The effect of concentration of hydrophilic (hydroxypropyl methylcellulose [HPMC]) and hydrophobic polymers (hydrogenated castor oil [HCO], ethylcellulose) on the release rate of tramadol was studied. Hydrophilic matrix tablets were prepared by wet granulation technique, while hydrophobic (wax) matrix tablets were prepared by melt granulation technique and in vitro dissolution studies were performed using United States Pharmacopeia (USP) apparatus type II. Hydrophobic matrix tablets resulted in sustained in vitro drug release (>20 hours) as compared with hydrophilic matrix tablets (<14 hours). The presence of ethylcellulose in either of the matrix systems prolonged the release rate of the drug. Tablets prepared by combination of hydrophilic and hydrophobic polymers failed to prolong the drug release beyond 12 hours. The effect of ethylcellulose coating (Surelease) and the presence of lactose and HPMC in the coating composition on the drug release was also investigated. Hydrophobic matrix tablets prepared using HCO were found to be best suited for modulating the delivery of the highly water-soluble drug, tramadol hydrochloride.
This is a preview of subscription content, log in to check access.
Buy single article
Instant access to the full article PDF.
Price includes VAT for USA
Subscribe to journal
Immediate online access to all issues from 2019. Subscription will auto renew annually.
This is the net price. Taxes to be calculated in checkout.
Lehmann KA. Tramadol in acute pain. Drugs. 1997, 53 (suppl 2): 25–33.
Scott LJ, Perry CM. Tramadol: a review of its use in perioperative pain. Drugs. 2000;60(1):139–176.
Salsa T, Veiga F, Pina ME. Oral controlled-release dosage forms. I. Cellulose ether polymers in hydrophilic matrices. Drug Dev Ind Pharm. 1997;23:929–938.
Alderman DA. A review of cellulose ethers in hydrophilic matrices for oral controlled-release dosage forms. Int J Pharm Tech Prod Mfr. 1984;5:1–9.
Liu J, Zhang F, McGinity JW. Properties of lipophilic matrix tablets containing phenylpropanolamine hydrochloride prepared by hot-melt extrusion. Eur J Pharm Biopharm. 2001;52:181–190.
Vickers MD, O Flaherty D, Szekely SM, Read M, Yushizumi J. Tramadol: pain relief by an opioid without depression of respiration. Anaesthesia. 1992;47:291–296.
Houmes RJ, Votes MA, Verkaaik A, Erdmann W, Lachmann B. Efficacy and safety of tramadol for moderate and severe postoperative pain with special regard to respiratory depression. Anesth Analg. 1992;74:510–514.
Liao S, Hill JF, Nayk RK. Pharmacokinetics of tramadol following single and multiple oral doses in man. Pharm Res. 1992;9 suppl:308.
Tegeder I, Lotsch J, Geisslinger G. Pharmacokinetics of opioids in liver disease. Clin Pharmacokinet. 1999;37(July); 17–40.
Hummel T, Roscher S, Pauli E, Frank M, Liefhold J, Fleischer W, Kobal G. Assessment of analgesia in man: tramadol controlled release formula vs tramadol standard formulation. Eur J Clin Pharmacol. 1996;51(1):31–38.
Malonne H, Fontaine J, Moes A. In vitro/in vivo characterization of a tramadol HCl depot system composed of monoolein and water. Biol Pharm Bull. 2000;23(5):627–631.
Zhang ZY, Ping QN, Xiao B. Microencapsulation and characterization of tramadol-resin complexes. J Control Release. 2000;66(2–3):107–113.
Hogan JE. Hydroxypropyl methylcellulose sustained release technology. Drug Dev Ind Pharm. 1989;15(27):975–999.
Kibbe AH. Handbook of Pharmaceutical Excipients. 3rd ed. London, UK: Pharmaceutical Press. 2000:94–95.
Yonezawa Y, Ishida S, Sunanda H. Release from or through a wax matrix system. I. Basic release properties of the wax matrix system. Chem Pharm Bull. 2001;49:1448–1451.
Ayliman A. Obaidat, Rana M. Obaidat, Controlled release of tramadol hydrochloride from matrices prepared using glycerbehenate. Eur J Pharm Biopharm. 2001;52:231–235.
Sanchez-Lafuente C, Teresa Faucci M, Fernandez-Arevalo M, Alvarez-Fuentes J, Rabasco AM, Mura P. Development of sustained release matrix tablets of didanosine containing methacrylic and ethylcellulose polymers. Int J Pharm. 2002;234(1–2):213–221.
Sadeghi F, Ford JL, Rubinstein MH, Rajabi-Siahboomi AR. Study of drug release from pellets coated with Surelease containing hydroxypropyl methylcellulose. Drug Dev Ind Pharm. 2000; 27(5):419–430.
Tang L, Schwartz JB, Porter SC, Schanaare RL, Wigent RJ. Drug release from film-coated chlorpheniramine maleate nonpareil beads: effect of water-soluble polymer, coating level, and soluble core material. Pharm Dev Tech. 2000;5(3):383–390.
About this article
Cite this article
Tiwari, S.B., Murthy, T.K., Raveendra Pai, M. et al. Controlled release formulation of tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS PharmSciTech 4, 18–23 (2003). https://doi.org/10.1208/pt040331
- hydrogenated vegetable oil
- hydroxypropyl methylcellulose
- melt granulation