Abstract
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.
Keywords: tramadol, hydrogenated vegetable oil, hydroxypropyl methylcellulose, ethylcellulose, melt granulation
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References
- 1.Lehmann KA. Tramadol in acute pain. Drugs. 1997;53(suppl 2):25–33. doi: 10.2165/00003495-199700532-00007. [DOI] [PubMed] [Google Scholar]
- 2.Scott LJ, Perry CM. Tramadol: a review of its use in perioperative pain. Drugs. 2000;60(1):139–176. doi: 10.2165/00003495-200060010-00008. [DOI] [PubMed] [Google Scholar]
- 3.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. doi: 10.3109/03639049709148697. [DOI] [PubMed] [Google Scholar]
- 4.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. [Google Scholar]
- 5.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. doi: 10.1016/S0939-6411(01)00162-X. [DOI] [PubMed] [Google Scholar]
- 6.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. doi: 10.1111/j.1365-2044.1992.tb02166.x. [DOI] [PubMed] [Google Scholar]
- 7.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. doi: 10.1213/00000539-199204000-00007. [DOI] [PubMed] [Google Scholar]
- 8.Liao S, Hill JF, Nayk RK. Pharmacokinetics of tramadol following single and multiple oral doses in man. Pharm Res. 1992;9(suppl):308–308. [Google Scholar]
- 9.Tegeder I, Lotsch J, Geisslinger G. Pharmacokinetics of opioids in liver disease. Clin Pharmacokinet. 1999;37(July):17–40. doi: 10.2165/00003088-199937010-00002. [DOI] [PubMed] [Google Scholar]
- 10.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. doi: 10.1007/s002280050156. [DOI] [PubMed] [Google Scholar]
- 11.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. doi: 10.1248/bpb.23.627. [DOI] [PubMed] [Google Scholar]
- 12.Zhang ZY, Ping QN, Xiao B. Microencapsulation and characterization of tramadol-resin complexes. J Control Release. 2000;66(2–3):107–113. doi: 10.1016/S0168-3659(99)00273-4. [DOI] [PubMed] [Google Scholar]
- 13.Hogan JE. Hydroxypropyl methylcellulose sustained release technology. Drug Dev Ind Pharm. 1989;15(27):975–999. doi: 10.3109/03639048909043660. [DOI] [Google Scholar]
- 14.Kibbe AH. Handbook of Pharmaceutical Excipients. 3rd ed. London, UK: Pharmaceutical Press; 2000. pp. 94–95. [Google Scholar]
- 15.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. doi: 10.1248/cpb.49.1448. [DOI] [PubMed] [Google Scholar]
- 16.Obaidat Ayliman A., Rana M. Obaidat, Controlled release of tramadol hydrochloride from matrices prepared using glycerbehenate. Eur J Pharm Biopharm. 2001;52:231–235. doi: 10.1016/S0939-6411(01)00173-4. [DOI] [PubMed] [Google Scholar]
- 17.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. doi: 10.1016/S0378-5173(01)00962-0. [DOI] [PubMed] [Google Scholar]
- 18.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. doi: 10.1081/DDC-100104317. [DOI] [PubMed] [Google Scholar]
- 19.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. doi: 10.1081/PDT-100100554. [DOI] [PubMed] [Google Scholar]