Sustained release and biological availability of dalarelin from the biodegradable coacervate microcapsules.
A complex coacervation method was used to prepare microcapsules containing 74.8 +/- 1.5% of the 125I labelled dalarelin incorporated in the gelatine-algin coating. Microcapsules (62 +/- 1.7%) formed, did not exceed a size of 108 microm. The high content of the small size allowed this formulation to be administered by intramuscular injection to rats. It was found that the 125I labelled dalarelin in the form of microcapsules had better bioavailability and was active longer in the rat when compared with the 125I labelled dalarelin solution injections. Dalarelin administered in the microcapsular form was characterised by a higher biological availability. The degree of relative biological availability was calculated as 123% for the dalarelin in the microcapsular form.
Ryszka
Florian
F
Department of Applied Pharmacy and Drug Technology, Silesian Medical Academy, ul. Kasztanowa 3, 41-205 Sosnowiec, Poland. zekfar@informed.slam.katowice.pl
Dolińska
Barbara
B
Waleczek
Danuta
D
D000464:Alginates / Q000737:chemistry; D000818:Animals; D019540:Area Under Curve; D001673:Biodegradation, Environmental; D001682:Biological Availability; D002214:Capsules; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding; D005260:Female; D005780:Gelatin / Q000737:chemistry; D007987:Gonadotropin-Releasing Hormone / Q000031:analogs & derivatives* / Q000097:blood* / Q000737:chemistry; D007273:Injections, Intramuscular; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar
D000464:Alginates; D002214:Capsules; D003692:Delayed-Action Preparations; D004337:Drug Carriers; C404725:dalarelin; D007987:Gonadotropin-Releasing Hormone; D005780:Gelatin