UA81335C2 - Оральная дозированная форма саквинавира мезилата - Google Patents
Оральная дозированная форма саквинавира мезилата Download PDFInfo
- Publication number
- UA81335C2 UA81335C2 UAA200601231A UAA200601231A UA81335C2 UA 81335 C2 UA81335 C2 UA 81335C2 UA A200601231 A UAA200601231 A UA A200601231A UA A200601231 A UAA200601231 A UA A200601231A UA 81335 C2 UA81335 C2 UA 81335C2
- Authority
- UA
- Ukraine
- Prior art keywords
- dosage form
- pharmaceutically acceptable
- granules
- saquinavir
- saquinavir mesylate
- Prior art date
Links
- IRHXGOXEBNJUSN-YOXDLBRISA-N Saquinavir mesylate Chemical compound CS(O)(=O)=O.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 IRHXGOXEBNJUSN-YOXDLBRISA-N 0.000 title claims abstract description 57
- 229960003542 saquinavir mesylate Drugs 0.000 title claims abstract description 56
- 239000006186 oral dosage form Substances 0.000 title description 4
- 239000002552 dosage form Substances 0.000 claims abstract description 61
- 239000012458 free base Substances 0.000 claims abstract description 22
- 239000007884 disintegrant Substances 0.000 claims abstract description 21
- 239000007787 solid Substances 0.000 claims abstract description 18
- 239000011230 binding agent Substances 0.000 claims abstract description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 14
- 239000003232 water-soluble binding agent Substances 0.000 claims abstract description 8
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims abstract description 5
- 239000008187 granular material Substances 0.000 claims description 46
- 239000000203 mixture Substances 0.000 claims description 34
- 239000002775 capsule Substances 0.000 claims description 18
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 18
- 229960001852 saquinavir Drugs 0.000 claims description 16
- 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 claims description 16
- 230000001050 lubricating effect Effects 0.000 claims description 13
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 11
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 11
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 11
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 11
- 239000002245 particle Substances 0.000 claims description 10
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 10
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 10
- 239000003937 drug carrier Substances 0.000 claims description 9
- 239000007888 film coating Substances 0.000 claims description 9
- 238000009501 film coating Methods 0.000 claims description 9
- 235000019359 magnesium stearate Nutrition 0.000 claims description 9
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 8
- 238000005469 granulation Methods 0.000 claims description 8
- 230000003179 granulation Effects 0.000 claims description 8
- 239000000843 powder Substances 0.000 claims description 8
- 229920002785 Croscarmellose sodium Polymers 0.000 claims description 7
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical group [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 7
- 229960001681 croscarmellose sodium Drugs 0.000 claims description 7
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 7
- 238000001035 drying Methods 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 7
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical group 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 6
- 229960001021 lactose monohydrate Drugs 0.000 claims description 6
- 238000000034 method Methods 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 5
- 238000011282 treatment Methods 0.000 claims description 4
- 239000012052 hydrophilic carrier Substances 0.000 claims description 3
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 239000008383 extra-granule composition Substances 0.000 claims description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 2
- 239000007921 spray Substances 0.000 claims description 2
- RHWXXFCIPRZHCO-UHFFFAOYSA-K CS(=O)(=O)[O-].[B+3].CS(=O)(=O)[O-].CS(=O)(=O)[O-] Chemical compound CS(=O)(=O)[O-].[B+3].CS(=O)(=O)[O-].CS(=O)(=O)[O-] RHWXXFCIPRZHCO-UHFFFAOYSA-K 0.000 claims 1
- 229960000913 crospovidone Drugs 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 1
- 239000007892 solid unit dosage form Substances 0.000 abstract 1
- 239000000306 component Substances 0.000 description 14
- 238000004090 dissolution Methods 0.000 description 13
- 229940069328 povidone Drugs 0.000 description 7
- 229940079593 drug Drugs 0.000 description 5
- 239000003814 drug Substances 0.000 description 5
- 239000000945 filler Substances 0.000 description 5
- 239000012530 fluid Substances 0.000 description 5
- 239000008188 pellet Substances 0.000 description 5
- 229940079832 sodium starch glycolate Drugs 0.000 description 5
- 239000008109 sodium starch glycolate Substances 0.000 description 5
- 229920003109 sodium starch glycolate Polymers 0.000 description 5
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 4
- 238000011049 filling Methods 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 239000008213 purified water Substances 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 238000007906 compression Methods 0.000 description 3
- 230000006835 compression Effects 0.000 description 3
- -1 for example Chemical compound 0.000 description 3
- 230000002496 gastric effect Effects 0.000 description 3
- 235000012054 meals Nutrition 0.000 description 3
- 229910001220 stainless steel Inorganic materials 0.000 description 3
- 239000010935 stainless steel Substances 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- 239000000454 talc Substances 0.000 description 3
- 229910052623 talc Inorganic materials 0.000 description 3
- 241000725303 Human immunodeficiency virus Species 0.000 description 2
- 239000004698 Polyethylene Substances 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 230000000798 anti-retroviral effect Effects 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 238000000227 grinding Methods 0.000 description 2
- 230000000968 intestinal effect Effects 0.000 description 2
- 238000005461 lubrication Methods 0.000 description 2
- 239000002777 nucleoside Substances 0.000 description 2
- 150000003833 nucleoside derivatives Chemical class 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 229920000573 polyethylene Polymers 0.000 description 2
- 239000011164 primary particle Substances 0.000 description 2
- 238000005507 spraying Methods 0.000 description 2
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 229920002261 Corn starch Polymers 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
- 238000010521 absorption reaction Methods 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 238000000889 atomisation Methods 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 235000021152 breakfast Nutrition 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000011436 cob Substances 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 238000010579 first pass effect Methods 0.000 description 1
- 230000009246 food effect Effects 0.000 description 1
- 235000021471 food effect Nutrition 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 239000001087 glyceryl triacetate Substances 0.000 description 1
- 235000013773 glyceryl triacetate Nutrition 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 229940031705 hydroxypropyl methylcellulose 2910 Drugs 0.000 description 1
- 230000036737 immune function Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 239000008184 oral solid dosage form Substances 0.000 description 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 1
- 229940124531 pharmaceutical excipient Drugs 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 230000010076 replication Effects 0.000 description 1
- 230000000630 rising effect Effects 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
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
- 238000000870 ultraviolet spectroscopy Methods 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- 238000011179 visual inspection Methods 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Твердая единичная оральная фармацевтическая дозированная форма саквинавира мезилата предусматривает содержание от 60 % до 80 % микронизированного саквинавира мезилата, исходя из соли мезилата, 4 % - 8 % водорастворимого связующего, дезинтегратора и носителя, где каждый процент является процентом веса ядра дозированной формы. Твердая единичная оральная фармацевтическая дозированная форма саквинавира мезилата, которая имеет вес от 400 мг до 1,5 г, предусматривает содержание микронизированного саквинавира мезилата в количестве от 200 мг до 800 мг, в расчете для свободной основы, фармацевтически приемлемого связующего, дезинтегратора и водорастворимого носителя.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US48660003P | 2003-07-11 | 2003-07-11 | |
| PCT/EP2004/007309 WO2005004836A2 (en) | 2003-07-11 | 2004-07-05 | Saquinavir mesylate oral dosage form |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA81335C2 true UA81335C2 (ru) | 2007-12-25 |
Family
ID=36923757
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UAA200601231A UA81335C2 (ru) | 2003-07-11 | 2004-05-07 | Оральная дозированная форма саквинавира мезилата |
Country Status (3)
| Country | Link |
|---|---|
| CN (1) | CN1822822B (ru) |
| GT (1) | GT200400131A (ru) |
| UA (1) | UA81335C2 (ru) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104096216B (zh) * | 2014-07-08 | 2016-03-09 | 滨州医学院 | 甲磺酸沙奎拉韦在制备预防或治疗缺血性心脑血管疾病的药物中的应用 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6039975A (en) * | 1995-10-17 | 2000-03-21 | Hoffman-La Roche Inc. | Colon targeted delivery system |
| US6514530B2 (en) * | 1997-09-09 | 2003-02-04 | Alza Corporation | Dosage form comprising means for changing drug delivery shape |
| US20030068356A1 (en) * | 2001-07-10 | 2003-04-10 | Pather S. Indiran | Sequential drug delivery systems |
-
2004
- 2004-05-07 UA UAA200601231A patent/UA81335C2/ru unknown
- 2004-07-05 CN CN200480019933.XA patent/CN1822822B/zh not_active Expired - Lifetime
- 2004-07-08 GT GT200400131A patent/GT200400131A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN1822822A (zh) | 2006-08-23 |
| CN1822822B (zh) | 2010-06-16 |
| GT200400131A (es) | 2005-02-22 |
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