k-卡拉胶在挤出滚圆法制备缬沙坦速释微丸中的应用
Application of k-carrageenan in valsartan immediate-release pellets by extrusion-spheronization
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摘要: 对挤出滚圆法制备缬沙坦速释微丸的成球促进剂进行筛选，并对缬沙坦速释微丸处方进行优化。通过单因素考察评价并比较微晶纤维素(MCC)、低取代羟丙基纤维素(L-HPC)、交联聚维酮(PVPP)、预胶化淀粉(PCS)及k-卡拉胶5种辅料制得的碳酸钙微丸的质量，初步筛选可用的成球促进剂；进一步评价并比较MCC、L-HPC及k-卡拉胶制得的缬沙坦速释微丸的质量，确定k-卡拉胶为制备缬沙坦速释微丸的最佳成球促进剂。采用Box-Behnken响应面法对该缬沙坦速释微丸的处方进行优化，确定最优处方:k-卡拉胶含量16.98 g，HPMC E5含量2.03 g，SLS含量0.26 g，在此条件下制备出的微丸的收率为91.23%，长径比为1.14，预测值与实际值相符。结果表明k-卡拉胶制得的缬沙坦速释微丸圆整度好、收率高、溶出迅速。Abstract: The aim of the study was to select a suitable pelletisation aid of valsartan immediate-release pellets in the extrusion process and optimized the formulation. The properties of the pellets with five excipients which were microcrystalline cellulose(MCC), low-substituted hydroxypropyl cellulose(L-HPC), crospovidone(PVPP), pregelatinized starch(PCS)and k-carrageenan were evaluated and compared by the single factor test. And the pelletisation aids were chosen preliminary. The properties of the pellets with MCC, L-HPC, k-carrageenan respectively were evaluated and compared and k-carrageenan was determined as the most appropriate pelletisation aid. The Box-Behnken design was employed to optimize the formulation. The optimised formulation was k-carrageenan 16. 98 g, HPMC-E5 2. 03 g, SLS 0. 26 g. The yield and aspect ratio of pellets was 91. 23% and 1. 14, respectively. And there was no significant difference between observed and predictive responses. The results showed k-carrageenan pellets owned properties of a high yield, acceptable sphericity and fast drug release.
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