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首页> 外文期刊>The Journal of Supercritical Fluids >Micronization of cyclosporine using dense gas techniques
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Micronization of cyclosporine using dense gas techniques

机译：使用致密气体技术将环孢霉素微粉化

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摘要

Most pharmaceutical compounds are administered to the human body as tablets or by injection.If the dissolution of a drug is low,high dosage is needed and hence may cause some side effects to the human body.One method of enhancing the dissolution rate of a drug into the biological environment is to reduce the particle size.Cyclosporine A,one of the immunosuppressant drugs that have been commonly used for the treatment of respiratory tract infections,was chosen as the drug of interest since it has low solubility and high permeability(Class 2)in water.The phase behaviour of the cyclosporine-carbon dioxide(CO_2)system was investigated prior to the micronization process.The melting point of cyclosporine substantially decreased from 150 deg C at 1 bar to 25 deg C at 55 bar when exposed to CO_2 at high pressure.Micron-sized cyclosporine was successfully produced by both rapid expansion of supercritical solution(RESS)and particles from gas-saturated solution(PGSS)techniques.After micronization,the average particle size of cyclosporine precipitated by both techniques was found to be less than 1 mu m,which is related to a 97% reduction compared with the unprocessed cyclosporine.No significant change in the morphology and particle size was observed with respect to the extraction temperature and pre-expansion pressure,whilst an increase in nozzle diameter resulted in a slight increase in particle size and decrease in degree of aggregation.The fine particle mass(FPM)of micronized cyclosporine produced by RESS and PGSS was found to be 48 and 59%,respectively.
机译：大多数药物以片剂或注射剂的形式给药于人体。如果药物的溶出度低，则需要高剂量，因此可能对人体产生一些副作用。一种提高药物溶出率的方法环孢菌素A是一种常用的治疗呼吸道感染的免疫抑制剂，因其溶解度低和通透性高而被选为关注药物（2类）在微粉化之前研究了环孢素-二氧化碳（CO_2）系统的相行为。当暴露于CO_2时，环孢素的熔点从1 bar的150℃降至55 bar的25℃基本上降低了超临界溶液（RESS）和气体饱和溶液（PGSS）技术中的颗粒快速膨胀，成功地制得了微米级的环孢菌素。 ，发现两种方法沉淀的环孢菌素的平均粒径均小于1微米，与未加工的环孢菌素相比，降低了97％。萃取温度和预膨胀压力下，喷嘴直径的增加导致粒径略有增加，凝集度降低。RESS和PGSS生产的微粉化环孢菌素的细颗粒质量（FPM）为48和分别为59％。

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