Mucoadhesive drug release system is a preferably unidirectional release system where mucosal epithelial exterior is enclosed by the mucus deposit that interacts with the bio-adhesive drug delivery system and swelling time of the buccal dosage form which is amplified by mucin molecules at the location of administration. Eplerenone is an Anti-hypertensive drug that undergoes hepatic first pass metabolism and shows 69% of bioavailability. In order to bypass the hepatic first pass metabolism the drug is designed to be delivered through buccal cavity to avoid the first pass metabolism. Eplerenone buccal tablets were formulated by using direct compression method with different polymers like HPMC K 100M, Carbopol 934P, Carbopol 974P, Xantham Gum, Eudragit L100 and NaCMC in various concentrations and compositions. Incompatibility complications were not observed from the FTIR spectrums. The formulated and prepared buccal solid dosage forms were evaluated for pre-compressions and post- compression parameters such as hardness, weight variation, thickness, friability, surface pH, swelling index, in-vitro dissolution studies, drug content uniformity, mucoadhesion strength and mucoadhesion time. Evaluation results of formulation F12 are proven to be the optimal formulation showing highest mucoadhesion time, mucoadhesion strength and in-vitro drug release for prolonged period of time about 8 hours. Eplerenone is best delivered through buccal drug delivery system to enhance its oral bioavailability and bypass the hepatic first pass metabolism.
fter oral administration of Abacavir, rapid absorption occurs from upper part of gastro intestinal tract with peak concentrations occurring at 0.63 - 1 hr after dosing. Conventional drug therapy with tablets produce relatively rapid and high peak blood levels that requires frequent administration to maintain effective range of plasma drug levels. This conventional therapy leads to reduced effectiveness with poor therapeutic management. To overcome the inadequacy of conventional therapy with tablets, floating sustained release Abacavir tablets were developed. Floating sustained release Abacavir Sulphate tablets were prepared by using direct compression method. Tablet were formulated using Ethyl Cellulose with hydrocolloids like Hydroxypropyl Methylcellulose (HPMC K4M) and Carbopol 974P as release retarding polymers, Sodium bicarbonate (NaHCO3) and Citric acid as effervescent agents. Tablets were then evaluated for various physical parameters including hardness, thickness, weight variation, friability, drug content, in-vitro buoyancy, Swelling index and Invitro gastro retentive drug release were conducted. Drug and excipient compatibility studies show that they are compatible with each other. The optimized formulation (F9) shows the hardness of 5.7kg/cm2, tablet thickness of 2.74mm, 0.45% of friability, in-vitro buoyancy was up to 6 hours and % drug release was 90.56% in 6 hours. Drug release kinetics was found to follow non-fickian diffusion. Hence, F9 is considered as optimized formulation based on invitro buoyancy and % drug release.
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