ZA200603421B - A controlled release pharmaceutical composition and a process for preparing the same - Google Patents
A controlled release pharmaceutical composition and a process for preparing the same Download PDFInfo
- Publication number
- ZA200603421B ZA200603421B ZA200603421A ZA200603421A ZA200603421B ZA 200603421 B ZA200603421 B ZA 200603421B ZA 200603421 A ZA200603421 A ZA 200603421A ZA 200603421 A ZA200603421 A ZA 200603421A ZA 200603421 B ZA200603421 B ZA 200603421B
- Authority
- ZA
- South Africa
- Prior art keywords
- pharmaceutically acceptable
- composition
- release formulation
- controlled release
- amount
- Prior art date
Links
- 238000013270 controlled release Methods 0.000 title claims description 45
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 25
- 238000004519 manufacturing process Methods 0.000 title description 4
- 239000000203 mixture Substances 0.000 claims description 104
- NQDJXKOVJZTUJA-UHFFFAOYSA-N nevirapine Chemical compound C12=NC=CC=C2C(=O)NC=2C(C)=CC=NC=2N1C1CC1 NQDJXKOVJZTUJA-UHFFFAOYSA-N 0.000 claims description 30
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 27
- 238000009472 formulation Methods 0.000 claims description 25
- HBOMLICNUCNMMY-XLPZGREQSA-N zidovudine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 HBOMLICNUCNMMY-XLPZGREQSA-N 0.000 claims description 21
- 229940079593 drug Drugs 0.000 claims description 20
- 239000003814 drug Substances 0.000 claims description 20
- 229960002555 zidovudine Drugs 0.000 claims description 20
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims description 19
- 229940122313 Nucleoside reverse transcriptase inhibitor Drugs 0.000 claims description 18
- 230000000798 anti-retroviral effect Effects 0.000 claims description 18
- 229960001627 lamivudine Drugs 0.000 claims description 18
- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 claims description 18
- 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 description 17
- 239000003085 diluting agent Substances 0.000 claims description 17
- 229960003804 efavirenz Drugs 0.000 claims description 17
- 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 description 17
- 159000000007 calcium salts Chemical class 0.000 claims description 16
- 229960000689 nevirapine Drugs 0.000 claims description 15
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 14
- 239000002253 acid Substances 0.000 claims description 14
- 229920003086 cellulose ether Polymers 0.000 claims description 14
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 14
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 12
- 239000000314 lubricant Substances 0.000 claims description 11
- 150000007513 acids Chemical class 0.000 claims description 10
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 10
- 229920001477 hydrophilic polymer Polymers 0.000 claims description 10
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 9
- 239000001506 calcium phosphate Substances 0.000 claims description 9
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 9
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 9
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 9
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 8
- 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 8
- 229920000642 polymer Polymers 0.000 claims description 8
- 235000019739 Dicalciumphosphate Nutrition 0.000 claims description 7
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 7
- 239000001913 cellulose Substances 0.000 claims description 7
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 claims description 7
- 229940038472 dicalcium phosphate Drugs 0.000 claims description 7
- 229910000390 dicalcium phosphate Inorganic materials 0.000 claims description 7
- 229920002472 Starch Polymers 0.000 claims description 6
- 239000011230 binding agent Substances 0.000 claims description 6
- 235000010216 calcium carbonate Nutrition 0.000 claims description 6
- 235000019359 magnesium stearate Nutrition 0.000 claims description 6
- 239000008107 starch Substances 0.000 claims description 6
- 229940032147 starch Drugs 0.000 claims description 6
- 235000019698 starch Nutrition 0.000 claims description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 5
- 235000010443 alginic acid Nutrition 0.000 claims description 5
- 229920000615 alginic acid Polymers 0.000 claims description 5
- 239000001175 calcium sulphate Substances 0.000 claims description 5
- 235000011132 calcium sulphate Nutrition 0.000 claims description 5
- 238000007906 compression Methods 0.000 claims description 5
- 230000006835 compression Effects 0.000 claims description 5
- 239000007884 disintegrant Substances 0.000 claims description 5
- 229920003124 powdered cellulose Polymers 0.000 claims description 5
- 235000019814 powdered cellulose Nutrition 0.000 claims description 5
- 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 claims description 4
- 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 claims description 4
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 4
- 229920002907 Guar gum Polymers 0.000 claims description 4
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- 229920000881 Modified starch Polymers 0.000 claims description 4
- 239000004480 active ingredient Substances 0.000 claims description 4
- 235000010410 calcium alginate Nutrition 0.000 claims description 4
- 239000000648 calcium alginate Substances 0.000 claims description 4
- 229960002681 calcium alginate Drugs 0.000 claims description 4
- 229960003563 calcium carbonate Drugs 0.000 claims description 4
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims description 4
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 4
- 229920003123 carboxymethyl cellulose sodium Polymers 0.000 claims description 4
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 claims description 4
- 235000010417 guar gum Nutrition 0.000 claims description 4
- 239000000665 guar gum Substances 0.000 claims description 4
- 229960002154 guar gum Drugs 0.000 claims description 4
- 239000008101 lactose Substances 0.000 claims description 4
- 229960001375 lactose Drugs 0.000 claims description 4
- 239000000594 mannitol Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 4
- 229920000609 methyl cellulose Polymers 0.000 claims description 4
- 238000002156 mixing Methods 0.000 claims description 4
- 238000002360 preparation method Methods 0.000 claims description 4
- 235000010413 sodium alginate Nutrition 0.000 claims description 4
- 239000000661 sodium alginate Substances 0.000 claims description 4
- 229940005550 sodium alginate Drugs 0.000 claims description 4
- 229920003109 sodium starch glycolate Polymers 0.000 claims description 4
- 239000008109 sodium starch glycolate Substances 0.000 claims description 4
- 229940079832 sodium starch glycolate Drugs 0.000 claims description 4
- 235000021355 Stearic acid Nutrition 0.000 claims description 3
- 235000013539 calcium stearate Nutrition 0.000 claims description 3
- 239000008116 calcium stearate Substances 0.000 claims description 3
- 235000010981 methylcellulose Nutrition 0.000 claims description 3
- 239000001923 methylcellulose Substances 0.000 claims description 3
- 229940042402 non-nucleoside reverse transcriptase inhibitor Drugs 0.000 claims description 3
- 239000002726 nonnucleoside reverse transcriptase inhibitor Substances 0.000 claims description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 3
- 229940069328 povidone Drugs 0.000 claims description 3
- 239000000377 silicon dioxide Substances 0.000 claims description 3
- 235000012239 silicon dioxide Nutrition 0.000 claims description 3
- 239000008117 stearic acid Substances 0.000 claims description 3
- 239000000454 talc Substances 0.000 claims description 3
- 229910052623 talc Inorganic materials 0.000 claims description 3
- 235000012222 talc Nutrition 0.000 claims description 3
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 claims description 2
- 244000215068 Acacia senegal Species 0.000 claims description 2
- 235000006491 Acacia senegal Nutrition 0.000 claims description 2
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 2
- 108010010803 Gelatin Proteins 0.000 claims description 2
- 229920000084 Gum arabic Polymers 0.000 claims description 2
- 229920000569 Gum karaya Polymers 0.000 claims description 2
- 229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 claims description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 2
- 229920001615 Tragacanth Polymers 0.000 claims description 2
- VEUACKUBDLVUAC-UHFFFAOYSA-N [Na].[Ca] Chemical compound [Na].[Ca] VEUACKUBDLVUAC-UHFFFAOYSA-N 0.000 claims description 2
- 235000010489 acacia gum Nutrition 0.000 claims description 2
- 229940072056 alginate Drugs 0.000 claims description 2
- 239000000783 alginic acid Substances 0.000 claims description 2
- 229960001126 alginic acid Drugs 0.000 claims description 2
- 150000004781 alginic acids Chemical class 0.000 claims description 2
- 235000010407 ammonium alginate Nutrition 0.000 claims description 2
- 239000000728 ammonium alginate Substances 0.000 claims description 2
- KPGABFJTMYCRHJ-YZOKENDUSA-N ammonium alginate Chemical compound [NH4+].[NH4+].O1[C@@H](C([O-])=O)[C@@H](OC)[C@H](O)[C@H](O)[C@@H]1O[C@@H]1[C@@H](C([O-])=O)O[C@@H](O)[C@@H](O)[C@H]1O KPGABFJTMYCRHJ-YZOKENDUSA-N 0.000 claims description 2
- 239000000305 astragalus gummifer gum Substances 0.000 claims description 2
- 239000001110 calcium chloride Substances 0.000 claims description 2
- 229910001628 calcium chloride Inorganic materials 0.000 claims description 2
- 235000011148 calcium chloride Nutrition 0.000 claims description 2
- 229910000389 calcium phosphate Inorganic materials 0.000 claims description 2
- 235000011010 calcium phosphates Nutrition 0.000 claims description 2
- OKHHGHGGPDJQHR-YMOPUZKJSA-L calcium;(2s,3s,4s,5s,6r)-6-[(2r,3s,4r,5s,6r)-2-carboxy-6-[(2r,3s,4r,5s,6r)-2-carboxylato-4,5,6-trihydroxyoxan-3-yl]oxy-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylate Chemical compound [Ca+2].O[C@@H]1[C@H](O)[C@H](O)O[C@@H](C([O-])=O)[C@H]1O[C@H]1[C@@H](O)[C@@H](O)[C@H](O[C@H]2[C@H]([C@@H](O)[C@H](O)[C@H](O2)C([O-])=O)O)[C@H](C(O)=O)O1 OKHHGHGGPDJQHR-YMOPUZKJSA-L 0.000 claims description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 2
- 229940105329 carboxymethylcellulose Drugs 0.000 claims description 2
- 235000010980 cellulose Nutrition 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 239000011248 coating agent Substances 0.000 claims description 2
- 238000000576 coating method Methods 0.000 claims description 2
- 239000003086 colorant Substances 0.000 claims description 2
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 2
- 229960000913 crospovidone Drugs 0.000 claims description 2
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 2
- 229920000159 gelatin Polymers 0.000 claims description 2
- 239000008273 gelatin Substances 0.000 claims description 2
- 235000019322 gelatine Nutrition 0.000 claims description 2
- 235000011852 gelatine desserts Nutrition 0.000 claims description 2
- 229940071826 hydroxyethyl cellulose Drugs 0.000 claims description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 2
- 235000010494 karaya gum Nutrition 0.000 claims description 2
- 239000011777 magnesium Substances 0.000 claims description 2
- 229910052749 magnesium Inorganic materials 0.000 claims description 2
- 235000001055 magnesium Nutrition 0.000 claims description 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 2
- 235000010408 potassium alginate Nutrition 0.000 claims description 2
- 239000000737 potassium alginate Substances 0.000 claims description 2
- MZYRDLHIWXQJCQ-YZOKENDUSA-L potassium alginate Chemical compound [K+].[K+].O1[C@@H](C([O-])=O)[C@@H](OC)[C@H](O)[C@H](O)[C@@H]1O[C@@H]1[C@@H](C([O-])=O)O[C@@H](O)[C@@H](O)[C@H]1O MZYRDLHIWXQJCQ-YZOKENDUSA-L 0.000 claims description 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 2
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 2
- 235000010493 xanthan gum Nutrition 0.000 claims description 2
- 239000000230 xanthan gum Substances 0.000 claims description 2
- 229920001285 xanthan gum Polymers 0.000 claims description 2
- 229940082509 xanthan gum Drugs 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group 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 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 description 11
- 239000006187 pill Substances 0.000 description 10
- LHCOVOKZWQYODM-CPEOKENHSA-N 4-amino-1-[(2r,5s)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one;1-[(2r,4s,5s)-4-azido-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1.O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 LHCOVOKZWQYODM-CPEOKENHSA-N 0.000 description 7
- 238000002560 therapeutic procedure Methods 0.000 description 7
- 229940000425 combination drug Drugs 0.000 description 6
- 239000008187 granular material Substances 0.000 description 6
- 208000030507 AIDS Diseases 0.000 description 5
- 229940124522 antiretrovirals Drugs 0.000 description 4
- 239000000890 drug combination Substances 0.000 description 4
- 239000003903 antiretrovirus agent Substances 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 229940080431 lamivudine 150 mg Drugs 0.000 description 3
- 229940102247 zidovudine 300 mg Drugs 0.000 description 3
- 239000001856 Ethyl cellulose Substances 0.000 description 2
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 2
- 241000237858 Gastropoda Species 0.000 description 2
- 208000031886 HIV Infections Diseases 0.000 description 2
- 208000037357 HIV infectious disease Diseases 0.000 description 2
- 241000725303 Human immunodeficiency virus Species 0.000 description 2
- 229960004748 abacavir Drugs 0.000 description 2
- MCGSCOLBFJQGHM-SCZZXKLOSA-N abacavir Chemical compound C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 MCGSCOLBFJQGHM-SCZZXKLOSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 2
- WHBIGIKBNXZKFE-UHFFFAOYSA-N delavirdine Chemical compound CC(C)NC1=CC=CN=C1N1CCN(C(=O)C=2NC3=CC=C(NS(C)(=O)=O)C=C3C=2)CC1 WHBIGIKBNXZKFE-UHFFFAOYSA-N 0.000 description 2
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 description 2
- 238000001647 drug administration Methods 0.000 description 2
- 235000019325 ethyl cellulose Nutrition 0.000 description 2
- 229920001249 ethyl cellulose Polymers 0.000 description 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 description 2
- 244000005700 microbiome Species 0.000 description 2
- 230000035772 mutation Effects 0.000 description 2
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 1
- QAGYKUNXZHXKMR-UHFFFAOYSA-N CPD000469186 Natural products CC1=C(O)C=CC=C1C(=O)NC(C(O)CN1C(CC2CCCCC2C1)C(=O)NC(C)(C)C)CSC1=CC=CC=C1 QAGYKUNXZHXKMR-UHFFFAOYSA-N 0.000 description 1
- BXZVVICBKDXVGW-NKWVEPMBSA-N Didanosine Chemical compound O1[C@H](CO)CC[C@@H]1N1C(NC=NC2=O)=C2N=C1 BXZVVICBKDXVGW-NKWVEPMBSA-N 0.000 description 1
- 239000005434 MCC/mannitol excipient Substances 0.000 description 1
- NCDNCNXCDXHOMX-UHFFFAOYSA-N Ritonavir Natural products C=1C=CC=CC=1CC(NC(=O)OCC=1SC=NC=1)C(O)CC(CC=1C=CC=CC=1)NC(=O)C(C(C)C)NC(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-UHFFFAOYSA-N 0.000 description 1
- XNKLLVCARDGLGL-JGVFFNPUSA-N Stavudine Chemical compound O=C1NC(=O)C(C)=CN1[C@H]1C=C[C@@H](CO)O1 XNKLLVCARDGLGL-JGVFFNPUSA-N 0.000 description 1
- WREGKURFCTUGRC-POYBYMJQSA-N Zalcitabine Chemical compound O=C1N=C(N)C=CN1[C@@H]1O[C@H](CO)CC1 WREGKURFCTUGRC-POYBYMJQSA-N 0.000 description 1
- GLWHPRRGGYLLRV-XLPZGREQSA-N [[(2s,3s,5r)-3-azido-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)[C@@H](N=[N+]=[N-])C1 GLWHPRRGGYLLRV-XLPZGREQSA-N 0.000 description 1
- 229940066321 abacavir 300 mg Drugs 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 125000005907 alkyl ester group Chemical group 0.000 description 1
- 229960001830 amprenavir Drugs 0.000 description 1
- YMARZQAQMVYCKC-OEMFJLHTSA-N amprenavir Chemical compound C([C@@H]([C@H](O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1COCC1)C1=CC=CC=C1 YMARZQAQMVYCKC-OEMFJLHTSA-N 0.000 description 1
- 230000036436 anti-hiv Effects 0.000 description 1
- 238000011225 antiretroviral therapy Methods 0.000 description 1
- 229940127555 combination product Drugs 0.000 description 1
- 229940014461 combivir Drugs 0.000 description 1
- 229960005319 delavirdine Drugs 0.000 description 1
- 229960002656 didanosine Drugs 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 229960004667 ethyl cellulose Drugs 0.000 description 1
- 235000010944 ethyl methyl cellulose Nutrition 0.000 description 1
- 239000001761 ethyl methyl cellulose Substances 0.000 description 1
- 239000007941 film coated tablet Substances 0.000 description 1
- 239000003979 granulating agent Substances 0.000 description 1
- 229960001936 indinavir Drugs 0.000 description 1
- CBVCZFGXHXORBI-PXQQMZJSSA-N indinavir Chemical compound C([C@H](N(CC1)C[C@@H](O)C[C@@H](CC=2C=CC=CC=2)C(=O)N[C@H]2C3=CC=CC=C3C[C@H]2O)C(=O)NC(C)(C)C)N1CC1=CC=CN=C1 CBVCZFGXHXORBI-PXQQMZJSSA-N 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 125000005395 methacrylic acid group Chemical class 0.000 description 1
- 229960002900 methylcellulose Drugs 0.000 description 1
- 229960000884 nelfinavir Drugs 0.000 description 1
- QAGYKUNXZHXKMR-HKWSIXNMSA-N nelfinavir Chemical compound CC1=C(O)C=CC=C1C(=O)N[C@H]([C@H](O)CN1[C@@H](C[C@@H]2CCCC[C@@H]2C1)C(=O)NC(C)(C)C)CSC1=CC=CC=C1 QAGYKUNXZHXKMR-HKWSIXNMSA-N 0.000 description 1
- 239000002777 nucleoside Substances 0.000 description 1
- 150000003833 nucleoside derivatives Chemical class 0.000 description 1
- 239000012735 once-a-day formulation Substances 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 229960000311 ritonavir Drugs 0.000 description 1
- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 description 1
- 229960001852 saquinavir Drugs 0.000 description 1
- QWAXKHKRTORLEM-UGJKXSETSA-N saquinavir Chemical compound C([C@@H]([C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)C=1N=C2C=CC=CC2=CC=1)C1=CC=CC=C1 QWAXKHKRTORLEM-UGJKXSETSA-N 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 229960001203 stavudine Drugs 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 229940111527 trizivir Drugs 0.000 description 1
- 230000017613 viral reproduction Effects 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 229960000523 zalcitabine Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Virology (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN417MU2003 | 2003-10-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200603421B true ZA200603421B (en) | 2007-09-26 |
Family
ID=34611194
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200603421A ZA200603421B (en) | 2003-10-01 | 2006-04-28 | A controlled release pharmaceutical composition and a process for preparing the same |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20070231385A1 (zh) |
| EP (1) | EP1673072B1 (zh) |
| CN (1) | CN1863512A (zh) |
| AP (1) | AP1826A (zh) |
| AT (1) | ATE358470T1 (zh) |
| BR (1) | BRPI0415322A (zh) |
| DE (1) | DE602004005734T2 (zh) |
| EA (1) | EA008944B1 (zh) |
| ES (1) | ES2286716T3 (zh) |
| MX (1) | MXPA06003479A (zh) |
| UA (1) | UA82564C2 (zh) |
| WO (1) | WO2005048978A2 (zh) |
| ZA (1) | ZA200603421B (zh) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006114709A1 (en) * | 2005-04-25 | 2006-11-02 | Aurobindo Pharma Limited | Pharmaceutical compositions of antiretrovirals |
| UA97971C2 (ru) | 2007-06-08 | 2012-04-10 | Берингер Ингельхайм Интернациональ Гмбх | Препарат невирапина пролонгированного высвобождения |
| CA2767335C (en) * | 2009-07-14 | 2013-09-24 | Hill's Pet Nutrition, Inc. | Pet food compositions including a sustained-release lipoic acid and methods of manufacture and use thereof |
| CN102247332B (zh) * | 2011-01-27 | 2015-03-25 | 济南久创化学有限责任公司 | 一种拉米夫定片及其制备方法 |
| CN102225069B (zh) * | 2011-04-29 | 2013-05-08 | 陶珍珠 | 一种耐药性显著降低的药物组合物及其制备方法和其应用 |
| US20140193491A1 (en) * | 2011-05-30 | 2014-07-10 | Cipla Limited | Pharmaceutical antiretroviral composition |
| WO2013111147A1 (en) * | 2011-12-19 | 2013-08-01 | Hetero Research Foundation | Extended release compositions of nevirapine |
| CN107334743B (zh) * | 2016-07-15 | 2020-04-21 | 安徽贝克生物制药有限公司 | 一种齐多夫定、拉米夫定、奈韦拉平复方片及其制备方法 |
| CN114392239B (zh) * | 2022-01-10 | 2023-06-27 | 安徽贝克生物制药有限公司 | 一种拉米夫定、齐多夫定和依非韦伦的复方片及其制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL108838C (zh) * | 1956-03-27 | |||
| GB8707421D0 (en) * | 1987-03-27 | 1987-04-29 | Wellcome Found | Pharmaceutical formulations |
| US6177435B1 (en) * | 1992-05-13 | 2001-01-23 | Glaxo Wellcome Inc. | Therapeutic combinations |
| IT1264696B1 (it) * | 1993-07-09 | 1996-10-04 | Applied Pharma Res | Forme farmaceutiche destinate alla somministrazione orale in grado di rilasciare sostanze attive a velocita' controllata e differenziata |
| US6113920A (en) * | 1996-10-31 | 2000-09-05 | Glaxo Wellcome Inc. | Pharmaceutical compositions |
| GB9821000D0 (en) * | 1998-09-28 | 1998-11-18 | Glaxo Group Ltd | Antiviral combinations |
| ZA200110500B (en) * | 2001-05-11 | 2002-04-03 | Cipla Medpro Pty Ltd | Pharmaceutical composition. |
-
2004
- 2004-09-29 ES ES04817650T patent/ES2286716T3/es not_active Expired - Lifetime
- 2004-09-29 AT AT04817650T patent/ATE358470T1/de not_active IP Right Cessation
- 2004-09-29 EP EP04817650A patent/EP1673072B1/en not_active Expired - Lifetime
- 2004-09-29 EA EA200600679A patent/EA008944B1/ru not_active IP Right Cessation
- 2004-09-29 US US10/574,320 patent/US20070231385A1/en not_active Abandoned
- 2004-09-29 BR BRPI0415322-7A patent/BRPI0415322A/pt not_active IP Right Cessation
- 2004-09-29 WO PCT/IN2004/000306 patent/WO2005048978A2/en active IP Right Grant
- 2004-09-29 AP AP2006003597A patent/AP1826A/xx active
- 2004-09-29 DE DE602004005734T patent/DE602004005734T2/de not_active Expired - Lifetime
- 2004-09-29 CN CNA2004800288530A patent/CN1863512A/zh active Pending
- 2004-09-29 MX MXPA06003479A patent/MXPA06003479A/es active IP Right Grant
- 2004-09-29 UA UAA200604821A patent/UA82564C2/uk unknown
-
2006
- 2006-04-28 ZA ZA200603421A patent/ZA200603421B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| UA82564C2 (uk) | 2008-04-25 |
| AP2006003597A0 (en) | 2006-04-30 |
| AP1826A (en) | 2008-02-08 |
| MXPA06003479A (es) | 2006-06-08 |
| ES2286716T3 (es) | 2007-12-01 |
| EA008944B1 (ru) | 2007-10-26 |
| EA200600679A1 (ru) | 2006-08-25 |
| DE602004005734T2 (de) | 2007-12-27 |
| US20070231385A1 (en) | 2007-10-04 |
| BRPI0415322A (pt) | 2006-12-05 |
| WO2005048978A3 (en) | 2006-02-23 |
| ATE358470T1 (de) | 2007-04-15 |
| CN1863512A (zh) | 2006-11-15 |
| EP1673072B1 (en) | 2007-04-04 |
| DE602004005734D1 (de) | 2007-05-16 |
| EP1673072A2 (en) | 2006-06-28 |
| WO2005048978A2 (en) | 2005-06-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ZA200603421B (en) | A controlled release pharmaceutical composition and a process for preparing the same | |
| AU2001268719B2 (en) | Composition and dosage form for delayed gastric release of alendronate and/or other bis-phosphonates | |
| JP6122098B2 (ja) | オルメサルタンメドキソミルとロスバスタチンまたはその塩とを含む医薬組成物 | |
| CA2518734A1 (en) | A process for preparing sustained release tablets | |
| US20070243249A1 (en) | Novel formulation of pyridoxal-5'-phosphate and method of preparation | |
| KR100202154B1 (ko) | 파라세타몰 및 돔페리돈을 함유한 필름 피복 정제 | |
| JP2007519608A (ja) | 時間治療用剤形 | |
| JP2011168596A (ja) | トラネキサム酸製剤 | |
| JP2002524410A (ja) | リプスタチン誘導体−可溶性繊維錠剤 | |
| AU2015228545B2 (en) | Ondansetron extended release solid dosage forms for treating either nausea, vomiting or diarrhea symptoms | |
| WO2004078111A2 (en) | Extended release minocycline compositions and processes for their preparation | |
| KR20060103330A (ko) | 서방성 톨스마이드 제형 | |
| US20060159751A1 (en) | Controlled release pharmaceutical compositions of carbidopa and levodopa | |
| EP1589957A1 (en) | Pharmaceutical compositions and process of production thereof | |
| CA2925960A1 (en) | Pharmaceutical composition comprising capecitabine and cyclophosphamide | |
| AU2005235237A1 (en) | Clarithromycin extended release formulation | |
| WO2018028841A1 (en) | Solid pharmaceutical composition of abacavir, lamivudine, and efavirenz | |
| KR102409102B1 (ko) | 제약 조성물 | |
| EP3334419A1 (en) | Solid pharmaceutical composition of abacavir, lamivudine, and efavirenz | |
| SK50222004A3 (sk) | Kompozície matrice s modifikovaným uvoľňovaním, s dlhodobým účinkom | |
| JPS62246512A (ja) | 反復作用製剤 | |
| US20040192706A1 (en) | Method and compositions for treating anxiety | |
| US20120201883A1 (en) | Antiviral compositons |