甲磺酸多沙唑嗪片制剂处方工艺探讨(1)
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2011年1月15日
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[摘要] 目的：筛选甲磺酸多沙唑嗪片的最佳处方组成。方法：通过全面考察市售品外观，崩解时限，溶出度，溶出曲线，含量测定等，了解该产品的特征；以市售品上述指标为依据，以片剂外观、可压性、崩解时限、溶出度为基本指标进行处方筛选。结果：最佳处方组成为每片含甲磺酸多沙唑嗪2.43 mg(相当于多沙唑嗪2 mg)，乳糖75 mg，微晶纤维素45 mg，羧甲基淀粉钠7 mg，10%PVPk30乙醇溶液(50%)100 mg，吐温0.03 g，硬脂酸镁1.2 mg。结论：采用本处方及工艺制得的甲磺酸多沙唑嗪片溶出度符合中国药典要求，与市售甲磺酸多沙唑嗪片相似，且制备工艺简单，适于工业化生产。
[关键词] 甲磺酸多沙唑嗪片；处方；含量；溶出度
[中图分类号] R943 [文献标识码] B[文章编号] 1674-4721(2011)01(b)-120-04
Prescription and technology research of mesylate doxazosin tablets
JIANG Yuping
(The People's Hospital of Danyang City, Jiangsu Province, Danyang 212300, China)
[Abstract] Objective: To screen mesylate tablets doxazosin composed of the best prescription. Methods: Goods sold through the appearance of a comprehensive study, disintegration, dissolution, dissolution curve, determination and so on, to understand the characteristics of the product; to market products based on the above-mentioned indicators, the appearance of a tablet can be pressure, the collapse of time dissolution of the basic indicators for the screening prescription. Results: The best prescription for every film with the composition of mesylate doxazosin 2.43 mg (equivalent to doxazosin 2 mg), lactose 75 mg, microcrystalline cellulose 45 mg, carboxymethyl starch sodium 7 mg, 10% PVPk30 ethanol solution (50%) 100 mg, Twain 0.03 g, magnesium stearate 1.2 mg. Conclusion: The use of the prescription and technology obtained mesylate doxazosin tablet dissolution requirements in line with the Chinese Pharmacopoeia, and the market mesylate doxazosin film similar to the preparation process is simple and suitable for industrial manufacture.
[Key words] Mesylate doxazosin tablets; Prescription; Content; Dissolution
甲磺酸多沙唑嗪(doxazosin mesylate)的化学名为1-(4-氨基-6，7-二甲氧基-2-喹唑啉基)-4-(1，4-苯骈二恶烷-2-甲酰基)哌嗪甲磺酸盐。分子式为C23H25N5O5·CH3SO3H，分子量为547.59。甲磺酸多沙唑嗪片是长效α1受体阻滞剂，有明显的降压和降脂作用，且对缓解良性前列腺肥大症状效果明显。已被FDA批准作为治疗高血压的一线药物。该药的特点是[1]：①对α1受体选择性强。②半衰期长，为9 h，可qd服药。③无首剂效应(首次服药较少引起低血压)。④长期使用不产生耐药性，与其他抗高血压药不产生交叉耐药性。⑤不引起反射性心动过速，不影响肾血流量，不增加肾素分泌。
1 甲磺酸多沙唑嗪片的制备
1.1制备供试品
1.1.1 将甲磺酸多沙唑嗪粉碎过120目筛，其他辅料过100目筛,备用；配制10%PVPK30乙醇溶液(50%)，并加入0.03 g吐温80，摇匀，备用。
1.1.2 称取处方量的甲磺酸多沙唑嗪2.0 g(以多沙唑嗪计)、乳糖75 g、羧甲基淀粉钠7 g，混合20 min；再称取处方量的微晶纤维素45 g，与上述混粉混合20 min；加入上述溶液作黏合剂制软材；将软材过20目筛制颗粒；湿颗粒于55~60℃干燥2 h；将烘干的颗粒取出 ......
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