Design of controlled-release formulation for ivermectin using silicone.
The purpose of this study was to design a formulation using silicone as carrier, so that release of ivermectin (IVM) can be controlled for a long period of time. The lateral side of a cylindrical matrix-type formulation composed of IVM and silicone was covered with silicone to obtain a covered-rod (CR) formulation. With this formulation, linear release of IVM was obtained. With addition of polyethylene glycol 4000 (PEG), release of IVM was accelerated. In a trial with subcutaneous administration to mice, blood concentration of IVM was maintained within one-order over a period of 3 months. The velocity of release of IVM from CR preparation depended on the change in solubility of IVM by additives, and in the case of a formulation with addition of desoxycholate sodium, linear in vitro release of IVM was observed over a period of 1 year.
Maeda
H
H
Formulation research Laboratories, Sumitomo Pharmaceuticals Co. Ltd., 3-45 Kurakakiuchi 1-Chome, Ibaraki-shi, 567-0878, Osaka, Japan. maedah@sumitomopharm.co.jp
Brandon
M
M
Sano
A
A
D000279:Administration, Cutaneous; D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations; D003840:Deoxycholic Acid; D004337:Drug Carriers; D005079:Excipients; D007559:Ivermectin / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D051379:Mice; D012826:Silicone Elastomers; D012995:Solubility
D000871:Anthelmintics; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005079:Excipients; D012826:Silicone Elastomers; D003840:Deoxycholic Acid; D007559:Ivermectin