Sustained release of naltrexone from glyceride implants.
Solid dispersions of naltrexone in natural glycerides were used to form injectable implants which continously release narcotic antagonists in vivo. The dispersions were formed and tested either as small cylindrical pellets, e.g. 1x3.0 mm in size, or as particles with diameters in size ranges between 125-250 mu, that are suspended in an aqueous methyl cellulose solution. Both types of implants delivered naltrexone to mice at rates that were effective in blocking the antiociceptive action of morphine for at least one month. The rate of naltrexone release was controlled by altering its concentration in the dispersion and by varying the glyceride composition. Degradation and absorption of the implants were found to depend on their composition, dimensions and location in the body. No appreciable tissue incompatibility was seen in mice, rats, rabbits, monkeys and swine, even when long-lasting preparations were removed a year after treatment.
D000818:Animals; D001673:Biodegradation, Environmental; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004343:Drug Implants; D005989:Glycerides; D006648:Histocompatibility; D051379:Mice; D009020:Morphine / Q000037:antagonists & inhibitors; D009270:Naloxone / Q000031:analogs & derivatives*; D009271:Naltrexone / Q000008:administration & dosage* / Q000378:metabolism / Q000494:pharmacology; D011930:Reaction Time / Q000187:drug effects; D013997:Time Factors
D004343:Drug Implants; D005989:Glycerides; D009270:Naloxone; D009271:Naltrexone; D009020:Morphine