A Suppositories

Scale (mg/suppository) Item Material Name Quantity/1000 Suppositories (g) 

Dissolve butylhydroxy toluene in the warm vitamin A, add cremophor, and mix with the molten Lutrol E grades. 

Fill into molds of suppositories to obtain the weight of 2 g. 

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ASA appears to be the active component of sulfasalazine without the sulfa component, and is free of the serious side effects seen with sulfasalazine. It is used orally, in a delay-release formulation, as a retention enema, and as a suppository. It is well tolerated in most patients. 

IMBALANCED BODY TEMPERATURE If the patient is receiving the analgesic for reduction of elevated body temperature the nurse checks the temperature immediately before and 45 to 60 minutes after administration of the drug. If a suppository fonn of the drug is used, it is important to check the patient after 30 minutes for retention of the suppository. If the drug fails to lower an elevated temperature, the nurse notifies the primary health care provider because other means of temperature control, such as a cooling blanket, may be necessary. 

To avoid the side effects of sulfapyridine, various preparations to target 5-ASA directly to sites of disease have been formulated. Also known as mesalamine, 5-ASA has been formulated in oral forms (Pentasa, Asacoi). Pentasa is a time-release capsule that releases the drug throughout the GI tract. Asacoi is a pH-dependent-release preparation that delivers drug to the distal small bowel and colon. The response of ulcerative colitis to this formulation appears to be identical to that seen with sulfasalazine. Mesalamine can also be administered as a suppository (Canasa) or enema (Rowasa) for distal colonic disease. 

Takahashi, H., et al. 1997. The enhancing mechanism of capric acid (CIO) from a suppository on rectal drug absorption through a paracellular pathway. Biol Pharm Bull 20 446. 

CyDs are known to be able to solubilize lipophilic drugs as well as lipophilic absorption enhancers, leading to the improvement of the enhancer s efficiency. There are some reports on the use of CyDs as a candidate for a coenhancer. For example, Yanagi et al. [35] reported that CyDs may promote the potency of absorption enhancers in rectum of rabbits. Inclusion complex of decanoic acid (CIO), an absorption enhancer, with a-CyD was prepared as an additive of cefmetazole sodium suppository and rectally administered to rabbits. Plasma concentration and area under the curve (AUC) of cefmetazole sodium after rectal administration of a suppository containing ClO-a-CyD complex to rabbits increased more significantly than those with no additive. 

Nakanishi, K., et al. 1994. Improvement of the rectal bioavailability of latamoxef sodium by adjuvants following administration of a suppository. Biol Pharm Bull 17 1496. 

A suppository formulation based on progesterone was proposed to prevent cystic hyperplasia of the endometrium and possible cancer formation during postmenopausal long-term estrogen therapy [31]. 

Fractionated palm oil is a solid obtained by fractionation and hydrogenation and is used as a suppository base... 

Cocoa seeds contain 35-50% of oil (cocoa butter or theobroma oil), 1-4% theobromine and 0.2-0.5% caffeine, plus tannins and volatile oils. During fermentation and roasting, most of the theobromine from the kernel passes into the husk, which thus provides a convenient source of the alkaloid. Theobroma oil or cocoa butter is obtained by hot expression from the ground seeds as a whitish solid with a mild chocolate taste. It is a valuable formulation aid in pharmacy where it is used as a suppository base. It contains glycerides of oleic (35%), stearic (35%), palmitic (26%), and linoleic (3%) acids (see page 44). 

Pilewort has astringent and demulcent properties. Traditionally, it is used for hemorrhoids, and specifically for internal or prolapsed piles with or without hemorrhage, by topical application as an ointment or a suppository. 

Other barbiturates are manufactured as a powder that is injected into the patient s vein. In addition, pentobarbital is manufactured as a suppository that is inserted in the rectum. Pentobarbital is also available in capsule, tablet, elixir, and injection dosages. Phenobarbital is produced in capsule, tablet, injection, and elixir dosages. 

Suppositories are dissolved in a separatory funnel with O.OIjV hydrochloric acid and chloroform. After the suppository has dissolved, the chloroform layer is discarded and the aqueous layer is chromatographically assayed. Three devices have been compared as useful in vitro models for measuring drug release from a suppository [58]. 

A cylindrical geometry would be a better shape than a slab for a suppository. The partially swollen cross-section of a slab and solid rod are shown in Figure 2a and 2b. In each case half the original dry polymer remains, as shown by the hatched areas the interfacial swollen/unswollen boundary of the slab has been reduced by 8% from the initial perimeter, but by 29% of the circumference of... 

Administration Most sulfa drugs are well absorbed after oral administration. Sulfasalazine [sul fa SAL a zeen], when administered orally or as a suppository, is reserved for treatment of chronic inflammatory bowel disease (for example, Crohn s disease or ulcerative colitis), because it is not absorbed. Similarly, succinylsulfathiazole [suks in ill sul fa THI a zole] is used for the treatment of salmonella and shigella carriers. Intravenous sulfonamides are generally reserved for patients who are unable to take oral preparations. Because of the risk of sensitization, sulfas are not usually applied topically. In burn units, creams of mafenide acetate (p-aminomethylbenzensulfonamide) or silver sulfadiazine have been effective in reducing burn sepsis. However, superinfections with resistant bacteria or fungi may occur. 

Thus, broader effective coverage can be obtained than is possible in the United States, where there must be some unusual relationship between the carrier and the active substance or where the composition must have a special form—for example, a suppository. 

Administered orally, ergotamine and sumatriptan have only limited bioavailability. Dihydroergotamine may be given by i.m. or slow i.v. injection, sumatriptan subcutaneously, by nasal spray, or as a suppository. When given orally, other triptans such as zolmitriptan, naratriptan, and rizatriptan have higher bioavailability than sumatriptan. 

If the medication is not to be administered by any of the routes mentioned above, for example, a pomade or a suppository, all excipients must to be mentioned, except for perfuming agents. Perfumes can be designated as such without the need to mention the specific components. 

Toxicity. The estimated minimum lethal dose after intravenous administration is 0.1 g fatalities have occurred after oral doses of 8.4 mg/kg in a child and after 25 to 100 mg/kg of aminophylline given as a suppository. Recovery has been reported after ingestion of choline theophyllinate equivalent to 12.8 g of theophylline. Toxic effects are usually associated with plasma concentrations greater than 30 pg/ml and fatalities with concentrations above 50pg/ml premature neonates appear to be relatively resistant to theophylline poisoning. 

McEvoy, E., Donegan, S., Power, J., Altria, K.D. Optimisation and validation of a rapid and efficient microemulsion liquid chromatographic (MELC) method for the determination of paracetamol (acetaminophen) content in a suppository formulation. J. Pharm. Biomed. Anal. 44, 137-143 (2007)... 

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. 

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