Application of solid dispersions of nifedipine with enteric coating agent to prepare a sustained-release dosage form.
- 1 January 1985
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 33 (4), 1615-1619
- https://doi.org/10.1248/cpb.33.1615
Abstract
Pre-formulation studies were carried out the develop a sustained-release dosage form of nifedipine with good bioavailability. Granules were prepared by spray-coating nifedipine-enteric coating agent solid dispersions on an inert core material. Typical enteric coating agents, hydroxypropylmethylcellulose phthalate and methacrylic acid-methacrylic acid methyl ester copolymer, were used as carriers of the solid dispersions. Dissolution of nifedpine from granules coated with solid dispersions was practically nil in JPX [Japanese Pharmacopeia] 1st fluid, but a supersaturation phenomenon was observed in JPX 2nd fluid. These granules resulted in prolonged absorption of the drug with good bioavailability in beagle dogs and human volunteers. This absorption characteristic arises from the pH dependency of the dissolution behavior of these solid dispersions, i.e., dissolution of nifedipine was suppressed in acidic medium and showed supersaturation in comparatively neutral medium. The granules were evidently transported through the gastrointesinal tract and showed prolonged drug release behavior with good bioavailability.This publication has 8 references indexed in Scilit:
- Erythromycin absorption in healthy volunteers from single and multiple doses of enteric-coated pellets and tabletsEuropean Journal of Clinical Pharmacology, 1983
- Acute and long-term hypotensive effects and plasma concentrations of nifedipine in patients with essential hypertensionEuropean Journal of Clinical Pharmacology, 1982
- Stability and bioavailability of nifedipine in fine granules.CHEMICAL & PHARMACEUTICAL BULLETIN, 1982
- The Gastric Emptying of Pellets Contained in Hard Gelatin CapsulesDrug Development and Industrial Pharmacy, 1982
- Stability of nifedipine-polyvinylpyrrolidone coprecipitate.CHEMICAL & PHARMACEUTICAL BULLETIN, 1981
- Antihypertensive effect of fractionated sublingual administration of nifedipine in moderate essential hypertensionEuropean Journal of Clinical Pharmacology, 1980
- Identification of nifedipine metabolites and their determination by gas chromatography.CHEMICAL & PHARMACEUTICAL BULLETIN, 1980
- Dissolution and Absorption of Nipedipine from Nifedipine-Polyvinylpyrrolidone CoprecipitateDrug Development and Industrial Pharmacy, 1980