新型抗抑郁药LPM单室渗透泵片的制备及体外释放评价

Preparation of new antidepressant LPM monolithic osmotic pump tablet and evaluation of its in vitrorelease

目的:制备新型抗抑郁药LPM的单室渗透泵片,并考察其体外释放。方法:采用包合技术提高LPM的溶解度,以聚氧乙烯(PEO)和氯化钠(NaCl)相结合作为渗透压促进剂,以醋酸纤维素为膜材,制备单室渗透泵片。以单因素考察和正交试验设计对处方组成进行优化。结果:采用包合技术,LPM在去离子水中的溶解度可达59.2 g·L-1。最优处方组成为:包合物50%,PEO17%,NaCl 17%,包衣厚度14%。该制剂可以达到12 h的零级释放,累积释放度达80%以上,药物的释放不受介质pH和转速的影响。结论:制备成LPM的单室渗透泵片,其药物释放完全,释药行为符合零级动力学方程。

OBJECTIVE To prepare monolithic osmotic pump tablet of the new antidepressant LPM and to study its in vitro release. METHODS The inclusion technique was used to improve the solubility of LPM. The monolithic osmotic pump tablets were prepared based on the polyoxyethylene（PEO）and sodium chloride （NaC1）as the osmotic promoting agents and cellulose acetate as membrane material. The formulations were optimized by single factor test and orthogonal design. RESULTS The solubility of LPM was improved up to 59. 2 g.L-1 by the inclusion technique. The optimal formulation consisted of cyclodextrin complex 50%, PEO 17%, NaCl 17% and coating weight 14~/00. The monolithic osmotic pump tablets could meet with zero-order release for 12 hours and the cumulative release was more than 80%. The drug release was not influenced by the pH of the release media and agitational intensity. CONCLUSION The release behavior of monolithic osmotic pump tablets of LPM followed zero order kinetics equation and the drug could be released completely.