFZKLTI-IUCAKERBSA-N 1S,5S-(-)-alpha-Pinene Natural products CC1=CC[C@@H]2C(C)(C)[C@H]1C2 GRWFGVWFFZKLTI-IUCAKERBSA-N 0.000 claims description 2
- GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 claims description 2
- 208000007848 Alcoholism Diseases 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000000103 Anorexia Nervosa Diseases 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 208000020925 Bipolar disease Diseases 0.000 claims description 2
- PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical group OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 235000019739 Dicalciumphosphate Nutrition 0.000 claims description 2
- 208000014094 Dystonic disease Diseases 0.000 claims description 2
- 208000009386 Experimental Arthritis Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- 208000005176 Hepatitis C Diseases 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- RJQXTJLFIWVMTO-TYNCELHUSA-N Methicillin Chemical compound COC1=CC=CC(OC)=C1C(=O)N[C@@H]1C(=O)N2[C@@H](C(O)=O)C(C)(C)S[C@@H]21 RJQXTJLFIWVMTO-TYNCELHUSA-N 0.000 claims description 2
- 206010028813 Nausea Diseases 0.000 claims description 2
- 206010029098 Neoplasm skin Diseases 0.000 claims description 2
- 208000012902 Nervous system disease Diseases 0.000 claims description 2
- 208000025966 Neurological disease Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 206010034620 Peripheral sensory neuropathy Diseases 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- PXRCIOIWVGAZEP-UHFFFAOYSA-N Primaeres Camphenhydrat Natural products C1CC2C(O)(C)C(C)(C)C1C2 PXRCIOIWVGAZEP-UHFFFAOYSA-N 0.000 claims description 2
- WTARULDDTDQWMU-UHFFFAOYSA-N Pseudopinene Natural products C1C2C(C)(C)C1CCC2=C WTARULDDTDQWMU-UHFFFAOYSA-N 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- 241000191967 Staphylococcus aureus Species 0.000 claims description 2
- 206010001584 alcohol abuse Diseases 0.000 claims description 2
- 208000025746 alcohol use disease Diseases 0.000 claims description 2
- RGZSQWQPBWRIAQ-LSDHHAIUSA-N alpha-Bisabolol Natural products CC(C)=CCC[C@@](C)(O)[C@@H]1CCC(C)=CC1 RGZSQWQPBWRIAQ-LSDHHAIUSA-N 0.000 claims description 2
- VYBREYKSZAROCT-UHFFFAOYSA-N alpha-myrcene Natural products CC(=C)CCCC(=C)C=C VYBREYKSZAROCT-UHFFFAOYSA-N 0.000 claims description 2
- MVNCAPSFBDBCGF-UHFFFAOYSA-N alpha-pinene Natural products CC1=CCC23C1CC2C3(C)C MVNCAPSFBDBCGF-UHFFFAOYSA-N 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 229930006722 beta-pinene Natural products 0.000 claims description 2
- 229930006739 camphene Natural products 0.000 claims description 2
- ZYPYEBYNXWUCEA-UHFFFAOYSA-N camphenilone Natural products C1CC2C(=O)C(C)(C)C1C2 ZYPYEBYNXWUCEA-UHFFFAOYSA-N 0.000 claims description 2
- 229940117948 caryophyllene Drugs 0.000 claims description 2
- 238000000354 decomposition reaction Methods 0.000 claims description 2
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 claims description 2
- 229940038472 dicalcium phosphate Drugs 0.000 claims description 2
- 229910000390 dicalcium phosphate Inorganic materials 0.000 claims description 2
- 208000010643 digestive system disease Diseases 0.000 claims description 2
- 208000010118 dystonia Diseases 0.000 claims description 2
- 206010015037 epilepsy Diseases 0.000 claims description 2
- LCWMKIHBLJLORW-UHFFFAOYSA-N gamma-carene Natural products C1CC(=C)CC2C(C)(C)C21 LCWMKIHBLJLORW-UHFFFAOYSA-N 0.000 claims description 2
- 235000011187 glycerol Nutrition 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 229960003085 meticillin Drugs 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 230000008693 nausea Effects 0.000 claims description 2
- 208000004296 neuralgia Diseases 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 230000000926 neurological effect Effects 0.000 claims description 2
- 208000021722 neuropathic pain Diseases 0.000 claims description 2
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- 201000005572 sensory peripheral neuropathy Diseases 0.000 claims description 2
- 238000000926 separation method Methods 0.000 claims description 2
- 208000007056 sickle cell anemia Diseases 0.000 claims description 2
- 201000002859 sleep apnea Diseases 0.000 claims description 2
- 238000003860 storage Methods 0.000 claims description 2
- 229940078499 tricalcium phosphate Drugs 0.000 claims description 2
- 229910000391 tricalcium phosphate Inorganic materials 0.000 claims description 2
- 235000019731 tricalcium phosphate Nutrition 0.000 claims description 2
- 240000004308 marijuana Species 0.000 claims 1
- 230000000699 topical effect Effects 0.000 abstract description 8
- 241000218236 Cannabis Species 0.000 description 19
- -1 masks Substances 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 6
- 239000004615 ingredient Substances 0.000 description 6
- 208000035475 disorder Diseases 0.000 description 5
- 229940098465 tincture Drugs 0.000 description 5
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 238000011282 treatment Methods 0.000 description 4
- 241000196324 Embryophyta Species 0.000 description 3
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 3
- 230000008901 benefit Effects 0.000 description 3
- 239000011230 binding agent Substances 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- HCAWPGARWVBULJ-IAGOWNOFSA-N delta8-THC Chemical class C1C(C)=CC[C@H]2C(C)(C)OC3=CC(CCCCC)=CC(O)=C3[C@@H]21 HCAWPGARWVBULJ-IAGOWNOFSA-N 0.000 description 3
- 239000003085 diluting agent Substances 0.000 description 3
- 239000007884 disintegrant Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000000314 lubricant Substances 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- 208000030507 AIDS Diseases 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 2
- 229930091371 Fructose Natural products 0.000 description 2
- 239000005715 Fructose Substances 0.000 description 2
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 2
- 208000010412 Glaucoma Diseases 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 2
- DLRVVLDZNNYCBX-UHFFFAOYSA-N Polydextrose Polymers OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(O)O1 DLRVVLDZNNYCBX-UHFFFAOYSA-N 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- 150000001408 amides Chemical class 0.000 description 2
- 230000003474 anti-emetic effect Effects 0.000 description 2
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000003086 colorant Substances 0.000 description 2
- 238000001647 drug administration Methods 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 239000000796 flavoring agent Substances 0.000 description 2
- 235000019634 flavors Nutrition 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 229960001375 lactose Drugs 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 239000003002 pH adjusting agent Substances 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 229920000642 polymer Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 230000000391 smoking effect Effects 0.000 description 2
- 239000000600 sorbitol Substances 0.000 description 2
- 235000010356 sorbitol Nutrition 0.000 description 2
- 239000005720 sucrose Substances 0.000 description 2
- 150000005846 sugar alcohols Chemical class 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- 239000000454 talc Substances 0.000 description 2
- 229910052623 talc Inorganic materials 0.000 description 2
- 235000012222 talc Nutrition 0.000 description 2
- LOUSQMWLMDHRIK-IAGOWNOFSA-N (6ar,10ar)-9-(hydroxymethyl)-6,6-dimethyl-3-pentyl-6a,7,10,10a-tetrahydrobenzo[c]chromen-1-ol Chemical compound C1C(CO)=CC[C@H]2C(C)(C)OC3=CC(CCCCC)=CC(O)=C3[C@@H]21 LOUSQMWLMDHRIK-IAGOWNOFSA-N 0.000 description 1
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- 244000215068 Acacia senegal Species 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 1
- 102000018208 Cannabinoid Receptor Human genes 0.000 description 1
- 108050007331 Cannabinoid receptor Proteins 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 1
- 208000000094 Chronic Pain Diseases 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 229920002785 Croscarmellose sodium Polymers 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004386 Erythritol Substances 0.000 description 1
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 description 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 208000004547 Hallucinations Diseases 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 235000019501 Lemon oil Nutrition 0.000 description 1
- 208000019693 Lung disease Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 229920002774 Maltodextrin Polymers 0.000 description 1
- 239000005913 Maltodextrin Substances 0.000 description 1
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 1
- 235000014435 Mentha Nutrition 0.000 description 1
- 241001072983 Mentha Species 0.000 description 1
- 208000019695 Migraine disease Diseases 0.000 description 1
- 239000004909 Moisturizer Substances 0.000 description 1
- 208000008238 Muscle Spasticity Diseases 0.000 description 1
- HSHXDCVZWHOWCS-UHFFFAOYSA-N N'-hexadecylthiophene-2-carbohydrazide Chemical compound CCCCCCCCCCCCCCCCNNC(=O)c1cccs1 HSHXDCVZWHOWCS-UHFFFAOYSA-N 0.000 description 1
- 244000061176 Nicotiana tabacum Species 0.000 description 1
- 235000002637 Nicotiana tabacum Nutrition 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 1
- 229920001100 Polydextrose Polymers 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- DFPAKSUCGFBDDF-ZQBYOMGUSA-N [14c]-nicotinamide Chemical compound N[14C](=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-ZQBYOMGUSA-N 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000012675 alcoholic extract Substances 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- WLDHEUZGFKACJH-UHFFFAOYSA-K amaranth Chemical compound [Na+].[Na+].[Na+].C12=CC=C(S([O-])(=O)=O)C=C2C=C(S([O-])(=O)=O)C(O)=C1N=NC1=CC=C(S([O-])(=O)=O)C2=CC=CC=C12 WLDHEUZGFKACJH-UHFFFAOYSA-K 0.000 description 1
- 229940035676 analgesics Drugs 0.000 description 1
- 208000022531 anorexia Diseases 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 230000001773 anti-convulsant effect Effects 0.000 description 1
- 229940125683 antiemetic agent Drugs 0.000 description 1
- 239000002111 antiemetic agent Substances 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 229960005069 calcium Drugs 0.000 description 1
- 229910000389 calcium phosphate Inorganic materials 0.000 description 1
- 235000011010 calcium phosphates Nutrition 0.000 description 1
- 239000000378 calcium silicate Substances 0.000 description 1
- 229910052918 calcium silicate Inorganic materials 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 235000013539 calcium stearate Nutrition 0.000 description 1
- 239000008116 calcium stearate Substances 0.000 description 1
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 229940105329 carboxymethylcellulose Drugs 0.000 description 1
- 229940084030 carboxymethylcellulose calcium Drugs 0.000 description 1
- 229950008138 carmellose Drugs 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- OIQPTROHQCGFEF-UHFFFAOYSA-L chembl1371409 Chemical compound [Na+].[Na+].OC1=CC=C2C=C(S([O-])(=O)=O)C=CC2=C1N=NC1=CC=C(S([O-])(=O)=O)C=C1 OIQPTROHQCGFEF-UHFFFAOYSA-L 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
- 230000001276 controlling effect Effects 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 229940099112 cornstarch Drugs 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- 229960001681 croscarmellose sodium Drugs 0.000 description 1
- 229960000913 crospovidone Drugs 0.000 description 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
- 238000009109 curative therapy Methods 0.000 description 1
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 1
- 206010061428 decreased appetite Diseases 0.000 description 1
- SSQJFGMEZBFMNV-PMACEKPBSA-N dexanabinol Chemical compound C1C(CO)=CC[C@@H]2C(C)(C)OC3=CC(C(C)(C)CCCCCC)=CC(O)=C3[C@H]21 SSQJFGMEZBFMNV-PMACEKPBSA-N 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- JFVXEJADITYJHK-UHFFFAOYSA-L disodium 2-(3-hydroxy-5-sulfonato-1H-indol-2-yl)-3-oxoindole-5-sulfonate Chemical compound [Na+].[Na+].Oc1c([nH]c2ccc(cc12)S([O-])(=O)=O)C1=Nc2ccc(cc2C1=O)S([O-])(=O)=O JFVXEJADITYJHK-UHFFFAOYSA-L 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 125000002587 enol group Chemical group 0.000 description 1
- 235000019414 erythritol Nutrition 0.000 description 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 1
- 229940009714 erythritol Drugs 0.000 description 1
- 150000002170 ethers Chemical class 0.000 description 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 239000000989 food dye Substances 0.000 description 1
- 229960002737 fructose Drugs 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 229960001031 glucose Drugs 0.000 description 1
- 239000001341 hydroxy propyl starch Substances 0.000 description 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 235000013828 hydroxypropyl starch Nutrition 0.000 description 1
- 239000003326 hypnotic agent Substances 0.000 description 1
- 230000000147 hypnotic effect Effects 0.000 description 1
- 230000004410 intraocular pressure Effects 0.000 description 1
- 239000000832 lactitol Substances 0.000 description 1
- 235000010448 lactitol Nutrition 0.000 description 1
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 description 1
- 229960003451 lactitol Drugs 0.000 description 1
- 229960001021 lactose monohydrate Drugs 0.000 description 1
- 239000010501 lemon oil Substances 0.000 description 1
- FFVXQGMUHIJQAO-BFKQJKLPSA-N levonantradol Chemical compound C([C@@H](C)OC=1C=C(OC(C)=O)C=2[C@@H]3C[C@H](O)CC[C@H]3[C@H](C)NC=2C=1)CCC1=CC=CC=C1 FFVXQGMUHIJQAO-BFKQJKLPSA-N 0.000 description 1
- 229950005812 levonantradol Drugs 0.000 description 1
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 208000020816 lung neoplasm Diseases 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- 235000010449 maltitol Nutrition 0.000 description 1
- 239000000845 maltitol Substances 0.000 description 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 1
- 229940035436 maltitol Drugs 0.000 description 1
- 229940035034 maltodextrin Drugs 0.000 description 1
- 229960002160 maltose Drugs 0.000 description 1
- 229960001855 mannitol Drugs 0.000 description 1
- 229940057917 medium chain triglycerides Drugs 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 206010027599 migraine Diseases 0.000 description 1
- 230000001333 moisturizer Effects 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 229940035363 muscle relaxants Drugs 0.000 description 1
- 239000003158 myorelaxant agent Substances 0.000 description 1
- GECBBEABIDMGGL-RTBURBONSA-N nabilone Chemical compound C1C(=O)CC[C@H]2C(C)(C)OC3=CC(C(C)(C)CCCCCC)=CC(O)=C3[C@@H]21 GECBBEABIDMGGL-RTBURBONSA-N 0.000 description 1
- 229960002967 nabilone Drugs 0.000 description 1
- 238000002638 palliative care Methods 0.000 description 1
- HXYVTAGFYLMHSO-UHFFFAOYSA-N palmitoyl ethanolamide Chemical compound CCCCCCCCCCCCCCCC(=O)NCCO HXYVTAGFYLMHSO-UHFFFAOYSA-N 0.000 description 1
- 239000013618 particulate matter Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 239000001259 polydextrose Substances 0.000 description 1
- 235000013856 polydextrose Nutrition 0.000 description 1
- 229940035035 polydextrose Drugs 0.000 description 1
- 229940100474 polyethylene glycol 1450 Drugs 0.000 description 1
- 229940057838 polyethylene glycol 4000 Drugs 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 229950008882 polysorbate Drugs 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 229940068968 polysorbate 80 Drugs 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 229940116317 potato starch Drugs 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 229940088417 precipitated calcium carbonate Drugs 0.000 description 1
- 239000000955 prescription drug Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 230000000506 psychotropic effect Effects 0.000 description 1
- 230000002040 relaxant effect Effects 0.000 description 1
- 229940100486 rice starch Drugs 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000000779 smoke Substances 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 229940083542 sodium Drugs 0.000 description 1
- 235000015424 sodium Nutrition 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 1
- 230000000475 sunscreen effect Effects 0.000 description 1
- 239000000516 sunscreening agent Substances 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- UEUXEKPTXMALOB-UHFFFAOYSA-J tetrasodium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O UEUXEKPTXMALOB-UHFFFAOYSA-J 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 230000037317 transdermal delivery Effects 0.000 description 1
- 238000013271 transdermal drug delivery Methods 0.000 description 1
- 235000012141 vanillin Nutrition 0.000 description 1
- MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 description 1
- FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 229940100445 wheat starch Drugs 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A24—TOBACCO; CIGARS; CIGARETTES; SIMULATED SMOKING DEVICES; SMOKERS' REQUISITES
- A24F—SMOKERS' REQUISITES; MATCH BOXES; SIMULATED SMOKING DEVICES
- A24F7/00—Mouthpieces for pipes; Mouthpieces for cigar or cigarette holders
- A24F7/02—Mouthpieces for pipes; Mouthpieces for cigar or cigarette holders with detachable connecting members
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A24—TOBACCO; CIGARS; CIGARETTES; SIMULATED SMOKING DEVICES; SMOKERS' REQUISITES
- A24F—SMOKERS' REQUISITES; MATCH BOXES; SIMULATED SMOKING DEVICES
- A24F40/00—Electrically operated smoking devices; Component parts thereof; Manufacture thereof; Maintenance or testing thereof; Charging means specially adapted therefor
- A24F40/40—Constructional details, e.g. connection of cartridges and battery parts
-
- A—HUMAN NECESSITIES
- A24—TOBACCO; CIGARS; CIGARETTES; SIMULATED SMOKING DEVICES; SMOKERS' REQUISITES
- A24F—SMOKERS' REQUISITES; MATCH BOXES; SIMULATED SMOKING DEVICES
- A24F40/00—Electrically operated smoking devices; Component parts thereof; Manufacture thereof; Maintenance or testing thereof; Charging means specially adapted therefor
- A24F40/40—Constructional details, e.g. connection of cartridges and battery parts
- A24F40/48—Fluid transfer means, e.g. pumps
- A24F40/485—Valves; Apertures
Definitions
- cannabinoid formulations and methods of use associated therewith. Specifically, disclosed are topical or transdermal formulations having a cannabinoid in combination with a phyto-compound excipient that facilitates absorption and bioavailability of the cannabinoid.
- Cannabis is believed to provide benefits in the treatment of multiple disorders with safer and fewer serious side effects than most prescription drugs currently used as antiemetics, muscle relaxants, hypnotics, and analgesics.
- a disadvantage in treating patients with cannabis is the psychoactive effect, especially in “naive” cannabis users.
- Cannabis has also been used to treat the symptoms in patients suffering from serious medical conditions. For example, cannabis has been used to alleviate symptoms associated with cancer, anorexia, AIDS, chronic pain, muscle spasticity, glaucoma, arthritis, migraine, and many other illnesses. Cannabis is recognized as having antiemetic properties and has been successfully used to treat nausea and vomiting in cancer patients undergoing chemotherapy. Cannabis has also been used in treating the weight loss syndrome of AIDS and in treating glaucoma by reducing intraocular pressure. Cannabis is also known for its muscle relaxing and anti-convulsant effects.
- Cannabis smoke carries more tar and other particulate matter than tobacco and may be a cause of lung diseases including lung cancer. Furthermore, many patients find the act of smoking unappealing, as well as generally unhealthy.
- formulations comprising: at least one cannabinoid or a derivative thereof and at least one phyto-compound excipient, wherein said at least one phyto-compound excipient is a skin penetration enhancer that facilitates absorption and bioavailability of said at least one cannabinoid or said derivative thereof in a subject.
- the formulation is a topical or a transdermal formulation.
- the formulation includes a first cannabinoid (e.g., THC or THCa) and a second cannabinoid (CBD or CBDa).
- the formulation includes a first polymer (e.g., polyethylene glycol 1450) and a second polymer (e.g., polyethylene glycol 4000).
- kits for treating a disease or disorder in a subject comprising administering to the subject, for example topically administering, a formulation disclosed herein.
- the method comprises the steps of providing one or more cannabinoids; providing one or more phyto-compound excipients; and mixing said one or more cannabinoids with said one or more phyto-compound excipients.
- metered dose devices having a formulation disclosed herein.
- the device comprises a regulated pump. In certain embodiments, the device comprises a metered-dosing mechanism. In certain embodiments, the device comprises an air-tight container to store the formulation. In certain embodiments, the device comprises the formulation in a plurality of metered doses. In certain embodiments, the device is an aerosol spray device.
- treatment or “therapy” (as well as different forms thereof) include preventative (e.g., prophylactic), curative, or palliative treatment.
- treating includes alleviating or reducing at least one adverse or negative effect or symptom of a condition, disease, or disorder.
- transdermal drug delivery is meant administration of a drug to the skin surface of an individual so that the drug passes through the skin tissue and into the individual's blood stream.
- Topical administration is used in its conventional sense to mean delivery of an active agent to a body surface such as the skin or mucosa, as in, for example, topical drug administration in the prevention or treatment of various disorders, the application of cosmetics and cosmeceuticals (including moisturizers, masks, sunscreens, etc.), and the like.
- Topical administration in contrast to transdermal administration, provides a local rather than a systemic effect.
- transdermal is used herein, as in “transdermal drug administration” and “transdermal drug delivery systems,” it is to be understood that unless explicitly indicated to the contrary, “topical” administration and systems are intended as well.
- subject refers to an animal, for example a human, to whom treatment, including prophylactic treatment with the pharmaceutical formulation, is provided.
- the inventor of the instant application surprisingly and unexpectedly discovered a formulation which includes, in part, one or more cannabinoids in combination with one or more phyto-compound excipients.
- the presence of a phyto-compound excipient in the formulation facilitates absorption of a cannabinoid through an epidermis and a dermis. Furthermore, the presence of a phyto-compound excipient improves bioavailability of a cannabinoid.
- formulations comprising: at least one cannabinoid or a derivative thereof and at least one phyto-compound excipient, wherein said at least one phyto-compound excipient is a skin penetration enhancer that facilitates absorption and bioavailability of said at least one cannabinoid or said derivative thereof in a subject.
- the formulation is a topical formulation. In other embodiments, the formulation is a transdermal formulation.
- compositions of one or more cannabinoids to provide, for example, a topical or a transdermal delivery of said one or more cannabinoids.
- the cannabinoids are easily prepared and formulated to provide consistent, therapeutically effective dosage forms from lot to lot.
- said formulation facilitates administration via a regulated pump or a metered-dosing device. In certain embodiments, said formulation is a homogeneous formulation.
- said cannabinoid is an extract from a cannabis plant.
- the formulation has a combination of at least two cannabinoids. In certain embodiments, the formulation comprises a combination of at least two cannabinoids. In certain embodiments, the two cannabinoids are selected from Tetrahydrocannabinolic acid (THCa), Cannabidiolic acid (CBDa), Cannabinolic acid (CBNa), Cannabichromenic acid (CBCa), Tetrahydrocannabinol (THC), Cannabidiol (CBD), Cannabigerol (CBG), Cannabigerolic Acid (CBGa), Cannabichromene (CBC), Cannabinol (CBN), Cannabielsoin (CBE), iso-Tetrahydrocannabinol (iso-THC), Cannabicyclol (CBL), Cannabicitran (CB T), Cannabivarin (CBV), Tetrahydrocannabivarin (THCV), Cannabidivarin (CBDV
- the cannabinoid is a cannabinoid extract that contains a combination of at least two of the following: Tetrahydrocannabinolic acid (THCa), Cannabidiolic acid (CBDa), Cannabinolic acid (CBNa), Cannabichromenic acid (CBCa), Tetrahydrocannabinol (THC), Cannabidiol (CBD), Cannabigerol (CBG), Cannabigerolic Acid (CBGa), Cannabichromene (CBC), Cannabinol (CBN), Cannabielsoin (CBE), iso-Tetrahydrocannabinol (iso-THC), Cannabicyclol (CBL), Cannabicitran (CBT), Cannabivarin (CBV), Tetrahydrocannabivarin (THCV), Cannabidivarin (CBDV), Cannabichromevarin (CBCV), Cannabigerovarin (CBGV),
- cannabinoids extract is well known in the art.
- the cannabis plants are grown, harvested, and the cannabinoids are extracted through, for example, a CO 2 extraction process.
- At least two cannabinoids are in a 1:1 proportion by weight. In certain embodiments, at least two cannabinoids are in a 10:1 proportion by weight. In certain embodiments, at least two cannabinoids are in a 20:1 proportion by weight. In certain embodiments, two cannabinoids are THC and CBD. In certain embodiments, two cannabinoids are THCa and CBDa.
- the two cannabinoids are in a 1:1 proportion by weight. In certain embodiments, the two cannabinoids are in a 10:1 proportion by weight. In certain embodiments, the two cannabinoids are in a 20:1 proportion by weight. In certain embodiments, the two cannabinoids are THC and CBD. In certain embodiments, the two cannabinoids are THCa and CBDa.
- the formulation includes a first cannabinoid and a second cannabinoid.
- the first and second cannabinoids are in a ratio ranging from about 1:1 to about 20:1 proportion by weight. In certain embodiments, the first and second cannabinoids are in a 1:1 proportion by weight. In other embodiments, the first and second cannabinoids are in a 10:1 proportion by weight. In yet other embodiments, the first and second cannabinoids are in a 20:1 proportion by weight.
- the first cannabinoid is THC or THCa and the second cannabinoid is CBD or CBDa.
- the first cannabinoid is THC and the second cannabinoid is CBD.
- the first cannabinoid is THCa and the second cannabinoid is CBDa.
- the at least one cannabinoid is THC or THCa present in an amount ranging from about 0.01 mg to about 200 mg. In certain embodiments, the at least one cannabinoid is CBD or CBDa present in an amount ranging from about 0.01 mg to about 200 mg.
- the first cannabinoid can be present in an amount ranging from about 0.01 mg to about 200 mg.
- the second cannabinoid also can be present in an amount ranging from about 0.01 mg to about 200 mg.
- the cannabinoids are in equal proportion such as, for example, 2.5 mg THC to 2.5 mg CBD.
- Other embodiments include proportions of THC/CBD of 0.25 mg THC to 5.0 mg CBD or 5.0 mg THC to 0.25 mg CBD.
- the cannabinoid of the invention is any member of a group of substances that are structurally related to tetrahydrocannabinol and that bind to a cannabinoid receptor such as CB1 or CB2 or both (‘THC’).
- the cannabinoid can be a naturally occurring compound (e.g., present in Cannabis), a compound metabolized by a plant or animal, or a synthetic derivative.
- the cannabinoid may be included in its free form or in the form of a salt; an acid addition salt of an ester; an amide; an enantiomer; an isomer; a tautomer; a prodrug; a derivative of an active agent; different isomeric forms (e.g., enantiomers and diastereoisomers), both in pure form and in admixture, including racemic mixtures; or enol forms.
- the cannabinoids are further meant to encompass natural cannabinoids, natural cannabinoids that have been purified or modified, and synthetically derived cannabinoids.
- Methods for purifying cannabinoids from plant material are well known in the art and fully described in, for example, United States Patent Application Publication 2005/0266108, which is incorporated by reference herein in its entirety.
- the cannabinoids can be any of 9-tetrahydrocannabinol, 8-tetrahydrocannabinol, (+)-1,1-dimethylheptyl analog of 7-hydroxy-delta-6-tetrahydrocannabinol, 3-(5-cyano-1′,1′-dimethylpentyl)-1-(4-N-morpholinobutyryloxy)-delta-8-tetrahydrocannabinol hydrochloride, dexanabinol, nabilone, levonantradol, and N-(2-hydroxyethyl)hexadecanoamide.
- the cannabinoids can be any of the non-psychotropic cannabinoid 3-dimethylnepty 11 carboxylic acid homologine 8 and delta-8-tetrahydrocannabinol.
- the cannabinoid extract comprises cannabinoids tincture.
- tincture refers to an alcoholic extract of plant material. Methods of tincture preparation are well known in the art and are described, for example, in the U.S. Pat. No. 9,468,865, hereby incorporated by reference in its entirety.
- the method of tincture preparation according to the present invention comprises the steps of combining medium chain triglycerides and polysorbate in a mixing vessel to form a first combination; mixing the first combination; adding the cannabinoid extract to the first combination to form a second combination; mixing the second combination; adding 200 proof ethanol to the second combination to form a third combination; and mixing the third combination for an extended period of time in order to obtain the cannabinoids tincture.
- the duration of the final mixing step may vary depending on many factors and can be easily optimized by a skilled artisan.
- the final mixing step ranges from about 5 to about 60 minutes.
- the final mixing step ranges from about 10 to about 50 minutes.
- the final mixing step ranges from about 15 to about 45 minutes.
- the final mixing step ranges from about 20 to about 40 minutes.
- formulations further comprising one or more phyto-compound excipients.
- the at least one phyto-compound excipient facilitates absorption of said at least one cannabinoid or said derivative through an epidermis or a dermis of the subject.
- the at least one phyto-compound excipient improves bioavailability of said at least one cannabinoid or said derivative in said subject.
- Examples of a phyto-compound excipient include, for example, but are not limited to, a terpene, an essential oil, papain, piperine, capsaicin, or an extract of Myristica fragrans.
- the at least one phyto-compound excipient is a terpene, an essential oil, papain, piperine, capsaicin, or an extract of Myristica fragrans.
- terpene examples include, for example, but are not limited to, beta-myrcene, limonene, beta caryophyllene, caryophyllene oxide, terpineol, citronellol, linalool, humulene, beta-amyrin, cycloartenol, farnesol, menthol, eucalyptol, eugenol, and borneol.
- the terpene is selected from beta-myrcene, limonene, beta caryophyllene, caryophyllene oxide, terpineol, citronellol, linalool, humulene, beta-amyrin, cycloartenol, farnesol, menthol, eucalyptol, eugenol, and borneol.
- an essential oil examples include, for example, but are not limited to, eucalyptus oil, niaouli oil, fennel oil, cumin oil, almond oil, basil oil, Alpinia oxyphylla oil, turpentine oil, rosemary oil, and cardamom oil.
- the essential oil is selected from eucalyptus oil, niaouli oil, fennel oil, cumin oil, almond oil, basil oil, Alpinia oxyphylla oil, turpentine oil, rosemary oil, and cardamom oil.
- the minor and major phyto-compounds in the formulation are used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the topical formulation. In other embodiments, the minor and major phyto-compounds in the formulation are used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the topical formulation.
- the minor and major phyto-compounds in the formulation are used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the formulation. In other embodiments, the minor and major phyto-compounds in the formulation are used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the formulation.
- the total cannabinoid content in the formulation is used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the topical formulation. In certain embodiments, the total cannabinoid content forms about 0.05% to 5% by weight based on 100 parts by weight of the topical formulation. In certain embodiments, the total cannabinoid content in the formulation is used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the topical formulation. In certain embodiments, the total cannabinoid content forms about 1.1% by weight based on 100 parts by weight of the topical formulation.
- the total cannabinoid content in the formulation is used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the formulation. In certain embodiments, the total cannabinoid content forms about 0.05% to 5% by weight based on 100 parts by weight of the formulation. In certain embodiments, the total cannabinoid content in the formulation is used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the formulation. In certain embodiments, the total cannabinoid content forms about 1.1% by weight based on 100 parts by weight of the formulation.
- the formulation of the invention may also include additional ingredients such as solvents, carriers, or excipients.
- the formulation further comprises a solvent.
- the solvent comprises ethanol, methanol, isopropanol, chloroform, propylene glycol, polyethylene glycol, glycerine, limonene, myrcene, linalool, alpha bisabolol, delta 3 carene, borneol, alpha-pinene, beta-pinene, eucalyptol, terpineol, caryophyllene, camphene, or combinations thereof.
- the solvent is ethanol.
- the formulation further comprises a pharmaceutically acceptable carrier.
- the carrier comprises cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, starch, pregelatinized starch, dicalcium phosphate, tricalcium phosphate, or mixtures thereof.
- the carrier may be comprised of a water-soluble sugar or sugar alcohol. Examples include, but not limited to, lactose, sucrose, dextrose, polydextrose, fructose, maltose, maltodextrin, dextrate, dextrin, lactitol, mannitol, erythritol, maltitol, sorbitol, or xylitol, and mixtures thereof.
- the formulation may further contain an ingredient commonly used in the pharmaceutical field.
- the ingredient include, but are not limited to, a diluent, a disintegrant, a binder, a lubricant, a colorant, a pH adjusting agent, a surfactant, a stabilizing agent, a sour agent, a flavor, a glidant, and the like. These ingredients are used in an amount commonly used in the pharmaceutical field unless otherwise specifically stated.
- diluent examples include, but are not limited to, a sugar or a sugar alcohol such as lactose (e.g., lactose monohydrate), fructose, glucose, mannitol or sorbitol; a starch such as corn starch, potato starch, wheat starch, rice starch, partially pregelatinized starch, pregelatinized starch or porous starch; microcrystalline cellulose; anhydrous calcium phosphate, precipitated calcium carbonate, calcium silicate, and the like.
- lactose e.g., lactose monohydrate
- fructose glucose
- starch such as corn starch, potato starch, wheat starch, rice starch, partially pregelatinized starch, pregelatinized starch or porous starch
- microcrystalline cellulose anhydrous calcium phosphate, precipitated calcium carbonate, calcium silicate, and the like.
- the diluent is used in an amount to give a content of from 5% to 95% by weight based on 100 parts by weight of the formulation.
- Examples of a disintegrant include, but are not limited to, carboxymethyl cellulose, carboxymethyl cellulose calcium, carboxymethyl starch sodium, croscarmellose sodium, carmellose calcium, crospovidone, low-substituted hydroxypropyl cellulose, and hydroxypropyl starch.
- the amount of the disintegrant can be an amount to give a content of from 0.5 to 25 parts by weight based on 100 parts by weight of the formulation or the topical formulation.
- binder examples include, but are not limited to, hydroxypropyl cellulose (e.g., grade: L, SL, SSL (trade name); Nippon Soda Co., Ltd.), hydroxypropylmethyl cellulose (e.g., hypromello se 2910 (e.g., TC-5 (grade: MW, E, EW, R, RW) (trade name); Shin-Etsu Chemical Co., Ltd.)), polyvinylpyrrolidone (povidone), and gum arabic.
- hydroxypropyl cellulose e.g., grade: L, SL, SSL (trade name); Nippon Soda Co., Ltd.
- hydroxypropylmethyl cellulose e.g., hypromello se 2910 (e.g., TC-5 (grade: MW, E, EW, R, RW) (trade name); Shin-Etsu Chemical Co., Ltd.)
- polyvinylpyrrolidone povidone
- the binder is used in an amount to give a content of from 1% to 20% by weight based on 100 parts by weight of the formulation or the topical formulation.
- the lubricant examples include, but are not limited to, magnesium stearate, calcium stearate, talc, sucrose fatty acid ester, sodium stearyl fumarate and the like.
- the used amount of the lubricant is an amount to give a content of from about 0.5% to 2% by weight based on 100 parts by weight.
- the colorant examples include, but are not limited to, a food dye (e.g., food yellow No. 5, food red No. 2, food blue No. 2), a food lake color, iron oxide red, and iron oxide yellow.
- a food dye e.g., food yellow No. 5, food red No. 2, food blue No. 2
- a food lake color e.g., iron oxide red, and iron oxide yellow.
- pH adjusting agent examples include, but are not limited to, citrate, phosphate, carbonate, tartrate, fumarate, acetate, and amino acid salt.
- surfactant examples include, but are not limited to, sodium lauryl sulfate, polysorbate 80, and polyoxyethylene (160) polyoxypropylene (30) glycol.
- the formulation may include a stabilizing agent that prevents separation or decomposition upon being transferred to a container or during transit or storage of said container.
- stabilizing agent examples include, but are not limited to, tocopherol, tetrasodium edetate, nicotinamide, and a cyclodextrin.
- sour agent examples include, but are not limited to, ascorbic acid, citric acid, tartaric acid, and malic acid.
- Examples of the flavor include, but are not limited to, menthol, Mentha oil, lemon oil, and vanillin.
- glidant examples include, but are not limited to, colloidal silicon dioxide, aqueous silicon dioxide, and talc.
- the above ingredients may be used by combining two or more members at an appropriate ratio.
- the formulations disclosed herein include a composition for daily administration.
- the therapeutic effect is maintained with one unit, twice daily.
- the therapeutic effect is maintained with one unit, three times daily.
- the duration of each dose's effect is between four (4) to six (6) hours.
- the formulation can be of any suitable form, for example, a cream, a lotion, or a gel. In certain embodiments, the formulation is a cream or lotion.
- provided herein are methods of treating a disease in a subject, the method comprising administering a formulation described herein. In other aspects, provided herein are methods of treating a disease in a subject, the method comprising administering to the subject a formulation described herein.
- the formulation is administered topically. In other embodiments, the formulation is administered transdermally.
- Examples of a disease or a disorder that can be treated by the invention include, but are not limited to, a skin disease or disorder, pain associated with cancer, neuropathic pain and HIV-associated sensory neuropathy, side effects of chemotherapy including nausea and pain, symptoms of neurological and neurodegenerative diseases such as Huntington's disease, Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, multiple sclerosis, epilepsy, post-traumatic stress disorder (PTSD), alcohol abuse, bipolar disorder, depression, anorexia nervosa; cancer such as gliomas, leukemia, skin tumors, colorectal cancer; diseases including hepatitis C, methicillin-resistant Staphylococcus aureus (MRSA), pruritus, psoriasis, asthma, sickle-cell disease, sleep apnea, digestive diseases, collagen-induced arthritis, atherosclerosis and dystonia.
- said administration is a topical administration.
- said administration is a transdermal administration.
- Examples of a skin disease or disorder include, but are not limited to, itch, pain, and inflammation.
- kits for manufacturing a formulation described herein may include the steps of: providing one or more cannabinoids; providing one or more phyto-compound excipients; and blending or mixing said one or more cannabinoids with said one or more phyto-compound excipients. These steps are carried out based on the techniques and processes known to one of skill in the art.
- the device is an aerosol spray device which can spray the formulation on a skin of a subject.
- the device includes a regulated pump.
- the device includes a metered-dosing mechanism.
- the device may include an air-tight container to store said formulation.
- the formulation is stored in a plurality of metered doses.
- the device comprises the formulation in a plurality of metered doses.
- the device is an aerosol spray device.
- the formulation is a therapeutic cream for topical or transdermal administration.
- the formulation includes a mixture of a therapeutic agent (e.g., cannabinoid extract) and a phyto-compound excipient.
- a therapeutic agent e.g., cannabinoid extract
- a phyto-compound excipient e.g., phyto-compound excipient
- the formulation is suitable for topical or transdermal administration using a metered-dose aerosol spray device.
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Inorganic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dermatology (AREA)
- Catching Or Destruction (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Disinfection, Sterilisation Or Deodorisation Of Air (AREA)
Abstract
Disclosed are cannabinoid formulations and methods of use associated therewith. Specifically, disclosed are topical or transdermal formulations having a cannabinoid in combination with a phyto-compound excipient that facilitates absorption and bioavailability of the cannabinoid.
Description
- This application claims the benefit of priority to U.S. Provisional Application No. 62/788,494, filed Jan. 4, 2019, the contents of which are incorporated herein by reference in their entirety.
- Disclosed are cannabinoid formulations and methods of use associated therewith. Specifically, disclosed are topical or transdermal formulations having a cannabinoid in combination with a phyto-compound excipient that facilitates absorption and bioavailability of the cannabinoid.
- The medicinal and psychoactive properties of the cannabis plant have been known for centuries. While it has been illegal in many countries, there is a growing population lobbying for legalization of its use, especially for medicinal purposes.
- Cannabis is believed to provide benefits in the treatment of multiple disorders with safer and fewer serious side effects than most prescription drugs currently used as antiemetics, muscle relaxants, hypnotics, and analgesics. A disadvantage in treating patients with cannabis is the psychoactive effect, especially in “naive” cannabis users. Furthermore, there have been reports of unpleasant reactions to cannabis, such as anxiety, panic, or hallucinations. It is believed that the undesirable side effects are most commonly associated with higher doses of cannabis and are related to the difficulty in controlling the dosage when the drug is smoked or eaten in cannabis-enriched confectionaries.
- Cannabis has also been used to treat the symptoms in patients suffering from serious medical conditions. For example, cannabis has been used to alleviate symptoms associated with cancer, anorexia, AIDS, chronic pain, muscle spasticity, glaucoma, arthritis, migraine, and many other illnesses. Cannabis is recognized as having antiemetic properties and has been successfully used to treat nausea and vomiting in cancer patients undergoing chemotherapy. Cannabis has also been used in treating the weight loss syndrome of AIDS and in treating glaucoma by reducing intraocular pressure. Cannabis is also known for its muscle relaxing and anti-convulsant effects.
- The most prevalent mode of administration of medical cannabis is by smoking. This mode of administration can have adverse effects on the lungs. Cannabis smoke carries more tar and other particulate matter than tobacco and may be a cause of lung diseases including lung cancer. Furthermore, many patients find the act of smoking unappealing, as well as generally unhealthy.
- Accordingly, there is significant interest in developing other means to administer cannabis to patients. There remains an unmet need for topical formulations for administering cannabis or cannabinoid.
- In one aspect, provided are formulations comprising: at least one cannabinoid or a derivative thereof and at least one phyto-compound excipient, wherein said at least one phyto-compound excipient is a skin penetration enhancer that facilitates absorption and bioavailability of said at least one cannabinoid or said derivative thereof in a subject. In certain embodiments, the formulation is a topical or a transdermal formulation.
- In some exemplary embodiments, the formulation includes a first cannabinoid (e.g., THC or THCa) and a second cannabinoid (CBD or CBDa). In other exemplary embodiments, the formulation includes a first polymer (e.g., polyethylene glycol 1450) and a second polymer (e.g., polyethylene glycol 4000).
- In another aspect, provided are methods for treating a disease or disorder in a subject, the methods comprising administering to the subject, for example topically administering, a formulation disclosed herein.
- In yet another aspect, provided are methods for manufacturing a formulation disclosed herein. In certain embodiments, the method comprises the steps of providing one or more cannabinoids; providing one or more phyto-compound excipients; and mixing said one or more cannabinoids with said one or more phyto-compound excipients.
- In a further aspect, provided are metered dose devices having a formulation disclosed herein.
- In a still further aspect, provided herein are devices comprising a formulation described herein. In certain embodiments, the device comprises a regulated pump. In certain embodiments, the device comprises a metered-dosing mechanism. In certain embodiments, the device comprises an air-tight container to store the formulation. In certain embodiments, the device comprises the formulation in a plurality of metered doses. In certain embodiments, the device is an aerosol spray device.
- Other features and advantages of the present disclosure will become apparent from the following detailed description and examples. It should be understood, however, that the detailed description and the specific examples, while indicating embodiments of the invention, are given by way of illustration only, since various changes and modifications within the spirit and scope of the invention will become apparent to those skilled in the art from this detailed description.
- The present subject matter may be understood more readily by reference to the following detailed description which forms a part of this disclosure. It is to be understood that this invention is not limited to the specific products, methods, conditions, or parameters described and/or shown herein, and that the terminology used herein is for the purpose of describing particular embodiments by way of example only and is not intended to be limiting of the claimed invention.
- Unless otherwise defined herein, scientific and technical terms used in connection with the present application shall have the meanings that are commonly understood by those of ordinary skill in the art. Further, unless otherwise required by context, singular terms shall include pluralities and plural terms shall include the singular.
- As employed above and throughout the disclosure, the following terms and abbreviations, unless otherwise indicated, shall be understood to have the following meanings.
- In the present disclosure the singular forms “a,” “an,” and “the” include the plural reference, and reference to a particular numerical value includes at least that particular value, unless the context clearly indicates otherwise. Thus, for example, a reference to “a compound” is a reference to one or more of such compounds and equivalents thereof known to those skilled in the art, and so forth. The term “plurality”, as used herein, means more than one. When a range of values is expressed, another embodiment includes from the one particular and/or to the other particular value. Similarly, when values are expressed as approximations, by use of the antecedent “about,” it is understood that the particular value forms another embodiment. All ranges are inclusive and combinable.
- As used herein, the terms “treatment” or “therapy” (as well as different forms thereof) include preventative (e.g., prophylactic), curative, or palliative treatment. As used herein, the term “treating” includes alleviating or reducing at least one adverse or negative effect or symptom of a condition, disease, or disorder.
- By “transdermal” drug delivery is meant administration of a drug to the skin surface of an individual so that the drug passes through the skin tissue and into the individual's blood stream.
- The term “topical administration” is used in its conventional sense to mean delivery of an active agent to a body surface such as the skin or mucosa, as in, for example, topical drug administration in the prevention or treatment of various disorders, the application of cosmetics and cosmeceuticals (including moisturizers, masks, sunscreens, etc.), and the like. Topical administration, in contrast to transdermal administration, provides a local rather than a systemic effect.
- Similarly, when the term “transdermal” is used herein, as in “transdermal drug administration” and “transdermal drug delivery systems,” it is to be understood that unless explicitly indicated to the contrary, “topical” administration and systems are intended as well.
- The terms “subject,” “individual,” and “patient” are used interchangeably herein, and refer to an animal, for example a human, to whom treatment, including prophylactic treatment with the pharmaceutical formulation, is provided.
- The inventor of the instant application surprisingly and unexpectedly discovered a formulation which includes, in part, one or more cannabinoids in combination with one or more phyto-compound excipients. The presence of a phyto-compound excipient in the formulation facilitates absorption of a cannabinoid through an epidermis and a dermis. Furthermore, the presence of a phyto-compound excipient improves bioavailability of a cannabinoid.
- In one aspect, provided are formulations comprising: at least one cannabinoid or a derivative thereof and at least one phyto-compound excipient, wherein said at least one phyto-compound excipient is a skin penetration enhancer that facilitates absorption and bioavailability of said at least one cannabinoid or said derivative thereof in a subject. In certain embodiments, the formulation is a topical formulation. In other embodiments, the formulation is a transdermal formulation.
- Certain embodiments of the invention relate to compositions of one or more cannabinoids to provide, for example, a topical or a transdermal delivery of said one or more cannabinoids. The cannabinoids are easily prepared and formulated to provide consistent, therapeutically effective dosage forms from lot to lot.
- In certain embodiments, said formulation facilitates administration via a regulated pump or a metered-dosing device. In certain embodiments, said formulation is a homogeneous formulation.
- In certain embodiments, said cannabinoid is an extract from a cannabis plant.
- In certain embodiments, the formulation has a combination of at least two cannabinoids. In certain embodiments, the formulation comprises a combination of at least two cannabinoids. In certain embodiments, the two cannabinoids are selected from Tetrahydrocannabinolic acid (THCa), Cannabidiolic acid (CBDa), Cannabinolic acid (CBNa), Cannabichromenic acid (CBCa), Tetrahydrocannabinol (THC), Cannabidiol (CBD), Cannabigerol (CBG), Cannabigerolic Acid (CBGa), Cannabichromene (CBC), Cannabinol (CBN), Cannabielsoin (CBE), iso-Tetrahydrocannabinol (iso-THC), Cannabicyclol (CBL), Cannabicitran (CB T), Cannabivarin (CBV), Tetrahydrocannabivarin (THCV), Cannabidivarin (CBDV), Cannabichromevarin (CBCV), Cannabigerovarin (CBGV), Cannabigerol Monomethyl Ether (CBGM), and derivatives thereof. Examples of derivatives include, but are not limited to, esters, amides, and ethers of the compounds disclosed herein.
- In some embodiments, the cannabinoid is a cannabinoid extract that contains a combination of at least two of the following: Tetrahydrocannabinolic acid (THCa), Cannabidiolic acid (CBDa), Cannabinolic acid (CBNa), Cannabichromenic acid (CBCa), Tetrahydrocannabinol (THC), Cannabidiol (CBD), Cannabigerol (CBG), Cannabigerolic Acid (CBGa), Cannabichromene (CBC), Cannabinol (CBN), Cannabielsoin (CBE), iso-Tetrahydrocannabinol (iso-THC), Cannabicyclol (CBL), Cannabicitran (CBT), Cannabivarin (CBV), Tetrahydrocannabivarin (THCV), Cannabidivarin (CBDV), Cannabichromevarin (CBCV), Cannabigerovarin (CBGV), Cannabigerol Monomethyl Ether (CBGM) and derivatives thereof. The cannabinoid may be natural or synthetic.
- The methods of making cannabinoids extract is well known in the art. The cannabis plants are grown, harvested, and the cannabinoids are extracted through, for example, a CO2 extraction process.
- In certain embodiments, at least two cannabinoids are in a 1:1 proportion by weight. In certain embodiments, at least two cannabinoids are in a 10:1 proportion by weight. In certain embodiments, at least two cannabinoids are in a 20:1 proportion by weight. In certain embodiments, two cannabinoids are THC and CBD. In certain embodiments, two cannabinoids are THCa and CBDa.
- In certain embodiments, the two cannabinoids are in a 1:1 proportion by weight. In certain embodiments, the two cannabinoids are in a 10:1 proportion by weight. In certain embodiments, the two cannabinoids are in a 20:1 proportion by weight. In certain embodiments, the two cannabinoids are THC and CBD. In certain embodiments, the two cannabinoids are THCa and CBDa.
- In some embodiments, the formulation includes a first cannabinoid and a second cannabinoid. In certain exemplary embodiments, the first and second cannabinoids are in a ratio ranging from about 1:1 to about 20:1 proportion by weight. In certain embodiments, the first and second cannabinoids are in a 1:1 proportion by weight. In other embodiments, the first and second cannabinoids are in a 10:1 proportion by weight. In yet other embodiments, the first and second cannabinoids are in a 20:1 proportion by weight.
- In certain embodiments, the first cannabinoid is THC or THCa and the second cannabinoid is CBD or CBDa.
- In certain embodiments, the first cannabinoid is THC and the second cannabinoid is CBD.
- In certain embodiments, the first cannabinoid is THCa and the second cannabinoid is CBDa.
- In certain embodiments, the at least one cannabinoid is THC or THCa present in an amount ranging from about 0.01 mg to about 200 mg. In certain embodiments, the at least one cannabinoid is CBD or CBDa present in an amount ranging from about 0.01 mg to about 200 mg.
- In certain embodiments, the first cannabinoid can be present in an amount ranging from about 0.01 mg to about 200 mg. The second cannabinoid also can be present in an amount ranging from about 0.01 mg to about 200 mg.
- In some embodiments, the cannabinoids are in equal proportion such as, for example, 2.5 mg THC to 2.5 mg CBD. Other embodiments include proportions of THC/CBD of 0.25 mg THC to 5.0 mg CBD or 5.0 mg THC to 0.25 mg CBD.
- In some embodiments, the cannabinoid of the invention is any member of a group of substances that are structurally related to tetrahydrocannabinol and that bind to a cannabinoid receptor such as CB1 or CB2 or both (‘THC’). The cannabinoid can be a naturally occurring compound (e.g., present in Cannabis), a compound metabolized by a plant or animal, or a synthetic derivative.
- The cannabinoid may be included in its free form or in the form of a salt; an acid addition salt of an ester; an amide; an enantiomer; an isomer; a tautomer; a prodrug; a derivative of an active agent; different isomeric forms (e.g., enantiomers and diastereoisomers), both in pure form and in admixture, including racemic mixtures; or enol forms.
- The cannabinoids are further meant to encompass natural cannabinoids, natural cannabinoids that have been purified or modified, and synthetically derived cannabinoids. Methods for purifying cannabinoids from plant material, are well known in the art and fully described in, for example, United States Patent Application Publication 2005/0266108, which is incorporated by reference herein in its entirety.
- The cannabinoids can be any of 9-tetrahydrocannabinol, 8-tetrahydrocannabinol, (+)-1,1-dimethylheptyl analog of 7-hydroxy-delta-6-tetrahydrocannabinol, 3-(5-cyano-1′,1′-dimethylpentyl)-1-(4-N-morpholinobutyryloxy)-delta-8-tetrahydrocannabinol hydrochloride, dexanabinol, nabilone, levonantradol, and N-(2-hydroxyethyl)hexadecanoamide. In some embodiments, the cannabinoids can be any of the non-psychotropic cannabinoid 3-dimethylnepty 11 carboxylic acid homologine 8 and delta-8-tetrahydrocannabinol.
- In some embodiments, the cannabinoid extract comprises cannabinoids tincture. The term “tincture”, as used herein, refers to an alcoholic extract of plant material. Methods of tincture preparation are well known in the art and are described, for example, in the U.S. Pat. No. 9,468,865, hereby incorporated by reference in its entirety. In certain embodiments, the method of tincture preparation according to the present invention comprises the steps of combining medium chain triglycerides and polysorbate in a mixing vessel to form a first combination; mixing the first combination; adding the cannabinoid extract to the first combination to form a second combination; mixing the second combination; adding 200 proof ethanol to the second combination to form a third combination; and mixing the third combination for an extended period of time in order to obtain the cannabinoids tincture. The duration of the final mixing step may vary depending on many factors and can be easily optimized by a skilled artisan. In certain embodiments, the final mixing step ranges from about 5 to about 60 minutes. In other embodiments, the final mixing step ranges from about 10 to about 50 minutes. In other embodiments, the final mixing step ranges from about 15 to about 45 minutes. In other embodiments, the final mixing step ranges from about 20 to about 40 minutes.
- In another aspect, provided are formulations further comprising one or more phyto-compound excipients. In certain embodiments, the at least one phyto-compound excipient facilitates absorption of said at least one cannabinoid or said derivative through an epidermis or a dermis of the subject. In certain embodiments, the at least one phyto-compound excipient improves bioavailability of said at least one cannabinoid or said derivative in said subject.
- Examples of a phyto-compound excipient include, for example, but are not limited to, a terpene, an essential oil, papain, piperine, capsaicin, or an extract of Myristica fragrans. In certain embodiments, the at least one phyto-compound excipient is a terpene, an essential oil, papain, piperine, capsaicin, or an extract of Myristica fragrans.
- Examples of a terpene include, for example, but are not limited to, beta-myrcene, limonene, beta caryophyllene, caryophyllene oxide, terpineol, citronellol, linalool, humulene, beta-amyrin, cycloartenol, farnesol, menthol, eucalyptol, eugenol, and borneol. In certain embodiments, the terpene is selected from beta-myrcene, limonene, beta caryophyllene, caryophyllene oxide, terpineol, citronellol, linalool, humulene, beta-amyrin, cycloartenol, farnesol, menthol, eucalyptol, eugenol, and borneol.
- Examples of an essential oil include, for example, but are not limited to, eucalyptus oil, niaouli oil, fennel oil, cumin oil, almond oil, basil oil, Alpinia oxyphylla oil, turpentine oil, rosemary oil, and cardamom oil. In certain embodiments, the essential oil is selected from eucalyptus oil, niaouli oil, fennel oil, cumin oil, almond oil, basil oil, Alpinia oxyphylla oil, turpentine oil, rosemary oil, and cardamom oil.
- In some embodiments, the minor and major phyto-compounds in the formulation are used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the topical formulation. In other embodiments, the minor and major phyto-compounds in the formulation are used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the topical formulation.
- In some embodiments, the minor and major phyto-compounds in the formulation are used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the formulation. In other embodiments, the minor and major phyto-compounds in the formulation are used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the formulation.
- In some embodiments, the total cannabinoid content in the formulation is used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the topical formulation. In certain embodiments, the total cannabinoid content forms about 0.05% to 5% by weight based on 100 parts by weight of the topical formulation. In certain embodiments, the total cannabinoid content in the formulation is used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the topical formulation. In certain embodiments, the total cannabinoid content forms about 1.1% by weight based on 100 parts by weight of the topical formulation.
- In some embodiments, the total cannabinoid content in the formulation is used in an amount to give a content of from 0.05% to 5% by weight based on 100 parts by weight of the formulation. In certain embodiments, the total cannabinoid content forms about 0.05% to 5% by weight based on 100 parts by weight of the formulation. In certain embodiments, the total cannabinoid content in the formulation is used in an amount to give a content of about 1.1% by weight based on 100 parts by weight of the formulation. In certain embodiments, the total cannabinoid content forms about 1.1% by weight based on 100 parts by weight of the formulation.
- The formulation of the invention may also include additional ingredients such as solvents, carriers, or excipients.
- In certain embodiments, the formulation further comprises a solvent. In some embodiments, the solvent comprises ethanol, methanol, isopropanol, chloroform, propylene glycol, polyethylene glycol, glycerine, limonene, myrcene, linalool, alpha bisabolol, delta 3 carene, borneol, alpha-pinene, beta-pinene, eucalyptol, terpineol, caryophyllene, camphene, or combinations thereof. In certain embodiments, the solvent is ethanol.
- In certain embodiments, the formulation further comprises a pharmaceutically acceptable carrier. In some embodiments, the carrier comprises cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, starch, pregelatinized starch, dicalcium phosphate, tricalcium phosphate, or mixtures thereof. In other embodiments, the carrier may be comprised of a water-soluble sugar or sugar alcohol. Examples include, but not limited to, lactose, sucrose, dextrose, polydextrose, fructose, maltose, maltodextrin, dextrate, dextrin, lactitol, mannitol, erythritol, maltitol, sorbitol, or xylitol, and mixtures thereof.
- The formulation may further contain an ingredient commonly used in the pharmaceutical field. Examples of the ingredient include, but are not limited to, a diluent, a disintegrant, a binder, a lubricant, a colorant, a pH adjusting agent, a surfactant, a stabilizing agent, a sour agent, a flavor, a glidant, and the like. These ingredients are used in an amount commonly used in the pharmaceutical field unless otherwise specifically stated.
- Examples of the diluent include, but are not limited to, a sugar or a sugar alcohol such as lactose (e.g., lactose monohydrate), fructose, glucose, mannitol or sorbitol; a starch such as corn starch, potato starch, wheat starch, rice starch, partially pregelatinized starch, pregelatinized starch or porous starch; microcrystalline cellulose; anhydrous calcium phosphate, precipitated calcium carbonate, calcium silicate, and the like.
- In the formulation, the diluent is used in an amount to give a content of from 5% to 95% by weight based on 100 parts by weight of the formulation.
- Examples of a disintegrant include, but are not limited to, carboxymethyl cellulose, carboxymethyl cellulose calcium, carboxymethyl starch sodium, croscarmellose sodium, carmellose calcium, crospovidone, low-substituted hydroxypropyl cellulose, and hydroxypropyl starch. The amount of the disintegrant can be an amount to give a content of from 0.5 to 25 parts by weight based on 100 parts by weight of the formulation or the topical formulation.
- Examples of a binder include, but are not limited to, hydroxypropyl cellulose (e.g., grade: L, SL, SSL (trade name); Nippon Soda Co., Ltd.), hydroxypropylmethyl cellulose (e.g., hypromello se 2910 (e.g., TC-5 (grade: MW, E, EW, R, RW) (trade name); Shin-Etsu Chemical Co., Ltd.)), polyvinylpyrrolidone (povidone), and gum arabic.
- In the formulation, the binder is used in an amount to give a content of from 1% to 20% by weight based on 100 parts by weight of the formulation or the topical formulation.
- Examples of the lubricant include, but are not limited to, magnesium stearate, calcium stearate, talc, sucrose fatty acid ester, sodium stearyl fumarate and the like. The used amount of the lubricant is an amount to give a content of from about 0.5% to 2% by weight based on 100 parts by weight.
- Examples of the colorant include, but are not limited to, a food dye (e.g., food yellow No. 5, food red No. 2, food blue No. 2), a food lake color, iron oxide red, and iron oxide yellow.
- Examples of the pH adjusting agent include, but are not limited to, citrate, phosphate, carbonate, tartrate, fumarate, acetate, and amino acid salt.
- Examples of the surfactant include, but are not limited to, sodium lauryl sulfate, polysorbate 80, and polyoxyethylene (160) polyoxypropylene (30) glycol.
- The formulation may include a stabilizing agent that prevents separation or decomposition upon being transferred to a container or during transit or storage of said container.
- Examples of the stabilizing agent include, but are not limited to, tocopherol, tetrasodium edetate, nicotinamide, and a cyclodextrin.
- Examples of the sour agent include, but are not limited to, ascorbic acid, citric acid, tartaric acid, and malic acid.
- Examples of the flavor include, but are not limited to, menthol, Mentha oil, lemon oil, and vanillin.
- Examples of the glidant include, but are not limited to, colloidal silicon dioxide, aqueous silicon dioxide, and talc.
- The above ingredients may be used by combining two or more members at an appropriate ratio.
- The formulations disclosed herein include a composition for daily administration. In certain embodiments, the therapeutic effect is maintained with one unit, twice daily. In other embodiments, the therapeutic effect is maintained with one unit, three times daily. In certain exemplary embodiments, the duration of each dose's effect is between four (4) to six (6) hours.
- The formulation can be of any suitable form, for example, a cream, a lotion, or a gel. In certain embodiments, the formulation is a cream or lotion.
- In other aspects, provided herein are methods of treating a disease in a subject, the method comprising administering a formulation described herein. In other aspects, provided herein are methods of treating a disease in a subject, the method comprising administering to the subject a formulation described herein.
- In certain embodiments, the formulation is administered topically. In other embodiments, the formulation is administered transdermally.
- Examples of a disease or a disorder that can be treated by the invention include, but are not limited to, a skin disease or disorder, pain associated with cancer, neuropathic pain and HIV-associated sensory neuropathy, side effects of chemotherapy including nausea and pain, symptoms of neurological and neurodegenerative diseases such as Huntington's disease, Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, multiple sclerosis, epilepsy, post-traumatic stress disorder (PTSD), alcohol abuse, bipolar disorder, depression, anorexia nervosa; cancer such as gliomas, leukemia, skin tumors, colorectal cancer; diseases including hepatitis C, methicillin-resistant Staphylococcus aureus (MRSA), pruritus, psoriasis, asthma, sickle-cell disease, sleep apnea, digestive diseases, collagen-induced arthritis, atherosclerosis and dystonia. In certain embodiments, said administration is a topical administration. In other embodiments, said administration is a transdermal administration.
- Examples of a skin disease or disorder include, but are not limited to, itch, pain, and inflammation.
- In another aspect, provided herein are methods for manufacturing a formulation described herein. The methods may include the steps of: providing one or more cannabinoids; providing one or more phyto-compound excipients; and blending or mixing said one or more cannabinoids with said one or more phyto-compound excipients. These steps are carried out based on the techniques and processes known to one of skill in the art.
- In yet another aspect, provided herein are devices comprising: the formulation described herein. In certain embodiments, the device is an aerosol spray device which can spray the formulation on a skin of a subject. In some embodiments, the device includes a regulated pump. In other embodiments, the device includes a metered-dosing mechanism.
- The device may include an air-tight container to store said formulation. In some embodiments, the formulation is stored in a plurality of metered doses. In certain embodiments, the device comprises the formulation in a plurality of metered doses. In certain embodiments, the device is an aerosol spray device.
- All patents and literature references cited in the present specification are hereby incorporated by reference in their entirety.
- The present invention will be specifically explained by way of examples, but these examples are not intended to limit the present invention.
- In order that the invention described herein may be more fully understood, the following examples are set forth. The examples described in this application are offered to illustrate the compounds, pharmaceutical compositions, and methods provided herein and are not to be construed in any way as limiting their scope.
- Formulations described above are shown in Table 1 and are prepared using the methods described herein.
- The formulation is a therapeutic cream for topical or transdermal administration. The formulation includes a mixture of a therapeutic agent (e.g., cannabinoid extract) and a phyto-compound excipient.
- The formulation is suitable for topical or transdermal administration using a metered-dose aerosol spray device.
-
TABLE 1 The formulation having CBD and THC cannabinoid extract Concentration Ingredients (% w/w) CBD and THC cannabinoid extract 1.1% - Unless defined otherwise, all technical and scientific terms used herein have the same meanings as commonly understood by one of ordinary skill in the art.
- Having described embodiments of the present invention with reference to the accompanying drawings, it is to be understood that the present invention is not limited to the above-mentioned embodiments and that various changes and modifications can be affected by one skilled in the art without departing from the spirit or scope of the present invention as defined in the appended claims.
Claims (42)
1. A formulation comprising:
at least one cannabinoid or a derivative thereof; and
at least one phyto-compound excipient,
wherein said at least one phyto-compound excipient is a skin penetration enhancer that facilitates absorption and bioavailability of said at least one cannabinoid or said derivative thereof in a subject.
2. The formulation of claim 1 , wherein said formulation is a topical formulation.
3. The formulation of claim 1 , wherein said formulation is a transdermal formulation.
4. The formulation of any one of claims 1 -3 , wherein said formulation is a cream or a lotion.
5. The formulation of any one of claims 1 -4 , wherein said at least one phyto-compound excipient facilitates absorption of said at least one cannabinoid or said derivative through an epidermis or a dermis of said subject.
6. The formulation of any one of claims 1 -4 , wherein said at least one phyto-compound excipient improves bioavailability of said at least one cannabinoid or said derivative in said subject.
7. The formulation of any one of claims 1 -6 , wherein said formulation facilitates administration via a regulated pump or a metered-dosing device.
8. The formulation of any one of claims 1 -7 , wherein said formulation is a homogenous formulation.
9. The formulation of any one of claims 1 -8 , wherein said formulation further comprises a stabilizing agent that prevents separation or decomposition upon being transferred to a container or during transit or storage of said container.
10. The formulation of any one of claims 1 -9 , wherein said cannabinoid is an extract from a cannabis plant.
11. The formulation of any one of claims 1 -10 , wherein the formulation has a combination of at least two cannabinoids.
12. The formulation of claim 11 , wherein the two cannabinoids are selected from Tetrahydrocannabinolic acid (THCa), Cannabidiolic acid (CBDa), Cannabinolic acid (CBNa), Cannabichromenic acid (CBCa), Tetrahydrocannabinol (THC), Cannabidiol (CBD), Cannabigerol (CBG), Cannabigerolic Acid (CBGa), Cannabichromene (CBC), Cannabinol (CBN), Cannabielsoin (CBE), iso-Tetrahydrocannabinol (iso-THC), Cannabicyclol (CBL), Cannabicitran (CB T), Cannabivarin (CBV), Tetrahydrocannabivarin (THCV), Cannabidivarin (CBDV), Cannabichromevarin (CBCV), Cannabigerovarin (CBGV), Cannabigerol Monomethyl Ether (CBGM), and derivatives thereof.
13. The formulation of claim 11 or 12 , wherein the two cannabinoids are in a 1:1 proportion by weight.
14. The formulation of claim 11 or 12 , wherein the two cannabinoids are in a 10:1 proportion by weight.
15. The formulation of claim 11 or 12 , wherein the two cannabinoids are in a 20:1 proportion by weight.
16. The formulation of any one of claims 11 -15 , wherein the two cannabinoids are THC and CBD.
17. The formulation of any one of claims 11 -15 , wherein the two cannabinoids are THCa and CBDa.
18. The formulation of any one of claims 1 -17 , wherein said at least one cannabinoid is THC or THCa present in an amount ranging from about 0.01 mg to about 200 mg.
19. The formulation of any one of claims 1 -17 , wherein said at least one cannabinoid is CBD or CBDa present in an amount ranging from about 0.01 mg to about 200 mg.
20. The formulation of any one of claims 1 -19 , wherein the total cannabinoid content forms about 0.05% to 5% by weight based on 100 parts by weight of the topical formulation.
21. The formulation of any one of claims 1 -19 , wherein the total cannabinoid content forms about 1.1% by weight based on 100 parts by weight of the topical formulation.
22. The formulation of any one of claims 1 -21 , wherein said at least one phyto-compound excipient is a terpene, an essential oil, papain, piperine, capsaicin, or an extract of Myristica fragrans.
23. The formulation of claim 22 , wherein said terpene is selected from beta-myrcene, limonene, beta caryophyllene, caryophyllene oxide, terpineol, citronellol, linalool, humulene, beta-amyrin, cycloartenol, farnesol, menthol, eucalyptol, eugenol, and borneol.
24. The formulation of claim 22 , wherein said essential oil is selected from eucalyptus oil, niaouli oil, fennel oil, cumin oil, almond oil, basil oil, Alpinia oxyphylla oil, turpentine oil, rosemary oil, and cardamom oil.
25. The formulation of any one of claims 1 -24 , wherein the formulation further comprises a pharmaceutically acceptable carrier.
26. The formulation of claim 25 , wherein the pharmaceutically acceptable carrier is selected from cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, starch, pregelatinized starch, dicalcium phosphate, tricalcium phosphate, and mixtures thereof.
27. The formulation of claim 25 , wherein the pharmaceutically acceptable carrier is microcrystalline cellulose.
28. The formulation of any one of claims 1 -27 , wherein the formulation further comprises a solvent.
29. The formulation of claim 28 , wherein the solvent is selected from ethanol, methanol, isopropanol, chloroform, propylene glycol, polyethylene glycol, glycerine, limonene, myrcene, linalool, alpha bisabolol, delta 3 carene, borneol, alpha-pinene, beta-pinene, eucalyptol, terpineol, caryophyllene, camphene, and combinations thereof
30. The formulation of claim 28 , wherein the solvent is ethanol.
31. A method for treating a disease in a subject, the method comprising administering to the subject a formulation according to any one of the claims 1 -30 .
32. The method of claim 31 , wherein the disease is selected from a skin disease or disorder, pain associated with cancer, neuropathic pain and HIV-associated sensory neuropathy, side effects of chemotherapy including nausea and pain, symptoms of neurological and neurodegenerative diseases such as Huntington's disease, Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, multiple sclerosis, epilepsy, post-traumatic stress disorder (PTSD), alcohol abuse, bipolar disorder, depression, anorexia nervosa; cancer such as gliomas, leukemia, skin tumors, colorectal cancer;
diseases including hepatitis C, methicillin-resistant Staphylococcus aureus (MRSA), pruritus, psoriasis, asthma, sickle-cell disease, sleep apnea, digestive diseases, collagen-induced arthritis, atherosclerosis and dystonia.
33. The method of claim 31 , wherein said administration is a topical administration.
34. The method of claim 31 , wherein said administration is a transdermal administration.
35. The method of claim 32 , wherein said skin disease is an itch, inflammation, or pain.
36. A method for manufacturing a formulation of any one of claims 1 -30 , the method comprising the steps of:
providing one or more cannabinoids;
providing one or more phyto-compound excipients; and
mixing said one or more cannabinoids with said one or more phyto-compound excipients.
37. A device comprising a formulation according to any one of the claims 1 -30 .
38. The device of claim 37 , wherein said device comprises a regulated pump.
39. The device of claim 37 , wherein said device comprises a metered-dosing mechanism.
40. The device of claim 37 , wherein said device comprises an air-tight container to store said formulation.
41. The device of claim 37 , wherein said device comprises said formulation in a plurality of metered doses.
42. The device of claim 37 , wherein said device is an aerosol spray device.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US17/420,335 US20220105070A1 (en) | 2019-01-04 | 2020-01-03 | Topical formulations having cannabinoid |
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201962788484P | 2019-01-04 | 2019-01-04 | |
PCT/US2020/012187 WO2020142692A1 (en) | 2019-01-04 | 2020-01-03 | Topical formulations having cannabinoid |
US17/420,335 US20220105070A1 (en) | 2019-01-04 | 2020-01-03 | Topical formulations having cannabinoid |
Publications (1)
Publication Number | Publication Date |
---|---|
US20220105070A1 true US20220105070A1 (en) | 2022-04-07 |
Family
ID=69740517
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US17/420,335 Pending US20220105070A1 (en) | 2019-01-04 | 2020-01-03 | Topical formulations having cannabinoid |
US17/361,113 Pending US20210321668A1 (en) | 2019-01-04 | 2021-06-28 | Vaporizer mouthpiece |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US17/361,113 Pending US20210321668A1 (en) | 2019-01-04 | 2021-06-28 | Vaporizer mouthpiece |
Country Status (4)
Country | Link |
---|---|
US (2) | US20220105070A1 (en) |
EP (1) | EP3905906A1 (en) |
CA (1) | CA3125568A1 (en) |
WO (1) | WO2020142351A1 (en) |
Family Cites Families (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11344683B2 (en) * | 2010-05-15 | 2022-05-31 | Rai Strategic Holdings, Inc. | Vaporizer related systems, methods, and apparatus |
US20140174458A1 (en) * | 2012-12-21 | 2014-06-26 | Samuel Aaron Katz | Self-contained electronic smoking device that produces smoke and ash by incineration |
CN106028850B (en) * | 2014-02-12 | 2019-05-17 | 吉瑞高新科技股份有限公司 | Electronic cigarette and its flow controlling method of air |
KR20150000417U (en) * | 2014-05-15 | 2015-01-27 | 황일영 | Cover for drip tip and electric cigarette having the same |
WO2016079152A1 (en) * | 2014-11-17 | 2016-05-26 | Mcneil Ab | Disposable cartridge for use in an electronic nicotine delivery system |
GB2533135B (en) * | 2014-12-11 | 2020-11-11 | Nicoventures Holdings Ltd | Aerosol provision systems |
UA125169C2 (en) * | 2015-04-23 | 2022-01-26 | Олтріа Клайєнт Сервісиз Ллк | Unitary heating element and heater assemblies, cartridges, and e-vapor devices including a unitary heating element |
RU2715686C2 (en) * | 2015-06-12 | 2020-03-02 | Филип Моррис Продактс С.А. | Biological control in electronic smoking articles |
US9993025B2 (en) * | 2016-07-25 | 2018-06-12 | Fontem Holdings 1 B.V. | Refillable electronic cigarette clearomizer |
WO2018165769A1 (en) * | 2017-03-17 | 2018-09-20 | Poda Technologies Ltd. | Closed bottom vaporizer pod |
GB201717497D0 (en) * | 2017-10-24 | 2017-12-06 | British American Tobacco Investments Ltd | A mouthpiece assembly |
GB201717496D0 (en) * | 2017-10-24 | 2017-12-06 | British American Tobacco Investments Ltd | A cartridge for an aerosol provision device |
US10939702B2 (en) * | 2018-10-12 | 2021-03-09 | Rai Strategic Holdings, Inc. | Connectors for forming electrical and mechanical connections between interchangeable units in an aerosol delivery system |
MX2021004144A (en) * | 2018-10-15 | 2021-06-08 | Juul Labs Inc | Heating element. |
GB201818080D0 (en) * | 2018-11-06 | 2018-12-19 | Nicoventures Trading Ltd | Vapour provision systems |
GB201909883D0 (en) * | 2019-07-10 | 2019-08-21 | Nicoventures Trading Ltd | Vapour delivery systems |
CN110279162A (en) * | 2019-07-30 | 2019-09-27 | 深圳雾芯科技有限公司 | Atomising device and its method |
JP7235644B2 (en) * | 2019-11-28 | 2023-03-08 | 日本たばこ産業株式会社 | Power supply unit of aerosol generator, body unit of aerosol generator, aerosol generator, and non-combustion inhaler |
EP4008203A1 (en) * | 2020-12-04 | 2022-06-08 | Shenzhen Eigate Technology Co., Ltd. | Electronic cigarette comprising one-way valve |
AU2022309247A1 (en) * | 2021-07-15 | 2024-02-29 | Rai Strategic Holdings, Inc. | Non-combustible aerosol provision systems with atomizer-free consumables |
US20230172280A1 (en) * | 2021-12-07 | 2023-06-08 | Hava Health, inc. | Vaporization device |
-
2019
- 2019-12-26 WO PCT/US2019/068617 patent/WO2020142351A1/en unknown
- 2019-12-26 EP EP19858656.2A patent/EP3905906A1/en active Pending
- 2019-12-26 CA CA3125568A patent/CA3125568A1/en active Pending
-
2020
- 2020-01-03 US US17/420,335 patent/US20220105070A1/en active Pending
-
2021
- 2021-06-28 US US17/361,113 patent/US20210321668A1/en active Pending
Non-Patent Citations (6)
Title |
---|
"Derivative." Merriam-Webster.com Dictionary, Merriam-Webster, https://www.merriam-webster.com/dictionary/derivative. Accessed 9 May. 2024. (Year: 2024) * |
Bruni et. al. (2018), Cannabinoid Delivery Systems for Pain and Inflammation Treatment, Molecules, 28, 1 – 25 (Year: 2018) * |
CBD Alive (https://web.archive.org/web/20180813002822/https://www.cbdalive.org/cbd-salve/ ) (Year: 2018) * |
CBD Alive with wayback toolbar (https://web.archive.org/web/20180813002822/https://www.cbdalive.org/cbd-salve/ ; cited by applicant on IDS) (Year: 2018) * |
Semelka et. al. ,2016, Diagnosis and Treatment of Obstructive Sleep Apnea in Adults, American Family Physician, 94, 355-361 (Year: 2016) * |
Steigerwald, et. al., (2018, The Form and Content of Cannabis Products in the United States, J Gen Intern Med., 33, 1426-1428) (Year: 2018) * |
Also Published As
Publication number | Publication date |
---|---|
EP3905906A1 (en) | 2021-11-10 |
CA3125568A1 (en) | 2020-07-09 |
WO2020142351A1 (en) | 2020-07-09 |
US20210321668A1 (en) | 2021-10-21 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
EP3906025A1 (en) | Topical formulations having cannabinoid | |
US10307392B2 (en) | Compound and method for treatment of diseases and disorders | |
US11077086B2 (en) | Solid dosage form composition for buccal or sublingual administration of cannabinoids | |
US20200163931A1 (en) | Oral composition of extracted cannabinoids and methods of use thereof | |
EP0971743B1 (en) | Stabilized medicaments containing cysteinyl derivatives | |
US20200170994A1 (en) | Sublingual cannabinoid compositions | |
AU2007298814B2 (en) | Galenic form for the trans-mucosal delivery of active ingredients | |
CA3118895A1 (en) | Suppository formulations having cannabinoid | |
US20190374502A1 (en) | Cannabinoid-Containing Fatty Acid Formulations for Treating Disorders of the Nervous System | |
US20200384048A1 (en) | Compound and method for treatment of movement disorders | |
US20190183849A1 (en) | Compound and method for treatment of diseases and disorders | |
KR20240031326A (en) | Use of Sublingual Dexmedetomidine for the treatment of Agitation | |
WO2020146383A1 (en) | Inhalable dosage form of cannabinoid extract | |
US20190183953A1 (en) | Immunologically active phyto-mixture and its use in the prevention and in a method for treatment of efflorescences | |
US20220023220A1 (en) | Rapidly disintegrating oral tablet | |
US20220105070A1 (en) | Topical formulations having cannabinoid | |
US20210378967A1 (en) | Hard-pressed scored splittable marijuana tablets | |
US11903992B2 (en) | Composition comprising lidocaine, l-carnosine and dexpanthenol | |
US20230270766A1 (en) | Methods and compositions for the treatment of als | |
JP2024519537A (en) | COMPOSITIONS COMPRISING CANNABIDIOL FOR APPLICATION IN BODY CAVITIES - Patent application | |
Hu et al. | Advances and perspectives on pharmacological activities and mechanisms of the monoterpene borneol | |
DE29707005U1 (en) | Stabilized drug containing cysteinyl derivatives |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
STPP | Information on status: patent application and granting procedure in general |
Free format text: APPLICATION UNDERGOING PREEXAM PROCESSING |
|
AS | Assignment |
Owner name: COLUMBIA CARE LLC, NEW YORK Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:DELY, AARON MICHAEL;BEN-ARI, SHAUN;SIGNING DATES FROM 20200114 TO 20200120;REEL/FRAME:058269/0071 |
|
STPP | Information on status: patent application and granting procedure in general |
Free format text: DOCKETED NEW CASE - READY FOR EXAMINATION |
|
STPP | Information on status: patent application and granting procedure in general |
Free format text: NON FINAL ACTION MAILED |