Sustained-release characteristics of a new implantable formulation of disulfiram.
The object of this study was to evaluate the sustained-release characteristics of a new formulation of disulfiram. Solid rods (500 mg) made of a composite of 80% poly(glycolic-co-L-lactic acid) and 20% 14C-labeled disulfiram were implanted subcutaneously in five Wistar CD-1 rats; a control group received 100 mg of 14C-labeled disulfiram subcutaneously. Excretion of radiolabeled material in the urine and feces was monitored for 88 d. Sustained mobilization of drug was observed in the copolymer-disulfiram implant group, reaching a peak value 30 d after implantation. The control group exhibited first-order kinetics of drug mobilization. At necropsy, there was no encapsulation of the residual rods. The copolymer-disulfiram composite performed as a true sustained-release system, and improved formulations may have clinical applications in the treatment of alcoholic humans.
D000818:Animals; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004221:Disulfiram / Q000008:administration & dosage*; D004343:Drug Implants; D005243:Feces / Q000032:analysis; D008297:Male; D011108:Polymers; D051381:Rats; D011919:Rats, Inbred Strains; D013997:Time Factors
D003692:Delayed-Action Preparations; D004343:Drug Implants; D011108:Polymers; D004221:Disulfiram