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KMID : 0369819990290010021
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Jorunal of Korean Pharmaceutical Sciences
1999 Volume.29 No. 1 p.21 ~ p.27
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Release , Biocompatibility and Pharmacokinetics of Semi - solid Naloxone Implants of Poly ( ortho ester )
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임상희/Lim SH
박주애/김길수/Park JA/Kim KS
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Abstract
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Semi-solid poly(ortho esters) (POE) were prepared to provide bioerodible carriers for sustained drug delivery systems of naloxone (NLX) in the treatment of narcotic addiction. As the POE have viscous behavior at room temperature, a significant advantage of this polymer is that it can be injected without any surgical intervention. The POE was synthesized by a transesterification reaction between 1,2,6-hexanetriol and trimethyl orthoacetate, and the structure of the polymer was confirmed by IR. The in vitro release of the drug from POE was studied. The release rate of NLX decreased with increasing intrinsic viscosities of the polymer. In vivo biocompatibility studies were carried out in rats with NLX loaded POE. Histopathological analysis showed that NLX implants are well-tolerated by rats when used subcutaneously. Pharmacokinetic studies of POE-NLX implants of two different viscosities were carried out in rabbits. In all cases, plasma concentrations of NLX were maintained over 1 ng/ml for at least 168 hours, but initial burst effect was observed. Mean residence time(MRT) was found to depend on the viscosity of the polymer.
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KEYWORD
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Poly(ortho ester), Naloxone, Semi-solid implant, Biocompatibility, Pharmacokinetics
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