Mon, 18 Dec 2017

Design and Evaluation of Mucoadhesive Fast Disintegrating Sublingual Tablets Containing Poorly Soluble Drug for Enhancement of Oral Bioavailability

 

Laxminarayana Adepu 1, 2*, Lakshmi Sirisha Kotikalapudi3, Srinivasa Rao Yerraguntla1, Venkata Ramana Murthy Kolapalli3

1.Vignan Institute of Pharmaceutical Technology, Visakhapatnam, India

2.University College of Pharmaceutical Sciences, Acharya Nagarjuna University, Nagarjunanagar, Guntur, India

3.A.U. College of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India


 

ABSTRACT

The aim of this study was to prepare and evaluate sublingual fast-disintegrating mucoadhesive tablet (mFDT) containing a poorly soluble drug (carvedilol CAR) to avoid the first pass metabolism and to improve its bioavailability with reduction in dose and also dose related side effects. The tablets were prepared by direct compression method containing solid dispersion of surfactant and drug. The prepared tablets were tested for weight variation, hardness, drug content uniformity, bioadhesive strength and in vitro drug dissolution. The in vitro release of carvedilol was performed under sink conditions (phosphate buffer of pH 6.8, 37±0.5 ºC, 25 rpm) using USP‐XXIV dissolution apparatus. The acceptable in vitro drug release profile was achieved with the formulation F2 which contains the drug and poloxamer in the ratio of 1:2 and superdisintegrant of 3%. The bioadhesive strength of formulation F2 was found to be 13.8 g. The tablets (formulation F2) containing 6.25 mg of carvedilol exhibited > 80 % of drug release within 10 min. FTIR, XRD and DSC studies showed no evidence of interactions between drug, surfactant, and excipients. The tablets apart from fulfilling all official and other specifications, exhibited higher rate of release. The mucoadhesive fast disintegrating drug delivery system of carvedilol for sublingual delivery could be successfully formulated.


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