盐酸苄丝肼固体分散体制备工艺的研究

马桂芝1， 马亮英2， 李文英3， 滕亮4

(新疆医科大学1药学院， 乌鲁木齐830011；2第二附属医院药剂科， 乌鲁木齐830000；3第五附属医院药剂科， 乌鲁木齐830011；

4第一附属医院药学部， 乌鲁木齐830054)

摘要：目的优选具有缓释特征的盐酸苄丝肼固体分散体的制备工艺。方法以与左旋多巴微囊溶出行为的相似度为指标，采用均匀试验优选出满足缓释要求的盐酸苄丝肼固体分散体制备工艺，并对其制剂特征进行考察。结果优选出的盐酸苄丝肼固体分散体处方为：主药与辅料的质量比为1∶1，聚乙烯吡咯烷酮(PVP)与乙基纤维素(EC)的质量比为1∶3。结合X-衍射试验结果及释放度行为，采用优选工艺处方制得了盐酸苄丝肼固体分散体。初步稳定性试验表明盐酸苄丝肼固体分散体的理想贮存条件是室温、遮光密封干燥保存。结论优选出的盐酸苄丝肼固体分散体处方合理，制备工艺稳定、科学、可行。制得的固体分散体满足缓释的要求，同时盐酸苄丝肼的释放行为与左旋多巴的释放行为相似。

关键词：盐酸苄丝肼； 固体分散体； 制备工艺

中图分类号：R914文献标识码：A

doi:10.3969/j.issn.1009-5551.2015.07.015

[收稿日期：2015-01-12]

基金项目：新疆医科大学科研创新基金(XJC2012114)

作者简介：沈静(1977-)，女，硕士，副教授，硕士生导师，研究方向：药物质量控制研究。

The preparation of solid dispersion of benserazide hydrochloride

MA Guizhi1, MA Liangying2, LI Wenying3, TENG Liang4

(1CollegeofPharmacy,XinjiangMedicalUniversity,Urumqi830011,China;2Departmentof

Pharmacy,TheSecondAffiliatedHospitalofXinjiangMedicalUniversity,

Urumqi830000,China;3DepartmentofPharmacy,TheFifthAffiliatedHospitalofXinjiang

MedicalUniversity,Urumqi830011,China;4DepartmentofPharmacy,TheFirstAffiliated

HospitalofXinjiangMedicalUniversity,Urumqi83054,China)

Abstract:ObjectiveTo optimize the preparation program of solid dispersion of benserazide hydrochloride. MethodsAccording to the in vitro release behavior of levodopa microcapsules, the data which were analyzed by the statistical method-similar factor method were selected as indexes, the uniform design was used to optimize the process of benserazide solid dispersion. And the character of dosage form was elevated. ResultsThe selected preparation formula is as following: the mass ratio between benserazide and excipients is 1∶1, the mass ratio between polyvinyl pyrrolidone and ethyl cellulose is 1∶3. According to the results of X-ray and dissolution, benserazide solid dispersion is prepared successfully. Benserazide solid dispersion should be stored in shading and seal conditions. ConclusionThe selected preparation formula is reasonable. The condition of preparation is stable, reasonable and feasible. The solid dispersion has slow release behavior and the release behavior is the same as levodopa microcapsules.

Key words: benserazide hydrochloride; solid dispersion; preparation program

帕金森病(Parkinson′s disease，PD)又称为震颤麻痹，是一种中枢神经系统锥体外系功能障碍的慢性进行性疾病[1]。美国神经协会对各种抗帕金森病药物进行评估，结果表明复方左旋多巴制剂(美多芭等)是所有帕金森病药物治疗中最有效的药物[2-3]。……