Suppositories substances

In the hospitalized patient without GI disease, constipation may be related to the use of general anesthesia and/or opiate substances. Most orally or rectally administered laxatives may be used. For prompt initiation of a bowel movement, a tap-water enema or glycerin suppository is recommended, or milk of magnesia. 

C-ll, C-lll, C-IV, controlled substance schedule 2, 3, and 4, respectively cap, capsule chew tab, chewable tablet CINV, chemotherapy-induced nausea and vomiting liquid, oral syrup, concentrate, or suspension OTC, nonprescription Rx, prescription supp, rectal suppository tab, tablet. 

Gertain drugs are administered as sublingual tablets (they are placed under the tongue) and as rectal suppositories these substances can be absorbed in the mouth and rectum, respectively. 

For most purposes, it is convenient to classify suppository bases according to their physical characteristics into two main categories and a third miscellaneous group (i) fatty or oleaginous bases (ii) water-soluble or water-miscible bases, and (iii) miscellaneous bases, general combinations of lipophilic and hydrophilic substances (43). Appendix V presents a survey of commercial pharmaceutical suppositories and the respective suppository bases. 

Vaginal pessaries or suppositories (the terms often used interchangeably) containing such substances as natural gums, fatty acids, alum, and rock salts were originally used in ancient Egyptian times as contraceptives. One of the earliest technical papers describing a... 

Amiodarone hydrochloride Bulk and tablets TLC Ac0H-H20 (15 85), low-actinic flasks Dissolve in MeOH Silica HF2S4 w/AcOH-MeOH (9 1) C HC1 j-MeOH-CH jOOH 254 nm [1], GC [2], stability [1104) suppositories [155,175] CP, related substances, p. [1138]... 

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. 

A rigid bottle, a collapsible tube, or a flexible pouch made of plastic material may be used for liquid-based topical product. These preparations are marketed in a single- or multiple-unit container. For example, dissolved drug (or any substance, e.g., benzocaine) may diffuse in the suppository base and can, for instance, partition into polyethylene linings of the suppository wrap. 

Suppositories Conical or ovoid medicated solids intended for insertion into one of the several orifices of the body, excluding the mouth. Suppository use has been known as early as 2600 b.c., and was recommended in the works of Hippocrates (ca. 400 b.c). The term derives from the Latin suppositus, meaning to place under. Premodern suppositories were made by hand using soap or other semisolid fatty substances as the main vehicles. They were not commonly used until the seventeenth and eighteenth centuries and did not become popular until the mid-nineteenth... 

Surface-active agents are widely used in combination with other suppository bases. The inclusion of these agents in the formulation may improve the wetting and water-absorption properties of the suppository. In addition, emulsifying surfactants help to keep insoluble substances suspended in a fatty base suppository,... 

Dal Zotto M, Realdon N, Ragazzi E, et al. Effect of hydrophilic macromolecular substances on the drug release rate from suppositories with lipophilic excipient. Part 1 use of polyacrylic acids. Farmaco 1991 46 1459-1474. 

Selection of a suppository base cannot usually be made in the absence of knowledge of the physicochemical properties and intrinsic thermodynamic activity of the drug substance. Other drug-related factors that can affect release and absorption and which must therefore be considered are the particle... 

Certain fat-soluble medications, such as chloral hydrate, may depress the melting point when incorporated into a base. Similarly, when large amounts of an active substance, either solid or liquid, have to be dispersed into a base, the rheological characteristics of the resultant suppository may be changed, with concomitant effects on release and absorption. Careful selection of bases or the inclusion of additives may therefore be necessary. 

Studies have shown that yellow wax, when added to suppository formulations, increased the melting point of the preparation significantly and decreased the rate of release of the active substance. ... 

The influence of the aqueous solubility on in vitro release from fat-based suppositories is shown in Fig. 9.54, the results being collated from the smdy of 35 dmgs grouped into classes 1-V in decreasing order of water solubility. The results maybe explained as follows. The water-soluble active substances will be insoluble in the fatty base, while the less water-soluble material will tend to be soluble... 

A smdy of the effect of polyoxyethylene glycols on the rectal absorption of unionised sulfafurazole demonstrated the importance of the affinity of the dmg substance for base and for rectal mucosa. As the amount of Macrogol 4000 (polyoxyethylene glycol 4000) was increased, the partition coefficient (lipid/ vehicle) fell and absorption decreased correspondingly, because the affinity of the dmg for the suppository base increased and its tendency to partition to the rectal lipids decreased. In a similar way, incorporation of... 

Suppositories are probably more difficult to study in vitro than many other dosage forms because it is not easy to simulate the conditions in the rectum. In one system, shown in Fig. 12.5, a suppository is placed in a pH 7.8 buffer in a dialysis bag. This bag is placed in a second dialysis bag filled with octanol, the whole is suspended in a flow system at 37°C, and the amount of drug released into the outer liquid is monitored. The results from this set-up must be interpreted with care as it is possible for substances that complex with the drug to reduce transport across the dialysis membrane - something which may or may not happen in the body. 

With nifedipine, the plasma level of the coprecipitate reaches twice that of the pure substance after two hours and in the case of the phenobarbital suppositories, it even reaches three times the level of the pure active substance. Also in the case of Lonetil suppositories the use of a povidone coprecipitate could increase the resorption [146]. 

There are two main ways by which substances may be administered to humans the enteral and the parenteral routes. For enteral administration the substance is placed directly into the gastrointestinal tract by permitting a tablet to dissolve when it is placed under the tongue (sub-lingual administration), or by swallowing a tablet, capsule or a solution (oral) or by rectal administration as a suppository. In parenteral administration the substance in solution may be injected subcutaneously, intramuscularly or intravascularly, inhaled as an aerosol, applied topically to the skin as a cream or ointment, or, rarely, in the form of a pessary. 

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