五固体制剂2胶囊剂滴丸和膜剂.pptx

第一节 胶囊剂;The capsules are made in two parts by dipping metal rods in molten starch or cellulose solution. The capsules are supplied as closed units to the pharmaceutical manufacturer. Before use, the two halves are separated, the capsule is filled with powder (either by placing a compressed slug of powder into one half of the capsule, or by filling one half of the capsule with loose powder) and the other half of the capsule is pressed on. James Murdock patented the two-part telescoping gelatin capsule in London in 1847. ;In 1834, Mothes and Dublanc were granted a patent for a method to produce a single-piece gelatin capsule that was sealed with a drop of gelatin solution. They used individual iron moulds for their process, filling the capsules individually with a medicine dropper. All modern soft-gel encapsulation uses variations of a process developed by R.P. Scherer in 1933. His innovation was to use a rotary die to produce the capsules, with the filling taking place by blow molding. This method reduced wastage, and was the first process to yield capsules with highly repeatable dosage.;（1）能掩盖药物不良嗅味、提高药物稳定性； （2）药物在体内起效快； （3）液体药物的固体剂型化； （4）可延缓药物释放和定位释药.;（二）胶囊剂的分类;(1)硬胶囊剂：将一定量药物及适当的辅料（也可不加辅料）制成均匀的粉末或颗粒，填装于空心硬胶囊中制成.; (2)软胶囊剂：系将一定量的药物（或药材提取物）溶于适当液体辅料中，然后封闭于软胶囊中而成的一种圆形或椭圆形制剂. 根据制备方法不同，软胶囊剂又可分两种： 有缝胶丸：用压制法制成，中间往往有压缝； 无缝胶丸：用滴制法制成，呈圆球形而无缝.;二、胶囊剂的制备; 根据制备方法： A型明胶：由酸水解制得，等电点pH7～9 明胶 B型明胶：由碱水解制得，等电点pH4.7～5.2;制备空胶囊的辅料：;（2）空胶囊制备工艺;空胶囊制备机;（3）空胶囊的规格与质量;(1)物料的处理与填充 ①药物粒度适宜，能满足硬胶囊剂的填充要求，即可直接填充. ②若由于药物流动性差等方面原因，则需加一定的稀释剂、润滑剂用等辅料.;(2) 胶囊规格的选择与套合、封口 普通胶囊封口: 20%明胶+40%乙醇溶液 锁口胶囊，密闭性好，不必封口.;;1.影响软胶囊成型因素 (1) 囊壁组??的影响： 软胶囊囊壁: 明胶+增塑剂+水 重量比: 干明胶-干增塑剂-水=1:（0.4～0.6) :1 软胶囊特点：囊壁具有可塑性与弹性 常用增塑剂:甘油、山梨醇或二者混合物.;(2)药物性质与液体介质的影响 药物和附加剂对蛋白质性质无影响. 液体药物含5%水,或为水溶性、挥发性、小分子有机物均不宜制成软胶囊. 液体药物pH以2.5～7.5为宜，可选用磷酸盐、乳酸盐等缓冲液调整.;(3)药物为混悬液时对胶囊大小的影响 药物形式：混悬剂＝固体药物+油性分散介质 软胶囊大小:5.5～7.8ml; 滴制法2.制备方法 压制法;;定量药液;(三) 肠溶胶囊剂的制备;三、胶囊剂的质量检查与包装贮存;2.装量差异 20粒每粒装