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.