Nalidixic acid의 solvent deposition system의 용출특성 및 rat에서의 체내동태에 관한 연구

Abstract

Lactose 및 Potato starch를 사용하여 난용성 약물인 Nalidixic Acid의 Solvent Deposition System을 만들어 pH6.8 용출용매에서 그 용출특성을 검토하고 rat에 경구투여한 후 약물체내 동태를 검토하였다. Nalidixic Acid의 Solvent Deposition System은 matrix의 종류에 따라 표면에 침착되는 형태 및 용출속도에 차이를 보였다. 30분을 기준으로 할 때 Lactose System에서는 drug-to-matrix의 비가 1 : 5일때 Nalidixic Acid 원말의 약6.2배 1 : 2에서는 약 5.6배 1 : 10은 약 4.7배 증가하였고 Potato starch System의 경우 1 :5가 Nalidixic Acid 원말의 약 4.7배 1 : 10은 약 3.2배 1 : 2는 약 2.8배 증가하였다. 용출증대가 가장컸던 Nalidixic Acid-Lactose 1 : 5비의 Solvent Deposition System을 rat에 경구투여 했을 때 원말에 비해 AUC는 1.6배 증가하였고 C_(max)는 2.0배 증가하였다.;Nalidixic Acid was solvent deposited on lactose, potato starch by solvent deposition method in order to enhance the disslution rate of this water insoluble drug. Lactose, Potato starch were used as matrix at three different drug-to-matrix ratios. Dissolution characteristics and pharmacokinetics of Nalidixic Acid-Solvent Deposition System in rats were studied The experimental results are as follows : 1 ) In solvent deposition systems, the enhancement in dissolution rate of NA-SDS could be ordered as follows : potato starch < lactose. 2) The rank orders for the dissolution rate enhancement from lactose and potato starch system were found to be : 1 : 5 > 1 : 2 > 1 : 10 and 1 : 5 > 1 : 10 > 1 : 2 respectively. 3) A maximum dissolution rate and dissolution amount of NA was observed in NA-SDS( 1 : 5 ) Of lactose. 4) The pharmacokinetics studies on NA in rats was performed oral administration of NA-SDS ( 1 : 5 ) of lactose. From these studies, we have known that AUC and C_(max) were increased about 1.6 times and 2.0 times respectively.