Abstract
Low crystalline and crystalline polyvinyl alcohol–methyl acrylate (PVA-MA) copolymers were examined, because of their excellent flow and compressibility properties, as matrices for sustained-release tablets using phenylpropanolamine hydrochloride (PPA.HC1) as a model drug. Crystallinity of the copolymer affected the release characteristics from the tablet. Tablets made with low-crystalline PVA-MA provided sustained release of PPA, both in vitro and in vivo in dogs. PPA absorption from the low-crystalline PVA-MA tablet formulation was biphasic. An initial rapid phase was followed by a second, slower absorption phase which continued over 16 hr. Plasma PPA concentrations then declined with a half-life roughly parallel to the oral immediate-release half-lives. Oral bioavailability from the low-crystalline PVA-MA tablet formulation was 78.8 ± 3.9%.
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DiLuccio, R.C., Hussain, M.A., CoffinBeach, D. et al. Polyvinyl Alcohol–Methyl Acrylate Copolymers as a Sustained-Release Oral Delivery System. Pharm Res 6, 844–847 (1989). https://doi.org/10.1023/A:1015900303534
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DOI: https://doi.org/10.1023/A:1015900303534