MXPA99005003A - Lubricious self-standing (intact) gel for oral delivery of biologically-active ingredients - Google Patents
Lubricious self-standing (intact) gel for oral delivery of biologically-active ingredientsInfo
- Publication number
- MXPA99005003A MXPA99005003A MXPA/A/1999/005003A MX9905003A MXPA99005003A MX PA99005003 A MXPA99005003 A MX PA99005003A MX 9905003 A MX9905003 A MX 9905003A MX PA99005003 A MXPA99005003 A MX PA99005003A
- Authority
- MX
- Mexico
- Prior art keywords
- agents
- further characterized
- active ingredient
- analgesics
- biologically active
- Prior art date
Links
- 239000004480 active ingredient Substances 0.000 title claims abstract description 62
- 239000000203 mixture Substances 0.000 claims abstract description 53
- 229920002148 Gellan gum Polymers 0.000 claims abstract description 35
- 239000000216 gellan gum Substances 0.000 claims abstract description 23
- 239000004615 ingredient Substances 0.000 claims abstract description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 11
- 239000002207 metabolite Substances 0.000 claims abstract description 6
- 239000003814 drug Substances 0.000 claims description 63
- 229940079593 drugs Drugs 0.000 claims description 41
- -1 meclofentamate Chemical compound 0.000 claims description 31
- 239000000730 antalgic agent Substances 0.000 claims description 30
- 239000003795 chemical substances by application Substances 0.000 claims description 26
- 229940035676 ANALGESICS Drugs 0.000 claims description 24
- 230000000202 analgesic Effects 0.000 claims description 24
- 235000010492 gellan gum Nutrition 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 19
- 229920000591 gum Polymers 0.000 claims description 15
- 150000001768 cations Chemical class 0.000 claims description 14
- 238000002156 mixing Methods 0.000 claims description 14
- 239000011782 vitamin Substances 0.000 claims description 14
- 235000013343 vitamin Nutrition 0.000 claims description 14
- 229930003231 vitamins Natural products 0.000 claims description 14
- 229940088594 Vitamin Drugs 0.000 claims description 12
- 235000015872 dietary supplement Nutrition 0.000 claims description 12
- 150000003722 vitamin derivatives Chemical class 0.000 claims description 12
- XLOMVQKBTHCTTD-UHFFFAOYSA-N zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 claims description 12
- 239000011787 zinc oxide Substances 0.000 claims description 12
- 235000014692 zinc oxide Nutrition 0.000 claims description 12
- 238000001879 gelation Methods 0.000 claims description 11
- 230000001050 lubricating Effects 0.000 claims description 11
- CNQOEXOJUIMDHW-FVGYRXGTSA-N (2S)-2-(6-methoxynaphthalen-2-yl)propanoic acid;sodium Chemical group [Na].C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CNQOEXOJUIMDHW-FVGYRXGTSA-N 0.000 claims description 10
- CGIGDMFJXJATDK-UHFFFAOYSA-N Indometacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims description 10
- 230000001225 therapeutic Effects 0.000 claims description 10
- CMWTZPSULFXXJA-VIFPVBQESA-N Naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims description 9
- 229910052500 inorganic mineral Inorganic materials 0.000 claims description 9
- 235000010755 mineral Nutrition 0.000 claims description 9
- 239000011707 mineral Substances 0.000 claims description 9
- 229960002009 naproxen Drugs 0.000 claims description 9
- 239000003792 electrolyte Substances 0.000 claims description 8
- 238000004519 manufacturing process Methods 0.000 claims description 8
- 102000004169 proteins and genes Human genes 0.000 claims description 8
- 108090000623 proteins and genes Proteins 0.000 claims description 8
- 239000001263 FEMA 3042 Substances 0.000 claims description 7
- 229940033123 Tannic Acid Drugs 0.000 claims description 7
- LRBQNJMCXXYXIU-NRMVVENXSA-N Tannic acid Chemical compound OC1=C(O)C(O)=CC(C(=O)OC=2C(=C(O)C=C(C=2)C(=O)OC[C@@H]2[C@H]([C@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)O2)OC(=O)C=2C=C(OC(=O)C=3C=C(O)C(O)=C(O)C=3)C(O)=C(O)C=2)O)=C1 LRBQNJMCXXYXIU-NRMVVENXSA-N 0.000 claims description 7
- 239000004599 antimicrobial Substances 0.000 claims description 7
- 238000001816 cooling Methods 0.000 claims description 7
- 239000000314 lubricant Substances 0.000 claims description 7
- 229940021182 non-steroidal anti-inflammatory drugs Drugs 0.000 claims description 7
- 238000005063 solubilization Methods 0.000 claims description 7
- 235000015523 tannic acid Nutrition 0.000 claims description 7
- 229920002258 tannic acid Polymers 0.000 claims description 7
- 229940035674 ANESTHETICS Drugs 0.000 claims description 6
- 229940116904 ANTIINFLAMMATORY THERAPEUTIC RADIOPHARMACEUTICALS Drugs 0.000 claims description 6
- 229940022659 Acetaminophen Drugs 0.000 claims description 6
- 229940023808 Albuterol Drugs 0.000 claims description 6
- 208000006673 Asthma Diseases 0.000 claims description 6
- KUVIULQEHSCUHY-XYWKZLDCSA-N Beclometasone dipropionate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O KUVIULQEHSCUHY-XYWKZLDCSA-N 0.000 claims description 6
- 229940092703 Beclomethasone Dipropionate Drugs 0.000 claims description 6
- 229960005274 Benzocaine Drugs 0.000 claims description 6
- BLFLLBZGZJTVJG-UHFFFAOYSA-N Benzocaine Chemical compound CCOC(=O)C1=CC=C(N)C=C1 BLFLLBZGZJTVJG-UHFFFAOYSA-N 0.000 claims description 6
- XWTYSIMOBUGWOL-UHFFFAOYSA-N Bricaril Chemical compound CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1 XWTYSIMOBUGWOL-UHFFFAOYSA-N 0.000 claims description 6
- QWOJMRHUQHTCJG-UHFFFAOYSA-N CC([CH2-])=O Chemical compound CC([CH2-])=O QWOJMRHUQHTCJG-UHFFFAOYSA-N 0.000 claims description 6
- 229940105847 Calamine Drugs 0.000 claims description 6
- PUFQVTATUTYEAL-UHFFFAOYSA-N Cinchocaine Chemical compound C1=CC=CC2=NC(OCCCC)=CC(C(=O)NCCN(CC)CC)=C21 PUFQVTATUTYEAL-UHFFFAOYSA-N 0.000 claims description 6
- 229940030606 DIURETICS Drugs 0.000 claims description 6
- 229940120099 Dibucaine Drugs 0.000 claims description 6
- 229960000385 Dyclonine Drugs 0.000 claims description 6
- BZEWSEKUUPWQDQ-UHFFFAOYSA-N Dyclonine Chemical compound C1=CC(OCCCC)=CC=C1C(=O)CCN1CCCCC1 BZEWSEKUUPWQDQ-UHFFFAOYSA-N 0.000 claims description 6
- RDJGLLICXDHJDY-UHFFFAOYSA-N Fenoprofen Chemical compound OC(=O)C(C)C1=CC=CC(OC=2C=CC=CC=2)=C1 RDJGLLICXDHJDY-UHFFFAOYSA-N 0.000 claims description 6
- 229960001419 Fenoprofen Drugs 0.000 claims description 6
- 229940088597 Hormone Drugs 0.000 claims description 6
- DKYWVDODHFEZIM-UHFFFAOYSA-N Ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims description 6
- 229940065725 Leukotriene receptor antagonists for obstructive airway diseases Drugs 0.000 claims description 6
- HYYBABOKPJLUIN-UHFFFAOYSA-N Mefenamic acid Chemical compound CC1=CC=CC(NC=2C(=CC=CC=2)C(O)=O)=C1C HYYBABOKPJLUIN-UHFFFAOYSA-N 0.000 claims description 6
- 229940074726 OPHTHALMOLOGIC ANTIINFLAMMATORY AGENTS Drugs 0.000 claims description 6
- QYSPLQLAKJAUJT-UHFFFAOYSA-N Piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 claims description 6
- DQKXQSGTHWVTAD-UHFFFAOYSA-N Pramocaine Chemical compound C1=CC(OCCCC)=CC=C1OCCCN1CCOCC1 DQKXQSGTHWVTAD-UHFFFAOYSA-N 0.000 claims description 6
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N Prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 claims description 6
- MVFGUOIZUNYYSO-UHFFFAOYSA-N Prilocaine Chemical compound CCCNC(C)C(=O)NC1=CC=CC=C1C MVFGUOIZUNYYSO-UHFFFAOYSA-N 0.000 claims description 6
- NDAUXUAQIAJITI-UHFFFAOYSA-N Salbutamol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-UHFFFAOYSA-N 0.000 claims description 6
- 229960005105 Terbutaline Sulfate Drugs 0.000 claims description 6
- 229960002372 Tetracaine Drugs 0.000 claims description 6
- GKCBAIGFKIBETG-UHFFFAOYSA-N Tetracaine Chemical compound CCCCNC1=CC=C(C(=O)OCCN(C)C)C=C1 GKCBAIGFKIBETG-UHFFFAOYSA-N 0.000 claims description 6
- UPSPUYADGBWSHF-UHFFFAOYSA-N Tolmetin Chemical compound C1=CC(C)=CC=C1C(=O)C1=CC=C(CC(O)=O)N1C UPSPUYADGBWSHF-UHFFFAOYSA-N 0.000 claims description 6
- GFNANZIMVAIWHM-OBYCQNJPSA-N Triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 claims description 6
- 229930003268 Vitamin C Natural products 0.000 claims description 6
- NNJVILVZKWQKPM-UHFFFAOYSA-N Xylocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims description 6
- 229960001296 Zinc Oxide Drugs 0.000 claims description 6
- NWONKYPBYAMBJT-UHFFFAOYSA-L Zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 claims description 6
- 230000003444 anaesthetic Effects 0.000 claims description 6
- 230000001396 anti-anti-diuretic Effects 0.000 claims description 6
- 230000001387 anti-histamine Effects 0.000 claims description 6
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 6
- 230000001754 anti-pyretic Effects 0.000 claims description 6
- 239000003529 anticholesteremic agent Substances 0.000 claims description 6
- 239000000935 antidepressant agent Substances 0.000 claims description 6
- 239000000739 antihistaminic agent Substances 0.000 claims description 6
- 239000002221 antipyretic Substances 0.000 claims description 6
- 239000003443 antiviral agent Substances 0.000 claims description 6
- 239000002249 anxiolytic agent Substances 0.000 claims description 6
- 239000003212 astringent agent Substances 0.000 claims description 6
- 229950000210 beclometasone dipropionate Drugs 0.000 claims description 6
- 230000000271 cardiovascular Effects 0.000 claims description 6
- 229960001747 cinchocaine Drugs 0.000 claims description 6
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 6
- 239000002934 diuretic Substances 0.000 claims description 6
- 239000003995 emulsifying agent Substances 0.000 claims description 6
- 239000003193 general anesthetic agent Substances 0.000 claims description 6
- 229910052864 hemimorphite Inorganic materials 0.000 claims description 6
- 239000005556 hormone Substances 0.000 claims description 6
- 239000003018 immunosuppressive agent Substances 0.000 claims description 6
- 229960000991 ketoprofen Drugs 0.000 claims description 6
- 239000003199 leukotriene receptor blocking agent Substances 0.000 claims description 6
- 229960004194 lidocaine Drugs 0.000 claims description 6
- 229960003464 mefenamic acid Drugs 0.000 claims description 6
- 229910052751 metal Inorganic materials 0.000 claims description 6
- 239000002184 metal Substances 0.000 claims description 6
- 150000002739 metals Chemical class 0.000 claims description 6
- RZVAJINKPMORJF-UHFFFAOYSA-N p-acetaminophenol Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 6
- 229960005489 paracetamol Drugs 0.000 claims description 6
- 229960002702 piroxicam Drugs 0.000 claims description 6
- 229920000642 polymer Polymers 0.000 claims description 6
- 229960001896 pramocaine Drugs 0.000 claims description 6
- 229940093883 pramoxine Drugs 0.000 claims description 6
- 229960004618 prednisone Drugs 0.000 claims description 6
- 229960001807 prilocaine Drugs 0.000 claims description 6
- 230000000241 respiratory Effects 0.000 claims description 6
- 229960002052 salbutamol Drugs 0.000 claims description 6
- 239000003352 sequestering agent Substances 0.000 claims description 6
- 150000003431 steroids Chemical class 0.000 claims description 6
- 230000000152 swallowing Effects 0.000 claims description 6
- 229960001017 tolmetin Drugs 0.000 claims description 6
- 229960005294 triamcinolone Drugs 0.000 claims description 6
- 235000019154 vitamin C Nutrition 0.000 claims description 6
- 239000011718 vitamin C Substances 0.000 claims description 6
- 150000003700 vitamin C derivatives Chemical class 0.000 claims description 6
- 229960001763 zinc sulfate Drugs 0.000 claims description 6
- 229910000368 zinc sulfate Inorganic materials 0.000 claims description 6
- CPYIZQLXMGRKSW-UHFFFAOYSA-N zinc;iron(3+);oxygen(2-) Chemical compound [O-2].[O-2].[O-2].[O-2].[Fe+3].[Fe+3].[Zn+2] CPYIZQLXMGRKSW-UHFFFAOYSA-N 0.000 claims description 6
- 229960000905 Indomethacin Drugs 0.000 claims description 5
- ABBQHOQBGMUPJH-UHFFFAOYSA-M Sodium salicylate Chemical group [Na+].OC1=CC=CC=C1C([O-])=O ABBQHOQBGMUPJH-UHFFFAOYSA-M 0.000 claims description 5
- 230000000118 anti-eoplastic Effects 0.000 claims description 5
- 239000002246 antineoplastic agent Substances 0.000 claims description 5
- 235000013305 food Nutrition 0.000 claims description 5
- 230000036571 hydration Effects 0.000 claims description 5
- 238000006703 hydration reaction Methods 0.000 claims description 5
- 229960001680 ibuprofen Drugs 0.000 claims description 5
- 230000000631 nonopiate Effects 0.000 claims description 5
- 238000002360 preparation method Methods 0.000 claims description 5
- 229960004025 sodium salicylate Drugs 0.000 claims description 5
- PTTPUWGBPLLBKW-UHFFFAOYSA-M sodium;2-[4-(2-methylpropyl)phenyl]propanoate Chemical compound [Na+].CC(C)CC1=CC=C(C(C)C([O-])=O)C=C1 PTTPUWGBPLLBKW-UHFFFAOYSA-M 0.000 claims description 5
- 239000000725 suspension Substances 0.000 claims description 4
- 239000000654 additive Substances 0.000 claims description 3
- 229910052783 alkali metal Inorganic materials 0.000 claims description 3
- 229910052784 alkaline earth metal Inorganic materials 0.000 claims description 3
- 229910052708 sodium Inorganic materials 0.000 claims description 3
- 239000011734 sodium Substances 0.000 claims description 3
- 229920000858 Cyclodextrin Polymers 0.000 claims description 2
- 229940097362 Cyclodextrins Drugs 0.000 claims description 2
- 150000001340 alkali metals Chemical class 0.000 claims description 2
- 150000001342 alkaline earth metals Chemical class 0.000 claims description 2
- 150000001413 amino acids Chemical class 0.000 claims description 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-O ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims description 2
- 239000002563 ionic surfactant Substances 0.000 claims description 2
- 239000002736 nonionic surfactant Substances 0.000 claims description 2
- KEAYESYHFKHZAL-UHFFFAOYSA-N sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims description 2
- 210000003169 Central Nervous System Anatomy 0.000 claims 10
- 241000208680 Hamamelis mollis Species 0.000 claims 5
- 229940035363 MUSCLE RELAXANTS Drugs 0.000 claims 5
- 229940083876 Muscle relaxants FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE Drugs 0.000 claims 5
- MLKXDPUZXIRXEP-MFOYZWKCSA-N Sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 claims 5
- 229940118846 Witch Hazel Drugs 0.000 claims 5
- 230000001773 anti-convulsant Effects 0.000 claims 5
- 239000001961 anticonvulsive agent Substances 0.000 claims 5
- 230000036772 blood pressure Effects 0.000 claims 5
- 230000000747 cardiac effect Effects 0.000 claims 5
- 229960001760 dimethyl sulfoxide Drugs 0.000 claims 5
- 230000002255 enzymatic Effects 0.000 claims 5
- 230000002496 gastric Effects 0.000 claims 5
- 239000003158 myorelaxant agent Substances 0.000 claims 5
- 239000000021 stimulant Substances 0.000 claims 5
- 108091008136 Waterwitch Proteins 0.000 claims 1
- 235000016709 nutrition Nutrition 0.000 claims 1
- 150000003385 sodium Chemical group 0.000 claims 1
- 239000000499 gel Substances 0.000 description 68
- 239000000243 solution Substances 0.000 description 21
- 230000035492 administration Effects 0.000 description 12
- 239000006187 pill Substances 0.000 description 8
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 8
- 230000000670 limiting Effects 0.000 description 7
- 241001465754 Metazoa Species 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 239000007924 injection Substances 0.000 description 6
- 229920000615 alginic acid Polymers 0.000 description 5
- 235000010443 alginic acid Nutrition 0.000 description 5
- 229920001285 xanthan gum Polymers 0.000 description 5
- 239000000230 xanthan gum Substances 0.000 description 5
- 235000010493 xanthan gum Nutrition 0.000 description 5
- 229940082509 xanthan gum Drugs 0.000 description 5
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 4
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 4
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N Theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 150000004676 glycans Polymers 0.000 description 4
- 229920001282 polysaccharide Polymers 0.000 description 4
- 239000005017 polysaccharide Substances 0.000 description 4
- 150000004804 polysaccharides Polymers 0.000 description 4
- 239000001103 potassium chloride Substances 0.000 description 4
- 235000011164 potassium chloride Nutrition 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 229940086709 Ascorbic Acid 250 MG/ML Drugs 0.000 description 3
- 229940113118 Carrageenan Drugs 0.000 description 3
- 241001391944 Commicarpus scandens Species 0.000 description 3
- BAUYGSIQEAFULO-UHFFFAOYSA-L Iron(II) sulfate Chemical compound [Fe+2].[O-]S([O-])(=O)=O BAUYGSIQEAFULO-UHFFFAOYSA-L 0.000 description 3
- 229960003940 Naproxen sodium Drugs 0.000 description 3
- 229940056360 Penicillin G Drugs 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 235000010418 carrageenan Nutrition 0.000 description 3
- 239000000679 carrageenan Substances 0.000 description 3
- 229920001525 carrageenan Polymers 0.000 description 3
- 239000007897 gelcap Substances 0.000 description 3
- 239000003349 gelling agent Substances 0.000 description 3
- 229910000358 iron sulfate Inorganic materials 0.000 description 3
- CDBRNDSHEYLDJV-FVGYRXGTSA-M naproxen sodium Chemical compound [Na+].C1=C([C@H](C)C([O-])=O)C=CC2=CC(OC)=CC=C21 CDBRNDSHEYLDJV-FVGYRXGTSA-M 0.000 description 3
- 235000010987 pectin Nutrition 0.000 description 3
- 239000001814 pectin Substances 0.000 description 3
- 229920001277 pectin Polymers 0.000 description 3
- 239000008188 pellet Substances 0.000 description 3
- 239000011780 sodium chloride Substances 0.000 description 3
- 239000000829 suppository Substances 0.000 description 3
- AOJJSUZBOXZQNB-TZSSRYMLSA-N ADRIAMYCIN Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 description 2
- 229940009456 Adriamycin Drugs 0.000 description 2
- AVKUERGKIZMTKX-NJBDSQKTSA-N Ampicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=CC=C1 AVKUERGKIZMTKX-NJBDSQKTSA-N 0.000 description 2
- 229940064005 Antibiotic throat preparations Drugs 0.000 description 2
- 229940083879 Antibiotics FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE Drugs 0.000 description 2
- 229940042052 Antibiotics for systemic use Drugs 0.000 description 2
- 229940042786 Antitubercular Antibiotics Drugs 0.000 description 2
- OROGSEYTTFOCAN-DNJOTXNNSA-N Codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 description 2
- 229960004679 Doxorubicin Drugs 0.000 description 2
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 2
- 229920002581 Glucomannan Polymers 0.000 description 2
- 229940093922 Gynecological Antibiotics Drugs 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 210000004185 Liver Anatomy 0.000 description 2
- 229940023488 Pill Drugs 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N Salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- 229960002180 Tetracycline Drugs 0.000 description 2
- OFVLGDICTFRJMM-WESIUVDSSA-N Tetracycline Chemical compound C1=CC=C2[C@](O)(C)[C@H]3C[C@H]4[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]4(O)C(O)=C3C(=O)C2=C1O OFVLGDICTFRJMM-WESIUVDSSA-N 0.000 description 2
- 239000004098 Tetracycline Substances 0.000 description 2
- 229960000278 Theophylline Drugs 0.000 description 2
- 229940024982 Topical Antifungal Antibiotics Drugs 0.000 description 2
- 229940029983 VITAMINS Drugs 0.000 description 2
- 229940021016 Vitamin IV solution additives Drugs 0.000 description 2
- 229940072056 alginate Drugs 0.000 description 2
- 229960003022 amoxicillin Drugs 0.000 description 2
- LSQZJLSUYDQPKJ-NJBDSQKTSA-N amoxicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=C(O)C=C1 LSQZJLSUYDQPKJ-NJBDSQKTSA-N 0.000 description 2
- 229960000723 ampicillin Drugs 0.000 description 2
- 239000003242 anti bacterial agent Substances 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 230000003115 biocidal Effects 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- UXVMQQNJUSDDNG-UHFFFAOYSA-L cacl2 Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 2
- 239000001110 calcium chloride Substances 0.000 description 2
- 229910001628 calcium chloride Inorganic materials 0.000 description 2
- 235000009508 confectionery Nutrition 0.000 description 2
- 229960000520 diphenhydramine Drugs 0.000 description 2
- 239000012153 distilled water Substances 0.000 description 2
- 229960003276 erythromycin Drugs 0.000 description 2
- 238000000855 fermentation Methods 0.000 description 2
- 230000004151 fermentation Effects 0.000 description 2
- 238000005755 formation reaction Methods 0.000 description 2
- 235000015203 fruit juice Nutrition 0.000 description 2
- 229920000159 gelatin Polymers 0.000 description 2
- 239000008273 gelatin Substances 0.000 description 2
- 235000019322 gelatine Nutrition 0.000 description 2
- 235000011852 gelatine desserts Nutrition 0.000 description 2
- 239000000017 hydrogel Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 229940079866 intestinal antibiotics Drugs 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000006011 modification reaction Methods 0.000 description 2
- 229940005935 ophthalmologic Antibiotics Drugs 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 235000019364 tetracycline Nutrition 0.000 description 2
- LUEWUZLMQUOBSB-FSKGGBMCSA-N (2S,3S,4S,5S,6R)-2-[(2R,3S,4R,5R,6S)-6-[(2R,3S,4R,5S,6S)-4,5-dihydroxy-2-(hydroxymethyl)-6-[(2R,4R,5S,6R)-4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxan-3-yl]oxy-4,5-dihydroxy-2-(hydroxymethyl)oxan-3-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol 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]2[C@H](O[C@@H](OC3[C@H](O[C@@H](O)[C@@H](O)[C@H]3O)CO)[C@@H](O)[C@H]2O)CO)[C@H](O)[C@H]1O LUEWUZLMQUOBSB-FSKGGBMCSA-N 0.000 description 1
- 229940086223 Acetaminophen 100 MG/ML Drugs 0.000 description 1
- 241000251468 Actinopterygii Species 0.000 description 1
- 229940023040 Acyclovir Drugs 0.000 description 1
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 229920001817 Agar Polymers 0.000 description 1
- 241000416162 Astragalus gummifer Species 0.000 description 1
- SEBMTIQKRHYNIT-UHFFFAOYSA-N Azatadine Chemical compound C1CN(C)CCC1=C1C2=NC=CC=C2CCC2=CC=CC=C21 SEBMTIQKRHYNIT-UHFFFAOYSA-N 0.000 description 1
- 229960003071 Bacitracin Drugs 0.000 description 1
- 108010001478 Bacitracin Proteins 0.000 description 1
- 229960000686 Benzalkonium Chloride Drugs 0.000 description 1
- ISAOCJYIOMOJEB-UHFFFAOYSA-N Benzoin Chemical compound C=1C=CC=CC=1C(O)C(=O)C1=CC=CC=C1 ISAOCJYIOMOJEB-UHFFFAOYSA-N 0.000 description 1
- 229960002130 Benzoin Drugs 0.000 description 1
- 239000004342 Benzoyl peroxide Substances 0.000 description 1
- KGBXLFKZBHKPEV-UHFFFAOYSA-N Boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- ZDIGNSYAACHWNL-UHFFFAOYSA-N Brompheniramine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Br)C=C1 ZDIGNSYAACHWNL-UHFFFAOYSA-N 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 229960001777 Castor Oil Drugs 0.000 description 1
- SOYKEARSMXGVTM-UHFFFAOYSA-N Chlorphenamine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 SOYKEARSMXGVTM-UHFFFAOYSA-N 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- 229940009997 Cromolyn Drugs 0.000 description 1
- 229920002558 Curdlan Polymers 0.000 description 1
- 239000001879 Curdlan Substances 0.000 description 1
- 229960001140 Cyproheptadine Drugs 0.000 description 1
- JJCFRYNCJDLXIK-UHFFFAOYSA-N Cyproheptadine Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2C=CC2=CC=CC=C21 JJCFRYNCJDLXIK-UHFFFAOYSA-N 0.000 description 1
- 229940020371 Dextromethorphan 5 MG/ML Drugs 0.000 description 1
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N Diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 1
- KBAUFVUYFNWQFM-UHFFFAOYSA-N Doxylamine succinate Chemical compound OC(=O)CCC(O)=O.C=1C=CC=NC=1C(C)(OCCN(C)C)C1=CC=CC=C1 KBAUFVUYFNWQFM-UHFFFAOYSA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241000283086 Equidae Species 0.000 description 1
- 241000282326 Felis catus Species 0.000 description 1
- 229940013317 Fish Oils Drugs 0.000 description 1
- 210000001035 Gastrointestinal Tract Anatomy 0.000 description 1
- 229920001503 Glucan Polymers 0.000 description 1
- 229940093912 Gynecological Sulfonamides Drugs 0.000 description 1
- 241000208690 Hamamelis Species 0.000 description 1
- VKYKSIONXSXAKP-UHFFFAOYSA-N Hexamethylenetetramine Chemical compound C1N(C2)CN3CN1CN2C3 VKYKSIONXSXAKP-UHFFFAOYSA-N 0.000 description 1
- LLPOLZWFYMWNKH-CMKMFDCUSA-N Hydrocodone Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)CC(=O)[C@@H]1OC1=C2C3=CC=C1OC LLPOLZWFYMWNKH-CMKMFDCUSA-N 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 229940033518 INSECTICIDES AND REPELLENTS Drugs 0.000 description 1
- OMPJBNCRMGITSC-UHFFFAOYSA-N Incidol Chemical compound C=1C=CC=CC=1C(=O)OOC(=O)C1=CC=CC=C1 OMPJBNCRMGITSC-UHFFFAOYSA-N 0.000 description 1
- PWWVAXIEGOYWEE-UHFFFAOYSA-N Isophenergan Chemical compound C1=CC=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 PWWVAXIEGOYWEE-UHFFFAOYSA-N 0.000 description 1
- 235000019900 KELCOGEL® Nutrition 0.000 description 1
- DLNKOYKMWOXYQA-APPZFPTMSA-N L-Norpseudoephedrine Chemical compound C[C@@H](N)[C@H](O)C1=CC=CC=C1 DLNKOYKMWOXYQA-APPZFPTMSA-N 0.000 description 1
- 235000010643 Leucaena leucocephala Nutrition 0.000 description 1
- 240000007472 Leucaena leucocephala Species 0.000 description 1
- 229940029985 MINERAL SUPPLEMENTS Drugs 0.000 description 1
- 235000011430 Malus pumila Nutrition 0.000 description 1
- 235000015103 Malus silvestris Nutrition 0.000 description 1
- 229940041655 Meperidine Drugs 0.000 description 1
- USSIQXCVUWKGNF-UHFFFAOYSA-N Methadone Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 description 1
- 229960004011 Methenamine Drugs 0.000 description 1
- 208000010125 Myocardial Infarction Diseases 0.000 description 1
- 235000000380 Nyssa aquatica Nutrition 0.000 description 1
- 241000283898 Ovis Species 0.000 description 1
- 206010033799 Paralysis Diseases 0.000 description 1
- 229940049954 Penicillin Drugs 0.000 description 1
- XADCESSVHJOZHK-UHFFFAOYSA-N Petidina Chemical compound C=1C=CC=CC=1C1(C(=O)OCC)CCN(C)CC1 XADCESSVHJOZHK-UHFFFAOYSA-N 0.000 description 1
- 229960000395 Phenylpropanolamine Drugs 0.000 description 1
- 108010093965 Polymyxin B Proteins 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 240000005204 Prunus armeniaca Species 0.000 description 1
- 235000009827 Prunus armeniaca Nutrition 0.000 description 1
- 229960003908 Pseudoephedrine Drugs 0.000 description 1
- KWGRBVOPPLSCSI-WCBMZHEXSA-N Pseudoephedrine Chemical compound CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WCBMZHEXSA-N 0.000 description 1
- 240000004808 Saccharomyces cerevisiae Species 0.000 description 1
- 229940069764 Shark liver oil Drugs 0.000 description 1
- 241000790234 Sphingomonas elodea Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 240000008975 Styrax benzoin Species 0.000 description 1
- 235000000126 Styrax benzoin Nutrition 0.000 description 1
- MNQYNQBOVCBZIQ-JQOFMKNESA-A Sucralfate Chemical compound O[Al](O)OS(=O)(=O)O[C@@H]1[C@@H](OS(=O)(=O)O[Al](O)O)[C@H](OS(=O)(=O)O[Al](O)O)[C@@H](COS(=O)(=O)O[Al](O)O)O[C@H]1O[C@@]1(COS(=O)(=O)O[Al](O)O)[C@@H](OS(=O)(=O)O[Al](O)O)[C@H](OS(=O)(=O)O[Al](O)O)[C@@H](OS(=O)(=O)O[Al](O)O)O1 MNQYNQBOVCBZIQ-JQOFMKNESA-A 0.000 description 1
- 229960004291 Sucralfate Drugs 0.000 description 1
- 241000282887 Suidae Species 0.000 description 1
- 235000008411 Sumatra benzointree Nutrition 0.000 description 1
- 244000269722 Thea sinensis Species 0.000 description 1
- 229940116362 Tragacanth Drugs 0.000 description 1
- 229920001615 Tragacanth Polymers 0.000 description 1
- XEFQLINVKFYRCS-UHFFFAOYSA-N Triclosan Chemical compound OC1=CC(Cl)=CC=C1OC1=CC=C(Cl)C=C1Cl XEFQLINVKFYRCS-UHFFFAOYSA-N 0.000 description 1
- 229960003962 Trifluridine Drugs 0.000 description 1
- VSQQQLOSPVPRAZ-RRKCRQDMSA-N Trifluridine Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(C(F)(F)F)=C1 VSQQQLOSPVPRAZ-RRKCRQDMSA-N 0.000 description 1
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K Trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 description 1
- 229940054492 Unisom Drugs 0.000 description 1
- 229960003636 Vidarabine Drugs 0.000 description 1
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Vitamin C Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 1
- 241000589636 Xanthomonas campestris Species 0.000 description 1
- 229960004150 aciclovir Drugs 0.000 description 1
- 230000002378 acidificating Effects 0.000 description 1
- 239000011149 active material Substances 0.000 description 1
- MKUXAQIIEYXACX-UHFFFAOYSA-N acyclovir Chemical compound N1C(N)=NC(=O)C2=C1N(COCCO)C=N2 MKUXAQIIEYXACX-UHFFFAOYSA-N 0.000 description 1
- 239000008272 agar Substances 0.000 description 1
- 235000010419 agar Nutrition 0.000 description 1
- 230000003110 anti-inflammatory Effects 0.000 description 1
- 230000000259 anti-tumor Effects 0.000 description 1
- 239000007798 antifreeze agent Substances 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 229960000383 azatadine Drugs 0.000 description 1
- 235000008452 baby food Nutrition 0.000 description 1
- CLKOFPXJLQSYAH-ABRJDSQDSA-N bacitracin A Chemical compound C1SC([C@@H](N)[C@@H](C)CC)=N[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]1C(=O)N[C@H](CCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2N=CNC=2)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC1 CLKOFPXJLQSYAH-ABRJDSQDSA-N 0.000 description 1
- 229960003328 benzoyl peroxide Drugs 0.000 description 1
- 235000019400 benzoyl peroxide Nutrition 0.000 description 1
- 229960000626 benzylpenicillin Drugs 0.000 description 1
- 239000004327 boric acid Substances 0.000 description 1
- 229960002645 boric acid Drugs 0.000 description 1
- 229960000725 brompheniramine Drugs 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 235000015218 chewing gum Nutrition 0.000 description 1
- 229960003291 chlorphenamine Drugs 0.000 description 1
- 229960004126 codeine Drugs 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 229960000265 cromoglicic acid Drugs 0.000 description 1
- 235000019316 curdlan Nutrition 0.000 description 1
- 229940078035 curdlan Drugs 0.000 description 1
- 239000002781 deodorant agent Substances 0.000 description 1
- PCHPORCSPXIHLZ-UHFFFAOYSA-N diphenhydramine hydrochloride Chemical compound [Cl-].C=1C=CC=CC=1C(OCC[NH+](C)C)C1=CC=CC=C1 PCHPORCSPXIHLZ-UHFFFAOYSA-N 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- VLARUOGDXDTHEH-UHFFFAOYSA-L disodium cromoglycate Chemical compound [Na+].[Na+].O1C(C([O-])=O)=CC(=O)C2=C1C=CC=C2OCC(O)COC1=CC=CC2=C1C(=O)C=C(C([O-])=O)O2 VLARUOGDXDTHEH-UHFFFAOYSA-L 0.000 description 1
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 1
- 229910000397 disodium phosphate Inorganic materials 0.000 description 1
- 235000019800 disodium phosphate Nutrition 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 238000005538 encapsulation Methods 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 239000004083 gastrointestinal agent Substances 0.000 description 1
- 239000012213 gelatinous substance Substances 0.000 description 1
- 229940046240 glucomannan Drugs 0.000 description 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 235000019382 gum benzoic Nutrition 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 235000010299 hexamethylene tetramine Nutrition 0.000 description 1
- 235000012907 honey Nutrition 0.000 description 1
- 229960000240 hydrocodone Drugs 0.000 description 1
- 239000003317 industrial substance Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000000977 initiatory Effects 0.000 description 1
- 229940079867 intestinal antiinfectives Sulfonamides Drugs 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 229960001797 methadone Drugs 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 239000003094 microcapsule Substances 0.000 description 1
- 235000020786 mineral supplement Nutrition 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 229960004927 neomycin Drugs 0.000 description 1
- 229920000847 nonoxynol Polymers 0.000 description 1
- 229940005938 ophthalmologic antiinfectives Sulfonamides Drugs 0.000 description 1
- 235000015205 orange juice Nutrition 0.000 description 1
- 239000008385 outer phase Substances 0.000 description 1
- 230000036961 partial Effects 0.000 description 1
- 239000002304 perfume Substances 0.000 description 1
- 229960000482 pethidine Drugs 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 239000000419 plant extract Substances 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229960005266 polymyxin B Drugs 0.000 description 1
- 229920000024 polymyxin B Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 229960003910 promethazine Drugs 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 230000035807 sensation Effects 0.000 description 1
- 239000010686 shark liver oil Substances 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- 235000019982 sodium hexametaphosphate Nutrition 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229940026752 topical Sulfonamides Drugs 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- 239000011778 trisodium citrate Substances 0.000 description 1
- 235000019263 trisodium citrate Nutrition 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- ZTHWFVSEMLMLKT-CAMOTBBTSA-N vidarabine monohydrate Chemical compound O.C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@@H]1O ZTHWFVSEMLMLKT-CAMOTBBTSA-N 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N β-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 1
Abstract
The present invention relates to a composition comprising-gellan gum, water and a biologically-active ingredient for subsequent providing to and release of said ingredient, active metabolite thereof and/or active derivative thereof or mixtures thereof and the like in a human or animal from a self-lubricated, free-standing gel via effective administration thereto.
Description
SELF-CONTAINED LUBRICANT GEL (INTACT) FOR SUPPLY
ORAL BIOLOGICALLY ACTIVE INGREDIENTS
The present invention relates to a self-contained (intact) lubricating (self-lubricating) hydrogel composition comprising gellan gum and a biologically active medicinal ingredient. This invention also relates to a process for preparing said composition comprising gellan gum for subsequent delivery to a human or animal, whereby a therapeutically effective amount of the biologically active ingredient is provided and administered by any of the oral, vaginal and other administrations. rectal in a useful and effective way for the recipient (patient).
BACKGROUND OF THE INVENTION
It has sometimes been difficult to administer oral medications to people who have difficulty swallowing pills such as children, the elderly, paralyzed people or victims of heart attacks and strokes. Some patients can not eat from a bowl and spoon or have physical or physical difficulty swallowing whole pills. Patients weakened by illness and radiation therapy may have trouble taking pills. Some forms of drug can not or should not be chewed. Pediatric or geriatric patients do not want to take pills. Sometimes the pills are crushed in hospitals, after which the powder pellet is placed in a paper or plastic medicine cup and a suspension vehicle is added, such as orange juice, apricot juice, mashed apple, honey or baby food. However, care must be taken when crushing medications, as one medication could be easily mixed with another medication. In all cases, the patient must obtain the full prescribed dosage. Sub-dosing of a patient can occur when a patient does not get his full dose of an active therapeutic agent. This underdosing does not provide the answer sought by the doctor. Overdose may cause adverse reactions that may be harmful to the patient. The slow or uncertain response time for the initiation of an observable reaction to a drug in pill form when taken orally makes it difficult to determine when a suitable dose has been administered for a particular patient; the doctor can not know in an hour if the patient has been underdosed or overdosed. It is extremely important that there is agreement between the medical staff and patients, which is manifested in providing the right amount of medication at the appropriate intervals. Sometimes injections may be given to avoid the use of oral administration routes. However, injecting a drug (usually intravenously or intramuscularly) can cause rapid entry of the drug into the patient's bloodstream. The injection changes the rate of elimination of the drug from the body because the drug is not delivered to the liver of the body at the same speed as with a pill. In addition, injections are not for everyone. Sometimes injections can cause physical strain and worsen a patient's weakened condition, so injections may be undesirable in such situations. This invention provides an alternative to the use of pellets and pellet and injection grinding techniques for administering certain known (known) therapeutic amounts of medicament to patients by the use of a self-contained (intact) lubricating gel containing a certain (known) therapeutic amount. of medication for the patient. A.M.Bhakoo, S. Woerty and R. Duncan, Reléase of Antibiotics and
Antitumour Agents from Alginate and Gellan Gum Gels. Proceed. Intem. Symp. Control. Re!. Bioact. Mater., 18 (1991), Controlled Relay Society.
Inc., describe hydrogels that have been developed as controlled release matrices for pharmaceutically active chemicals. This reference describes that alginate gels (high M or high G) and gellan gum were first prepared and then loaded with drugs (adriamycin, theophylline, ampicillin, amoxicillin, tetracycline and erythromycin) by inhibition over a period of 24 hours, and subsequently determined the degree of entrapment, not known before gel formation.
Document WPO9402029-A1 describes an article of manufacture consisting of a spongy matrix whose pores are controlled in size and / or distribution, and which is made of a co-processed mixture comprising (a) glucomannan and (b) at least one other aqueous gel-forming polysaccharide. However, apparently no procedure is provided to incorporate drugs or minerals, vitamins or supplements, or therapeutic agents or other biologically active ingredients in said gels. Japanese Patent Application 89-0724239, "Transparent Gel-Like Composition", describes a polysaccharide of high molecular weight at 0.1-1.3.
% by weight based on the total amount of a composition that is added to water, and the mixture is heated (e.g., to 90 ° C), stirred, dissolved and then cooled (e.g., to about 50 ° C). C), after which a volatile substance selected from perfumes, deodorants, moth proofing agents, insecticides and repellents, a suitable amount of a surface active agent (e.g., a non-ionic substance) is added for solubilization and, if necessary, an antifreeze agent (eg, polyhydric alcohol) and an antiseptic agent, and the mixture is further stirred, allowed to cool (eg, to about 40 ° C), placed in a container and allowed to cool further to room temperature. environment to obtain the composition. Japanese Patent Application 87-126943, "Heat-Resistant Water-based Gel", discloses that an aqueous suspension of gellan gum is heated to about 95 ° C above the solution formation temperature to obtain a homogeneous aqueous solution; To the solution is added an acid (eg, citric acid, fruit juice, etc.) and calcium chloride, etc., reporting that the solution is gelatinized by cooling to below the gelling temperature to obtain the water-based gel resistant to the desired heat. Japanese patent application 87-126942, "Gelation of Gellan Gum", describes a mixture of water and gellan gum which is reported as a type of polysaccharide which is produced in advance and which is heated to approximately 85 ° C, which is a solution temperature of gellan gum. The aqueous gellan gum solution produced is added with an acid (e.g., citric acid, fruit juice) and the mixture is cooled to below the gelatinization temperature to carry out the gelatinization of the solution and obtain the gel water gel gelano desired. The amount of the acid is preferably 15% of the gellan gum. Japanese patent application 88-309150"Production of Instant Gelatinous Substance" discloses gellan gum compositions dissolved after heating or being dispersed and suspended in water at room temperature to prepare an aqueous solution at approximately 1.0-2% by weight of gellan gum . It is disclosed that an alkaline earth metal salt and / or alkali metal salt and / or acidic substance, such as an organic or inorganic acid and acid salts, induce gelation at room temperature. It is said that the utility is for food, medicine, industrial chemicals, etc. The patent of E.U. No. 5,342,626, which was issued to Philip E. Winston Jr. and others on August 30, 1994, describes "Composition and Process for Gelatin-Free Soft Capsules" and refers to a polymer composition comprising gelano, carrageenan and gums of morning tea and a process for producing flexible films for encapsulation comprising the composition of gelano, carrageenan and morning gum. It is reported that said films can be used for the production of capsules or microcapsules. It is believed that the capsules are characterized by a dry outer phase (film membrane) which contains a different liquid or solid ingredient in its internal phase. The patent of E.U. No. 4,857,331, which was issued to James J. Shaw et al. On August 15, 1989, describes self-contained pectin / algin / gelatin gels that require a structuring agent to increase gel strength, and in particular this patent also discloses a sugar-free ingestible gel confectionery delivery system that includes a pectin gel component, an algin gel component and a polymer network gel component in sufficient quantities to form a unit of gel confectionery The delivery system may also include an additional active ingredient such as a drug, drug or nutritional supplement.
However, the industry has continued to recognize the need for an improved method for providing consent to the delivery of drugs to patients, which is provided by this invention.
OBJECTS OF THE INVENTION
It is an object of the invention to provide a novel system and method as a utility for effectively delivering a known effective amount of drug, such as a unit amount, to patients who are unable to tolerate currently available drug delivery systems and methods. Yet another object of this invention is to administer a pharmaceutical preparation that is non-tacky, palatable, easy to swallow, or easy to break if needed, from a unit dose, to people of all ages (e.g., pediatric or geriatric patients) and animals, thus achieving consent with the desired mechanism. Another object of the invention is to provide an effective drug delivery system for those who can not tolerate pills, tablets, capsules, troches, pallets and chewing gums containing medicaments, and the like. Still another object of the invention is to provide a useful method for delivering drugs to people who have difficulty swallowing.
A further object of this invention is to provide an easy-to-break gel, if desired, to mix it with food or to produce smaller and easier pieces to swallow by humans and animals. Another object of this invention is to provide an easy-to-administer intact lubricant gel for oral and / or vaginal and / or rectal applications. A further object of this invention is to provide an effective drug delivery system for animals. These and other objects are satisfied in the invention, which is described hereinafter more particularly in detail.
BRIEF DESCRIPTION OF THE INVENTION
This invention comprises a self-contained (intact) lubricating gel and a process for the production of a self-contained (intact) lubricating gel containing an effective and known amount of a biologically active (medicinal) ingredient to subsequently deliver to, and release into a biological system human or animal a therapeutic amount of a biologically active medicinal ingredient, by means of which the biologically active ingredient is delivered to the biological systems of the patient for effective medical relief of the patient. These self-contained lubricating gels can be used for any type of administration including oral, vaginal or rectal. The product and method of the present invention also include a composition in which the gel delivery system can be molded directly or configured to fit the receptacle that is used to supply and deliver the medication unit to the consumer. The process for the preparation of the gels of this invention comprises mixing gellan gum with water at a concentration of about 0.05% to about 5% and preferably about 0.25% to about 2.5% by weight of said gum to form a composition containing gum , with or without a sequestrant, and maintaining said gum composition at a temperature sufficiently hot to achieve hydration of said gum in a hot solution, such that gelation occurs after subsequent cooling, and mixing a known amount of a biologically active medicinal ingredient with said hot solution and optionally mixing with it solubilization and suspension aids, and optionally mixing cations and subsequently cooling said hot solution containing said biologically active ingredient at a temperature in sufficient scale to induce gelation in molds of f desired orms where said self-contained (intact) lubricating gel containing a known amount of active is formed.
DETAILED DESCRIPTION OF THE INVENTION
This invention comprises a process for the production of a self-contained (intact) lubricating gel containing a known and effective amount of a biologically active ingredient for subsequent release into a human or animal biological system, which comprises mixing gellan gum with water to a concentration of about 0.05% to about 5% and preferably about 0.25% to about 2.5% by weight of said gum to form a gum-containing composition, with or without a sequestrant, and maintaining said gum composition at a temperature sufficiently hot to achieve hydration of said gum, such that gelation occurs after subsequent cooling; mixing a biologically active ingredient with said hot solution and optionally mixing with it solubilization and suspension aids (for the biologically active ingredient, i.e., the drug) and optionally mixing other polymers or additives, if desired, to alter the characteristics of resistance or release of the gel; optionally mixing cations and subsequently cooling said hot solution containing said biologically active ingredient at a temperature in sufficient scale to induce gelation, whereby said self-contained (intact) lubricating gel is formed.
As used herein, the term "self-contained" includes, but is not limited to, a gel or gels that are capable of maintaining or remaining in an erect state and that are generally non-pourable or flowable. As used herein, the term "lubricant" includes, but is not limited to, a gel having a wet, substantially wet (wet) or partially moist surface, such that the gel has the feel of a wet surface for the patient (or a manual sensation for suppositories). Gellan gum is a known natural polysaccharide that is produced by inoculating a carefully formulated fermentation medium with the microorganism Sphingomonas elodea (ATTC 31461). Gellan gum is available in transparent forms (KELCOGEL®) and (GELRITE®) available from Monsanto Company, E.U.A. The gelation mechanism of gellan gum is based on the association of macromolecular chains induced by cations. As used herein, the term gellan gum includes the non-transparent, transparent and partially transparent, native, deacylated and partially deacylated forms, as well as mixtures thereof. Useful gellan gums include those commercially available, but are not limited to those sold commercially by Monsanto Company, 800 North Lindbergh BIvd., St. Louis, Missouri, 63167, E.U.A. The processes for preparing gellan gum include those described in the U.S. patents. Nos. 4,326,052 and 4,236,053 to Kang, both of which are incorporated herein by reference in their entirety. The processes for preparing a gel composition of this invention are preferably carried out at a temperature in step 1 (a) from about 50 ° C to about 100 ° C, and are maintained at or near that temperature until that temperature is reached. the gum is hydrated or hydrated substantially. Alternatively, hydration can be achieved at room temperature in the presence of suitable sequestrants. The hydration process is carried out until it is completed or substantially completed, which is when the gum is completely or nearly or sufficiently hydrated, usually resulting in a clear or substantially transparent solution. The method of mixing the above biologically active medicinal ingredient is typically carried out at a temperature above the gel fixation point for a time that is necessary to solubilize or effectively suspend said biologically active ingredient. In this way, the biologically active ingredient is inside or in the gel. If desired, other polymers (organic or natural) or additives may be added to the composition to alter the texture characteristics and / or release of the gels. Such polymers include but are not limited to one or more of the following: xanthan gum, cellulose derivatives, carrageenan, glucan, curdlan, agar, gelatin, alginates, starch, pectin.
mixtures of xanthan gum with gaicomannans and / or glucomannans, mixtures thereof and the like. An illustrative xanthan gum which may be employed herein includes the sold xanthan gum (s) and are trademarks owned by Monsanto Company, 800 North Lindbergh BIvd, St.
Louis, Missouri, 63167 E.U.A. Xanthan gum is an exocellular heteropolysaccharide typically produced by a fermentation process of the bacterium Xanthomonas campestris. If desired, suitable sequestrants which may be employed herein include sodium citrate, sodium hexametaphosphate (SHMP), disodium phosphate, mixtures thereof, and the like. The sequestering amount employed may be from about 0.05% by weight to about 0.5% by weight. If desired, larger and smaller amounts of sequestrant can be used. The scale that is preferred for an additional optimal cation usage level herein is generally from about 0.5 to about 500 mM, or about (0.5 to about 15 mM for divalent cations and about 10 to about 500 mM for monovalent cations for example). If desired, solubilization aids (which without being limited by theory are believed to help solubilize the biologically active ingredients) and are preferably selected from the group consisting of ionic or non-ionic surfactants and cyclodextrins, mixtures thereof, may be employed. and similar. In an embodiment in which the cations are employed with the process of this invention, the cations that are preferred are those selected from the group consisting of alkali metals, alkaline earth metals and ammonium. In another embodiment of the invention, it is preferred that the cations used be part of the biologically active ingredient if desired. The amount of any solubilization aid employed depends on the application. This may vary from about 0.1% to about 50% or more. The biologically active ingredient is not limited and includes, but is not limited to, one or more biologically active ingredients that provide a therapeutic and / or medicinal and / or pharmacological value to a recipient, either by themselves or through an active metabolite and / or active derivative. The biologically active ingredient includes any ingredient or similar ingredient that provides said or a similar value completely or in part, initially or subsequently, directly or indirectly such as through active metabolites or active derivatives of any kind, in whole or in part, mixtures of the same, to a receiver. The biologically active ingredient is preferably (but not limited to) one or more selected from the group consisting of nutritional supplements (eg, vitamins, minerals, mineral supplements, plant extracts, amino acids, electrolytes and proteins), anti-inflammatory agents (e.g. , NSAIDS such as ibuprofen, ketoprofen, fenoprofen, indomethacin, meclofentamate, mefenamic acid, naproxen, fenibutazone, piroxicam, tolmetin, suiindac and dimethyl sulfoxide), analgesics, antipyretics, anesthetics including benzocaine, pramoxine, dibucaine, dyclonine, lidocaine, mepycaine , prilocaine and tetracaine; emulsifiers (including benzoin, acacia, tragacanth, polyvinyl alcohol and glycerin); analgesics that include opiate analgesics (eg, codeine or hydrocodone), non-opiate analgesics (eg, meperidine or methadone), non-narcotic analgesics that include acetaminophen and astringents that include calamine, zinc oxide, tannic acid, water of Hamamelis, zinc sulfate; (for example, benzalkonium chloride, carbamate peroxide, tannic acid, salicylic acid, triclosan, benzoyl peroxide and boric acid); natural or synthetic steroids including triamcinolone, acetonide, prednisone, beclomethasone dipropionate; asthmatic drugs that include terbutaline sulfate, albuterol, leukotriene receptor antagonists; electrolytes, metals and minerals; anti-anxiety and antidepressant agents; antimicrobial and antiviral agents (e.g., acyclovir, neomycin, bacitracin, polymyxin B, vidarabine, trifluridine, zidovucine, methenamine, nonoxynol sulfonamides and other antibiotics); (for example, fish oils, shark liver oil, castor oil, sucralfate and liver yeast cell derivatives); antihistamines and respiratory agents (e.g., diphenhydramine, promethazine, cromolyn, cyproheptadine and azatadine); immunosuppressive agents; cholesterol lowering agents; agents for high blood pressure, cardiovascular and diuretics, hormones, proteins and active agents of enzyme, antineoplastics, gastrointestinal agents, adriamycin, theophylline, ampicillin, amoxicillin, tetracycline and erythromycin, and mixtures thereof and the like. Mixtures of any one or more of these and many acceptable ingredients can be employed. Illustrative but not limiting examples of useful biologically active ingredients that may be employed herein include without limitation those mentioned in the American Society of Pharmacologists of the Health System, 1997, [AFHS Drug Information 97] edited by Gerald K. McEvoy, Bethesda, MD; American Society of Health-System Pharmacists which is incorporated herein by reference in its entirety. Illustrative and non-limiting examples of biologically active ingredients useful herein include also those without limitation as described Hardman, G.G; [Goodman & Gilman's The Pharmacological basis of Therapeutics], 9a. edition, 1996; NY; McGraw-Hill, Health Professions Division which is also incorporated herein by reference in its entirety. After reading this description including the examples, those skilled in the art will recognize that a wide variety of such biologically active ingredients can be employed in the practice of this invention. A non-limiting example of a useful biologically active ingredient is a nutritional supplement and a non-limiting example thereof is a vitamin. Vitamin C can be used herein as a vitamin in the practice of this invention. Potassium chloride is a non-limiting example of a mineral useful herein. Other useful and non-limiting biologically active ingredients include sodium naproxen, sodium salicylate and ibuprofen, mixtures thereof and the like. Additional non-limiting examples are shown in the table on page 23. A therapeutically effective amount of a biologically active ingredient is preferably employed in the gel or gels of this invention. Typically, the amount of biologically active ingredient used in each gel is the amount that is considered therapeutically effective for use, etc., and it is also an amount that the gel will be able to handle. Higher or lower active ingredient loads may be employed in the gels if desired. Typically, for sodium naproxen, from about 50 mg / ml to about 125 mg / ml (mg of active / ml gel can be used (see examples). Higher or lower amounts can be used if desired, depending on the use, drug and other factors. Unit or partial dosages may be employed in one or more gels in the practice of this invention. The composition or gel compositions of this invention can be conveniently molded or shaped into various forms or mixtures of non-critical forms. Preferred forms are those that are pleasing to patients and of a size and shape that is desirable and swallowable or easy to administer for rectal and vaginal administration to, and by the patient or with help. Illustratively, the composition is poured into a suitable mold where gelation occurs, resulting in a molded composition that is coupled to the shape of the mold and is suitable for the patient. The compositions of this invention can then be removed from the mold and administered to patients and animals. Administration can be oral, vaginal and rectal by means of a suppository, with or without the help of an applicator. The method for administering the compositions of this invention is carried out by the patient, an assistant assisting the patient or a combination thereof. The shape, texture (hardness of the gel), amount of ingredient, size and other characteristics of the gel will be adjusted by those skilled in the art depending on the administration, patient, age of the patient and conditions, preferences of the physician, drug employed and many others. factors that depend on the use. The biologically active ingredient or ingredients employed in this invention include both water-soluble and water-insoluble biologically active ingredients, without limitation. An effective (therapeutic) amount of biologically active ingredient is preferably employed. The effective (therapeutic) amount of said ingredient will be that amount which is effective for the recipient patient receiving the medicament in the practice of this invention and will typically be that which is indicated on the label of the medicament or which is prescribed by a medical doctor. or veterinarian The supply is achieved in an effective manner and time and takes into account the patient, the drug and the patient's ability to receive the form of supply and the ingredient, among many factors. The patient may swallow or otherwise consume (e.g., rectal and vaginal administration) the gel composition of this invention comprising at least one biologically active ingredient. The medicament is thus provided to the patient internally and is then made available to the patient's gastrointestinal tract or other areas for beneficial use by the patient, such as when taken orally. The vaginal and rectal administration of the gels will be apparent to those skilled in the art following known procedures for administering gels by vaginal and rectal administration (suppositories) with and without an application aid. In another embodiment, this invention comprises a method employed by a patient to facilitate the swallowing of a biologically active ingredient, which comprises administering a gel prepared by the method of this invention to a human or animal. Illustrative animals to which they can give and effectively provide the gels of this invention include cats, dogs, horses, sheep, fish, pigs, cattle and the like. One or more gels of this invention can be administered and taken at a time to provide an effective and safe amount of drugs during consumption.
In another embodiment, this invention comprises a method for a patient to easily break a gel and mix it with food for humans and animals. The gel of this invention can be made easy to break, if needed, and can be mixed with food to produce smaller and easier entities to swallow by a human. In another embodiment, this invention comprises a method for facilitating vaginal or rectal administration of a lubricating gel of this invention. The texture of the gel or gels of this invention can be modified appreciably depending on the method of administration contemplated and the desired receptor. The shape can be molded into those shapes that are aesthetically pleasing, if desired or coded or marked with colors to provide increased consent measures. The shape and texture of the gel can also be configured and textured to provide such increased consent measures. For example, the mold may contain the name of the drug dose, form, etc.
EXAMPLES
The examples produced herein are only illustrations of various embodiments of this invention and are not intended to limit it in any way.
EXAMPLE 1 Preparation of sodium naproxen qeles
A 0.5% solution of GELRITE® gelling agent is prepared (GELRITE® is a registered trademark of Monsanto Company, 800 North Lindbergh BIvd., St. Louis, Missouri, 63167, USA in distilled water adding 0.125 g of GELRITE® to 25 milliliters of distilled water with agitation by means of a stirring rod The GELRITE® solution is heated at 90-95 ° C for 3-5 minutes to hydrate the GELRITE® gum and produce a clear solution The gelling agent GELRITE® It is cooled to approximately 75-78 ° C and mixed with 2.5 g of sodium naproxen until the drug dissolves completely.This produces a drug concentration of 100 mg / ml of solution.The hot drug solution is poured into molds. The solution gels when the temperature drops below 40 ° C and forms self-contained and easy-to-mold lubricating gels (intact) containing sodium naproxen which illustrates a biologically active ingredient. (Naproxen sodium is an approved medication sold over the counter as an anti-inflammatory medicine). This produced a gel containing a biologically active ingredient that illustrates this invention. For example, when 2 ml of solution was poured into the mold, the final gels contained 200 mg of naproxen sodium.
The following examples were prepared following the general procedure of example 1.
Concentration Concentration Dose of naproxen
Example of solution of naproxen resulting in gels number GELRITE® of 2ml sodium
2 0.25% 125 mg / mL 250 mg 3 0.50% 125 mg / mL 250 mg 4 '0.50% 62 mg / mL 124 mg 5 1.00% 125 mg / mL 250 mg 6 1.00% 62 mg / mL 124 mg 7 0.50% 100 mg / mL 200 mg
EXAMPLES 8-20
Several biologically active materials (sodium naproxen, ascorbic acid, ibuprofen, penicillin, etc.) were incorporated into the Gelrite® gelling agent to polish the preparation of a gel of this invention. In all cases, the preparation of the gel containing a biologically active ingredient illustrative of these examples was made according to the procedure described in example 1. The hardness was measured in an Instron model 4201 apparatus. The data are given in kilos, which represent the point of rupture of the gels under test in the Instron apparatus. (Instron Test Instrument Model 4201, Instron, 100 Royale Street, Canton, Massachusetts, 02021, E.U.A). The breaking point was measured to show that the gels of this invention were free and could be broken into smaller pieces if necessary.
Concentration Biological initial material Concentration Hardness
Example Active active GELRITE® (kqs.)
7 * 0.50% Naproxen sodium 100 mg / mL 0.78
8 0.50% Potassium chloride 25 mg / mL 0.67
9 0.75% Potassium chloride 25 mg / mL 1.60
1 .00% Potassium chloride 25 mg / mL 1.94
1 1 0.50% Iron sulfate 100 mg / mL 0.52
12 0.75% Iron sulfate 100 mg / mL 0.89
13 1.00% Iron sulfate 100 mg / mL 1.12
14 0.50% Ascorbic acid 250 mg / mL 0.37
0.75% Ascorbic acid 250 mg / mL 0.63
16 1.00% Ascorbic acid 250 mg / mL 1.00
17 0.75% Ibuprofen 75 mg / mL 0.78
18 0.25% Ibuprofen 150 mg / mL 0.36
19 0.50% Penicillin G 100 mg / mL 0.47
0.75% Penicillin G 250 mg / mL 0.48
21 1.00% Penicillin G 250 mg / mL 0.67
* The same as the previous page (with hardness given).
Other examples 22-27 were prepared below as previously described, adding calcium chloride to the hot solution, such that the total calcium concentration in the gel was 6 mM.
Concentration Initial material of ^ biologically Concentration Hardness
Example Active active GELRITE® (kas.)
22 0.75 Pseudoephedrine HCl 30 mg / mL 1.59
23 0.75 Phenylpropanolamine HCl 12.5 mg / mL 1.60 2 244 0 0..7755 Chlorphenamine 2 mg / mL 1.89
0.75 Bromopheniramine 2 mg / mL 2.18
26 0.75 Dextromethorphan 5 mg / mL 1.89
27 0.75 Diphenhydramine HCl 12.5 mg / mL 1.76
28 0.75 Acetaminophen 100 mg / mL 2.02
By way of comparison, commercially available soft gels (eg, Pfizer® Unisom SIeepgeIs) registered trademark of
Pfizer, Inc., distributed by Cosumer Health Care Group, Pfizer, Inc., New
York, NY, 10017 E.U.A or Gelcaps (Vons® Liquid-Gelcaps) Cough & Cold Liquid Liquid-Gelcaps, The Von Companies, Inc., P.O. Box 3338, Los Angeles, CA
90051, E.U.A. they could not be broken in the Instron (e.g., the force limit is 37.3 kilos). Thus, it is apparent that a novel composition, a drug delivery system, a method and methods for facilitating the swallowing and / or administration of biologically active drug (s) have been provided in accordance with the present invention. ) or metabolites or derivatives or medicine, which fully satisfies the objects and advantages set forth herein. Although the invention has been described with respect to several specific examples and embodiments thereof, it is understood that the invention is limited thereto and that many alternatives, modifications and variations will be apparent to those skilled in the art in the light of the description. previous. Accordingly, it is desired to cover all those alternatives, modifications and variations that fall within the spirit and broad scope of the invention.
Claims (36)
1. - A method for preparing a self-contained lubricant gel (intact) containing a therapeutic amount of a biologically active ingredient, for the subsequent provision and / or effective release of said active ingredient, or an active derivative or active metabolite, to or in a biological system human or animal, which comprises: a. mixing gellan gum with water to form a concentration of about 0.05% to about 5% by weight of gellan gum, optionally adding a sequestrant and polymers / additives, and maintaining said composition at a temperature sufficiently hot to achieve said gum hydration gelano, so that the gelation occurs after the subsequent cooling in a (suitable) mold that is desired; b. mixing said biologically active ingredient with said hot solution and optionally mixing with it suitable solubilization and suspension aids, and optionally mixing with the same suitable cation (s) and c. cooling said hot solution containing said biologically active ingredient to a temperature sufficient to induce gelation, whereby said lubricating gel is formed intact.
2. The process according to claim 1, further characterized in that said temperature of step 1 (a) is from about 20 ° C to about 100 ° C and is maintained at or near that temperature until said gum is hydrated.
3. The process according to claim 1, further characterized in that said preparation of the hot solution in step 1 (b) is maintained at a temperature of about 35 ° C to about 85 ° C for a time necessary to solubilize or suspending substantially said biologically active ingredient.
4. The method according to claim 1, further characterized in that the cation used to induce gelation of the gel is or has been provided complete or in part, or is or has been part of said biologically active ingredient.
5. The method according to claim 1, further characterized in that said drug solubilization aids are used and can be selected from the group consisting of ionic or non-ionic surfactants and cyclodextrins or mixtures thereof.
6. The method according to claim 1, further characterized in that said cations are provided with an external source and are used in step 1 (b).
7. The process according to claim 5, further characterized in that said cations are selected from the group consisting of alkali metals, alkaline earth metals, ammonium and mixtures thereof.
8. - The method according to claim 1, further characterized in that said biologically active ingredient is selected from the group consisting of nutritional supplements, amino acids, electrolytes, proteins, anti-inflammatory agents (for example, NSAIDS (non-steroidal anti-inflammatory drugs) such as s- ibuprofen, ketoprofen, fenoprofen, indomethacin, meclofentamate, mefenamic acid, naproxen, fenibutazone, piroxicam, tolmetin, sulindac, and dimethyl sulfoxide), analgesics, antipyretics, anesthetics including benzocaine, pramoxine, dibucaine, dyclonine, lidocaine, mepycaine, prilocaine, and tetracaine; emulsifiers; analgesics including opiate analgesics, non-opiate analgesics, non-narcotic analgesics including acetaminophen and astringents including calamine, zinc oxide, tannic acid, witch hazel, zinc sulfate; natural or synthetic steroids including triamcinolone, acetonide, prednisone, beclomethasone dipropionate; asthmatic drugs including terbutaline sulfate, albuterol, leukotriene receptor antagonists; electrolytes, metals and minerals; anti-anxiety and antidepressant agents; antimicrobial and antiviral agents; antihistamines; immunosuppressive agents; cholesterol lowering agents; agents of high cardiac blood pressure, stimulants of the CNS (central nervous system), anticonvulsants, muscle relaxants, psychotherapeutic agents, cardiovascular, diuretics, hormones, proteins and enzymatic agents, antineoplastics, gastrointestinal and respiratory agents and mixtures thereof.
9. - The method according to claim 2, further characterized in that said complete nutritional is a vitamin.
10. The method according to claim 3, further characterized in that said vitamin is vitamin C. 1.
The method according to claim 2, further characterized in that said active ingredient is sodium naproxen or ibuprofen.
12. The process according to claim 2, further characterized in that said active ingredient is sodium sakycylate.
13. A self-contained (intact) self-lubricating gel composition comprising an intact lubricant gel containing and / or providing a therapeutic amount of a biologically active ingredient or metabolite or derivative for its subsequent provision and release into a human biological system or animal, which also comprises gellan gum, water and a biologically active ingredient.
14. The gel according to claim 13, further characterized in that said biologically active ingredient is selected from the group consisting of nutritional supplements, anti-inflammatory agents (for example, NSAIDS such as s-ibuprofen, ketoprofen, fenoprofen, ndometacin, meclofentamate , mefenamic acid, naproxen, fenibutazone, piroxicam, tolmetin, sulindac and dimethyl sulfoxide), analgesics, antipyretics, anesthetics including benzocaine, pramoxine, dibucaine, dyclonine, lidocaine, mepycaine, prilocaine and tetracaine; emulsifiers; analgesics including opiate analgesics, non-opiate analgesics, non-narcotic analgesics including acetaminophen and astringents including calamine, zinc oxide, tannic acid, witch hazel, zinc sulfate; natural or synthetic steroids including triamcinolone, acetonide, prednisone, beclomethasone dipropionate; asthmatic drugs including terbutaline sulfate, albuterol, leukotriene receptor antagonists; electrolytes, metals and minerals; anti-anxiety and antidepressant agents; antimicrobial and antiviral agents; antihistamines; immunosuppressive agents; cholesterol lowering agents; agents of high cardiac blood pressure, stimulants of the CNS (central nervous system), anticonvulsants, muscle relaxants, psychotherapeutic agents, cardiovascular, diuretics, hormones, proteins and enzymatic agents, antineoplastics, gastrointestinal and respiratory agents and mixtures thereof.
15. The gel according to claim 14, further characterized in that said nutritional supplement is a vitamin.
16. The gel according to claim 14, further characterized in that said vitamin is vitamin C.
17. The gel according to claim 14, further characterized in that said active ingredient is sodium naproxen or ibuprofen.
18. The gel according to claim 14, further characterized in that said active ingredient is sodium salicylate.
19. - A drug delivery system comprising an intact lubricant gel containing a therapeutic amount of an ingredient (medicinal) biologically active for its subsequent release into a human or animal biological system, which further comprises gum and a biologically active medicinal ingredient.
20. The drug delivery system according to claim 19, further characterized in that said biologically active ingredient is selected from the group consisting of: nutritional supplements, anti-inflammatory agents (e.g., NSAIDS such as s-ibuprofen, ketoprofen, fenoprofen , indomethacin, meclofentamate, mefenamic acid, naproxen, fenibutazone, piroxicam, tolmetin, sulindac and dimethyl sulfoxide), analgesics, antipyretics, anesthetics including benzocaine, pramoxine, dibucaine, dyclonine, lidocaine, mepycaine, prilocaine and tetracaine; emulsifiers; analgesics including opiate analgesics, non-opiate analgesics, non-narcotic analgesics including acetaminophen and astringents including calamine, zinc oxide, tannic acid, witch hazel, zinc sulfate; natural or synthetic steroids including triamcinolone, acetonide, prednisone, beclomethasone dipropionate; asthmatic drugs including terbutaline sulfate, albuterol, leukotriene receptor antagonists; electrolytes, metals and minerals; anti-anxiety and antidepressant agents; antimicrobial and antiviral agents; antihistamines; immunosuppressive agents; cholesterol lowering agents; agents of high cardiac blood pressure, stimulants of the CNS (central nervous system), anticonvulsants, muscle relaxants, psychotherapeutic agents, cardiovascular, diuretics, hormones, proteins and enzymatic agents, antineophasics, gastrointestinal and respiratory agents and mixtures thereof.
21. The drug delivery system according to claim 20, further characterized in that said nutritional supplement is a vitamin.
22. The drug delivery system according to claim 20, further characterized in that said vitamin is vitamin C.
23. The drug delivery system according to claim 21, further characterized in that said active ingredient is naproxen of sodium or buprofen.
24. The drug delivery system according to claim 21, further characterized in that said active ingredient is sodium salicylate.
25. The use of an intact gel or of a broken or reduced-size gel, optionally mixed with food, comprising gellan gum in combination with a biologically active ingredient, for the manufacture of a medicament for facilitating the swallowing of said ingredient biologically active for a human or animal.
26. The use according to claim 25, further characterized in that said biologically active ingredient is selected from the group consisting of nutritional supplements, anti-inflammatory agents (for example, NSAIDS such as s-ibuprofen, ketoprofen, fenoprofen, indomethacin, meclofentamate, mefenamic acid, naproxen, fenibutazone, piroxicam, tolmetin, sulindac and dimethyl sulfoxide), analgesics, antipyretics, anesthetics including benzocaine, pramoxine, dibucaine, dyclonine, lidocaine, mepycaine, prilocaine and tetracaine; emulsifiers; analgesics that include opiate analgesics, analgesics that are not opiate, non-narcotic analgesics that include acetaminophen and astringents that include calamine, zinc oxide, tannic acid, water Witch hazel, zinc sulfate; natural or synthetic steroids including triamcinolone, acetonide, prednisone, beclomethasone dipropionate; asthmatic drugs including terbutaline sulfate, albuterol, leukotriene receptor antagonists; electrolytes, metals and minerals; anti-anxiety and antidepressant agents; antimicrobial and antiviral agents; antihistamines; immunosuppressive agents; cholesterol lowering agents; agents of high cardiac blood pressure, stimulants of the CNS (central nervous system), anticonvulsants, muscle relaxants, psychotherapeutic agents, cardiovascular, diuretics, hormones, proteins and enzymatic agents, antineoplastics, gastrointestinal and respiratory agents and mixtures thereof.
27. The use according to claim 25, further characterized in that said nutritional supplement is a vitamin.
28. The use according to claim 25, further characterized in that said vitamin is vitamin C.
29. - The use according to claim 25, further characterized in that said active ingredient is sodium naproxen or ibuprofen.
30. The use according to claim 25, further characterized in that said active ingredient is sodium salicylate.
31.- The use of an intact lubricant gel that contains a biologically active ingredient in the manufacture of a medication to facilitate vaginal administration and rectal administration in a human or animal.
32. The use according to claim 31, further characterized in that said biologically active ingredient is selected from the group consisting of nutritional supplements, anti-inflammatory agents (for example, NSAIDS such as s-ibuprofen, ketoprofen, fenoprofen, indomethacin, meclofentamate, mefenamic acid, naproxen, fenibutazone, piroxicam, tolmetin, sulindac and dimethyl sulfoxide), analgesics, antipyretics, anesthetics including benzocaine, pramoxine, dibucaine, dyclonine, lidocaine, mepycaine, prilocaine and tetracaine; emulsifiers; analgesics including opiate analgesics, non-opiate analgesics, non-narcotic analgesics including acetaminophen and astringents including calamine, zinc oxide, tannic acid, witch hazel, zinc sulfate; natural or synthetic steroids including triamcinolone, acetonide, prednisone, beclomethasone dipropionate; asthmatic drugs including terbutaline sulfate, albuterol, leukotriene receptor antagonists; electrolytes, metals and minerals; anti-anxiety and antidepressant agents; antimicrobial and antiviral agents; antihistamines; immunosuppressive agents; cholesterol lowering agents; agents of high cardiac blood pressure, stimulants of the CNS (central nervous system), anticonvulsants, muscle relaxants, psychotherapeutic agents, cardiovascular, diuretics, hormones, proteins and enzymatic agents, antineoplastics, gastrointestinal and respiratory agents and mixtures thereof.
33. The use according to claim 31, further characterized in that said nutritional supplement is a vitamin.
34. The use according to claim 31, further characterized in that said vitamin is vitamin C.
35. The use according to claim 31, further characterized in that said active ingredient is sodium naproxen or ibuprofen.
36. The use according to claim 31, further characterized in that said active ingredient is sodium salicylate.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US758543 | 1996-11-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA99005003A true MXPA99005003A (en) | 2000-02-02 |
Family
ID=
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US10668013B2 (en) | Chewable gelled emulsions | |
| JP5555184B2 (en) | Compositions and methods for assisting in swallowing | |
| CN100408029C (en) | Composite dosage forms with a coating portion | |
| RU2445977C2 (en) | Water-soluble films containing low-viscosity alginates | |
| WO1997025024A1 (en) | Jellied medicinal composition for oral administration | |
| JPS60222427A (en) | Foa mable anhydrous composition | |
| JP2006515598A (en) | Edible film to reduce cough or pharyngitis related symptoms | |
| NZ280609A (en) | Gelling liquid polyethylene glycol compostions which includes water and calcium acetate, and its use in medicaments, cosmetics and dental care | |
| US20070134280A1 (en) | Thixotropic ingestible formulation to treat sore throat | |
| EP0946197A1 (en) | Lubricious self-standing (intact) gel for oral delivery of biologically-active ingredients | |
| JP4309481B2 (en) | Jelly oral pharmaceutical composition | |
| US20060165795A1 (en) | Medicinal compositions comprising a core and a film based on modified cellulose derivatives | |
| EP1079810A1 (en) | Orally administrable compositions comprising cation cross-linked polysaccharide and a polymer digestible in the lower gastrointestinal tract | |
| Dongare et al. | Floating drug delivery system: A better approach | |
| Sunil et al. | Pharmaceutical Jellies: A novel way of drug delivery | |
| CN102058608A (en) | New application of glucosamine in treating dental ulcer | |
| Chaudhary et al. | Recent Development in Floating Drug Delivery System: An Overview | |
| MXPA99005003A (en) | Lubricious self-standing (intact) gel for oral delivery of biologically-active ingredients | |
| CA2623306C (en) | Oral vehicle for systemic pharmaceuticals | |
| WO1989005630A1 (en) | Oral dosage units for pharmaceuticals and their use and preparation | |
| WO2011048388A2 (en) | Oral pharmaceutical and nutraceutical compositions | |
| AU1292199A (en) | Controlled release compositions comprising gellan gum gels | |
| US20230100269A1 (en) | Carrier for the oral absorption of an active substance by animals, method for preparing same and uses thereof | |
| AU666666B2 (en) | Rapidly disintegratable multiparticulate tablet | |
| Tishyadhigama | Development of in situ gel for artificial saliva and satisfaction study |