head JofIMAB
Journal of IMAB - Annual Proceeding (Scientific Papers)
Publisher: Peytchinski Publishing
ISSN: 1312-773X (Online)
Issue: 2018, vol. 24, issue4
Subject Area: Medicine
DOI: 10.5272/jimab.2018244.2303
Published online: 17 December 2018

Original article

J of IMAB. 2018 Oct-Dec;24(4):2303-2312
Nadezhda A. Ivanova1ORCID logo Corresponding Autoremail, Tsvetelina S. Stefanova2ORCID logo, Ivelin R. Iliev2ORCID logo, Georgi S. Stoyanov3, 4ORCID logo, Kameliya Zh. Bratoeva5ORCID logo,
1) Department of Pharmaceutical Technologies, Faculty of Pharmacy, Medical University, Varna, Bulgaria
2) Students at Faculty of Pharmacy, Medical University, Varna, Bulgaria
3) Department of General and Clinical Pathology, Forensic Medicine and Deontology, Faculty of Medicine, Medical University, Varna, Bulgaria
4) Department of Anatomy and Cell Biology, Faculty of Medicine, Medical University, Varna, Bulgaria
5) Department of Physiology and Pathophysiology, Division of Pathophysiology, Faculty of Medicine, Medical University, Varna, Bulgaria.

The present study aims to reveal the role of a semi-solid vehicle in the composition of Indomethacin dosage forms for their physical and chemical stability, in vitro and ex vivo behavior. Three types of hydrogels and emulgels were prepared with gelling agents Methylcellulose 2%, Poloxamer 407 20% and Carbomer 940 1%. Each preparation was observed for physical and chemical stability at 5°C and 25°C within 3 months. Test formulations, along with USP standard Indomethacin gel and combined marked product Indextol,were subjected to in vitro drug release test and ex vivo permeation study, using porcine intestinal mucosa on Franz diffusion cell. A hypothesis was built to predict steady-state plasma concentration (Css) of Indomethacin for each formulation following mucosal administration. Results revealed sustained chemical stability of all emulgels for the period observed and significantly lower chemical stability of the corresponding hydrogels. Methylcellulose hydrogel (at both temperatures) and emulgel (at 25°C) showed signs of phase separation, while all other formulations kept their physical appearance for the duration of the study. Methylcellulose emulgel along with Poloxamer 407 hydrogel showed highest cumulative drug release in 12 hours (58.01% and 55.00%, respectively). Same formulations exhibited also highest drug permeation rate (Jss) through mucosa (10.55 µg.cm-2.h-1 and 13.20 µg.cm-2.h-1, respectively) and highest predicted value of plasma concentration (Css up to 100.49 µg.l-1 and 125.71 µg.l-1, respectively), whereas highest drug deposition in mucosal tissue was detected for Poloxamer 407 emulgel (2.1 mg.cm-3).

Keywords: herbal medicines, menopause, alternative therapy,

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Please cite this article as: Ivanova NA, Stefanova TS, Iliev IR, Stoyanov GS, Bratoeva KZ. Kinetic modeling on amide hydrolysis, drug release and mucosal permeation of Indomethacin in the composition of selected semisolid vehicles. J of IMAB. 2018 Oct-Dec;24(4):2303-2312.
DOI: 10.5272/jimab.2018244.2303

Corresponding AutorCorrespondence to: Nadezhda A. Ivanova, Department of Pharmaceutical Technologies, Faculty of Pharmacy, Medical University – Varna; 84, Tsar Osvoboditel str., Varna, Bulgaria; E-mail: nadejda__iv@abv.bg

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Received: 25 June 2018
Published online: 17 December 2018

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