DESIGN, OPTIMIZATION, DEVELOPMENT AND EVALUATION OF ONCE A DAY CONTROLLED RELEASE FORMULATION OF RIVASTIGMINE TARTARATE
Rivastigmine, an Anti-Alzheimerâ€™s drug suffer from a major limitation of sever GI adverse events such as nausea, vomiting, diarrhea, loss of appetite, weight loss and increase dosing frequency . The present work aim at design, optimization and development of rivastigmine once a day controlled release formulation to minimize the above limitation and increase patientâ€™s compliance. Based on the target in-vitro release profile derived from pharmacokinetic simulation , a once a day matrix tablet with the simulated dose was developed. The simple direct compression process was followed as a manufacturing process, the percentage of Polymer HPMC K100M, Polyethylene oxide (PEO WSR303) and insoluble excipients microcrystalline cellulose used in the formulation were optimized using 23 full factorial design. The formulations were then evaluated for the physical characteristics of blend, tablets, swelling index, percentage of erosion, drug release and release rate kinetic. The quadratic model was suggested, contour and 3D graphs were generated. The optimized formulation was subjected to stability studies. The final optimized formulation showed a comparative release profile similar to that the desired in-vitro target release profile, which followed zero order release kinetics and a stable formulation.
Keywords: Controlled Release Formulation, Rivastigmine Tartarate, Anti-Alzheimerâ€™s drug, HPMC K100M, Polyethylene oxide (PEO WSR303)
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 4.0 International (CC BY-NC 4.0). that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).