Polyvinyl alcohol-methyl acrylate copolymers as a sustained-release oral delivery system.
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.HCl) 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%.
DiLuccio
R C
RC
DuPont Company, Medical Products Department, Wilmington, Delaware.
Hussain
M A
MA
CoffinBeach
D
D
Torosian
G
G
Shefter
E
E
Hurwitz
A R
AR
D000179:Acrylates; D000818:Animals; D001682:Biological Availability; D003460:Crystallization; D003692:Delayed-Action Preparations; D004285:Dogs; D005260:Female; D006207:Half-Life; D010665:Phenylpropanolamine / Q000008:administration & dosage / Q000493:pharmacokinetics; D011108:Polymers; D011142:Polyvinyl Alcohol; D013607:Tablets; D014961:X-Ray Diffraction
D000179:Acrylates; D003692:Delayed-Action Preparations; D011108:Polymers; D013607:Tablets; D010665:Phenylpropanolamine; D011142:Polyvinyl Alcohol; C035956:methyl acrylate