Improved dissolution and absorption of drugs using low molecular gelatin.

Acta pharmaceutica Nordica Pub Date : 1990-01-01
S Kimura, T Nishiyama, T Imai, M Otagiri
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Abstract

Kneaded mixtures of a basic drug, meclizine dihydrochloride (MZ), and a neutral drug, prednisolone (PN), with low molecular gelatin at the weight ratio of 1:1 were prepared, and their in vitro dissolution and in vivo absorption behaviour were examined. The dissolution rate of drugs from the kneaded mixtures was significantly faster than that of the drugs themselves. The low molecular gelatin enhanced the dissolution rate of MZ and PN by improving the wettability of the drug particles without any interaction in solution and the solid state. After oral administration of the kneaded mixture to beagle dogs, the initial serum concentration was significantly higher than that of the drug alone. However, the AUC value of the drug from the kneaded mixture was almost same as that of drug alone.

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利用低分子明胶改善药物的溶解和吸收。
将盐酸美氯嗪(MZ)与中性药物强的松龙(PN)与低分子明胶按1:1的质量比揉制成混合物,考察其体外溶出度和体内吸收行为。揉制混合物中药物的溶出速度明显快于药物本身的溶出速度。低分子明胶通过改善药物颗粒的润湿性,提高了MZ和PN的溶解速率,而药物颗粒在溶液和固体中没有相互作用。经揉捏的混合物口服给beagle犬后,初始血清浓度明显高于单独给药。但经揉制的混合药的AUC值与单独药物的AUC值基本相同。
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