Abstract
Objective: Tinidazole, a nitroimidazole derivative is having low aqueous solubility which is a major barrier for systemic drug absorption. The aim of the present research was to develop gastro retentive raft forming tablets of tinidazole to achieve prolonged gastric residence time and thus higher bioavailability.Methods: Solid dispersion of tinidazole was prepared by kneading method by using methanol and polyvinylpyrrolidone (PVP). Different concentration of sodium alginate and hydroxypropyl methylcellulose (HPMC) was used to formulate a suitable raft forming tablets and then evaluated for drug content, floating lag time, raft strength, raft volume, raft weight, drug release and release kinetics.Results: Fourier transform infra-red (FT-IR) study confirms compatibility between drug and polymer. The floating lag time was found in the range of 40±4 to 60±5 s for all the formulation. Raft strength for all the formulations was within the range from 3.03±0.12 to 5.92±0.06 g. The raft volume for all the formulation was found within the range of 7.37±1.86 to 9.84±2.76 ml. Raft weight was measured after completion of raft formation for each formulation and was found in the range of 5.21±1.17 to 7.88±1.95 g. In vitro dissolution was carried up to 8 h and percentage of drug release was found to vary between 79.71±2.18 to 94.32±1.79 %.Conclusion: It can be concluded that the combination of solid dispersion and raft formation increases the bioavailability of tinidazole in tablet formulation.
Highlights
Oral administration is the most convenient route for any drug delivery to the systemic circulation with high patient compliance and flexibility in formulation [1, 2]
Fourier transform infra-red (FTIR) spectrum of tinidazole, solid dispersion of tinidazole, sodium alginate, hydroxypropyl methylcellulose (HPMC), PVP and formulation were shown in fig
FTIR spectrum of tinidazole shows a peak at 3290.81 cm-1 for aromatic CH stretching which can be observed in the formulation (3286.81 cm1) and solid dispersion of drug (3283.08 cm-1)
Summary
Oral administration is the most convenient route for any drug delivery to the systemic circulation with high patient compliance and flexibility in formulation [1, 2]. The conventional oral dosage form shows limited bioavailability due to fast gastric emptying [3, 4]. Raft-forming systems [7] have a carbonate components and upon reaction with gastric acid, bubbles form in gel, enabling the floating [8, 9]. The floating behaviour of the raft is obtained by the buoyancy and low density created by carbon dioxide formation. G. alginic acid) and sodium bicarbonate which forms a foaming sodium alginate gel (raft) when in contact with gastric fluids [10]. In the presence of gastric acid, the bicarbonate is converted to carbon dioxide which becomes entrapped within the gel precipitate, converting it into foam which floats on the surface of the gastric contents, much like a raft on water [8, 11]
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