Development and Characterization of Tramadol Hydrochloride Rectal Suppository
DOI:
https://doi.org/10.22270/ajdhs.v2i3.29Keywords:
Tramadol, Rectal suppositories, PVP, HPMC, AgarAbstract
Tramadol is a centrally acting analgesic drug. Rectal administration of tramadol is useful in the treatment of post-operative pain or malignant pain in cases where it cannot be administered orally. Rectal suppositories of tramadol hydrochloride were prepared using different bases and polymers and the effect of different additives on in vitro release of tramadol hydrochloride was studied. The agar-based suppositories were non-disintegrating/non-dissolving. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content and hardness. In vitro release study was performed by USP type I apparatus. Addition of 10% w/w propylene glycol accelerates the release of tramadol hydrochloride significantly (P<0.05) as in A1, which may be due to decrease in the gel matrix of agar. In formulation A2, A3 Addition of HPMC (1%, 3% w/w) and in formulation A3 and A4 addition of PVP (1%, 3% w/w) retards the release significantly (P<0.05), which may be due to increase in the viscosity and gel strength of the polymer matrix. Hence, PVP, HPMC and similar polymers in higher concentration can be used to formulate sustained released suppositories. The sustained release suppositories can be prepared by addition of PVP, HPMC in agar-based suppositories.
Keywords: Tramadol, Rectal suppositories, PVP, HPMC, Agar.
References
Goodman DO. Pharmacokinetics: Disposition and metabolism of drugs. In: Munson PL, Muller RA, Breese GR. editors. Principles of pharmacology, 1st ed. New York: Chapman and Hall; 2001. p. 47.
Sanyal P, Roy G. Preparation and evaluation of suppositories of paracetamol. East Pharma 2001; 49:95-7.
Nair L, Bhargava HN. Comparison of in vitro dissolution and permeation of fluconazole from different suppository bases. Drug Develop Ind Pharm1999; 25:691-4. https://doi.org/10.1081/DDC-100102227
Akala EO, Adedoyn A, Ogunbona FA. Suppository formulations of amodiaquine: In vitro release characteristics. Drug Develop Ind Pharm 1991; 17:303-7. https://doi.org/10.3109/03639049109043827
Kamlinder KS, Deshpande SG, Baichwal MR. Studies on suppository bases: Design and evaluation of sodium CMC and agar bases. Indian Drugs 1994; 31:149-54.
Jayaprakash S, Jawahar N, Dhachina MD, Ramkanth S, Mohamed Anzar A, Nagarajan M. Design and evaluation of timed release matrix suppositories of indomethacin. Pharm Rev 2006; 4:100-2.
Dayer P, Collart L, Desmeules J. The pharmacology of tramadol. Drugs. 1994; 47(Suppl):3-7. https://doi.org/10.2165/00003495-199400471-00003
Grond S, Sablotzki A. Clinical pharmacology of tramadol. Clin Pharmacokinet. 2004; 43:879-923. https://doi.org/10.2165/00003088-200443130-00004
Micromedex Healthcare Series: Document 2007. Tramadol. Available from: http://www.thomsonhc.com/ hcs/librarian/ND_PR/Main/SBK/3/PFPUI/7z16hW4.
Petrone D, Kamin M, Olson W. Slowing the titration rate of tramadol HCl reduces the incidence of discontinuation due to nausea and/ or vomiting: a double-blind randomized trial. J Clin Pharm Ther. 1999; 24:115-23. https://doi.org/10.1046/j.1365-2710.1999.00203.x
Mercadante S, Arcuri E, Fusco F, Tirelli W, Villari P, Bussolino C, Campa T, De Conno F, Ripamonti C. Randomized double-blind, double-dummy crossover clinical trial of oral tramadol versus rectal tramadol administration in opioid-native cancer patients with pain. Support Care Cancer. 2005; 13:702-7. https://doi.org/10.1007/s00520-004-0760-9
Allen LV Jr. Compounding suppositories. Part I: theoretical considerations. Int J Pharm Compound. 2000; 4:289-93.
Patel AN, Rai JP, Jain DK, Banweer JI. Formulation, development and evaluation of cefaclor extended release matrix tablet. Int J Pharm Pharm Sci. 2012; 4(4):355-7.
Jain P, Nair S, Jain N, Jain DK, Jain S. Formulation and evaluation of solid dispersion of lomefloxacin hydrochloride. Int J Res Pharm Sci 2012; 3(4):604-608.
Block LH. Medicated topicals. In: Gennaro AR. editors. Remington: The science and practice of pharmacy. 21st ed. Vol. 2. Noida: Lippincott Williams and Wilkins; 2005. p. 885-6.
British Pharmacopoieal Convention. British Pharmacopoeia. Vol. 2. London: H.M Stationery Offi ce; 1993.
Coben LJ, Liberman HA. Suppositories. In: Lachman L, Liberman HA, Kanig JL, editors. Theory and practice of industrial pharmacy. 3rd ed. Mumbai: Varghese Publishing House; 1989. p. 580.
Senthil Kumaran K, Thiruganasambantham P, Viswanathan S, Shree Rammurthy M. Development and evaluation of Andrographolide (from Andrographis paniculata) rectal suppositories. Indian Drugs 2002; 39:648-51.
Hammouda YE, Kasim NA, Nada AH. Formulation and in vitro evaluation of verapamil HCL suppositories. Int J Pharm 1993; 89:111-117. https://doi.org/10.1016/0378-5173(93)90111-R
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