改良润湿法改善坎地沙坦西莱西酯的溶解度和溶出度,表面活性剂与改性表面活性剂在不同配比下的比较研究

S. Gaonkar, Iosr Phr, R. Gaud, R. S. G. S. P. Bhilegaonkar
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引用次数: 3

摘要

坎地沙坦西列地酯是一种难溶性降压药,其溶解度生物利用度有限(15%)。为了启动增溶过程,非常有必要置换表面的空气,并用与药物相容的不挥发性溶剂/表面活性剂润湿药物表面。这里使用的溶剂是不同药物:溶剂(1:1-1:9)比例的表面活性剂(Tween 20)和改性表面活性剂(Transcutol),用于制备吸附剂。然后将吸附剂转化为自由流动的粉末,作为液固压块,并压缩成片剂。评价了液体固体压实剂对坎地沙坦西莱西酯的饱和溶解度和溶解性的改善。红外光谱和x射线衍射证实,所有体系在不影响药物结构的情况下,在溶解性和溶解性方面都表现出很好的优势。增加与药物的溶剂比,在溶解度和溶出度方面没有明显的优势。
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Improved Wetting For Improved Solubility and Dissolution of Candesartan Cilexetil, Comparative Study Of Surfactant And Modified Surfactant In Varying Ratios
Candesartan cilexetil is a poorly soluble antihypertensive agent with solubility limited bioavailability (15%). To initiate process of solubilization , it is very much necessary to displace the air at the surface and wet the drug surface with a non volatile solvent / surfactant ,with which drug is compatible . Solvents used here are surfactant (Tween 20) and modified surfactant (Transcutol) in different drug:solvent (1:1-1:9) ratio’s for preparation of adsorbates. Adsorbates were then converted into free flowing powders as liquisolid compacts and compressed to form tablets. Liquisolid compacts were evaluated for improvement in saturation solubility and dissolution of candesartan cilexetil. All systems exhibited a promising advantage in terms of solubility and dissolution without affecting the drug structure as confirmed by IR and XRD. No considerable advantage in terms of solubility and dissolution was seen by increasing solvent ratio with drug.
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