盐酸多西环素缓释片的研制与体外评价  

Preparation of doxycycline hydrochloride delayed release tablets and its in vitro evaluation

作　　者：朱舒荣 龚杰 刘晓鸣 程刚[1] ZHU Shurong;GONG Jie;LIU Xiaoming;CHENG Gang(School of Pharmacy,Shenyang Pharmacertical University,Shenyang 110016,China;Zhejiang Huahai Pharmaceutical Co.,Ltd.,Taizou 318000,China)

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]浙江华海药业股份有限公司,浙江台州318000

出　　处：《中国药剂学杂志(网络版)》2025年第2期76-89,共14页Chinese Journal of Pharmaceutics:Online Edition

摘　　要：目的研制盐酸多西环素缓释片,研究其体外溶出。方法采用挤出滚圆工艺制备载药微丸,然后进行缓释包衣,最后将缓释微丸与辅料混合,压制成片,研究其处方工艺对体外溶出的影响,并对最终处方下的自研片剂进行体外评价。结果建立了切实可行的处方工艺,体外溶出结果表明在0.06 mol·L^(-1)HCl溶出介质下,自研与原研的溶出曲线相似因子f_(2)为49,与原研未匹配,但在20 min时的溶出小于30%,溶出表现与原研基本一致。p H5.5介质下,自研与原研的溶出曲线相似因子f_(2)为68,与原研匹配。结论自研的盐酸多西环素缓释片达到研制目标,体外溶出与参比制剂相似,可继续进行体内生物等效性试验。Objective To prepare doxycycline hydrochloride delayed release tablets,and evaluate its in vitro release and pharmacokinetic parameters.Methods The extrusion and spheronization process was used to make drug loaded pellets first,and then the pellets were coated with delayed release materials.Finally,the delayed release pellets were mixed with auxiliary materials and pressed into tablets.The influence of formulation and process on dissolution in vitro were studied.Then the in vitro release of final self-made product was evaluated.Results A feasible formulation and process was established.In vitro dissolution data summarized that in 0.06 mol·L^(-1) HCl dissolution medium,the similarity factor𝑓f2 between the self-made product and the RLD was 49,indicating a mismatch with the RLD.However,the dissolution at 20 min in HCl dissolution medium was less than 30%,the dissolution behavior was generally consistent with RLD.In the pH 5.5 medium,the similarity factor𝑓f2 between the self-made product and the RLD was 68,indicating a match with RLD.Conclusion The self-developed doxycycline hydrochloride delayed release tablets achieved the development goal.The in vivo bioequivalence study can be conducted.

关 键 词：盐酸多西环素 缓释片 溶出曲线 

分 类 号：TQ460.6[化学工程—制药化工] R944.4[医药卫生—药剂学]