Design And Optimization Of Bilayer Tablets Of Identified Category Drugs By Using Factorial Design

Abstract

We demonstrated the bilayer formulation of telmisartan and Cilnidipine antihypertensive drugs. Telmisartan gives an immediate release effect, and Cilnidipine has a sustained release effect in the systemic circulation. We used the double compression method for the bilayer tablet. The granules were prepared by using the wet granulation method. Drugs characterized by low solubility, such as telmisartan, can be challenging to formulate into effective pharmaceutical products. In this study, we aimed to improve the solubility of telmisartan by incorporating it with beta-cyclodextrin. To optimize the formulation, we evaluated the effects of different super disintegrants, namely sodium starch glycolate and croscarmellose sodium, in the final mixture. The results indicated that the optimized formulation of telmisartan with beta-cyclodextrin and the chosen super disintegrants could enhance the solubility and promote effective drug delivery.It gives a super disintegrant effect in the immediate release layer. For sustain release layer HPMC K-100 M was used, which gives a satisfactory effect for up to 12 hrs. For formula optimisation,a 3^2 factorial design was used. The drug excipient compatibility study using DSC found no interaction between the drug and the excipient. The FTIR was performed, and peaks for drugs were observed. An in-vitro drug release study was carried out using the USP type II apparatus. The telmisartan immediate release optimised batch shows 95.51% drug release in 15 min. Cilnidipine sustain release optimised batch shows 96.46% drug release upto 12 hrs. In bilayer tablets, the combination drug gives a synergistic effect and improves patient compliance. newlineIn this pharmacokinetics study, the HPLC method was used to simultaneously estimate telmisartan and Cilnidipine in rabbit plasma. The combination bilayer tablet was formulated using HPMC K100m as a polymer for sustained release. The optimised formulation pharmacokinetics study was carried out using rabbit plasma. The Gemini C-18 column with a DAD detector wa