<abstract xmlns="http://www.w3.org/1999/xhtml"> Background: 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. In Thailand, tramadol is available only as a capsule for oral use and as a solution for injection.Objective: Develop tramadol hydrochloride rectal suppositories and rectal gel preparations.Methods: Tramadol rectal suppository and rectal gel were prepared. Physicochemical properties (viscosity, gel strength, mucoadhesive force) and the in vitro release of tramadol hydrochloride were investigated from different bases (Witepsol H15, polyethylene glycol, poloxamer, and hydroxyethylcellulose). The analgesic activity of rectal tramadol hydrochloride using the hot plate test was evaluated in rats.Results: Tramadol hydrochloride rectal gel using poloxamer was more mucoadhesive to the rectal mucous membrane than was the gel with the hydroxyethylcellulose base. Tramadol hydrochloride was released rapidly in vitro from both the Witepsol H15 and polyethylene glycol bases. It was completely released from the polyethylene glycol suppository base within 15 minutes. The amount of tramadol hydrochloride release from the Witepsol H15 suppository base was about 93% at 120 minutes. When using poloxamer or hydroxyethylcellulose as a rectal base, tramadol hydrochloride was released from both bases rapidly and completely released within 15 minutes. Administration of a tramadol hydrochloride suppository in rats exhibited a more pronounced analgesic effect with the polyethylene glycol base than with the Witepsol H15-based suppositories. The rectal gel had a less pronounced analgesic effect when made with the hydroxyethylcellulose base than with the poloxamer base.Conclusion: Tramadol hydrochloride suppositories and rectal gels with different bases showed rapid and almost complete drug release from the bases, prolonging the latency of a nociceptive response in in vivo experiments.</abstract>

Background: 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. In Thailand, tramadol is available only as a capsule for oral use and as a solution for injection.Objective: Develop tramadol hydrochloride rectal suppositories and rectal gel preparations.Methods: Tramadol rectal suppository and rectal gel were prepared. Physicochemical properties (viscosity, gel strength, mucoadhesive force) and the in vitro release of tramadol hydrochloride were investigated from different bases (Witepsol H15, polyethylene glycol, poloxamer, and hydroxyethylcellulose). The analgesic activity of rectal tramadol hydrochloride using the hot plate test was evaluated in rats.Results: Tramadol hydrochloride rectal gel using poloxamer was more mucoadhesive to the rectal mucous membrane than was the gel with the hydroxyethylcellulose base. Tramadol hydrochloride was released rapidly in vitro from both the Witepsol H15 and polyethylene glycol bases. It was completely released from the polyethylene glycol suppository base within 15 minutes. The amount of tramadol hydrochloride release from the Witepsol H15 suppository base was about 93% at 120 minutes. When using poloxamer or hydroxyethylcellulose as a rectal base, tramadol hydrochloride was released from both bases rapidly and completely released within 15 minutes. Administration of a tramadol hydrochloride suppository in rats exhibited a more pronounced analgesic effect with the polyethylene glycol base than with the Witepsol H15-based suppositories. The rectal gel had a less pronounced analgesic effect when made with the hydroxyethylcellulose base than with the poloxamer base.Conclusion: Tramadol hydrochloride suppositories and rectal gels with different bases showed rapid and almost complete drug release from the bases, prolonging the latency of a nociceptive response in in vivo experiments.

Physicochemical properties, in vitro release and in vivo evaluation of tramadol hydrochloride rectal suppository and rectal gel

Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90110,

Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla 90110,

Asian Biomedicine

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Background: Tramadol is a centrally acting analgesic drug. Rectal administration of tramadol is useful in the treatment of post-operative pain or malignant...

Physicochemical properties, in vitro release and in vivo evaluation of tramadol hydrochloride rectal suppository and rectal gel

Article Category: Brief communication (Original)

Online veröffentlicht: 04. Feb. 2017

Seitenbereich: 269 - 275

DOI: https://doi.org/10.5372/1905-7415.0502.037

Schlüsselwörter
Analgesic, rectal gel, release study, suppository, tramadol

© 2017

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Physicochemical properties, in vitro release and in vivo evaluation of tramadol hydrochloride rectal suppository and rectal gel

Article Category: Brief communication (Original)

Online veröffentlicht: 04. Feb. 2017

Seitenbereich: 269 - 275

DOI: https://doi.org/10.5372/1905-7415.0502.037

SchlüsselwörterAnalgesic, rectal gel, release study, suppository, tramadol

© 2017

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Schlüsselwörter
Analgesic, rectal gel, release study, suppository, tramadol