硫酸氢氯吡格雷片的制备及其处方工艺优化

发布时间：2018-12-15 17:01

【摘要】：目的:制备硫酸氢氯吡格雷片并优化其处方工艺。方法:采用单因素试验联合相容性试验对片剂的填充剂、崩解剂、黏合剂、润滑剂和制备方法进行筛选;以黏冲情况和崩解时间的综合评分为指标,采用正交试验优选崩解剂[低取代羟丙基纤维素(L-HPC)]、润滑剂(氢化植物油和聚乙二醇6000)的用量,并进行验证;考察所制片剂与进口制剂(波立维)在水、p H 2.0盐酸盐缓冲液、p H 4.5磷酸盐缓冲液(PBS)、p H 6.8 PBS中的溶出情况并进行影响因素试验。结果:采用干法制粒,最优处方(1 000片)为硫酸氢氯吡格雷97.8 g、甘露醇84 g、预胶化淀粉36 g、L-HPC 8 g、氢化植物油8 g、聚乙二醇6000 6 g;所制片剂压片无黏冲现象且崩解时间适中,其与波立维在4种溶出介质中溶出曲线均相似;影响因素试验结果与波立维比较无明显差异。结论:成功制得硫酸氢氯吡格雷片,且处方合理、工艺可行、质量稳定可控。
[Abstract]:Objective: to prepare clopidogrel sulfate tablets and optimize its formulation. Methods: single factor test combined with compatibility test was used to screen the fillers, disintegrants, adhesives, lubricants and preparation methods of tablets. The dosage of disintegrant [low substituted hydroxypropyl cellulose (L-HPC)] and lubricant (hydrogenated vegetable oil and polyethylene glycol 6000) was selected and verified by orthogonal test. The dissolution of the tablets and imported preparations (Polydovir) in water, p H 2.0 hydrochloride buffer, p H 4.5 phosphate buffer (PBS), p H 6.8 PBS was investigated and the influencing factors were tested. Results: dry granulation was used. The optimum prescription was 97.8 g clopidogrel sulfate, 84 g mannitol, 36 g pre-gelatinized starch L-HPC, 8 g hydrogenated vegetable oil and 6000 g polyethylene glycol. There is no viscosity and impact phenomenon and the disintegration time is moderate, and the dissolution curves of the tablets are similar to those of Polydovir in four kinds of dissolution media, and there is no significant difference between the experimental results of influencing factors and that of Poly. Conclusion: hydroclopidogrel sulfate tablets were successfully prepared with reasonable formulation, feasible process and stable and controllable quality.
【作者单位】：江苏康缘药业股份有限公司;中药制药过程新技术国家重点实验室;
【分类号】：R943

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