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毫微囊制法聚 D,L-乳酰胺(PLA,分子量120 000)125mg,溶于25ml 丙酮,加入混合磷酯(Epikuron 170)250mg 加热溶解,再加入含有吲哚美辛12.5mg 的苯甲酸苄酯0.5ml。混合液在中速电磁搅拌下倒入含有250mg poloxamer 的50ml 水中,此时水层立即转化成乳状,呈蓝乳白色。表明形成了毫微囊。减压除去丙酮,并浓缩除去部分水,使胶悬液最后总体积为10ml。毫微囊评定毫微囊经0.5％磷钨酸溶液背景染色后用透射电镜进行形态研究,微粒体积分布用激光散射仪测定,上清液中的未包裹药物在超滤和离心后测定,将毫微囊完全溶于乙腈中,测定药物总量,二者相减即得毫微囊中药物含量。吲哚美辛的含量用 HPLC 法测定。
Polycaprolactam polylactic acid (PLA, molecular weight 120 000) 125mg, dissolved in 25ml of acetone, was added mixed phospholipids (Epikuron 170) 250mg heated to dissolve, and then added with indomethacin 12.5mg of benzoic acid Benzyl chloride 0.5 ml. The mixture was stirred under medium speed electromagnetic stirring into 50ml of water containing 250mg poloxamer, at which time the water layer immediately converted into a milky, milky white. The formation of the nanocapsules was shown. Acetone was removed under reduced pressure and part of the water was concentrated to give a final total volume of the gel suspension of 10 ml. The nanocapsules were evaluated after the nanocapsules were stained by 0.5% phosphotungstic acid solution. The morphology of the nanocapsules was observed by transmission electron microscopy. Particle size distribution was measured by laser light scattering. The uncoated drugs in the supernatant were determined after ultrafiltration and centrifugation. The nanocapsules are completely dissolved in acetonitrile, and the total amount of the drugs is measured. The subtraction results in the content of the nanocapsules. The content of indomethacin was determined by HPLC method.