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Study on Mixed Solvency Concept in Formulation Development of Aqueous Injection of Poorly Water Soluble Drug

机译:难溶性药物水注射剂研制中的混合溶剂概念研究

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In the present investigation, mixed-solvency approach has been applied for the enhancement of aqueous solubility of a poorly water- soluble drug, zaltoprofen (selected as a model drug), by making blends (keeping total concentrations 40% w/v, constant) of selected water-soluble substances from among the hydrotropes (urea, sodium benzoate, sodium citrate, nicotinamide); water-soluble solids (PEG-4000, PEG-6000); and co-solvents (propylene glycol, glycerine, PEG-200, PEG-400, PEG-600). Aqueous solubility of drug in case of selected blends (12 blends) ranged from 9.091 ± 0.011 mg/ml–43.055 ± 0.14 mg/ml (as compared to the solubility in distilled water 0.072 ± 0.012 mg/ml). The enhancement in the solubility of drug in a mixed solvent containing 10% sodium citrate, 5% sodium benzoate and 25 % S cosolvent (25% S cosolvent contains PEG200, PEG 400, PEG600, Glycerine and Propylene glycol) was more than 600 fold. This proved a synergistic enhancement in solubility of a poorly water-soluble drug due to mixed cosolvent effect. Each solubilized product was characterized by ultraviolet and infrared techniques. Various properties of solution such as pH, viscosity, specific gravity and surface tension were studied. The developed formulation was studied for physical and chemical stability. This mixed solvency shall prove definitely a boon for pharmaceutical industries for the development of dosage form of poorly water soluble drugs.
机译:在本研究中,混合溶解法已通过混合制备(保持总浓度为40%w / v,保持恒定),以提高水溶性差的药物扎托洛芬(被选作模型药物)的水溶性从水溶助长剂中选择水溶性物质(尿素,苯甲酸钠,柠檬酸钠,烟酰胺);水溶性固体(PEG-4000,PEG-6000);和助溶剂(丙二醇,甘油,PEG-200,PEG-400,PEG-600)。在选定的混合物(12种混合物)的情况下,药物的水溶解度范围为9.091±0.011mlmg / ml–43.055±0.14mlmg / ml(与在蒸馏水中的溶解度为0.072±0.012 / mg / ml相比)。药物在包含10%柠檬酸钠,5%苯甲酸钠和25%S助溶剂(25%S助溶剂包含PEG200,PEG 400,PEG600,甘油和丙二醇)的混合溶剂中的溶解度提高了600倍以上。由于混合助溶剂的作用,这证明了水溶性差的药物的协同增效作用。通过紫外和红外技术表征每种增溶产物。研究了溶液的各种特性,例如pH,粘度,比重和表面张力。研究了开发的制剂的物理和化学稳定性。这种混合偿付能力无疑将为制药行业开发水溶性差的剂型带来福音。

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