The Improvement of the Dissolution and Release Characteristics of Ibuprofen Suppository Through Inclusion Complexes with

Abstract

Ibuprofen is classified as a BCS class II because of its low solubility and high permeability. Inclusion complex formation using β-cyclodextrin is one method to increase a drug’s solubility. In addition to the method of increasing the solubility, the choice of dosage form and route of administration has a big role in the success of therapy because it can increase the onset of action of drugs while avoiding side effects. Rectal suppositories can provide a faster antipyretic effect than oral preparations. The purpose of this study was to determine the effect of inclusion complexes formation with β-cyclodextrin in increasing the dissolution rate and release characteristics of ibuprofen suppositories. The suppository formulation used various concentrations of cetylalcohol to increase the consistency of the cocoa butter base. The release characteristics of ibuprofen in suppositories were evaluated, including, organoleptic, melting time, weight diversity, dissolution rate and dissolution efficiency, by comparing ibuprofen inclusion complex suppositories with β-cyclodextrin all three mole ratios, namely 1:1, 1:2 and 2:1, to pure ibuprofen suppositories. The inclusion complex of ibuprofen with β-cyclodextrin at a mole ratio of 2:1 showed to increase the solubility and dissolution rate of ibuprofen in suppositories with good physical and release characteristics.


Keywords: ibuprofen, inclusion complexes, suppository

References
[1] Wong T, Stang AS, Ganshorn H, Hartling L, Maconochie IK, Thomsen AM, et al. Cochrane Database Syst Rev. 2013;9(3):675–729.

[2] Indonesian Pediatric Association, Consensus on Fever Seizure Management. IDAI Publishing Agency; 2006.

[3] Autret E, Reboul-Marty J, Henry-Launois B, Laborde C, Courcier S, Goehrs JM, et al. Evaluation of ibuprofen versus aspirin and paracetamol on efficacy and comfort in children with fever. Eur J Clin Pharmacol. 1997;51(5):367–71.

[4] Handayani S, Hadinegoro SR, Sastroasmoro S. Paediatr Indones. 2005;45(9-10):211– 6.

[5] Lindenberg M, Kopp S, Dressman JB. Classification of orally administered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system. Eur J Pharm Biopharm. 2004 Sep;58(2):265–78.

[6] Sutriyo S, Rachmat H, Rosalina M. Pharmaceutical Science Magazine. 2008;5(1):1–8.

[7] Chaudhary A, Nagaich U, Gulati N, Sharma VK, Khosa RL. J Adv Pharm Educ Res. 2012;2(1):32–6.

[8] Loftsson T, Brewster ME. Pharmaceutical applications of cyclodextrins. 1. Drug solubilization and stabilization. J Pharm Sci. 1996 Oct;85(10):1017–25.

[9] Bushra R, Aslam N. An overview of clinical pharmacology of Ibuprofen. Oman Med J. 2010 Jul;25(3):155–1661.

[10] Allen LV, Ansel HC. Ansel’s Pharmaceutical Dosage Forms and Drug Delivery Systems. United States: Lippincott Williams & Wilkins; 2014.

[11] Ibrahim SA, El-Faham TH, Tous SS, Mostafa EM. Formulation, release characteristics and evaluation of ibuprofen suppositories. Int J Pharm. 1990;61(1-2):1–7.

[12] Jones D. FASTtrack Pharmaceutics-Dosage Form and Design. London: Pharmaceutical Press; 2008.

[13] Widjaja B, Radjaram A, Utami HW, Jurnal Farmasi dan Ilmu Kefarmasian Indonesia. 2014;1(1):31-33.

[14] Agustin R, Agoes G, Darijanto ST. J Farm Indones. 2007;3(3):21–7.

[15] Anonymous. Farmakope Indonesia V. Jakarta: BPOM RI; 2014.

[16] Florence A, Attwood D. Physicochemical Principles of Pharmacy. London: Pharmaceutical Press; 2006.

[17] Rowe RC, Paul JS, Marian EQ. Handbook of Pharmaceutical Excipient. London: Pharmaceutical Press; 2009.

[18] Trianggani DF, Permatasari D, Danimayostu AA. Formulasi dan Evaluasi Sistem Dispersi Padat Ibuprofen dengan Polimer Dekstrosa dalam Sediaan Suppositoria. Pharmaceutical Journal of Indonesia. 2017;2(2):51–6.

[19] A.S. Milala, A.T. Pradana, and A.P. Boehe, “Karakteristik Fisik dan Displacement Value Supositoria Neomisin Sulfat berbasis PEG.,” Jurnal Farmasi Indonesia. vol. 6, no. 3, pp. 172–176, 2013.

[20] Allen L. Suppositories. London: Pharmaceutical Press; 2008.