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首页> 外文学位 >Nanoparticle engineering processes: Evaporative precipitation into aqueous solution (EPAS) and antisolvent precipitation to enhance the dissolution rates of poorly water soluble drugs.
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Nanoparticle engineering processes: Evaporative precipitation into aqueous solution (EPAS) and antisolvent precipitation to enhance the dissolution rates of poorly water soluble drugs.

机译：纳米粒子工程过程：蒸发成水溶液（EPAS）沉淀和反溶剂沉淀，以提高水溶性差的药物的溶出度。

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It is estimated that more than 1/3 of the compounds being developed by the pharmaceutical industry are poorly water soluble. The bioavailability of these drugs is limited by their low dissolution rates. Two nanoparticle engineering processes, evaporative precipitation into aqueous solution (EPAS) and antisolvent precipitation were developed to enhance the dissolution rate of poorly water soluble drugs.; EPAS is a process by which a drug solution in a water immiscible organic solvent is sprayed through an atomizer into an aqueous solution containing hydrophilic stabilizer (s) at high temperature. The rapid evaporation of the small organic droplets results in fast nucleation leading to submicron to micron particles suspensions. The adsorption of water soluble stabilizers on the drug particle surfaces facilitates the dissolution rates of the final powder after drying. The suspensions may be used in parenteral formulations to enhance bioavailability or may be dried to produce oral dosage forms with high dissolution rates due to small particle size and hydrophilic stabilizer that enhances wetting. The influence of EPAS process parameters on the physicochemical properties of poorly water soluble drugs was determined. The influence of the dissociation of drug molecules on the stability of nanosuspensions at high suspension concentration, as high as 30 mg/ml with a drug-to-surfactant ratio of 3:1, was investigated. High-potency (≥90%) drug particles with high dissolution rates were produced by removing the non-adsorbed surfactant.; Antisolvent precipitation is a technique where a drug solution in a water miscible organic solvent is mixed with an aqueous solution containing a surfactant(s). Upon mixing, the supersaturated solution leads to nucleation and growth of drug particles, which may be stabilized by surfactants. Temperature was shown to have a large effect on the particle size distribution in the suspension. Crystalline drug particles with particle size of 300 nm were successfully recovered from the nanosuspensions by salt flocculation followed by filtration and vacuum drying with a drug yield higher than 92%. Upon redispersion, the average particle size was comparable to the value in the original aqueous suspension. The dissolution rate was correlated with the particle size after redispersion.
机译：据估计，制药工业开发的化合物中，有超过1/3的水溶性差。这些药物的生物利用度受到其低溶出度的限制。开发了两种纳米颗粒工程方法，即蒸发沉淀到水溶液中（EPAS）和反溶剂沉淀，以提高水溶性差的药物的溶解速度。 EPAS是一种方法，通过该方法，在高温下通过雾化器将与水不混溶的有机溶剂中的药物溶液喷雾到含有亲水性稳定剂的水溶液中。小有机液滴的快速蒸发导致快速成核，导致亚微米到微米的颗粒悬浮液。水溶性稳定剂在药物颗粒表面上的吸附促进了干燥后最终粉末的溶解速率。所述悬浮液可用于肠胃外制剂中以增强生物利用度，或者可由于小粒径和增强润湿性的亲水稳定剂而被干燥以产生具有高溶解速率的口服剂型。确定了EPAS工艺参数对水溶性差的药物的理化性质的影响。研究了在高悬浮液浓度（高达30 mg / ml，药物与表面活性剂比率为3：1）下，药物分子解离对纳米悬浮液稳定性的影响。通过去除未吸附的表面活性剂产生具有高溶出度的高效（≥90％）药物颗粒。反溶剂沉淀是一种将与水混溶的有机溶剂中的药物溶液与含有一种或多种表面活性剂的水溶液混合的技术。在混合时，过饱和溶液导致药物颗粒的成核和生长，这可以通过表面活性剂来稳定。已表明温度对悬浮液中的粒度分布有很大的影响。通过盐絮凝，然后过滤和真空干燥，成功地从纳米悬浮液中回收了粒径为300 nm的结晶药物颗粒，药物收率高于92％。重新分散后，平均粒度与原始水悬浮液中的值相当。溶解速率与再分散后的粒径相关。

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