Suppositories compounding

Allen LV. Compounding suppositories Part I Theoretical considerations. Int J Pharm Compound 2000 4(4) 289-293 324-325. Allen LV. Compounding suppositories Part II Extemporaneous preparation. Int J Pharm Compound 2000 4(5) 372-373, 404-405. 

A. Leal, M. Leite Inacio, A. Tavares, and M. Baptista, The incompatability of theophylline and phenobarbital in preparations of theophylline compound suppositories. Rev. Portuguesa Farmac., 29, 75-83 (1979). 

Compounding may hold different meanings to different pharmacists. It may mean the preparation of oral liquids, topicals, suppositories, the conversion of one dose or... 

Rectal administration For outpatient treatment when oral dosing is not possible, suppositories containing 25 mg metoclopramide have been extemporaneously compounded (5 pulverized oral tablets in polyethylene glycol). Administer 1 suppository 30 to 60 minutes before each meal and at bedtime. 

The effectiveness of 5-ASA therapy depends in part on achieving high drug concentration at the site of active disease. Thus, 5-ASA suppositories or enemas are useful in patients with ulcerative colitis or Crohn s disease confined to the rectum (proctitis) or distal colon (proctosigmoiditis). In patients with ulcerative colitis or Crohn s colitis that extends to the proximal colon, both the azo compounds and mesalamine formulations are useful. For the treatment of Crohn s disease involving the small bowel, mesalamine compounds, which release 5-ASA in the small intestine, have a theoretic advantage over the azo compounds. 

Lysergic acid is a well known component especially as its amide derviative - lysergic acid diethyl amide (LSD) - to be considered in the next section on CNS drugs. Today ergotamine can be used in the treatment of chronic migraine headache although its side effects do not make it an appropriate prophylactic. It is usually compounded with caffeine and administered orally, by inhalation or suppository. The caffeine increases oral and rectal absorption of the ergotamine. Oral dose is 2 mg at onset and 2 mg at 30 minute intervals up to 6 mg with no more than 10 mg administered per week. 

Dosages and routes of administration Morphine is available in different salt forms but the hydrochloride and sulfate (Vermeire and Remon, 1999) are used preferentially. The compound can be administered by the oral, parenteral or intraspinal route. Oral application is preferred for chronic pain treatment and various slow release forms have been developed to reduce the administration frequency to 2-3 times per day (Bourke et al., 2000). Parenteral morphine is used in intravenous or intramuscular doses of 10 mg, mostly for postoperative pain and self-administration devices are available for patient-controlled analgesia (PCA). Morphine is additionally used for intraspinal (epidural or intrathecal) administration. Morphine is absorbed reasonably well in the lower gastrointestinal tract and can be given as suppositories. 

The drug most commonly used in patients who do not respond to sildenafil is alprostadil, a PGE1 analog (see Chapter 18 The Eicosanoids Prostaglandins, Thromboxanes, Leukotrienes, Related Compounds) that can be injected directly into the cavernosa or placed in the urethra as a mini suppository, from which it diffuses into the cavemosal tissue. Phentolamine can be used by injection into the cavernosa. These drugs will cause erection in most men who do not respond to sildenafil. 

A decoction of the bark, which is more astringent than the leaves, checks external and internal hemorrhages, and this astringency, when in combination with the more specific principles of Pilewort, makes one of the most effective pile medicines known. The compound can be obtained in the form of both ointment and suppositories for external application. For varicose veins an extract of the fresh leaves and young twigs of Witch Hazel is applied on a lint bandage kept constantly moist. 

Aspirin is commercially available in numerous formulations (Table 7-1). It is compounded as a tablet, an enteric-coated tablet, a controlled-release tablet, and as a suppository. Enteric-coated aspirin, which decreases GI tract irritation, is recommended for chronic use but is rarely required for the treatment of acute ocular pain, which usually resolves over several days. Likewise, controlled-release aspirin, because of its relatively long onset of action, is not recommended for treatment of acute ocular pain. 

The fact that most vegetable oils and fats are nontoxic allows them to be used as reliable excipients or carriers in many pharmaceutical formulations. Vegetable oils and fats have been approved as excipients to facilitate delivery of bioactive compounds, to act as fillers, binders, lubricants, solubilizers, emulsifiers, and emollients in a variety of delivery forms including tablets, capsules, suppositories, emulsions (enteral/parenteral), ointments, creams, and lotions. Other nondirect applications include artificial blood, gene delivery, diagnostic imaging, and medical devices (27). 

Rectal absorption of drugs from aqueous or alcoholic solutions is generally much faster than from suppositories. Non-surfactant adjuvants, such as salicylates, increase rectal absorption of water-soluble drugs and also of high molecular weight compounds, such as insulin, heparin, and gastrin. 

Drug solubility also affects the choice of suppository base or other vehicle. Generally, the drug should have little tendency to remain in the vehicle upon melting or dissolution. Therefore, it is usually suggested that water soluble drugs are best delivered from fatty vehicles and that more lipophilic compounds from water-soluble vehicles. 

The large number of variables involved in complex coacervation (pH, ionic strength, macromolecule concentration, macromolecule ratio, and macromolecular weight) affect microcapsule production, resulting in a large number of controllable parameters. These can be manipulated to produce microcapsules with specific properties. Complex coacervate microcapsules have been formulated as suspensions or gels, and have been compounded within suppositories and tablets.[ l... 

Despite the fact that many such absorption-enhancing agents have been tried in mucosal delivery as well as in nasal delivery, only sodium caprate used in rectal suppositories of antibiotics has gained regulatory approval as an additive with absorption-enhancement activity.f Because most other compounds are not approved for mucosal application in the Pharmaco-peiae in many countries, specialized attention must be paid to putting these additives into practical use. For example, bile salts have been recognized as safe and... 

Pyrogenic reactions result from contamination of antivenom by endotoxin-like compounds. High fever develops 1-2 hours after treatment and is associated with rigors, followed by vasodilatation and a fall in blood pressure. Febrile convulsions can occur in children. Patients should be cooled and given antipyretic drugs by mouth, powdered and washed down a nasogastric tube, or by suppository. 

Phenol is incompatible with albumin and gelatin as they are precipitated. It forms a liquid or soft mass when triturated with compounds such as camphor, menthol, thymol, acetaminophen, phenacetin, chloral hydrate, phenazone, ethyl amino-benzoate, methenamine, phenyl salicylate, resorcinol, terpin hydrate, sodium phosphate, or other eutectic formers. Phenol also softens cocoa butter in suppository mixtures. 

Use Chemicals, especially stearates and stearate driers lubricants soaps pharmaceuticals and cosmetics accelerator activator dispersing agent and softener in rubber compounds shoe and metal polishes coatings food packaging suppositories and ointments. 

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