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 rec...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1984-12, Vol.73 (12), p.1718-1720
Main Authors: Phillips, Michael, Gresser, Joseph D.
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Chemistry, Pharmaceutical
Delayed-Action Preparations
Disulfiram - administration & dosage
Disulfiram-sustained-release implantable formulation
Disulfiram—sustained-release implantable formulation, rats, poly(glycolic-co-L-lactic acid)
Drug Implants
Feces - analysis
General pharmacology
Male
Medical sciences
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
poly(glycolic-co-L-lactic acid)
Polymers
Rats
Rats, Inbred Strains
Sustained-release formulations-implantable disulfiram
Sustained-release formulations—implantable disulfiram, poly(glycolic-co-L-lactic acid), rats
Time Factors
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Summary: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.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600731214