实验报告(1)

薄荷油滴丸的制备

摘要目的：通过本实验掌握制备滴丸的基本操作；了解滴丸制备的基本原理；熟悉滴丸的制备过程，了解各类栓剂基质的特点及适用情况；掌握热熔法制备栓剂的工艺；掌握置换价的测定方法和应用。实验指导：滴丸系指固体或液体药物与适宜的基质加热熔融后溶解、乳化或混悬于基质中，再滴入不相混溶、互不作用的冷凝液中，由于表面张力的作用，使液滴收缩成球状而制成的固体制剂。主要供口服，亦可供外用，如耳丸、眼丸等。这种滴法制丸的过程，实际上是将固体分散体制成滴丸的形式。常用的基质有聚乙二醇6000 、聚乙二醇4000 、硬脂酸钠和甘油明胶等。有时也用脂肪性基质，如用硬脂酸、单硬脂酸甘油酯、虫腊、氢化油及植物油等制备成缓释长效滴丸。冷却剂必须对基质和主药均不溶解，其比重轻于基质，但两者应相差极微，使滴丸滴入后逐渐下沉，给予充分的时间冷却。否则，如冷却剂比重较大，滴丸浮于液面；反之则急剧下沉，来不及全部冷却，滴丸会变形或合并。滴丸剂举例：用氢化植物油作基质，用稀醇作冷却剂制备维生素AD 丸；用聚乙二醇4000 作水溶性基质，以植物油为冷却剂制备巴比妥钠丸。

关键词：滴丸栓剂吲哚美辛半合成脂肪酸酯（山油脂）

Preparation of peppermint oil pills

Abstract Objective: Through the preparation of this study to master the basic operation of pills; understand the basic principles of preparation of pills; familiar with the Pill in the preparation process. Experimental guide: Pill means solid or liquid drug and the appropriate matrix melt was dissolved, emulsified or suspended in a matrix, and then trickle immiscible, and do not effect the condensate, due to surface tension, the droplet Shrink into a ball and made of solid preparation. Mainly for oral administration, also for external use, such as ear pills, eye balls. The drop pill legal process, in fact, into a solid dispersion is in the form of pills. Commonly used matrix in PEG 6000, PEG 4000, sodium stearate, and Gan Youming glue. Sometimes with fatty substrates, such as stearic acid, glycerin monostearate, insect wax, hydrogenated oil and vegetable oil into a sustained release preparation of long-acting pills. Coolant must not dissolve substrate and the main drugs, the proportion of light in the matrix, but the difference between the two should be minimal, so that drops gradually sinking pills, given sufficient time to cool. Otherwise, a larger proportion of the cooling agents, pills floating on the surface; otherwise rapidly sinking, and no time all the cool, pills will be deformed or merged. Pills for example: as a substrate with a hydrogenated vegetable oil, coolant used for the preparation of diluted ethanol AD vitamin pills; with polyethylene glycol 4000 as water-soluble matrix, the preparation of vegetable oil as coolant

sedative pills.

Keywords：Pill Drip system speed ，Suppository ，Indomethacin e mi-synthetic fatty acid esters (Mountain Oil)

滴丸的制备原理是基于固体分散法。用适宜的基质将主药溶解、混悬或乳化后，滴入一种不相混溶的液体冷却剂中，液滴由于表面张力作用而收缩成球形丸粒。由于药物在基质中成为高度分散的状态，增加药物的溶解度和溶出速度，故有利于提高药物的生物利用度，疗效迅速，同时能减少剂量而降低毒副作用，还可使液态药物固体化而便于应用。利用不同基质滴丸也可达到缓释或控释的目的。

滴丸剂制备的一般工艺流程如下：

滴丸常用基质有水溶性和非水溶性两类。水溶性基质有聚乙二醇、硬脂酸钠、甘油明胶等；非水溶性基质有硬酯酸、单硬脂酸甘油酯、虫蜡、蜂蜡、氢化植物油等。应根据相似者相溶的原则选择基质，即尽可能选用与主药极性相似的基质。常用的冷却剂有：水溶性基质可用液体石蜡、植物油、甲基硅油、煤油等。非水溶性基质可用水、不同浓度的乙醇等。

滴丸的制备是采用滴制法制备，即将药物溶解、乳化或混悬于适宜的熔融基质中，保持恒定的温度（80 ℃-100 ℃），并通过一定大小口径的滴管，滴入另一种不相混溶的冷却剂中，此时含有药物的基质骤然冷却，凝固形成丸粒。

制备栓剂的方法主要有：

1.热熔法