自制益智方渗透泵片的体外释放度考察

Study on in vitro release of Yizhi osmotic pump tablets

目的:考察激光打孔的孔径与释放条件对自制益智方渗透泵片体外释放的影响。方法:处方量主药与辅料混合均匀,70%乙醇制粒、压片、包衣,衣膜增重7%,熟化,激光打孔器双面打孔,制备孔径为0.2、0.4、0.6、0.8、1.0mm激光打孔片剂。考察不同测定方法(转篮法、桨法)、不同孔径、不同转速、不同渗透压条件下释放度,并比较4种有效成分(人参皂苷Rg1、人参皂苷Rb1、人参皂苷R1、桅子苷)释放度,探索其释放规律。结果:转篮法测定该渗透泵片,释放度重复性较好;激光打孔孔径为0.2-0.6mm时,近恒速释放;在50r/min转速条件下,0.4mm孔径片中4种成分12h累积释放度均达到了85%以上;释药度随着释放介质渗透压的升高而减少;4种检测成分间释放度相似因子均大于50;0.4mm孔径,转篮法50r/min条件下,10h释放较符合零级释放方程y=9.1034t+4.5482(r=0.9915)。结论:转篮法适于测定益智渗透泵片的释放度,激光打孔孔径对释放度有一定影响,衣膜内外渗透压是片剂释放动力,4种有效成分释放度相似,该制剂的释放符合零级释放方程。

Objective： To study the effect of diameter of laser drilling apertures and release conditions on the in vitro release of self-made Yizhi osmotic pump tablets. Methods： Drugs and excipients were mixed uniformly, granulated with 70% alcohol as binder, then compressed into tablets, coated, drilled by laser beam bilaterally with apertures size at 0.2, 0.4, 0.6, 0.8 and 1.0 mm respectively. Release behaviors were investigated with different measuring methods （rotating basket method, oar method）, at different apertures sizes, different rotating speeds and different osmotic pressure; release behaviors of four effective components were also compared and investigated. Results： Release with rotating basket method showed good reproducibility; Release rate was nearly constant when laser drilling apertures ranged from 0.2 to 0.6 mm; At the rotating speed of 50 rpm, accumulative release of four components in laser drilled tablets with 0.4 mm aperture reached more than 85% within the 12 hours; With osmotic pressure of release medium getting higher, the accumulative release degree decreased; f2 factors between these four components were all greater than 50; The release equation was y=9.1034t＋4.5482 （r = 0.9915） when laser drilled tablets with 0.4 mm apertures were detected by rotating basket method at 50 rpm within 10 hours. Conclusion： The rotating basket method was suit for determining the release degree of the osmotic pump tablets; the laser drilling apertures exerted a certain influence on the release; the internal and external osmotic pressure difference was the power of drug release; the release behaviors of the four components were similar, conforming to the zero-order kinetics.