马来酸氯苯那敏的直接压缩和体外释放:含流床干燥和冻干可可微晶纤维素片

N. Nwachukwu, K. Ugoeze, O. Okorie, S. Ofoefule
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摘要

目的:考察马来酸氯苯那敏(CM)片的力学性能和体外释放性能。该制剂以椰壳微晶纤维素(MCC)为原料,经流化床干燥和冻干后制成。研究设计:实验设计。学习地点和时间:2015年1月至2016年12月,尼日利亚大学恩苏卡分校制药技术与工业药剂系。方法:采用纯碱法对成熟果皮切片进行脱木质化,得到α -纤维素,再用无机酸(盐酸)水解得到CN- mcc。部分湿CN-MCC在60°C下流化床干燥2 h(编码MCCF-Cocos),其余CN-MCC在-45°C下冻干3 h(编码mcl - cocos)。MCC粉末分别以20%、30%和40% w/w的CM混合,并在9.81兆帕斯卡(mPa)下直接压缩。采用标准方法对含有MCCF-Cocos(编码CM- cf)和mcl - cocos(编码CM- cl)的CM片进行评价。结果:两个批次的片剂重量变化最小;CM-CL片的机械强度(P = 0.037)比CM-CF片的脆性小。CM-CL片崩解时间比CM-CF片长。与含AVC-102(编码CM- av)的CM片相比,含AVC-102的CM片机械强度更强,脆性更小,崩解时间更长。CM-AV的稀释电位大于CM-CL和CM-CF片。CM- cf中CM释放更快。CM- cf片、CM- cl片和CM- av片在30 min内CM的释放量均在80%以上。CM- cl片的机械强度虽然高于CM- cf片,但所获得的所有批次片的数据均在英国药典规定的无包衣片限量范围内。结论:马来酸氯苯那敏片含有牛皮草流化床干燥和冻干微晶纤维素,具有良好的力学性能和体外释放性能。
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Direct Compression and in vitro Release of Chlorpheniramine Maleate from Tablets Containing Fluid Bed Dried and Lyophilized Microcrystalline Cellulose Derived from Cocos nucifera
Aims: To investigate the mechanical and in vitro release properties of chlorpheniramine maleate (CM) tablets formulated with fluid bed dried and lyophilized microcrystalline cellulose (MCC) derived from the fruit husk of Cocos nucifera (CN). Study Design: Experimental design. Place and Duration of Study: Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka from January, 2015 to December, 2016. Methods: Chips of matured (CN) fruit husk were de-lignified by soda treatment methods to obtain alpha cellulose which was hydrolyzed with mineral acid (Hydrochloric acid) to obtain CN-MCC. A portion of the damp CN-MCC was fluid bed dried at 60°C for 2 h (coded MCCF-Cocos) and the remaining CN-MCC was lyophilized at -45°C for 3 h (coded MCCL-Cocos). The MCC powders were blended with 20, 30 and 40% w/w CM and directly compressed at 9.81 mega Pascal (mPa). The CM tablets containing MCCF-Cocos (coded CM-CF) and MCCL-Cocos (coded CM-CL) were evaluated using standard methods. Results: Both batches had tablets with minimal weight variation; CM-CL tablets were mechanically stronger (P = .037) and less friable than CM-CF tablets.  CM-CL tablets took a longer time to disintegrate than CM-CF tablets. Comparatively, CM tablets containing AVC-102 (coded CM-AV) were mechanically stronger, less friable and had a longer disintegration time than CM-CL and CM-CF tablets. The dilution potential of CM-AV was greater than CM-CL and CM-CF tablets. CM release was faster in CM-CF. There was more than 80 % release of CM from CM-CF, CM-CL and CM-AV tablets within 30 min. Although CM-CL tablets were mechanically stronger than CM-CF, the data for all batches of the tablets obtained fell within the British Pharmacopoeia set limits for uncoated tablets. Conclusion: Chlorpheniramine maleate tablets containing fluid bed dried and lyophilized microcrystalline cellulose obtained from C. nucifera had good mechanical and in vitro release properties.
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