目的 建立并验证具有区分力的甲磺酸地拉韦啶片(100 mg)体外溶出方法,为仿制药的开发提供参考。方法 建立了测定甲磺酸地拉韦啶片HPLC的体外溶出度方法,通过原料药的溶解性以及原研药品和自制制剂在pH 1.2、pH 4.5[4 mg·mL-1十二烷基硫酸钠(SDS)]、pH 6.0(4 mg·mL-1 SDS)和水(4 mg·mL-1 SDS)中的溶出行为,采用相似因子(f2)法评价溶出行为的相似性,筛选出具有区分力的溶出方法。结果 自制制剂B与原研药品在4种介质中溶出行为相似(f2均大于50),自制制剂A、C、D在4种介质中均存在f2小于50的情况。结论 采用桨法50 r·min-1在pH 4.5(0.4% SDS)、pH 6.0(0.4% SDS)和水(0.4% SDS)中测定本品溶出度具有一定区分力。
Abstract
OBJECTIVE To establish and validate the discriminating dissolution methods of delavirdine mesylate tablets (100 mg) in vitro, which provided reference for the development of generic drugs. METHODS High performance liquid chromatography (HPLC) was used to establish the methods for the determination of the dissolution of delavirdine mesylate tablets. The solubility of delavirdine mesylate in different pH solutions were measured. The dissolution curves of RESCRIPTOR®(100 mg) and self-made tablets were determined in pH 1.2, pH 4.5 (4 mg·mL-1 SDS), pH 6.0 (4 mg·mL-1 SDS) and water (4 mg·mL-1 SDS) four media, f2 similarity factor method was used to evaluate the similarity of dissolution curves. RESULTS The dissolution curves were similar between self-made tablet B and brand-name drugs in four different media (f2 were greater than 50), while the f2 of self-made tablet A, C, D in four media were not all greater than 50. CONCLUSION The discriminatory dissolution methods of delavirdine mesylate dispersible tablets are determined by paddle method, 50 r·min-1 rotation speed, the medium are pH 4.5 acetate buffer (4 mg·mL-1 SDS), pH 6.0 phosphate buffer (4 mg·mL-1 SDS) and water (4 mg·mL-1 SDS).
关键词
甲磺酸地拉韦啶片 /
原研药品 /
自制制剂 /
溶出度 /
区分力 /
相似因子法
{{custom_keyword}} /
Key words
delavirdine mesylate tablet /
brand-name drugs /
self-made preparation /
dissolution /
discrimination /
similarity factor method
{{custom_keyword}} /
中图分类号：
R944
{{custom_clc.code}}
({{custom_clc.text}})
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
参考文献
[1] BEHJA W, JEMAL M. Anti-HIV Drug Discovery, Development and Synthesis of Delavirdine: Review Article[J]. Int Res J Pure Appl Chem, 2019:1-16.
[2] XIE M F. The Dissolution Curve with Distinguishing Ability[J]. Chin J Pharm(中国医药工业杂志), 2014, 45(7) :687-689.
[3] BENET L Z, BROCCATELLI F, OPREA T I. BDDCS applied to over 900 drugs[J]. AAPS J, 2011, 13(4):519-547.
[4] HU C Y, HUANG P. Recent Research and Development on Determination of Solid Solubility [J]. Chin J Pharm Anal(药物分析杂志), 2010, 22(4): 761-766.
[5] XIE M F. Multiple Dissolution Profiles, the Agreement Evaluation Technology of Oral Solid Dosage Forms of Generic Drug [J]. Chin J Pharm(中国医药工业杂志), 2013, 44(4):411-414.
[6] ZHANG Q M, XIE M F, NING B M, et al. Evaluation of Solid Oral Products by Dissolution Profiles in Different Mediums [J]. Chin J Pharm(中国医药工业杂志), 2009, 40(12):946-950.
[7] WU J M, LIU H Y, LIU Y, et al. Effect of purity of sodium dodecyl sulfate on dissolution testing results of candesartan cilexetil [J]. Chin J Pharm Anal(药物分析杂志), 2015,35(4):742-746.
[8] RAJU V, MURTHY K V R. Development and Validation of New Discriminative Dissolution Method for Carvedilol Tablets[J]. Indian J Pharm Sci, 2012, 73(5):527-536.
[9] XIE M F. Evaluation Methods of Comparability of Dissolution Curve [J]. Chin J Pharm(中国医药工业杂志), 2009, 40(4):308-311.
[10] ZHANG C M, TIAN C, KE X, et al. Micromeritic Comparative Study of Co-processed Excipients of Different Proportions of Lactose and Microcrystalline Cellulose [J]. Chin J Pharm(中国医药工业杂志), 2014, 45(1):45-48.
{{custom_fnGroup.title_cn}}
脚注
{{custom_fn.content}}
PDF(1709 KB)
