Aceclofenac is a non-steroidal anti-inflammatory drug used for treatment of pain and inflammation. The short biological half-life (4 h) and dosing frequency more than once daily make aceclofenac a suitable candidate for sustained release formulations. Sustained release lipospheres of aceclofenac were prepared using cetyl alcohol and Compritol 888 ATO. The prepared lipospheres were characterized for their percentage yield, encapsulation efficiency, particle size, surface morphology, micromeritic properties and in-vitro release over 24 hours. The optimum formula was incorporated into a lyophilized system to produce sustained release orally disintegrating tablet (SR-ODT), which intended to disintegrate rapidly within the mouth into lipospheres that will deliver aceclofenac in sustained release manner after swallowing. The prepared SR-ODTs were evaluated regarding weight variation, friability, content uniformity, disintegration, in-vitro release and in-vivo pharmacokinetics in albino rabbits. All the prepared lipospheres showed satisfactory results regarding the investigated properties. According to the in-vitro release data, formula FI (prepared using cetyl alcohol at lipid: drug ratio of 1:1 and 0.5% PVA) was selected as the optimum formula, and thus, used for preparation of the SR-ODT. The prepared SR-ODT demonstrated acceptable weight variation, friability and content uniformity. Also, the SR-ODT showed rapid in-vitro disintegration time (10 s) and it was successful in sustaining drug release up to 24 hours. The results of pharmacokinetic studies showed that the SR-ODT exhibited longer MRT and lower Cmax when compared with the values of the commercial brand of aceclofenac immediate release tablet (Bristaflam®), confirming our target in the preparation a sustained release formula.
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