CA2796494A1 - Pharmaceutical composition - Google Patents
Pharmaceutical composition Download PDFInfo
- Publication number
- CA2796494A1 CA2796494A1 CA2796494A CA2796494A CA2796494A1 CA 2796494 A1 CA2796494 A1 CA 2796494A1 CA 2796494 A CA2796494 A CA 2796494A CA 2796494 A CA2796494 A CA 2796494A CA 2796494 A1 CA2796494 A1 CA 2796494A1
- Authority
- CA
- Canada
- Prior art keywords
- sodium
- efavirenz
- particles
- process according
- composition according
- 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.)
- Abandoned
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 22
- XPOQHMRABVBWPR-UHFFFAOYSA-N Efavirenz Natural products O1C(=O)NC2=CC=C(Cl)C=C2C1(C(F)(F)F)C#CC1CC1 XPOQHMRABVBWPR-UHFFFAOYSA-N 0.000 claims abstract description 74
- XPOQHMRABVBWPR-ZDUSSCGKSA-N efavirenz Chemical compound C([C@]1(C2=CC(Cl)=CC=C2NC(=O)O1)C(F)(F)F)#CC1CC1 XPOQHMRABVBWPR-ZDUSSCGKSA-N 0.000 claims abstract description 74
- 229960003804 efavirenz Drugs 0.000 claims abstract description 73
- 239000000203 mixture Substances 0.000 claims description 64
- 238000000034 method Methods 0.000 claims description 48
- 239000002245 particle Substances 0.000 claims description 43
- 239000003814 drug Substances 0.000 claims description 36
- 230000008569 process Effects 0.000 claims description 36
- -1 olefin sulphonate Chemical class 0.000 claims description 32
- 229920000642 polymer Polymers 0.000 claims description 24
- 239000004094 surface-active agent Substances 0.000 claims description 18
- 229930006000 Sucrose Natural products 0.000 claims description 16
- 239000008187 granular material Substances 0.000 claims description 16
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 16
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 16
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 16
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 16
- 229960004793 sucrose Drugs 0.000 claims description 16
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 15
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 14
- 239000006185 dispersion Substances 0.000 claims description 14
- 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 claims description 13
- 239000002002 slurry Substances 0.000 claims description 13
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 12
- 239000005720 sucrose Substances 0.000 claims description 12
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 11
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 11
- 229960000913 crospovidone Drugs 0.000 claims description 11
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 11
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 11
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 11
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 11
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 11
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 11
- 239000003381 stabilizer Substances 0.000 claims description 11
- 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 claims description 10
- 235000019329 dioctyl sodium sulphosuccinate Nutrition 0.000 claims description 10
- 229960000878 docusate sodium Drugs 0.000 claims description 10
- 229960001375 lactose Drugs 0.000 claims description 10
- 239000008101 lactose Substances 0.000 claims description 10
- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 claims description 10
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 claims description 9
- 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 claims description 9
- 238000009472 formulation Methods 0.000 claims description 9
- 229960001021 lactose monohydrate Drugs 0.000 claims description 9
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 7
- 239000004141 Sodium laurylsulphate Substances 0.000 claims description 7
- 229920002472 Starch Polymers 0.000 claims description 7
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 7
- 150000002148 esters Chemical class 0.000 claims description 7
- 239000000194 fatty acid Substances 0.000 claims description 7
- 229930195729 fatty acid Natural products 0.000 claims description 7
- 150000004665 fatty acids Chemical class 0.000 claims description 7
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 7
- 229920001223 polyethylene glycol Polymers 0.000 claims description 7
- 235000019698 starch Nutrition 0.000 claims description 7
- 238000011282 treatment Methods 0.000 claims description 7
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 6
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 6
- 229920002675 Polyoxyl Polymers 0.000 claims description 6
- 150000001408 amides Chemical class 0.000 claims description 6
- 239000011230 binding agent Substances 0.000 claims description 6
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 6
- 239000007884 disintegrant Substances 0.000 claims description 6
- SYELZBGXAIXKHU-UHFFFAOYSA-N dodecyldimethylamine N-oxide Chemical compound CCCCCCCCCCCC[N+](C)(C)[O-] SYELZBGXAIXKHU-UHFFFAOYSA-N 0.000 claims description 6
- 239000002552 dosage form Substances 0.000 claims description 6
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 6
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 6
- 229920000858 Cyclodextrin Polymers 0.000 claims description 5
- 239000000945 filler Substances 0.000 claims description 5
- 239000007788 liquid Substances 0.000 claims description 5
- 239000000314 lubricant Substances 0.000 claims description 5
- 229920000609 methyl cellulose Polymers 0.000 claims description 5
- 235000010981 methylcellulose Nutrition 0.000 claims description 5
- 239000001923 methylcellulose Substances 0.000 claims description 5
- 239000003921 oil Substances 0.000 claims description 5
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 5
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 5
- 239000008107 starch Substances 0.000 claims description 5
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims description 4
- 239000005913 Maltodextrin Substances 0.000 claims description 4
- 229920002774 Maltodextrin Polymers 0.000 claims description 4
- 239000002202 Polyethylene glycol Substances 0.000 claims description 4
- 229920003090 carboxymethyl hydroxyethyl cellulose Polymers 0.000 claims description 4
- 239000004359 castor oil Substances 0.000 claims description 4
- 235000019438 castor oil Nutrition 0.000 claims description 4
- 125000002091 cationic group Chemical group 0.000 claims description 4
- 235000013681 dietary sucrose Nutrition 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 4
- 150000002334 glycols Chemical class 0.000 claims description 4
- 235000010445 lecithin Nutrition 0.000 claims description 4
- 239000000787 lecithin Substances 0.000 claims description 4
- 229940067606 lecithin Drugs 0.000 claims description 4
- 229940035034 maltodextrin Drugs 0.000 claims description 4
- 238000003801 milling Methods 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 159000000000 sodium salts Chemical class 0.000 claims description 4
- 238000005507 spraying Methods 0.000 claims description 4
- DNIAPMSPPWPWGF-GSVOUGTGSA-N (R)-(-)-Propylene glycol Chemical class C[C@@H](O)CO DNIAPMSPPWPWGF-GSVOUGTGSA-N 0.000 claims description 3
- CMCBDXRRFKYBDG-UHFFFAOYSA-N 1-dodecoxydodecane Chemical compound CCCCCCCCCCCCOCCCCCCCCCCCC CMCBDXRRFKYBDG-UHFFFAOYSA-N 0.000 claims description 3
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims description 3
- IEORSVTYLWZQJQ-UHFFFAOYSA-N 2-(2-nonylphenoxy)ethanol Chemical compound CCCCCCCCCC1=CC=CC=C1OCCO IEORSVTYLWZQJQ-UHFFFAOYSA-N 0.000 claims description 3
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 3
- HRPVXLWXLXDGHG-UHFFFAOYSA-N Acrylamide Chemical compound NC(=O)C=C HRPVXLWXLXDGHG-UHFFFAOYSA-N 0.000 claims description 3
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical class [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 claims description 3
- QWZLBLDNRUUYQI-UHFFFAOYSA-M Methylbenzethonium chloride Chemical compound [Cl-].CC1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 QWZLBLDNRUUYQI-UHFFFAOYSA-M 0.000 claims description 3
- KWYHDKDOAIKMQN-UHFFFAOYSA-N N,N,N',N'-tetramethylethylenediamine Chemical compound CN(C)CCN(C)C KWYHDKDOAIKMQN-UHFFFAOYSA-N 0.000 claims description 3
- 229920001214 Polysorbate 60 Polymers 0.000 claims description 3
- 150000001298 alcohols Polymers 0.000 claims description 3
- 150000001412 amines Chemical class 0.000 claims description 3
- 239000000908 ammonium hydroxide Substances 0.000 claims description 3
- 239000003833 bile salt Substances 0.000 claims description 3
- 239000002775 capsule Substances 0.000 claims description 3
- 150000007942 carboxylates Chemical class 0.000 claims description 3
- 150000001733 carboxylic acid esters Chemical class 0.000 claims description 3
- 229920001577 copolymer Polymers 0.000 claims description 3
- 229960003964 deoxycholic acid Drugs 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 238000001035 drying Methods 0.000 claims description 3
- 229920003063 hydroxymethyl cellulose Polymers 0.000 claims description 3
- 229940031574 hydroxymethyl cellulose Drugs 0.000 claims description 3
- FPYJFEHAWHCUMM-UHFFFAOYSA-N maleic anhydride Chemical compound O=C1OC(=O)C=C1 FPYJFEHAWHCUMM-UHFFFAOYSA-N 0.000 claims description 3
- 229960002285 methylbenzethonium chloride Drugs 0.000 claims description 3
- 238000002156 mixing Methods 0.000 claims description 3
- PSZYNBSKGUBXEH-UHFFFAOYSA-N naphthalene-1-sulfonic acid Chemical compound C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1 PSZYNBSKGUBXEH-UHFFFAOYSA-N 0.000 claims description 3
- 229920000847 nonoxynol Polymers 0.000 claims description 3
- 229940066429 octoxynol Drugs 0.000 claims description 3
- 229920002113 octoxynol Polymers 0.000 claims description 3
- JRZJOMJEPLMPRA-UHFFFAOYSA-N olefin Natural products CCCCCCCC=C JRZJOMJEPLMPRA-UHFFFAOYSA-N 0.000 claims description 3
- NFHFRUOZVGFOOS-UHFFFAOYSA-N palladium;triphenylphosphane Chemical group [Pd].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 NFHFRUOZVGFOOS-UHFFFAOYSA-N 0.000 claims description 3
- 239000003208 petroleum Substances 0.000 claims description 3
- 229920000136 polysorbate Polymers 0.000 claims description 3
- 229940068965 polysorbates Drugs 0.000 claims description 3
- 239000000843 powder Substances 0.000 claims description 3
- 150000003242 quaternary ammonium salts Chemical class 0.000 claims description 3
- NRHMKIHPTBHXPF-TUJRSCDTSA-M sodium cholate Chemical compound [Na+].C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC([O-])=O)C)[C@@]2(C)[C@@H](O)C1 NRHMKIHPTBHXPF-TUJRSCDTSA-M 0.000 claims description 3
- FHHPUSMSKHSNKW-SMOYURAASA-M sodium deoxycholate Chemical compound [Na+].C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC([O-])=O)C)[C@@]2(C)[C@@H](O)C1 FHHPUSMSKHSNKW-SMOYURAASA-M 0.000 claims description 3
- 239000008297 liquid dosage form Substances 0.000 claims description 2
- JXLHNMVSKXFWAO-UHFFFAOYSA-N azane;7-fluoro-2,1,3-benzoxadiazole-4-sulfonic acid Chemical compound N.OS(=O)(=O)C1=CC=C(F)C2=NON=C12 JXLHNMVSKXFWAO-UHFFFAOYSA-N 0.000 claims 4
- 229910021653 sulphate ion Inorganic materials 0.000 claims 4
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical class NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 2
- 150000003973 alkyl amines Chemical class 0.000 claims 2
- 239000002280 amphoteric surfactant Substances 0.000 claims 2
- 239000003945 anionic surfactant Substances 0.000 claims 2
- 239000003093 cationic surfactant Substances 0.000 claims 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N ethylene glycol Natural products OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 2
- 239000002736 nonionic surfactant Substances 0.000 claims 2
- 229920000058 polyacrylate Polymers 0.000 claims 2
- 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 claims 2
- 125000000185 sucrose group Chemical group 0.000 claims 2
- 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 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- PMZURENOXWZQFD-UHFFFAOYSA-L sodium sulphate Substances [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 claims 1
- 235000011152 sodium sulphate Nutrition 0.000 claims 1
- 239000002105 nanoparticle Substances 0.000 abstract description 8
- 229940079593 drug Drugs 0.000 description 35
- 238000004090 dissolution Methods 0.000 description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 13
- 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 9
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 239000007909 solid dosage form Substances 0.000 description 8
- 239000008213 purified water Substances 0.000 description 7
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 6
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 6
- 150000003839 salts Chemical class 0.000 description 6
- 235000010980 cellulose Nutrition 0.000 description 5
- 229920002678 cellulose Polymers 0.000 description 5
- 239000001913 cellulose Substances 0.000 description 5
- 210000001035 gastrointestinal tract Anatomy 0.000 description 5
- 239000000243 solution Substances 0.000 description 5
- 241000725303 Human immunodeficiency virus Species 0.000 description 4
- 238000010521 absorption reaction Methods 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 239000003960 organic solvent Substances 0.000 description 4
- 239000007962 solid dispersion Substances 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- 238000003756 stirring Methods 0.000 description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- 229920002785 Croscarmellose sodium Polymers 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 229960001681 croscarmellose sodium Drugs 0.000 description 3
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 3
- 229940097362 cyclodextrins Drugs 0.000 description 3
- 238000011161 development Methods 0.000 description 3
- 239000000839 emulsion Substances 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- 238000001704 evaporation Methods 0.000 description 3
- 239000012530 fluid Substances 0.000 description 3
- 230000002496 gastric effect Effects 0.000 description 3
- 238000000265 homogenisation Methods 0.000 description 3
- 230000006872 improvement Effects 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 230000004048 modification Effects 0.000 description 3
- 238000012986 modification Methods 0.000 description 3
- 239000002159 nanocrystal Substances 0.000 description 3
- 235000019198 oils Nutrition 0.000 description 3
- 230000006320 pegylation Effects 0.000 description 3
- 238000001556 precipitation Methods 0.000 description 3
- 229920003109 sodium starch glycolate Polymers 0.000 description 3
- 239000008109 sodium starch glycolate Substances 0.000 description 3
- 229940079832 sodium starch glycolate Drugs 0.000 description 3
- 239000012453 solvate Substances 0.000 description 3
- 229940032147 starch Drugs 0.000 description 3
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 2
- 229920002261 Corn starch Polymers 0.000 description 2
- 239000004375 Dextrin Substances 0.000 description 2
- 229920001353 Dextrin Polymers 0.000 description 2
- 208000031886 HIV Infections Diseases 0.000 description 2
- 208000037357 HIV infectious disease Diseases 0.000 description 2
- 229920000881 Modified starch Polymers 0.000 description 2
- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 2
- 239000000443 aerosol Substances 0.000 description 2
- 235000010443 alginic acid Nutrition 0.000 description 2
- 229920000615 alginic acid Polymers 0.000 description 2
- 239000000783 alginic acid Substances 0.000 description 2
- 229960001126 alginic acid Drugs 0.000 description 2
- 150000004781 alginic acids Chemical class 0.000 description 2
- 125000000129 anionic group Chemical group 0.000 description 2
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 229910052791 calcium Inorganic materials 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 238000009833 condensation Methods 0.000 description 2
- 230000005494 condensation Effects 0.000 description 2
- 235000019425 dextrin Nutrition 0.000 description 2
- 230000008020 evaporation Effects 0.000 description 2
- 239000007888 film coating Substances 0.000 description 2
- 238000009501 film coating Methods 0.000 description 2
- 239000007789 gas Substances 0.000 description 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 description 2
- 230000002209 hydrophobic effect Effects 0.000 description 2
- 239000002609 medium Substances 0.000 description 2
- 235000019426 modified starch Nutrition 0.000 description 2
- 230000006911 nucleation Effects 0.000 description 2
- 238000010899 nucleation Methods 0.000 description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 2
- 239000006186 oral dosage form Substances 0.000 description 2
- 230000035699 permeability Effects 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000012071 phase Substances 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 235000010413 sodium alginate Nutrition 0.000 description 2
- 239000000661 sodium alginate Substances 0.000 description 2
- 229940005550 sodium alginate Drugs 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 230000000087 stabilizing effect Effects 0.000 description 2
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Classifications
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A61K9/2022—Organic macromolecular compounds
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- A61P31/12—Antivirals
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
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- A—HUMAN NECESSITIES
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- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
- Y10T428/00—Stock material or miscellaneous articles
- Y10T428/29—Coated or structually defined flake, particle, cell, strand, strand portion, rod, filament, macroscopic fiber or mass thereof
- Y10T428/2982—Particulate matter [e.g., sphere, flake, etc.]
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Chemical Kinetics & Catalysis (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| IN1296/MUM/2010 | 2010-04-20 | ||
| IN1296MU2010 | 2010-04-20 | ||
| PCT/GB2011/000620 WO2011131943A2 (en) | 2010-04-20 | 2011-04-20 | Pharmaceutical compositions |
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| CA2796494A1 true CA2796494A1 (en) | 2011-10-27 |
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| Country | Link |
|---|---|
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| EP (1) | EP2560617A2 (enExample) |
| JP (1) | JP2013525337A (enExample) |
| KR (1) | KR20130076818A (enExample) |
| CN (1) | CN102985072A (enExample) |
| AU (1) | AU2011244783B2 (enExample) |
| BR (1) | BR112012026843A2 (enExample) |
| CA (1) | CA2796494A1 (enExample) |
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| WO (1) | WO2011131943A2 (enExample) |
| ZA (1) | ZA201207670B (enExample) |
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| GB201115633D0 (en) * | 2011-09-09 | 2011-10-26 | Univ Liverpool | Compositions of efavirenz |
| US10646452B2 (en) * | 2013-03-15 | 2020-05-12 | New Jersey Institute Of Technology | System and method for fabrication of uniform polymer films containing nano and micro particles via continuous drying process |
| IN2013MU03370A (enExample) | 2013-10-25 | 2015-09-25 | Cipla Ltd | |
| WO2015071841A1 (en) | 2013-11-12 | 2015-05-21 | Druggability Technologies Holdings Limited | Complexes of dabigatran and its derivatives, process for the preparation thereof and pharmaceutical compositions containing them |
| WO2015140569A1 (en) * | 2014-03-20 | 2015-09-24 | Cipla Limited | Pharmaceutical composition |
| CN104224790A (zh) * | 2014-09-28 | 2014-12-24 | 苏州普罗达生物科技有限公司 | 一种依法韦仑组合物及其制备方法 |
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| US20230040901A1 (en) * | 2018-01-04 | 2023-02-09 | PlantTec Medical GmbH | Pharmaceutical composition for inhibiting postoperative adhesions |
| ES2732498B2 (es) * | 2018-05-21 | 2020-04-27 | Consejo Superior Investigacion | Uso de efavirenz para el tratamiento de enfermedades de almacenamiento lipidico. |
| WO2019226969A1 (en) | 2018-05-24 | 2019-11-28 | Elektrofi, Inc. | Particles comprising a therapeutic or diagnostic agent and suspensions and methods of use thereof |
| CN112236141A (zh) * | 2018-06-11 | 2021-01-15 | 大塚制药株式会社 | 包含德拉马尼的组合物 |
| AU2020214626B2 (en) | 2019-01-31 | 2025-10-16 | Halozyme Hypercon, Inc. | Particle formation and morphology |
| AU2020344675B2 (en) | 2019-09-13 | 2026-06-25 | Halozyme Hypercon, Inc. | Compositions and methods for the delivery of therapeutic biologics for treatment of disease |
| KR20220109430A (ko) | 2019-12-02 | 2022-08-04 | 아스트라제네카 아베 | 6-(2-클로로-6-메틸피리딘-4-일)-5-(4-플루오로페닐)-1,2,4-트리아진-3-아민의 고체 약학 제형 |
| US12377050B2 (en) | 2020-04-17 | 2025-08-05 | Elektrofi, Inc. | Methods of forming particles by continuous droplet formation and dehydration |
| WO2021216475A1 (en) * | 2020-04-20 | 2021-10-28 | Poviva Corp. | Compositions and methods for enhanced delivery of antiviral agents |
| CN112245400B (zh) * | 2020-11-10 | 2023-01-20 | 蓝龙药业(北京)有限公司 | 一种依法韦仑微片剂、制备方法及其应用 |
| CN114404377B (zh) * | 2022-01-10 | 2023-07-25 | 安徽贝克生物制药有限公司 | 一种阿巴卡韦、拉米夫定、依非韦伦复方片及其制备方法 |
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| UA72207C2 (uk) * | 1998-04-07 | 2005-02-15 | Брістол- Майєрс Сквібб Фарма Компані | Фармацевтична композиція ефавіренцу з добавкою дезінтегруючих агентів у вигляді швидкорозчинних капсул або таблеток та спосіб її виготовлення |
| EP1332757B1 (en) * | 1998-05-27 | 2012-06-13 | Merck Sharp & Dohme Corp. | Efavirenz compressed tablet formulation |
| PE20000559A1 (es) | 1998-05-27 | 2000-07-05 | Merck & Co Inc | Formulacion de tabletas comprimidas de efavirenz |
| AU2002359518A1 (en) * | 2001-11-27 | 2003-06-10 | Bristol-Myers Squibb Company | Efavirenz tablet formulation having unique biopharmaceutical characteristics |
| US20070003623A1 (en) * | 2005-06-29 | 2007-01-04 | Wyeth | Formulations of conjugated estrogens and bazedoxifene |
| US20080026062A1 (en) * | 2006-07-31 | 2008-01-31 | Isaac Farr | Pharmaceutical compositions including nano-sized active agent |
| TWI405590B (zh) * | 2007-04-06 | 2013-08-21 | 活效製藥股份有限公司 | 微粉碎化有機化合物粒子之製法 |
| CA2697150A1 (en) * | 2007-08-17 | 2009-02-26 | Teva Pharmaceutical Industries Ltd. | Methods and compositions for controlling the bioavailability of poorly soluble drugs |
| JP4606444B2 (ja) * | 2007-08-21 | 2011-01-05 | アピ株式会社 | アントシアニン含有経口投与用組成物及びその製造方法 |
| WO2010068899A1 (en) * | 2008-12-12 | 2010-06-17 | Creighton University | Nanoparticles comprising combinations of antiretroviral agents and use thereof |
| US10952965B2 (en) * | 2009-05-15 | 2021-03-23 | Baxter International Inc. | Compositions and methods for drug delivery |
| GB201006038D0 (en) * | 2010-04-12 | 2010-05-26 | Unilever Plc | Improvements relating to antiviral compositions |
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- 2011-04-20 NZ NZ602955A patent/NZ602955A/en not_active IP Right Cessation
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- 2011-04-20 EP EP11716002A patent/EP2560617A2/en not_active Withdrawn
- 2011-04-20 CN CN2011800201397A patent/CN102985072A/zh active Pending
- 2011-04-20 WO PCT/GB2011/000620 patent/WO2011131943A2/en not_active Ceased
- 2011-04-20 JP JP2013505533A patent/JP2013525337A/ja active Pending
- 2011-04-20 CA CA2796494A patent/CA2796494A1/en not_active Abandoned
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2013
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| RU2012149115A (ru) | 2014-05-27 |
| BR112012026843A2 (pt) | 2016-07-12 |
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| CN102985072A (zh) | 2013-03-20 |
| WO2011131943A2 (en) | 2011-10-27 |
| GT201200284A (es) | 2014-08-26 |
| WO2011131943A8 (en) | 2012-11-29 |
| US20130302415A1 (en) | 2013-11-14 |
| AU2011244783A1 (en) | 2012-11-01 |
| WO2011131943A3 (en) | 2011-12-29 |
| ZA201207670B (en) | 2013-05-29 |
| NZ602955A (en) | 2015-02-27 |
| AU2011244783B2 (en) | 2015-11-12 |
| JP2013525337A (ja) | 2013-06-20 |
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