CN104274417A - 他达拉非的口服药物制剂 - Google Patents
他达拉非的口服药物制剂 Download PDFInfo
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- CN104274417A CN104274417A CN201410563973.6A CN201410563973A CN104274417A CN 104274417 A CN104274417 A CN 104274417A CN 201410563973 A CN201410563973 A CN 201410563973A CN 104274417 A CN104274417 A CN 104274417A
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Abstract
Description
参数名称 | 希爱力片 | 口崩片 | 咀嚼片 | 口腔膜剂 | p |
Cmax(ng.ml-1) | 164(23.1) | 201(26.7) | 209(28.7) | 197(29.3) | <0.01 |
Tmax(h) | 3(1.0-4.0) | 4(1.0-4.0) | 4(1.0-4.0) | 3(1.0-4.0) | >0.05 |
Ke(h-1) | 0.0368 | 0.0371 | 0.0374 | 0.0369 | >0.05 |
T1/2b(h) | 18.6(12.6-34.5) | 18.2(10.8-31.3) | 18.5(11.2-33.4) | 18.3(12.9-35.7) | >0.05 |
AUC0-t(ng.h.ml-1) | 3790(35.3) | 4810(33.6) | 4870(32.1) | 4830(34.5) | <0.01 |
AUC0-∞(ng.h.ml-1) | 3920(35.3) | 4880(33.6) | 4930(32.1) | 4890(34.5) | <0.01 |
CL/F(L.h-1) | 2.79(30.7) | 2.81(29.2) | 2.82(31.0) | 2.77(29.4) | >0.05 |
V/F(L) | 73.3(20.1) | 73.7(25.8) | 72.1(23.9) | 71.2(22.2) | >0.05 |
他达拉非 | 100g | 10.0% |
聚乙烯吡咯烷酮(PVP) | 125g | 12.5% |
甘露醇 | 700g | 70% |
硬脂酸镁 | 15g | 1.5% |
柠檬酸 | 30g | 3% |
碳酸氢钠 | 30g | 3% |
他达拉非 | 20g | 10.0% |
羧甲基淀粉钠 | 27g | 13.5% |
羟丙甲基纤维素 | 10g | 5.0% |
甘露醇 | 140g | 70.0% |
阿司帕坦 | 1g | 0.5% |
滑石粉 | 2g | 1.0% |
他达拉非 | 10g | 5.0% |
交联聚维酮 | 27g | 13.5% |
羟丙基纤维素 | 10g | 5.0% |
蔗糖 | 150g | 75.0% |
甜菊素 | 1g | 0.5% |
硬脂酸镁 | 2g | 1.0% |
他达拉非 | 20g | 10.0% |
交联羧甲基纤维素钠 | 25g | 12.5% |
聚维酮K30 | 8g | 4.0% |
乳糖 | 140g | 70.0% |
薄荷香精 | 4g | 2.0% |
硬脂酸镁 | 3g | 1.5% |
他达拉非 | 10g | 5.0% |
交联羧甲基纤维素钠 | 26g | 13.0% |
聚维酮K30 | 8g | 4.0% |
乳糖 | 150g | 75.0% |
薄荷香精 | 4g | 2.0% |
硬脂酸镁 | 2g | 1.0% |
崩解时间(s) | 口感 | |
实施例1 | 18 | 无味 |
实施例2 | 16 | 味甜 |
实施例3 | 15 | 味甜 |
实施例4 | 13 | 味甜且清新 |
实施例5 | 12 | 味甜且清新 |
他达拉非 | 100g | 34.6% |
聚乙烯醇1788 | 133g | 46.0% |
聚乙二醇400 | 33g | 11.4% |
海藻酸钠 | 13g | 4.5% |
纯化水 | 10g | 3.5% |
他达拉非 | 100g | 33.7% |
聚乙烯醇1788 | 133g | 44.8% |
聚乙二醇400 | 33g | 11.1% |
海藻酸钠 | 13g | 4.4% |
阿司帕坦 | 3g | 1.0% |
吐温80 | 5g | 1.7% |
日落黄 | 0.05g | 0.017% |
乙醇水 | 10g | 3.4% |
他达拉非 | 100g | 33.7% |
聚乙烯醇1788 | 133g | 44.8% |
聚乙二醇400 | 33g | 11.1% |
海藻酸钠 | 13g | 4.4% |
薄荷香精 | 3g | 1.0% |
十二烷基硫酸钠 | 5g | 1.7% |
日落黄 | 0.05g | 0.017% |
乙醇水 | 10g | 3.4% |
崩解时间(s) | 口感 | |
实施例7 | 58 | 苦涩味 |
实施例8 | 46 | 味甜 |
实施例9 | 43 | 味甜且清新 |
他达拉非 | 20g | 10.0% |
羧甲基淀粉钠 | 10g | 5.0% |
聚维酮K30 | 18g | 9.0% |
微晶纤维素 | 150g | 75.0% |
橙子香精 | 1g | 0.5% |
滑石粉 | 1g | 0.5% |
他达拉非 | 5g | 2.5% |
交联聚维酮 | 12g | 6.0% |
羟丙基纤维素 | 15g | 7.5% |
预胶化淀粉 | 165g | 82.5% |
阿司帕坦 | 1g | 0.5% |
滑石粉 | 2g | 1.0% |
他达拉非 | 20g | 10.0% |
交联羧甲基纤维素钠 | 8g | 4.0% |
聚维酮K30 | 8g | 4.0% |
乳糖 | 155g | 77.5% |
薄荷香精 | 6g | 3.0% |
硬脂酸镁 | 3g | 1.5% |
他达拉非 | 10g | 5.0% |
交联羧甲基纤维素钠 | 8g | 4.0% |
聚维酮K30 | 8g | 4.0% |
乳糖 | 165g | 82.5% |
薄荷香精 | 6g | 3.0% |
硬脂酸镁 | 3g | 1.5% |
他达拉非 | 5g | 2.5% |
交联羧甲基纤维素钠 | 9g | 4.5% |
聚维酮K30 | 9g | 4.5% |
乳糖 | 168g | 84% |
薄荷香精 | 5g | 2.5% |
硬脂酸镁 | 4g | 2.0% |
有无砂砾感 | 口感评分 | |
实施例11 | 有 | 6.5 |
实施例12 | 略有 | 7.2 |
实施例13 | 无 | 9.5 |
实施例14 | 无 | 9.2 |
实施例15 | 无 | 9.1 |
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CN1363628A (zh) * | 2002-01-16 | 2002-08-14 | 郝喜海 | 调控水溶性薄膜的水溶解速度的方法 |
CN1846729A (zh) * | 2005-04-12 | 2006-10-18 | 天津药物研究院 | 一种在口腔中快速溶解的薄膜新剂型及其制备方法 |
CN102824333A (zh) * | 2012-09-26 | 2012-12-19 | 苏州大学 | 一种口腔速溶膜剂及其制备方法 |
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CN1363628A (zh) * | 2002-01-16 | 2002-08-14 | 郝喜海 | 调控水溶性薄膜的水溶解速度的方法 |
CN1846729A (zh) * | 2005-04-12 | 2006-10-18 | 天津药物研究院 | 一种在口腔中快速溶解的薄膜新剂型及其制备方法 |
CN102824333A (zh) * | 2012-09-26 | 2012-12-19 | 苏州大学 | 一种口腔速溶膜剂及其制备方法 |
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