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ABSTRACT:
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.
KEYWORDS: Eplerenone, HPMC K100M, NaCMC, Xantham Gum, Carbopol 934P, Carbopol 974P, Mucoadhesion Buccal drug delivery.
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INTRODUCTION:
Oral means of administration of drugs is mainly chosen by the patient and the clinician too. However, oral administration of drugs have drawbacks such as hepatic first pass metabolism and enzymatic deprivation within the GI region, that forbid oral administration of numerous drugs. Bioadhesion is definite as the adhesion flanked by two materials where one of the resources is of biological source. In mucoadhesion drug release systems, mucoadhesion takes put between the adjuvants of the formulation and organic tissue1.
Eplerenone is an Anti-hypersentive drug belongs to BCS class II. Eplerenone binds to the mineralocorticoid receptor and blocks the aldosterone to lower blood pressure. However, its safety profile is improved over spironolactone because of reduced progesterone and androgen-receptor effects. The half-life of Eplerenone is about 3 to 6 hrs. Orally administered Eplerenone was absorbed from...