Formulation and evaluation of taste masked Amlodipine Besylate Fast-dissolving Sublingual Tablets
Keywords:Amlodipine Besylate (AML), drug polymer complex (DPC), sublingual tablet (SLT), Eudragit EPO, sodium starch glycolate (SSG), croscarmellose sodium (CCS), crospovidone (CPV), direct compression, sodium carboxymethyl cellulose (SCMC), hot melt extrusion
Aim: In the present study was to taste mask the Amlodipine Besylate (AML) by forming complex with Eudragit EPO by and further to enhance the dissolution rate AML by formulating these drug polymer complex (DPC) into fast dissolving sublingual tablet (SLT) by direct compression technique.
Objectives: To prepare DPC by hot melt extrusion method. Physico-chemical characterization of DPC by FT-IR, DSC and XRD studies. To check the superiority of selected superdisintegrants [sodium starch glycolate (SSG), croscarmellose sodium (CCS), crosspovidone (CPV) and sodium carboxymethyl cellulose (SCMC)] in enhancing the dissolution rate of AML from its SLT. To fasten the onset of action, to decrease the hepatic metabolism and thereby increasing AML’s bioavailability in comparison to its conventional tablets.
Methods: Standard calibration curve of AML in pH 6.8 phosphate buffer was constructed by spectrophotometric method, drug-excipient compatibility was checked by FT-IR studies. All the Formulations were evaluated for pre- & post-compression studies. Accelerated stability studies up to 3 months were conducted for the optimized formulation in a HDPE container pack, as per ICH guidelines.
Results and Discussions: Superdisintegrants used in the study are compatible with AML. Pre- & post- compression parameters were within the acceptable limits for all formulations. In vitro dissolution kinetic studies indicate the release of AML from SLT increases with the increased concentration of superdisintegrants. The order of superdisintegrants in enhancing the dissolution rate of AML is CPV > SCMC > CCS > SSG. Formulation F3 with 8% w/w CPV, had the highest dissolution efficiency at 10 min (DE10 = 49.80 %); first order dissolution rate constant (K1 = 0.198 min-1) with a regression coefficient (r2 = 0. 956) and lesser time for 50% of drug release (t50 < 6 min), which shows min wetting time of 21.12 sec and min disintegration time of 17 sec, was considered as the optimal SLT. It passed the test for stability as per ICH guidelines.
Conclusion: An optimized taste masked AML SLT with the taste masked DPC in combination with the addition of artificial flavor and sweetener was formulated by the direct compression technique, with 8% w/w CPV as superdisintegrant, which will fasten the onset of action and enhances the bioavailability of AML in comparison to its conventional tablets.
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How to cite this article:
Thulluru A, Venkatesh K, Sarath Chowdhary ETS and Kakarla S. Formulation and evaluation of taste masked Amlodipine Besylate Fast-dissolving Sublingual Tablets. Int. J. Res. Dev. Pharm. L. Sci. 2017; 6(6): 2824-2832. Doi: 10.13040/IJRDPL.2278-0238.6(6). 2824-2832.
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