Tinidazole

This presented work is based on application of two multivariate calibration methods for simultaneous UV-Visible spectrophotometric determination of active substances in combined pharmaceutical formulation contained of Tinidazole (TINI) and Norfloxacin (NFX). The methods used were Partial Least Square (PLS) and Principal Component Regression (PCR). The spectra of both NFX and TINI were recorded at concentrations within their linear range 2.0-12.0 μg/mL for NFX and 5.0-30.0 μg/mL for TINI. The 29 set of mixtures were used for calibration and 07 set of mixtures were used for validation in the wavelength range of 260 to 320 nm with the wavelength interval λ= 0.2 nm in methanol. The methods were validated as per International Conference on Harmonization Q2 (R1) (ICH) guidelines. These methods were successfully applied for determination of drugs in pharmaceutical formulation (tablet) with no interference of the excipients as indicated by the recovery study results. The proposed methods are simple, rapid and can be easily used as an alternative analysis tool in the quality control as well as in process control of drugs and formulation.

The aim of the present study is to prepare Tinidazole microspheres by using different polymers. Microspheres were prepared by solvent evaporation method by using various polymers. Formulation is optimized on the basis of acceptable microspheres properties and in-vitro release. In order to obtain best optimized product, 6 different formulations were developed. Different polymers like Eudragit S100, HPMC 6000 and HPC 1000 were taken as variables. Particle size analysis, Shape and Surface Morphology, Flow properties, Degree of swelling, Drug entrapment efficacy, Invitro drug release study were studied as response variables. The different physical properties showed best comparable results with drug. But higher percentage of drug release was observed when the formulation contained Eudragit S 1000 in 1:1 ratio(f3) compared to other formulations. The formulation contained Eudragit was selected as optimized product.

  Amoebiasis is an infection of the large intestine caused by Entamoeba histolytica, and it is mainly present in the intra-intestinal lumen. The efficient treatment of amoebiasis and other colonic infections could be achieved by targeting the drug to the colon. Tinidazole is the drug of choice for intestinal amoebiasis and other colon infections and the best approach for this drug is to target the drug delivery to colon which would make the drug effective with low dose and prevent the potential hazards observed in conventional dose. The objective of the present investigation was to design a multiparticulate delivery system for site-specific delivery of Tinidazole using natural polysaccharides (pectin) and pH-sensitive polymer (Shellac) for the treatment of colonic diseases. An attempt was made to prepare and characterize Tinidazole microspheres for colon specific drug delivery in order to target the drug to the colon. Pectin microspheres were prepared using emulsion cross- linking technique. These microspheres were coated with Shellac using oil-in-oil solvent evaporation method. The method was optimized using different drug: polymer ratio (1:2, 1:3, 1:4 and 1:5) stirring rate (500, 1000, 1500, and 2000) and emulsifier concentration (1%, 1.25%, 1.5% and 2%) to produce microspheres of small size and narrow size distribution, high drug loading efficiency, and controlled drug release at the colonic pH. Microspheres prepared by using drug: polymer ratio 1:3, stirring speed 1000 rpm, and 1.25% w/v concentration of emulsifying agent were selected as an optimized formulation. Microspheres were evaluated for surface morphology, particle size and size distribution, swellability, percentage drug entrapment, in- vitro drug release in simulated gastrointestinal fluids (SGF) and stability study. The experimental results demonstrated that the prepared microspheres of Tinidazole for colon targeting may reduce the side effects of the drug caused by its absorption from the upper part of GIT when given in conventional dosage forms. Key words: Tinidazole; Amoebiasis; Colon targeting; Shellac; Pectin microspheres.