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乙酰半胱氨酸活性炭微囊的制备工艺筛选

         

摘要

目的:制备乙酰半胱氨酸活性炭微囊(ACNAC),并优化工艺条件。方法:以生物可降解材料明胶为囊材,采用乳化交联法制备ACNAC。以载药量、包封率和粒径分布百分数(粒径为80~140µm者所占百分数)的综合评价指标为指标,以药载比、明胶用量、搅拌速度、乳化剂用量为因素,采用单因素试验和正交试验优化处方工艺,验证并测定所制ACNAC的粒径分布。结果:最优处方工艺为药载比1∶1、明胶15%、乳化剂2.0%、搅拌速度1000 r/min。所制6批ACNAC的平均载药量为15.9%(RSD=1.21%),平均包封率为78.1%(RSD=1.11%),平均粒径分布百分数为81.9%。结论:成功制得ACNAC,且处方工艺合理、可行。%OBJECTIVE:To prepare Activated carbon N-acetylcysteine microcapsule (ACNAC),and to optimize preparation technology. METHODS:ACNAC was prepared by emulsion cross-linked method using biodegradable material gelatin as capsule wall material. Using comprehensive evaluation index of drug-loading amount,entrapment rate and particle size distribution percent-age(the percentage of 80-140 µm particle)as index,drug-loading ratio,amount of gelatin,mixing speed and the amount of emul-sifier as factors,single factor test and orthogonal test were used to optimize formulation technology. The technology was validated and distribution of particle size of ACNAC was determined. RESULTS:The optimal formulation technology was as follows as drug-loading ratio 1∶1,gelatin 15%,emulsifier 2.0%,mixing speed 1 000 r/min. Average drug-loading amount of 6 batches of ACNAC was 15.9%(RSD=1.21%),average encapsulation efficiency was 78.1%(RSD=1.11%)and average particle size distri-bution percentage was 81.9%. CONCLUSIONS:ACNAC is prepared successfully,and formulation technology is reasonable and feasible.

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