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Effect of Lipophilicity of Drugs on Dissolution Profiles of Self-nanoemulsifying Drug Delivery System

机译:药物亲脂性对自纳乳化药物递送系统溶出谱的影响

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The low solubility of poorly water-soluble drug is a major problem of oral drug adsorption. The self-emulsifying system can be applied to eliminate the drug dissolution step and improve the drug absorption. In this research, liquid self-nanoemulsifying drug delivery system (SNEDDS) composing of polyethoxylated castor oil, caprylic/capric glyceride and diethylene glycol monoethyl ether was developed. The drugs with similar structure but different lipophilicity (log P), nifedipine (NDP), felodipine (FDP) and manidipine (MDP), were investigated. Size and size distribution of emulsion after dilution in acid medium and in vitro drag dissolution were determined. The results showed that the size of emulsions obtained from dilution of SNEDDS in acidic medium ranged from 100-150 nm. Drug dissolution from SNEDDS was different depending on lipophilicity of drug, i.e., 98.6, 74.3 and 52.5% for NDP (log P 2.50), FDP (log P 4.46) and MDP (log P 5.46), respectively. The results suggested the inverse linearly relationship between drug dissolution from SNEDDS and log P.
机译:水溶性差的药物较低的溶解度是口服吸附的主要问题。可以应用自乳化系统来消除药物溶解步骤并改善药物吸收。在该研究中,液体自纳乳化药物输送系统(SNEDDS)组成聚氧化氧基化蓖麻油,辛烯/癸酸甘油酯和二甘醇单乙基醚。研究了具有类似结构但不同的亲脂性(LOG P),硝苯地平(NDP),FELODIPINE(FDP)和人偶(MDP)的药物。测定酸介质稀释后乳液的尺寸和尺寸分布和体外卷溶解。结果表明,从酸性介质中稀释的乳液中获得的乳液的尺寸范围为100-150nm。根据药物的亲脂性,即98.6,74.3和52.5%,分别对NDP(log p 2.50),FDP(log p 4.46)和MDP(log p 5.46)的亲脂,I.,98.6,74.3和52.5%的药物溶解。结果表明,来自Snedds和Log P的药物溶解之间的逆线性关系。

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