LEWIS, Andrew Lennard,TANG, Yiqing,GONZALEZ FAJARDO, Maria Victoria
申请号：
ES07704512
公开号：
ES2672625T3
申请日:
2007.02.09
申请国别(地区):
ES
年份:
2018
代理人:
摘要：
A process for forming drug-loaded polymeric particles comprising the steps of: a) contacting particles comprising a non-water-soluble polymer matrix having an anionic level in the range of 0.1 to 10 meq g-1, which forms a hydrogel in contact with water whose particles, when pure, are swellable in phosphate buffered saline (PBS) at room temperature to an equilibrium water content in the range of 40 to 99% by weight based on polymer plus PBS, with a solution of a drug having an aqueous solubility of less than 0.1 g / room temperature, in a first organic solvent that is miscible with water； whereby the drug solution in solvent is impregnated into the particles and the first solvent is selected for being able to swell pure particles； wherein the ratio of drug solubilities at room temperature in the first organic solvent and water is in the range of 10: 1 to 106: 1, preferably (at least) 102: 1； b) separating the drug solution that has not impregnated the particles from step a) from the impregnated particles； c) contacting the particles impregnated with aqueous liquid, whereby the drug precipitates in the nucleus of the particles； and d) rinsing the particles with drug precipitated in the nucleus with a second volatile solvent in which the particles are less inflatable, with respect to their swelling capacity in water, and which is a solvent for the drug, where the solubility of the drug in the second solvent it is at least 0.1 g / l, thereby removing the drug on and near the surface of the particles with the second solvent.Un proceso para formar partículas poliméricas cargadas con fármaco que comprende las etapas de: a) poner en contacto partículas que comprenden una matriz de polímero no hidrosoluble que tiene un nivel aniónico en el intervalo de 0,1 a 10 meq g-1, que forma un hidrogel en contacto con agua cuyas partículas, cuando están puras, son hinchables en solución salina tamponada con fosfato (PBS) a temperatura ambiente a un contenido de agua en equilibrio en el
