IN SITU GEL AS PLATFORM FOR KETOCONAZOLE SLOW RELEASE DOSAGE FORM

Methaq Hamad Sabar,Masar Basim Mohsin Mohamed,Iman Sabah Jaafar

doi:10.22159/ijap.2018v10i5.27849

Methaq Hamad Sabar, Masar Basim Mohsin Mohamed + Show 1 more

Open Access

https://doi.org/10.22159/ijap.2018v10i5.27849

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Abstract

Objective: The aim of this study was to formulate ketoconazole (keto) as oral floating in situ gel to slow the release of keto in the stomach.Methods: Sodium alginate (Na alginate) was used as a primary polymer in the preparation of the in situ gel and was supported by the following polymers: guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, K15M and carbapol 940 as viscosity enhancing agents. As a consequence, and to complete the gelation process of above formulations was by adding the calcium carbonate (CaCO3). The in situ gels were investigated by the following tests: floating lag time, floating duration, viscosity, drug content, in vitro gelling studies and in vitro release study.Results: The study showed that the faster release was obtained with F1 which contained Na alginate alone. Additionally, reduction in Na alginate concentration resulted in significant increase in drug release. It was also noted that the increase in GG (viscosity enhancing polymer) concentration resulted in non-significant decrease in percent drug release and the reduction in CaCO3 concentration led to significant increase in drug release. Moreover, the release of drug was also affected by grade of viscosity enhancing polymer, the faster release was observed with the formula which contained a polymer of low viscosity (HPMC K4M) and an opposite result was with the high viscosity polymer (HPMCK15M).Conclusion: This study showed the formulation of Na alginate with GG and CaCO3, led to gain floating in situ gel and a sustained release of keto.

Highlights

Gastro retentive dosage forms (GDF) have been studied extensively by researchers due to their essential characteristic of staying in the stomach for prolonged period of time which enabled slowing and sustaining the release of the selected drug in the stomach [1]
The in situ gel preparation is one of the gastro retentive dosage forms (GDF) that provide a controllable drug release in the stomach. This preparation is gelled upon contact to the stomach content and floats on the stomach surface fluid due to the influence of excipients having a lower density than the stomach fluid [4]. These properties were as a guide for many researchers to develop formulations that increased the efficacy of many drugs such as Rajinikanth et al who utilised amoxicillin as a model for in situ gelling and they found a better eradication of H. pylori in comparison with amoxicillin suspension [5]
guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, HPMC K15M and carbapol 940 were added to the solution of Na alginate to enhance its viscosity and to retard the release of keto upon gelation

Summary

Introduction

Gastro retentive dosage forms (GDF) have been studied extensively by researchers due to their essential characteristic of staying in the stomach for prolonged period of time which enabled slowing and sustaining the release of the selected drug in the stomach [1]. This preparation is gelled upon contact to the stomach content and floats on the stomach surface fluid due to the influence of excipients having a lower density than the stomach fluid [4] These properties were as a guide for many researchers to develop formulations that increased the efficacy of many drugs such as Rajinikanth et al who utilised amoxicillin as a model for in situ gelling and they found a better eradication of H. pylori in comparison with amoxicillin suspension [5]. Keto as antifungal is a broad spectrum, inhibits a plenty of grampositive bacteria and protozoa [7]

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Results

Conclusion