Kasperek Regina, Polski Andrzej, Zimmer Łukasz, Poleszak Ewa
Department of Applied Pharmacy, Faculty of Pharmacy, Medical University of Lublin, 1 Chodzki Str. 20-093, Lublin, Poland.
Sci Pharm. 2014 May 16;82(3):684-96. doi: 10.3797/scipharm.1310-19. Print 2014 Jul-Sep.
The influence of excipients on the disintegration times of tablets and the release of papaverine hydrochloride (PAP) from tablets were studied. Ten different formulations of tablets with PAP were prepared by direct powder compression. Different binders, disintegrants, fillers, and lubricants were used as excipients. The release of PAP was carried out in the paddle apparatus using 0.1 N HCl as a dissolution medium. The results of the disintegration times of tablets showed that six formulations can be classified as fast dissolving tablets (FDT). FDT formulations contained Avicel PH 101, Avicel PH 102, mannitol, (3-lactose, PVP K 10, gelatinized starch (CPharmGel), Prosolv Easy Tab, Prosolv SMCC 90, magnesium stearate, and the addition of disintegrants such as AcDiSol and Kollidon CL. Drug release kinetics were estimated by the zero- and first-order, Higuchi release rate, and Korsmeyer-Peppas models. Two formulations of the tablets containing PVP (K10) (10%), CPharmGel (10% and 25%), and Prosolv Easy Tab (44% and 60%) without the addition of a disintegrant were well-fitted to the kinetics models such as the Higuchi and zero-order, which are suitable for controlled- or sustained-release.
研究了辅料对片剂崩解时间以及盐酸罂粟碱（PAP）从片剂中释放的影响。采用直接粉末压片法制备了10种含PAP的不同片剂配方。使用不同的粘合剂、崩解剂、填充剂和润滑剂作为辅料。以0.1 N盐酸为溶出介质，在桨法装置中进行PAP的释放实验。片剂崩解时间的结果表明，六种配方可归类为速溶片（FDT）。FDT配方包含微晶纤维素PH 101、微晶纤维素PH 102、甘露醇、β-乳糖、聚乙烯吡咯烷酮K 10、糊化淀粉（CPharmGel）、Prosolv Easy Tab、Prosolv SMCC 90、硬脂酸镁，以及添加的崩解剂如AcDiSol和交联聚维酮。通过零级和一级、Higuchi释放速率以及Korsmeyer-Peppas模型估算药物释放动力学。两种不含崩解剂的含聚乙烯吡咯烷酮（K10）（10%）、CPharmGel（10%和25%）以及Prosolv Easy Tab（44%和60%）的片剂配方与Higuchi和零级等适用于控释或缓释的动力学模型拟合良好。
