Shailesh T Prajapati, Hitesh H Bulchandani, Dashrath M Patel, Suresh K Dumaniya, Chhaganbhai N Patel
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引用次数: 36
摘要
奥美沙坦美多索米是一种血管紧张素II型受体阻滞剂,抗高血压药物,口服。它具有高度亲脂性(log P 5.5),是一种水溶性差的药物,绝对生物利用度为26%。水不溶性药物溶出率差仍然是制药行业面临的主要问题。本研究的目的是为了提高奥美沙坦美多沙米的溶出度,研制液体固体致密剂。以丙烯酸溶胶el135为溶剂,Avicel PH为102,以富士苷和新木质素为载体,以Aerosil为包覆材料,按不同配比制备了液固压片。DSC和FT-IR表征了药物与辅料之间的相互作用,表明药物与辅料之间不存在相互作用。采用不同的流动参数评价粉末的特性,符合药典规定。结果表明,当丙烯溶胶EL - 135对药物的溶出度为80% w/w时,其释药速度明显高于常规片剂。在所使用的载体中,富士黄芩苷和新木林是较有效的液体吸附载体材料。
Formulation and evaluation of liquisolid compacts for olmesartan medoxomil.
Olmesartan medoxomil is an angiotensin type II receptor blocker, antihypertensive agent, administered orally. It is highly lipophilic (log P 5.5) and a poorly water-soluble drug with absolute bioavailability of 26%. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. The objective of the present investigation was to develop liquisolid compacts for olmesartan medoxomil to improve the dissolution rate. Liquisolid compacts were prepared using Acrysol El 135 as a solvent, Avicel PH 102, Fujicalin and Neusilin as carrier materials, and Aerosil as coating material in different ratios. The interaction between drug and excipients was characterized by DSC and FT-IR studies, which showed that there is no interaction between drug and excipients. The powder characteristics were evaluated by different flow parameters to comply with pharmacopoeial limits. The dissolution studies for liquisolid compacts and conventional formulations were carried out, and it was found that liquisolid compacts with 80% w/w of Acrysol EL 135 to the drug showed significant higher drug release rates than conventional tablets. Amongst carriers used Fujicalin and Neusilin were found to be more effective carrier materials for liquid adsorption.