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KMID : 0369820050350040273
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Jorunal of Korean Pharmaceutical Sciences
2005 Volume.35 No. 4 p.273 ~ p.278
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In Vivo Prediction and Biopharmaceutical Evaluation of Nicotine Transdermal Patch
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이우영/Lee WY
백승희/박은석/지상철/Baek SH/Park ES/Chi SC
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Abstract
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Nicotine transdermal therapeutic systems $(TTS_S)$ 수식 이미지 have been regarded as an effective mean to aid smoking cessation. However, most of nicotine $TTS_S$ 수식 이미지 in the market have some problems such as unpleasant side effects and skin irritation due to the excess amount of the drug permeated and the properties of the additives employed. In order to solve these problems, new nicotine $TTS_S$ 수식 이미지 were formulated using biocompatible additives. The optimized formula of the drug layer consisted of nicotine, propylene glycol and poloxamer 188 at the ratio of 1.2: 17.0: 2.0. The drug layer had the sickness of $1,250\;{\mu}m$ 수식 이미지, the pH of 8.12. The skin permeation rate of nicotine from optimized nicotine patch (NP) was $21.5\;{\mu}g/cm^2/h$ 수식 이미지. Transdermal administration of nicotine patch has been carried out for the determination of pharmacokinetic parameters in rats. Steady-state plasma concentration of nicotine following transdermal application of NP (area of patch = $15\;cm^2$ 수식 이미지) on the dorsal skin of rats was 143.2 ng/ml and AUC for 24 hrs was 3,022 ng h/ml. In case of $EXODUS^{\circledR}$ 수식 이미지 and Nicotinell $TTS^{\circledR}$ 수식 이미지, the steady-state plasma concentration of nicotine and ACU for 24 hrs were 428.9 ng/ml, $9,121\;ng{\cdot}hr/ml$ 수식 이미지 and 155.3 ng/ml, $3,152\;ng{\cdot}h/ml$ 수식 이미지, respectively. NP showed the experimental plasma nicotine concentration profile was very similar to the simulated one and had an appropriate skin permeation rate and a steady-state concentration of nicotine, which can show therapeutic blood levels of the drug for 24 hrs without severe side effects.
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KEYWORD
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In vivo prediction, Nicotine patch, Biopharmaceutical evaluation
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