Design of a polyvinyl alcohol hydrogen containing phospholipid as controlled-release vehicle for rectal administration of (+/-)-propranolol HCl.
Polyvinyl alcohol hydrogels which contained phospholipid, egg yolk lecithin or hydrogenated soya lecithin were designed as a transrectal delivery system for propranolol hydrochloride. The hydrogel preparations containing phospholipid were prepared by a low-temperature crystallization method. The release profile of propranolol from hydrogel preparations containing phospholipid complied with Fickian diffusion (Higuchi model). The release of propranolol from the hydrogel preparation decreased with higher contents of phospholipid (approximately 2% w/w). In rats plasma concentrations of propranolol after rectal administration of hydrogel preparations containing phospholipid (1 and 2% w/w) were prolonged compared with those of rats receiving preparations without phospholipid.
Morimoto
K
K
Department of Pharmaceutical Sciences, Osaka University of Pharmaceutical Sciences, Japan.
Fukanoki
S
S
Hatakeyama
Y
Y
Nagayasu
A
A
Morisaka
K
K
Hyon
S H
SH
Ikada
Y
Y
D000285:Administration, Rectal; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D005782:Gels; D008297:Male; D014677:Pharmaceutical Vehicles; D010713:Phosphatidylcholines / Q000737:chemistry; D010743:Phospholipids / Q000737:chemistry*; D011142:Polyvinyl Alcohol / Q000737:chemistry*; D011433:Propranolol / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051381:Rats; D011919:Rats, Inbred Strains
D003692:Delayed-Action Preparations; D005782:Gels; D014677:Pharmaceutical Vehicles; D010713:Phosphatidylcholines; D010743:Phospholipids; D011142:Polyvinyl Alcohol; D011433:Propranolol