Rectal preparations suppositories

Suppositories and other rectal dosage forms are more expensive to prepare and dispense than simple tablets. Therefore, unless there is a significant need and advantage by utilizing a rectal dosage form, suppositories are not likely to be used. Recently, techniques have been developed to prepare suppositories more efficiently which could lead to lower manufacturing costs. 

Suppositories and pessaries— These are preparations intended for either rectal or vaginal administration of drugs. They are formulated with a suitable base that melts at body temperature. 

The calculations involved here include determination of the amount of cocoa butter needed by using the displacement values as well as the amount of other ingredients. The calculations are shown in Examples 1-3. In this section, a brief overview is provided for the method of suppository preparation with cocoa butter. The first step is to decide whether cocoa butter is appropriate for the suppositories that are required to be prepared. If the use of cocoa butter is justified, the second step is to determine the weight of the suppository. Usually the adult rectal suppository with cocoa butter is 2 g, the children s suppository is 1 g, and the glycero-gelatin suppository for vagina is 5 g. The final step involves calculation of the amounts of all ingredients needed. 

Rectal administration The drug is also administered rectally in the form of suppositories and enema preparations which are absorbed from the colon. 

The hepatic first-pass effect can be avoided to a great extent by use of sublingual tablets and transdermal preparations and to a lesser extent by use of rectal suppositories. Sublingual absorption provides direct access to systemic—not portal—veins. The transdermal route offers the same advantage. Drugs absorbed from suppositories in the lower rectum enter vessels that drain into the inferior vena cava, thus bypassing the liver. However, suppositories tend to move upward in the rectum into a region where veins that lead to the liver predominate. Thus, only about 50% of a rectal dose can be assumed to bypass the liver. 

Of the xanthines, theophylline is the most effective bronchodilator, and it has been shown repeatedly both to relieve airflow obstruction in acute asthma and to reduce the severity of symptoms and time lost from work or school in patients with chronic asthma. Theophylline base is only slightly soluble in water, so it has been administered as several salts containing varying amounts of theophylline base. Most preparations are well absorbed from the gastrointestinal tract, but absorption of rectal suppositories is unreliable. 

A 0.1% ophthalmic preparation is recommended for prevention of postoperative ophthalmic inflammation and can be used after intraocular lens implantation and strabismus surgery. A topical gel containing 3% diclofenac is effective for solar keratoses. Diclofenac in rectal suppository form can be considered for preemptive analgesia and postoperative nausea. In Europe, diclofenac is also available as an oral mouthwash and for intramuscular administration. 

H. Suppositories Solid preparations which melt at body temperature delivering medication for at-site treatment or for absorption at that point (usually rectal, vaginal, or urethral). Excipients include cocoa butter, waxy fatty acids, and derivatives, polyethylene glycol, theobroma oil, as well as many ingredients found in G. 

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. 

Watanabe, K., et al. 1993. Investigation on rectal absorption of indomethacin from sustained-release hydrogel suppositories prepared with water-soluble dietary fibers, xanthan gum and locust bean gum. Biol Pharm Bull 16 391. 

Included in the FDA Inactive Ingredients Guide (oral suspensions, tablets ophthalmic, rectal, and topical preparations transdermal preparations, vaginal suppositories). Included in nonparenteral medicines licensed in Europe. Included in the Canadian Eist of Acceptable Non-medicinal Ingredients. 

In cosmetics and topical pharmaceutical preparations, medium-chain triglycerides are used as a component of ointments, creams, and liquid emulsions. In rectal formulations, medium-chain triglycerides have been used in the preparation of suppositories containing labile materials. 

Sesame oil may be used as a solvent in the preparation of subcutaneous injections, oral capsules, rectal suppositories, and ophthalmic preparations it may also be used in the formulation of suspensions and emulsions. Multiple-emulsion formulations, in which sesame oil was one of the oil phases incorporated, have been investigated as a prolonged-release system for rifampicin microemulsions containing sesame oil have been prepared for the transdermal delivery of ketoprofen. Sesame oil has also been used in the preparation of liniments, pastes, ointments, and soaps. A sesame paste... 

Bisacodyl is a laxative that is indicated in short-term treatment of constipation evacuation of colon for rectal and bowel evaluation preparation for delivery or surgery. Bisacodyl is the only diphenyhnethane derivative available in the United States. It is marketed as an enteric-coated preparation (Dulcolax, Correctol, others) and as a suppository for rectal administration. The usual oral daily dose of bisacodyl is 10 to 15 mg for adults and 5 to 10 mg for children 6 to 12 years old. The drug requires hydrolysis by endogenous esterases in the bowel for activation, and so the laxative effects after an oral dose usually are not produced in less than 6 hours taken at bedtime, it will produce its effect the next morning. Suppositories work much more rapidly. 

Bisacodyl is the only diphenylmethane derivative available in the U.S. It is marketed as an enteric-coated preparation (dulcolax, coRREcroL, others) arul as a suppository for rectal administration. The usual oral daily dose of bisacodyl is 10-15 mg for adults and 5-10 mg for children 6-12 years old. 

Mucoadhesion was already used as part of medicinal therapy in rectal dosage forms longer than 100 years ago. Viscosity-increasing polymers were used in the rectal solutions already at the beginning of the last century, so that that the preparation would adhere well and would not flow back [133]. A new achievement in this field is the development of mucoadhesive suppositories [18]. 

The nurse is preparing to administer a rectal suppository to a client. Which interventions should the nurse implement Select all that apply. 

Suppository is solid-like preparation made from drug and suitable bases for cavity administration. When inserted into cavities, they melt or soften, after which drug dissolution and absorption result in local or systemic effect. Whin rectal suppository is a common form which is usually used as laxatives. Administrated by rectum mucosa, suppositories possess many advantages compared with oral route. Firstly, it is a convenient administration way for infants or patients suffering from vomiting or gastrointestinal disturbances. 

Mishra MU et al. prepared rectal suppositories of mesalamine by using Sal fat and evaluated several important in vitro characteristics by comparing with the suppositories composed of cocoa butter as standard base. Their findings indicated that Sal fat can be a novel and cost effective suppository base for pharmaceutical formulations. 

For rectal administration an active substance can be formulated into a suppository (solid dosage form) or in an enema (liquid dosage form). The desired miset of action is important for the choice. For a rapid onset an enema is preferable, because a suppository base has to melt or to dissolve first. A suppository may be preferred because its use is easier and more patient-friendly. An enema is the best choice when a local effect over a large surface is desired, for instance in the treatment of ulcerative colitis. From a practical viewpoint an enema can be prepared faster, but is more sensitive to chemical degradation, due to the presence of water. 

Vaginal foams Medicated vaginal tampons From the rectal dosage forms the suppositories, enemas, ointments and creams are important as extemporaneous pharmacy preparations from the vaginal dosage forms fliese are the vaginal suppositories (pessaries), solutions, creams and gels. 

Suppositories are solid, single-dose preparations. Their shape, volume and consistency make them suitable for rectal administration. They contain one or more active substances dispersed or dissolved in a suitable basis that may be soluble or dispersible in water or may melt at body temperature. Excipients such as diluents, adsorbents, surface-active agents, lubricants, antimicrobial preservatives and colotulng matter, authorised by the competent authority, may be added if necessary (Ph. Eur.). 

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