Design and Invitro Evaluation of Transdermal patches of Tacrine

pharmacy

Tacrine is a centrally acting acetylcholinesterase inhibitor and indirect cholinergic agonist (parasympathomimetic). It was the first centrally acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease. It also acts as a histamine N-methyltransferase inhibitor.In present study transdermal drug delivery of Tacrine was developed to overcome the first pass metabolism and to reduce frequency of dosing compared to oral route. Oral drug delivery system has various drawbacks like poor bioavailability due to hepatic metabolism (first pass) and the tendency to produce rapid blood level spikes (both high and low), leading to a need for high and/or frequent dosing, which can be both cost prohibitive and inconvenient. Matrix type of transdermal patches was developed by using xanthan gum, chitosan and HPMC K100M polymers. Transdermal patches were prepared by employing solvent casting method. Drug excipient compatibility studies were carried out by using FTIR, and it was observed that there were no interactions. Formulations were prepared with the varying concentrations polymers ranging from F1-F9, and all the formulations were evaluated for various physical parameters Physical appearance, Flatness, Weight variation, Thickness, Folding endurance, Drug content, Moisture uptake, Moisture content and Swelling study and all the results were found to be with in the pharmacopeial limits, invitro drug release studies by using dialysis membrane. Among all the 9 formulations F5 formulation which contain Chitosan 150 mg had shown 97.52% cumulative drug release with in 12 hours.

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