采用第四代固体分散载体技术研制他他洛尔缓释片

U. Atneriya, Dharmendra Solanki, Komal Tikariya, Arpit Gawshinde
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摘要

他林洛尔是一种β - 1选择性肾上腺素受体拮抗剂,以其心脏保护和抗高血压活性而闻名。他利洛尔是一种受体阻滞剂。在生物制药分类系统中,第二类药物的特点是膜通透性高,溶出率低。他替洛尔是一种水溶性差的药物,导致生物利用度差。因此,本研究旨在以波洛沙姆407为载体,采用固体分散体技术制备他林洛尔速释片。poloxam407是一种亲水的合成嵌段共聚物,广泛用作溶解度增强剂。基本上有三种方法用于固体分散。熔融法或熔合法溶剂蒸发法。熔融溶剂法。溶剂蒸发法本方法选择一种既能溶解药物又能溶解亲水性载体的溶剂。溶剂蒸发技术是制备高分子纳米粒子的最常用方法之一,特别是用于药物制剂的载药高分子体系。对制备的固体分散体进行了产率、药物含量、溶解度、FTIR和DSC研究分析。制备的他立洛尔与P407的比例为1:5,30min溶出率最高,为75.28%。因此,固体分散技术与超分散剂相结合是制备他他洛尔高效快溶片的有效方法。研究结果表明,波洛沙姆407固体分散体介导快溶片成功地解决了他他洛尔溶出速度慢的问题。
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Development of fast release tablet of talinolol using fourth generation carrier of solid dispersion technique
Talinolol is a beta1-selective adreno receptor antagonist well known for its Cardio protective and antihypertensive activity. Talinolol is a beta blocker. In biopharmaceutical classification system the drugs which come under class II are characterized by more membrane permeability, less dissolution rate. Talinolol is a poor aqueous solubility drug leads to poor bioavailability. So, the aimed of this study was to develop immediate release tablet of talinolol by solid dispersions technique using poloxamer 407 as a carrier. Poloxamer 407 is a hydrophilic synthetic block copolymer widely used as a solubility enhancer. Basically there are three methods used for solid dispersion. Melting or fusion method solvent evaporation method. Melting solvent method. Solvent Evaporation Method In this method a suitable solvent is selected which can capable of solubilizing both drug and hydrophilic carrier. The solvent evaporation technique is one of the most commonly used methods to prepare polymeric nanoparticles, more specifically drug-loaded polymeric systems, for pharmaceutical formulations. The prepared solid dispersions were evaluated for production yield percent, drug content, solubility, FTIR, and DSC study analysis. The prepared formulation of Talinolol with P407 in the ratio of 1:5 gave highest dissolution rate of 75.28% at 30min.So it can be concluded that the combination of solid dispersion technology as well as using superdisintergrants an encouraging and effective technique to prepare efficient fast dissolving tablets of Talinolol.The outcome of this investigation presents poloxamer 407 solid dispersion mediated fast dissolving tablets successfully resolve problem of slow rate of dissolution of talinolol.
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