Patel Bhumika, Parikh R H, Swarnkar Deepali
Department of Pharmaceutics and Pharmaceutical Technology, Student and Faculty of Ramanbhai Patel College of Pharmacy, Charotar University of Science and Technology Education Campus Changa, Gujarat, India.
J Pharm Bioallied Sci. 2012 Mar;4(Suppl 1):S64-8. doi: 10.4103/0975-7406.94142.
The present study was aimed to increase the solubility of the poorly water soluble drug Telmisartan by using Surface solid dispersion (SSD) made of polymers like Poloxamer 407, PEG 6000 by Solvent evaporation method. The drug was solubilized by surfactants and/or polymers then adsorbed onto the surface of extremely fine carriers to increase its surface area and to form the SSD which give the more Surface area for absorption of the drug. A 2(2) full factorial design was used to investigate for each carrier the joint influence of formulation variables: Amount of carrier and adsorbent. Saturation solubility studies shows the improvement in solubility of drug batch SSD 8 give more solubility improvement than the other batch, in-vitro dissolution of pure drug, physical mixtures and SSDs were carried out in that SSDs were found to be effective in increasing the dissolution rate of Telmisartan in form of SSD when compared to pure drug. Also FT-IR spectroscopy, differential scanning calorimetry and X-ray diffractometry studies were carried out in order to characterize the drug and Surface solid dispersion. Furthermore, both DSC and X-ray diffraction showed a decrease in the melting enthalpy and reduced drug crystallinity consequently in SSDs. However, infrared spectroscopy revealed no drug interactions with the carriers.
本研究旨在通过溶剂蒸发法使用泊洛沙姆407、聚乙二醇6000等聚合物制备的表面固体分散体(SSD)来提高难溶性药物替米沙坦的溶解度。药物通过表面活性剂和/或聚合物增溶,然后吸附在极细载体的表面,以增加其表面积并形成表面固体分散体,从而为药物吸收提供更大的表面积。采用2(2)全因子设计研究每种载体中配方变量(载体和吸附剂的用量)的联合影响。饱和溶解度研究表明,药物批次SSD 8的溶解度提高,比其他批次的溶解度提高更多。对纯药物、物理混合物和表面固体分散体进行了体外溶出度研究,结果发现,与纯药物相比,表面固体分散体形式的替米沙坦在提高溶出速率方面是有效的。还进行了傅里叶变换红外光谱(FT-IR)、差示扫描量热法(DSC)和X射线衍射(XRD)研究,以表征药物和表面固体分散体。此外,DSC和XRD均显示表面固体分散体的熔融焓降低,药物结晶度降低。然而,红外光谱显示药物与载体之间没有相互作用。