盐酸坦洛新处方工艺的探讨

Study on the new formulation and preparation of tamsulosin hydrochlorid

目的:研究以海藻酸钠和羟丙基甲基纤维素(HPMC)为骨架材料制备盐酸坦洛新亲水凝胶骨架缓释片并考察其释放行为。方法:采用相似因子法考察工艺因素和处方因素对体外释放度的影响。工艺因素包括片重和压片压力的选择,处方因素包括骨架材料和阻释剂的选择和用量。结果:随着片重的增加,药物释放显著降低;压片压力增加,释放度有一定的下降趋势;最终选择片重为0.1g,压片压力为6～10kg。不同的阻释剂对药物的释放影响不同,均可在一定程度上阻碍药物释放。HPMC的黏度与用量对药物的释放影响最大,随着其黏度或用量的增加,释放度显著降低。结论:通过调节片重、压片压力、应用适当的阻释剂以及改变HPMC的黏度与用量均可以改善盐酸坦洛新亲水凝胶骨架缓释片的释药行为。

Objective： To prepare tamsulosin hydrochloride hydrophilic gel matrix sustained-release tablets with different matrix materials such as HPMC and sodium alginate.Methods： Similarity factor method was used to evaluate drug release in vitro,the technological factors of including the weight of tablets and the selection of the tablet pressure,the formulation factors including matrix materials,the selection and amount of the blockers.Results： The viscosity and amount of HPMC influenced the release properties significantly.Other factors,such as the tablet weight and tablet pressure as well as sorts of blockers also had some effects on drug release.The tablet weight was selected as 0.1 g,and the tablet pressure as 6~10 kg.The different blockers produced the different effects on drug release,which can inhibit the drug release to some degree.Conclusion： The drug release activity of tamsulosin hydrochloride hydrophilic gel matrix sustained release tablets can be improved by regulating the tablet weight,the tablet pressure,the suitable application of blockers,and improving the viscosity and amount of HPMC.