Sustained release implants of chloroquine phosphate for possible use in chemoprophylaxis of malaria.
Implants of chloroquine phosphate (CQP) using biodegradable polymer, gelatin (G) and cross-linked gelatin (CLG) were prepared and evaluated to assess their physicochemical properties and in vitro release profile. The mechanism and kinetics of release were studied to correlate the release phenomenon with the formulation parameters. Out of many batches of the implants investigated, the implant prepared with 20% gelatin at 2:1 drug polymer ratio, 10% crosslinking agent and 2% plasticizer (Batch J) was found to provide optimum release behavior conforming to the requirements of a long term implant for a week. In vivo studies conducted on albino rats showed consistent therapeutic blood level over a period of 7 days. Mean residence time (MRT) of the drug released in the body, calculated as the ratio of the area under the first moment curve (AUMC) to area under concentration time curve (AUC) was 72 hr for implant against 2.42 hr for subcutaneous injection.
Saparia
B
B
Pharmacy department, Faculty of Technology and Engineering, MS University of Baroda, Vadodara, India.
Solanki
A
A
Murthy RSR
D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage*; D018890:Chemoprevention; D002738:Chloroquine / Q000008:administration & dosage* / Q000031:analogs & derivatives*; D004305:Dose-Response Relationship, Drug; D004343:Drug Implants; D005260:Female; D005780:Gelatin / Q000737:chemistry; D016778:Malaria, Falciparum / Q000188:drug therapy / Q000517:prevention & control*; D008297:Male; D010963:Plasmodium falciparum; D051381:Rats
D000962:Antimalarials; D004343:Drug Implants; C023676:chloroquine diphosphate; D002738:Chloroquine; D005780:Gelatin