Vaginal and Rectal

溶液可以由较早表明或来自液体溶液或液体浓缩物的粉末制备。在使用液体浓缩物时，指示患者将规定量的浓缩物（通常是茶匙或脂肪）加入一定量的温水（通常是夸脱）。所得溶液以适当的强度含有适量的化学试剂。该试剂类似于为冲洗粉末描述的剂。

Powders are used to prepare solutions for vaginal douche, i.e., for irrigation cleansing of the vagina. The powders themselves may be prepared and packaged in bulk or as unit packages. A unit package is designed to contain the appropriate amount of powder to prepare the specifi ed volume of douche solution. The bulk powders are used by the teaspoonful or tablespoonful in preparation of the desired solution. The user simply adds the prescribed amount of powder to the appropriate volume of warm water and stirs until dissolved.

Douche Pocders的组件中有以下内容：

1. Boric acid or sodium borate
2. 收敛剂,例如钾、明矾、ammoniuM.alum, zinc sulfate
3. Antimicrobials, for example, oxyquinoline sulfate, povidone iodine
4. Quaternary ammonium compounds, for example, benzethonium chloride
5. Detergents, for example, sodium lauryl sulfate
6. Oxidizing agents, for example, sodium perborate
7. Salts, for example, sodium citrate, sodium chloride
8. Aromatics, for example, menthol, thymol, eucalyptol, methyl salicylate, phenol

Douche powders are used for their hygienic effects. A few douche powders containing specific therapeutic anti-infective agents such as those mentioned in the discussion of vaginal suppositories are used against monilial and trichomonal infections.

Retention Enema

局部给予许多溶液，用于局部效应（例如，氢化可源）或全身吸收（例如，氨茶碱）。在氨基啉基的情况下，直肠给药最小化与口服治疗相关的不期望的胃肠道反应。临床有效的药物通常在直肠滴注后30分钟内获得。皮质类固醇作为保留灌肠或连续滴水作为一些溃疡性结肠炎患者的辅助治疗。

Evacuation Enema

直肠灌肠用于清洁肠道。就像rcially, many enemas are available in disposable plastic squeeze bottles containing a premeasured amount of enema solution. The agents are solutions of sodium phosphate and sodium biphosphate, glycerin and docusate potassium, and light mineral oil. Instruction from a pharmacist is advantageous to ensure that the patient correctly uses these products. The patient should be advised to gently insert the tip of the product with steady pressure and be told that it is not absolutely necessary to squeeze all of the contents out of the disposable plastic bottle. The patient should be told that the product will most probably work within 5 to 10 minutes.

Suppositories are solid dosage forms intended for insertion into body orifices where they melt, soften, or dissolve and exert local or systemic effects. The derivation of the word suppository is from the Latin supponere, meaning “to place under,” as derived from sub (under) and ponere (to place).

Rectal Suppositories

直肠栓剂通常为约32毫米（1.5英寸），是圆柱形的，并且具有锥形锥形的一个或两个端部。一些直肠栓剂形状像子弹，鱼雷或小笨拙。取决于碱基和栓剂中的药物的密度，重量可以变化。当可可脂（神经罗马油）作为基础时，成人直肠栓剂的重量约为2克。婴儿和儿童使用的直肠栓剂大约是成人栓剂的重量和大小的一半，并假设更加笨拙的形状。

Urethral Suppositories

Suppositories for urethral administration tend to be thinner and tapered, often about 5 mm in diameter. They have been used in the treatment of local infections, and a much smaller urethral suppository has been introduced for the administration of alprostadil in the treatment of erectile dysfunction.

Vaginal Suppositories

These preparations are employed principally to combat infections in the female genitourinary tract, to restore the vaginal mucosa to its normal state, and for contraception. The usual pathogenic organisms areTrichomonas vaginalis, Candida (Monilia) albicans or other species,and嗜血杆菌阴道。在商业阴道制剂中的抗感染剂中是Nystatin，克拉咪唑，丁二烷唑硝酸盐，苯唑唑和咪康唑（抗真菌）和三磺酰胺，磺胺胺，聚酰胺碘，Clindamycin磷酸盐，甲硝唑和氧化碳酸胺（抗菌剂）。非氧基醇-9，一种杀菌剂，用于阴道避孕。在阴道制剂中发现雌激素等雌激素物质，以将阴道粘膜恢复到其正常状态。

The most commonly used base for vaginal suppositories consists of combinations of the various molecular weight polyethylene glycols. To this base is frequently added surfactants and preservative agents, commonly the parabens. Many vaginal suppositories and other types of vaginal dosage forms are buffered to an acid pH usually about 4.5, consistent with the normal vagina. This acidity discourages pathogenic organisms and provides a favorable environment for eventual recolonization by the acid- producing bacilli normally found in the vagina. The polyethylene glycol–based vaginal suppositories are water miscible and are generally suffi ciently fi rm for the patient to handle and insert without great diffi culty. However, to make the task easier, many manufacturers provide plastic insertion devices that are used to hold the suppository or tablet for proper placement within the vagina.

Packaging and Storage

甘油栓栓剂和甘油丙醇肽栓剂包装在紧密封闭的玻璃容器中，以防止含水量的变化。由可可脂碱制备的栓剂通常在隔间盒中单独包裹或以其他方式分离，以防止接触和粘附。含有光敏药物的栓剂在不透明材料中单独包裹，例如金属箔。实际上，大多数商业栓剂在铝箔或塑料中单独包裹。有些是在连续条带中包装，通过沿着穿孔撕裂而分开。栓剂也通常在滑动箱或塑料盒中包装。

Because suppositories are adversely affected by heat, it is necessary to maintain them in a cool place. Cocoa butter suppositories must be stored below 30°C (86°F), and preferably in a refrigerator (2°C to 8°C, or 36°F to 46°F). Glycerinated gelatin suppositories can be stored at controlled room temperature (20°C to 25°C, or 68°F to 77°F).

Suppositories made from a base of polyethylene glycol may be stored at usual room temperatures. Suppositories stored in high humidity may absorb moisture and tend to become spongy, whereas suppositories stored in places of extreme dryness may lose moisture and become brittle.

选择复合方法

1. By Hand Rolling

   With ready availability of suppository molds of accommodating shapes and sizes, there is little requirement for today’s pharmacist to shape suppositories by hand. Hand rolling and shaping is a historic part of the art of the pharmacist.

   • ADVANTAGES
     – Does not require special calculations
     - 不需要特殊设备
     - 可可脂是必需的
   • DISADVANTAGES
     - 需要经验和良好的技术
     - 不如融合所准备的那么优雅

2. By Fusion Molding

   This step involves first melting the suppository base, and then dispersing or dissolving the drug in the melted base. The mixture is removed from the heat and poured into a suppository mold. When the mixture has congealed, the suppositories are removed from the mold. The fusion method can be used with all types of suppositories and must be used with most of them.

   Suppositories are generally made from solid ingredients and drugs which are measured by weight. When they are mixed, melted, and poured into suppository mold cavities, they occupy a volume – the volume of the mold cavity. Since the components are measured by weight but compounded by volume, density calculations and mold calibrations are required to provide accurate doses.

   When a drug is placed in a suppository base, it will displace an amount of base as a function of its density. If the drug has the same density as the base, it will displace an equivalent weight of the base. If the density of the drug is greater than that of the base, it will displace a proportionally smaller weight of the base. Density factors for common drugs in cocoa butter are available in standard reference texts. The density factor is used to determine how much of a base will be displaced by a drug.

   • ADVANTAGES
     – Does not require well-developed manual compounding technique
     – Have an elegant, professional appearance
     
   • DISADVANTAGES
     – Special suppository molds are required
     - 将敏感的药物纳入敏感的药物时，必须使用小心
     – Required density calculations, mold calibrations or double-casting procedure to give accurate doses

3. By Compression

   Suppositories may be prepared by forcing the mixed mass of the base and the medicaments into special molds using suppository-making machines. In preparation for compression into the molds, the base and the other formulative ingredients are combined by thorough mixing, the friction of the process softening the base into a pastelike consistency. On a small scale, a mortar and pestle may be used. Heating the mortar in warm water (then drying it) greatly facilitates the softening of the base and the mixing. On a large scale, a similar process may be used, employing mechanical kneading mixers and a warm mixing vessel.

   Compression is especially suited for making suppositories that contain heat-labile medicinal substances or a great deal of substances that are insoluble in the base. In contrast to the molding method, compression permits no likelihood of insoluble matter settling during manufacture. The disadvantage to compression is that the special suppository machine is required and there is some limitation as to the shapes of suppositories that can be made.

   在准备栓剂与压缩chine, the suppository mass is placed in a cylinder; the cylinder is closed; pressure is applied from one end, mechanically or by turning a wheel; and the mass is forced out of the other end into the mold or die. When the die is filled with the mass, a movable end plate at the back of the die is removed, and when additional pressure is applied to the mass in the cylinder, the formed suppositories are ejected. The end plate is returned and the process is repeated until all of the mass has been used. Various sizes and shapes of dies are available. It is possible to prepare suppositories of uniform circumference by extrusion through a perforated plate and by cutting the extruded mass to the desired length.

4. 通过成型

   The steps in molding include (a) melting the base, (b) incorporating any required medicaments, (c) pouring the melt into molds, (d) allowing the melt to cool and congeal into suppositories, and (e) removing the formed suppositories from the mold. Cocoa butter, glycerinated gelatin, polyethylene glycol, and most other bases are suitable for preparation by molding