扎西他宾微孔渗透泵和单室渗透泵控释片的研究  

Micro-porous Osmotic Pump and Elementary Osmotic Pump Controlled-release Tablets of Zalcitabine

作　　者：张可蕊 符海娟[1] 王宇驰 张颖[1] 李旭东 张静[1] ZHANG Ke-rui;FU Hai-juan;WANG Yu-chi;ZHANG Ying;LI Xu-dong;ZHANG Jing(Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province,Sichuan Industrial Institute of Antibiotics,School of Pharmacy,Chengdu University,Chengdu 610052,China)

机构地区：[1]抗生素研究与再评价四川省重点实验室,四川抗菌素工业研究所,成都大学药学院,成都610052

出　　处：《中国药学杂志》2023年第5期435-446,共12页Chinese Pharmaceutical Journal

基　　金：抗生素研究与再评价四川省重点实验室开放课题资助(ARRLKF14-03)。

摘　　要：目的制备扎西他宾微孔渗透泵控释片和单室渗透泵控释片。方法建立了释放度测定方法,通过单因素实验确定促渗透活性物质的用量、致孔剂PEG400的用量和包衣增重为影响释放的重要因素,采用星点设计-效应面法得到扎西他宾微孔渗透泵控释片最优处方。在微孔渗透泵控释片最优处方的基础上,筛选出单室渗透泵控释片最优处方。分别按最优处方制备3批渗透泵控释片,并以累积释放度与时间进行零级方程拟合考察其释药特性。结果扎西他宾微孔渗透泵控释片处方优化结果为:促渗透活性物质乳糖的量(X1)为每片80 mg、致孔剂PEG400的量为(X2)9%、包衣增重(X3)为2.8%;单室渗透泵最优处方为:乳糖每片15 mg,包衣增重2.5%,激光单面打孔,打孔脉冲为20 ms。结论制备的2种扎西他宾渗透泵控释片工艺简单,质量可控。扎西他宾单室渗透泵片相对于微孔渗透泵片控释时间可延长至24 h,具有零级释药特征。OBJECTIVE To prepare micro-porous osmotic pump(MPOP)and elementary osmotic pump(EOP)controlled-release tablets of zalcitabine.METHODS A method to determine the drug release of the tablets was developed.Single-factor experiments revealed that quantities of osmogents and pore forming agents,as well as weight gains of coatings play important impacts on drug release.Central composite design was used to find the optimal formula of zalcitabine MPOP tablet,from which the optimal formula of EOP was screened.Zalcitabine MPOP and EOP tablets(3 batches each)were prepared according to the optimal formula and assessed by the zero-order equation fitting between cumulative release and time for their releasing character-izations.RESULTS The optimal formula of zalcitabine MPOP tablets are:quantities of lactose as the osmogent(X1)is 80 mg per tablet,PEG400 as the pore forming agent(X2)is 9%,the weight gain of coating(X3)is 2.8%.The optimal formula of EOP tablets are:quantities of lactose is 15 mg per tablet,the weight gain of coating is 2.5%,tablets were drilled on one side at a laser pulse of 20 microsecond.CONCLUSION The two osmotic pump tablets are prepared by simple processes with controlla-ble quality and good stability.Controlled releasing duration of EOP could be extended to 24hrs compared with that of CPOP with a zero-equation release characterization.

关 键 词：微孔渗透泵 单室渗透泵 控释片 扎西他宾 

分 类 号：R944[医药卫生—药剂学]