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Dosage Form Used to Deliver Medications

A suppository, a rather archaic yet persistent dosage form , is employed to introduce medications into the body. Its application involves insertion into a body orifice – any natural opening within the body’s architecture – where it subsequently dissolves or melts. This dissolution process liberates the active compound, allowing it to exert either localized effects on the surrounding tissues or systemic effects that ripple throughout the entire organism. The three primary orifices suited for suppository delivery are the rectum , the vagina , and, for males, the urethra .

Suppositories find their niche particularly with patient populations who present challenges for conventional oral administration. This includes infants, whose small size and potential for spitting out medication make oral routes difficult; elderly individuals, who may struggle with swallowing or have compromised digestive systems; and post-operative patients, who might be experiencing nausea or be restricted from oral intake. Furthermore, for individuals plagued by severe nausea and/or vomiting, where oral medications are immediately rejected, suppositories offer a reliable alternative. [1] [2] [3] The rectal route, specifically, is often favored for its potential to reduce the onset time of drug action, a critical factor in acute situations.

Composition

The foundation of any suppository is its base, a matrix that holds the medication and dictates its release characteristics. A variety of materials are employed for this purpose, each chosen based on the intended route of administration, the nature of the drug, and the environmental conditions the suppository is expected to endure. Common base ingredients include cocoa butter and its synthetic counterparts, which melt at body temperature, providing a familiar and effective vehicle. Polyethylene glycol bases offer a range of melting points and water solubility, allowing for tailored release profiles. Hydrogels and glycerinated gelatin are also utilized, particularly for specific applications where their properties are advantageous. The careful selection of the base is paramount to ensuring the suppository’s stability, its ability to melt or dissolve appropriately, and the efficient delivery of the embedded medication. [4]

Rectal Suppositories

Glycerin suppositories, a common example, function primarily as laxatives , drawing water into the bowel to stimulate evacuation.

In 1991, a study published in The Lancet proposed that a “torpedo” shape might enhance the internal travel of rectal suppositories, thereby increasing their efficacy. [5] However, it’s important to note that the evidence supporting this specific shape’s superiority is not robust enough to definitively dictate clinical practice. [6] Rectal suppositories are designed to address a spectrum of conditions, offering relief for both local issues within the rectal area and systemic effects throughout the body. They are frequently employed to alleviate pain, manage constipation, soothe irritation and inflammation, combat nausea and vomiting, reduce fever, treat migraines, manage allergic reactions, and induce sedation. [7] [8] While chronic or improper use could theoretically lead to rectal stricture due to persistent inflammation, the rectal route for drug delivery is generally considered safe and effective when administered correctly. [9] [10]

Four 500 mg paracetamol suppositories, illustrating a common formulation for pain and fever management.

Urethral Suppositories

Alprostadil pellets, a form of urethral suppository, have been used in the management of severe erectile dysfunction (impotence) . Marketed in the United States under the brand name Muse, these suppositories deliver medication directly into the urethra. However, with the advent of more convenient and widely accessible oral medications for erectile dysfunction, the use of urethral suppositories has seen a decline.

See Also

• Artesunate suppositories
• Enema
• Pessary

Notes

• ^ Jannin, Vincent; Lemagnen, Gilles; Gueroult, Pascale; Larrouture, Denis; Tuleu, Catherine (2014-06-30). “Rectal route in the 21st Century to treat children”. Advanced Drug Delivery Reviews. Drug delivery and the paediatric population: where are we at?. 73: 34–49. doi :10.1016/j.addr.2014.05.012. ISSN 0169-409X. PMID 24871671.
• ^ “Dulcolax 5 mg Suppositories - Summary of Product Characteristics (SmPC) - (emc)”. www.medicines.org.uk . Retrieved 2021-12-11.
• ^ Lowry, Michael (2016-02-22). “Rectal drug administration in adults: how, when, why”. Nursing Times. Vol. 112, no. 8, 12–14. Retrieved 2022-04-10.
• ^ Troy, David B.; Beringer, Paul (2006). Remington: The Science and Practice of Pharmacy. Lippincott Williams & Wilkins. pp. 884–885. ISBN 9780781746731.
• ^ Abd-El-Maeboud, K. H.; T. El-Naggar; E. M. M. El-Hawi; S. A. R. Mahmoud; S. Abd-El-Hay (28 September 1991). “Rectal suppository: commonsense and mode of insertion”. The Lancet. 338 (8770): 798–800. doi :10.1016/0140-6736(91)90676-G. PMID 1681170. S2CID 23190075.
• ^ Bradshaw, Ann; Lynda Price (20 December 2006). “Rectal suppository insertion: the reliability of the evidence as a basis for nursing practice” (PDF). Journal of Clinical Nursing. 16 (1): 98–103. doi :10.1111/j.1365-2702.2005.01519.x. PMID 17181671. Archived from the original (PDF) on 2020-02-29.
• ^ Hua, Susan (2019-10-16). “Physiological and Pharmaceutical Considerations for Rectal Drug Formulations”. Frontiers in Pharmacology. 10: 1196. doi :10.3389/fphar.2019.01196. ISSN 1663-9812. PMC 6805701. PMID 31680970.
• ^ “ANTIBIOTIC/ANESTHETIC/STEROID - RECTAL SUPPOSITORIES side effects, medical uses, and drug interactions”. MedicineNet. Retrieved 2021-12-11.
• ^ Ahmad, A; Krishnamurthy, P (June 2021). “Benign Rectal Strictures: A Review Article”. Practical Gastroenterology. 45 (6): 16-33.
• ^ Gupta, PJ (May 2007). “Suppositories in anal disorders: a review”. European Review for Medical and Pharmacological Sciences. 11 (3): 165–70. PMID 17970232.
• ^ “Muse Suppository - Facts and Comparisons”. Drugs.com. Retrieved 4 January 2013.