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. 2019 Dec 19;5(12):e02911.
doi: 10.1016/j.heliyon.2019.e02911. eCollection 2019 Dec.

Formulation development of chewable albendazole tablets with improved dissolution rate

Emmanuel Kimaro  1   2 , Prosper Tibalinda  3 , Raphael Shedafa  3   4 , Mary Temu  2 , Eliangiringa Kaale  3   4
Affiliations

Formulation development of chewable albendazole tablets with improved dissolution rate

Emmanuel Kimaro et al. Heliyon. .

Abstract

Background: Albendazole is an orally administered broad-spectrum anthelmintic. Currently it is mostly used in the treatment of soil transmitted helminthes, hydatidosis and neurocysticercosis caused Taenia solium.Aim of the study. To develop and optimize a formulation of chewable albendazole tablet with improved dissolution rate.

Methodology: This study was specifically focused on formulation development which passes compatibility studies and optimization of the developed formulation. The formulations were evaluated on assay, dissolution, friability, hardness, weight variation, disintegration and similarity in comparison with the reference product on the market. Analysis was required to be undertaken by High performance thin layer chromatography (HPTLC) analytical methods. Design of Expert version 7 software was used for selection or making scientific decisions in selecting the best composition of the best formulation.

Results: Five formulations out of ten (F-6, F-7, F-8, F-9 and F10) had all parameters in acceptable range. On optimization, one formulation with independent variables, Sodium Laury Sulphate (SLS) 1.911%, polyvinyl pyrrolidone (PVP-K30) 3.128%, and Sodium Cross carmellose (CCM) 4.95% was selected out of ten predictions made with Design expert version 7.0. It was found that assay of the best formulation is 99.23% which was within the in-house assay specification 95-105%. Dissolution single point in 30 min was found to be 91.5% disintegration between 2-5 min and friability 0.45%.The optimized formulation was tested and found to be within the acceptable limits. The formulation was comparable to the reference product on the market with similarity factor (f2) 62 and difference factor (f1) of 6 at pH1.2.

Conclusion: A new generic albendazole tablet with improved dissolution rate was formulated, developed and optimized by using a wet granulation method.

Keywords: Design of expert version 7; High performance thin layer chromatography; Optimezed formulation; Pharmaceutical chemistry.

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Figures

Figure 1
Figure 1
Chemical structure of Albendazole.
Figure 2
Figure 2
A typical densitogram of 5 μL application of Blank (methanol) mobile phase: ethyl acetate: Toluene: Glacial acetic acid (8:12:1v/v) acquired by UV detection at 247nm.
Figure 3
Figure 3
A typical 3D diagram showing no interference of a peak between albendazole active stored in a room condition (day 90) and albendazole standard.
Figure 4
Figure 4
A NIR overlay plot for albendazole active ingredients showing reflectance vs wavelength of the sample mixtures kept to a preformulated conditions (40 ± 2 °C/75 ± 5% RH- climatic chamber, 50 °C-Oven and Room uncontrolled room conditions with 30 ± 2 °C).
Figure 5
Figure 5
A NIR overlay plot for albendazole mixed with all excipients showing reflectance vs wavelength of the sample mixtures kept to a preformulated conditions (40 ± 2 °C/75 ± 5% RH- climatic chamber, 50 °C-Oven and Room uncontrolled room conditions with 30 ± 2 °C) from day 0–90.
Figure 6
Figure 6
Contour diagram indicating optimization of dependent variable and prediction of dissolution.
Figure 7
Figure 7
Contour diagram indicating optimization of the independent variables and prediction of friability.
Figure 8
Figure 8
Comparison of percentage release (Dissolution) between new albendazole formulation & zentel/innovator at pH 1.2.
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