Logarithmic Partition Coefficient ComparisonStudy and Molecular Weight of SynthesizedProdrugs of Ibuprofen+Paracetamol, DiclofenacSodium+Paracetamol and Ibuprofen+DiclofenacSodium

D. Sen, Jalpa Patel
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引用次数: 12

Abstract

Prodrug is a substance which after administration is metabolized into a pharmacologically active drug. Actually prodrug has least medicinal value in in-vitro/in-vivo but after biotransformation by metabolism in invivo it releases the active medicament. A drug is a substance which is a chemical entity, has definite structural skeleton, obtained by natural or synthetic or semisynthetic source, which can fit on bioreceptor platform having controlling capacity to control over the biochemical malfunction. Every drug is xenobiotic because it is coming from outer source (xeno) and active in biological unit (biotic). Prodrug is the precursor of drug which is made by derivatization of the same to enhance the bioavailability by pharmacokinetics, lipid solubility by partition coefficient and increase the physicochemical and biochemical parameters by pharmacodynamics. Ibuprofen, Diclofenac and Paracetamol have been taken as NSAID (Non-Steroidal Anti Inflammatory Drug) and three prodrugs have been synthesized by reacting with acid chloride of ibuprofen and diclofenac with paracetamol to get prodrug of ester linkage and acid chloride of ibuprofen has been reacted with diclofenac to get prodrug of amide linkage. All three prodrugs showed different logP values and molecular weights according to the solubility parameters and electronegativity: logP profile: Prodrug-C>Prodrug-B>prodrug-A; molecular weight profile: Prodrug-C>Prodrug-B>prodrug-A.
布洛芬+扑热息痛、双氯芬那钠+扑热息痛、布洛芬+双氯芬那钠合成前药的对数分配系数比较及分子量研究
前药是一种给药后代谢成药理活性药物的物质。实际上,前药在体外/体内的药用价值是最低的,但在体内通过代谢进行生物转化后释放出活性药物。药物是一种化学实体,具有明确的结构骨架,由天然或合成或半合成来源获得,能够适应具有控制生化功能的生物受体平台的物质。每一种药物都是外源性的,因为它来自外部来源(xeno),并在生物单位(biou)中起作用。前药是由原药衍生而成的药物前体,通过药代动力学提高生物利用度,通过配分系数提高脂溶性,通过药效学提高理化生化参数。以布洛芬、双氯芬酸和扑热息痛为非甾体抗炎药,分别与盐酸布洛芬和双氯芬酸与扑热息痛反应合成三种前药,得到酯链前药,盐酸布洛芬与双氯芬酸反应得到酰胺链前药。3种前药根据溶解度参数和电负性表现出不同的logP值和分子量:logP谱:前药c >前药b >前药a;分子量分布:前药c >前药b >前药a。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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