Alginate Based Gastro-Retentive Raft Forming Tablets for Enhanced Bioavailability of Tinidazole

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.

Formulation and Evaluation of Ibuprofen Controlled Release Matrix Tablets Using Its Solid Dispersion

“…The pellets were then scanned from 4000 to 400 cm -1 with a mirror speed of 2 mm/sec. Drug-excipient compatibility study was carried out by the FT-IR analysis of pure drug ibuprofen, and the formulation containing ibuprofen and polymers [20].…”

“…From the above drug solution, 1 ml was withdrawn and diluted with 9 ml of PH 7.2 phosphate buffer. The solution was then filtered using a Whatman filter paper [20]. The absorbance of the filtered drug solution was measured by using a UV-VIS spectrophotometer (Thermo Spectronic UV-1, USA) at λmax 220 nm and the drug content was determined by the following equation-…”

“…10 ml of sample was withdrawn at predetermined interval up to 8 h and the same volume of fresh dissolution medium was replaced for maintaining sink condition. The withdrawn samples were filtered and analyzed by UV-VIS spectrophotometer (Thermo Spectronic UV-1, USA) at λmax 220 nm using P H 7.2 phosphate buffer as a blank and the cumulative percentage of drug release was calculated [20].…”

Effect of Water Content in Kneading Method of Solid Dispersion Technique for Solubility Enhancement

“…Since the drug was encapsulated as inclusion complex in the carrier, the crystallinity of the drug was slightly altered. However, the sharp peaks in the formulated complex indicated the purity and crystal character of drug and the carrier [33,34].…”

Formulation and Evaluation of Simvastatin Gastroretentive Drug Delivery System

“…As the increase in volume is greater than the increase in mass during swelling, the densities of these devices decrease and the system starts to float after a short lag time. The influence of different processing and formulation parameters on the floating properties of matrix tablets has been studied [15,16]. Reduced floating lag times could be achieved by reducing the compression forces (thus, increasing tablet porosities), increasing polymer molecular weights and increasing the particle sizes of the matrix-forming polymer [17].…”