CN114425039A - 改进的依非韦伦速释制剂 - Google Patents
改进的依非韦伦速释制剂 Download PDFInfo
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- CN114425039A CN114425039A CN202011181598.0A CN202011181598A CN114425039A CN 114425039 A CN114425039 A CN 114425039A CN 202011181598 A CN202011181598 A CN 202011181598A CN 114425039 A CN114425039 A CN 114425039A
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- efavirenz
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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
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
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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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Abstract
Description
批号 | D(0.1)um | D(0.5)um | D(0.9)um |
001 | 0.8 | 2.8 | 12.3 |
002 | 1 | 2 | 6 |
003 | 1.7 | 6.1 | 15.2 |
004 | 1.6 | 8.1 | 39.9 |
名称 | 重量(g) |
依非韦伦(批号001) | 200 |
微晶纤维素 | 75 |
乳糖 | 75 |
羟丙基纤维素 | 8 |
十二烷基硫酸钠 | 8 |
交联羧甲基纤维素钠 | 30 |
硬脂酸镁 | 4 |
片重 | 400 |
名称 | 重量(g) |
依非韦伦(批号002) | 200 |
微晶纤维素 | 100 |
乳糖 | 50 |
羟丙甲纤维素 | 12 |
十二烷基硫酸钠 | 6 |
羧甲淀粉钠 | 30 |
硬脂酸镁 | 2 |
片重 | 400 |
名称 | 重量(g) |
依非韦伦(批号003) | 200 |
微晶纤维素 | 100 |
预胶化淀粉 | 50 |
羟丙基纤维素 | 16 |
十二烷基硫酸钠 | 10 |
交联羧甲基纤维素钠 | 20 |
硬脂酸镁 | 4 |
素片重 | 400 |
名称 | 重量(g) |
依非韦伦(批号004) | 200 |
微晶纤维素 | 75 |
乳糖 | 75 |
羟丙基纤维素 | 8 |
十二烷基硫酸钠 | 8 |
交联羧甲基纤维素钠 | 30 |
硬脂酸镁 | 4 |
素片重 | 400 |
5min | 10min | 15min | 20min | 30min | 45min | |
实施例1 | 45 | 73 | 94 | 96 | 98 | 98 |
实施例2 | 43 | 70 | 92 | 95 | 96 | 97 |
实施例3 | 48 | 75 | 93 | 96 | 98 | 98 |
实施例4 | 38 | 69 | 85 | 87 | 88 | 89 |
对比例1 | 25 | 45 | 63 | 76 | 87 | 92 |
施多宁 | 20 | 42 | 65 | 79 | 89 | 92 |
参数(单位) | 施多宁,R药 | 实施例1,T药 | 相对生物利用度 |
C<sub>max</sub>(ng/mL) | 738.5 | 1131.1 | 149.6% |
AUC<sub>0-72</sub>(h*ng/ml) | 19783.0 | 25096.8 | 126.6% |
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Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2010125572A1 (en) * | 2009-04-29 | 2010-11-04 | Hetero Research Foundation | Compressed tablets and capsules containing efavirenz |
CN102872019A (zh) * | 2012-09-17 | 2013-01-16 | 北京阜康仁生物制药科技有限公司 | 一种采用微粉化技术的依非韦伦制剂 |
CN102988316A (zh) * | 2012-11-22 | 2013-03-27 | 安徽贝克生物制药有限公司 | 依非韦伦片及其制备方法 |
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Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2010125572A1 (en) * | 2009-04-29 | 2010-11-04 | Hetero Research Foundation | Compressed tablets and capsules containing efavirenz |
CN102872019A (zh) * | 2012-09-17 | 2013-01-16 | 北京阜康仁生物制药科技有限公司 | 一种采用微粉化技术的依非韦伦制剂 |
CN102988316A (zh) * | 2012-11-22 | 2013-03-27 | 安徽贝克生物制药有限公司 | 依非韦伦片及其制备方法 |
Non-Patent Citations (2)
Title |
---|
石海涛等: "流化床制粒法制备甲磺酸吉米沙星片", 《中国当代医药》 * |
石海涛等: "流化床制粒法制备甲磺酸吉米沙星片", 《中国当代医药》, vol. 16, no. 15, 31 August 2009 (2009-08-31), pages 148 - 149 * |
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