Sattar, M;
Hadgraft, J;
Lane, ME;
(2015)
Preparation, characterization and buccal permeation of naratriptan.
International Journal of Pharmaceutics
, 493
(1-2)
pp. 146-151.
10.1016/j.ijpharm.2015.07.035.
Preview |
Text
1-s2.0-S0378517315300545-main.pdf Download (620kB) | Preview |
Abstract
Naratriptan (NAR) is currently used for the management of migraine as the hydrochloride salt (NAR.HCl) and is administered as an oral tablet. This work evaluates the feasibility of buccal delivery of NAR in order to ensure faster onset of action and avoid the side-effects associated with conventional oral formulations. We hypothesized that the unionized form of NAR would permeate buccal tissue to a greater extent than the salt. Therefore the first stage of this work required preparation of the free base from NAR.HCl. Characterisation of the base with thermal and elemental analyses confirmed its purity; logP and logD values were also determined. The pH permeation profile of NAR was also determined in the range 7.4-10. Solubility studies in non-aqueous solvents indicated that Transcutol™ (TC) and dipropylene glycol (DPG) were suitable vehicles for the free base. Maximum amounts of NAR which permeated after 6h were ∼130μg/cm(2). Based on the pH permeation results and studies conducted at two different doses NAR appears to permeate porcine buccal tissue via the transcellular route. Finally, estimates of likely systemic values suggest that optimised formulations should be taken forward for in vivo evaluation.
| Type: | Article |
|---|---|
| Title: | Preparation, characterization and buccal permeation of naratriptan. |
| Location: | Netherlands |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1016/j.ijpharm.2015.07.035 |
| Publisher version: | http://dx.doi.org/10.1016/j.ijpharm.2015.07.035 |
| Language: | English |
| Additional information: | Copyright © 2015 Elsevier B.V. All rights reserved. This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivs 4.0 International License. The images or other third party material in this article are included in the article's Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder in order to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by-nc-nd/4.0/ |
| Keywords: | Base, Buccal, Naratriptan, Permeation, Salt, pH |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics |
| URI: | https://discovery.ucl.ac.uk/id/eprint/1470017 |
Archive Staff Only
 |
View Item |
