The formulation of effervescent granules of RANITIDINE hydrochloride was performed by use of citric acid, tartaric acid and sodium bicarbonate as effervescent base of formulation. To find the best percent of each of these compounds, tertiary diagram was applied. Sixty six different mixtures obtained from diagram was prepared and compared in respect to characteristics. Like clarity, pH, taste and other physical properties. The best mixtures was selected and granulated with wet and dry granulation methods. Other ingredients such as flavor, sweetener, and granulator also determined by use of various amount from each of them, and determined the best formulation for each of granulation methods.

The pharmacokinetic parameters of domestic and imported RANITIDINE hydrochloride tablets (RANITIDINE, formulated and manufactured by Kharazmi Pharmaceuticals, Iran, and Zantac Ò manufactured by Glaxo, UK) were measured in 14 healthy subjects following oral administration of a single 300-mg dose of each brand and compared for bioequivalence evaluation. The pharmaceutical equivalency of both formulations was shown by in vitro characterization and dissolution testing. The comparative bioavailability of the two products was then determined in a single-blind, single dose, randomized, cross-over study in 14 healthy volunteers. A sensitive, rapid and precise high performance liquid chromatography (HPLC) method was used to measure concentrations of RANITIDINE in plasma samples collected up to 12 hours following each dose. Pharmacokinetic parameters, including Cmax, Tmax, AUC0-t, AUC0-¥ , elimination rate constant (k) and half life were determined for both formulations. Analysis of the data revealed that the variations in all pharmacokinetic parameters were not statistically significant (p> 0.05), and the 90% confidence intervals for the test/reference mean ratios of the plasma pharmacokinetic variables lie within the conventional bioequivalence range of 80-125%. Therefore, both formulations were comparable based on the in vitro characterization and were bioequivalent in terms of Cmax and AUC. The two formulations were considered to be bioequivalent.

Orally Disintegrating Tablets (ODT) have the advantages of both solid dosage form specially the stability and ease of handling and liquid dosage forms including ease of swallowing and pre-gastric absorption. We focused on taste masking and formulation of RANITIDINE ODT which disintegrates rapidly in the mouth within 60 sec using super-disintegrants, special polymers, water soluble and even insoluble excipients, sweeteners and essence. Various formulations were designed and made in four series. The amount of RANITIDINE in each formulation was 150 mg, and the final weight of tablets was around 500 mg. Prepared formulations were evaluated in terms of several physicochemical tests including powder/granule flowability, appearance, thickness, uniformity of weight, hardness, friability and disintegration time. Several taste masking techniques were investigated in each series of formulation, in order to cover the bitter taste of wRANITIDINE. These included the addition of sweetener, granulation, solid dispersion with soluble and insoluble agents and complex formation with cellulose derivatives. The best formulation(s) in each group was/were chosen for taste evaluations with the help of 10 volunteers. Finally, formulation F14 was selected as the ultimate formulation, based on its better taste and shorter disintegration time (around 5 seconds). Formulation F14 contained Na CMC, avicel, Na starch glycolate, xylitol, saccharin, Na benzoate and menthol. The chosen formulation successfully passed the complementary evaluations such as assay of active ingredient and dissolution time. Na CMC was found to be acceptable in terms of decreasing disintegration time and enhanced taste masking potential and can be used in further ODT formulations.

Purpose: The aim of this study was to design, formulate and physicochemically evaluate effervescent RANITIDINE hydrochloride (HCl) tablets since they are easily administered while the elderly and children sometimes have difficulties in swallowing oral dosage forms.Methods: Effervescent RANITIDINE HCl tablets were prepared in a dosage of 300 mg by fusion and direct compression methods. The powder blend and granule mixture were evaluated for various pre-compression characteristics, such as angle of repose, compressibility index, mean particle size and Hausner's ratio. The tablets were evaluated for post-compression features including weight variation, hardness, friability, drug content, dissolution time, carbon dioxide content, effervescence time, pH, content uniformity and water content. Effervescent systems with appropriate pre and post-compression qualities dissolved rapidly in water were selected as the best formulations.Results: The results showed that the flowability of fusion method is more than that of direct compression and the F5 and F6 formulations of 300 mg tablets were selected as the best formulations because of their physicochemical characteristics.Conclusion: In this study, citric acid, sodium bicarbonate and sweeteners (including mannitol, sucrose and aspartame) were selected. Aspartame, mint and orange flavors were more effective for masking the bitter taste of RANITIDINE. The fusion method is the best alternative in terms of physicochemical and physical properties.

Urinary excretion of RANITIDINE is known to be almost 70% of the intact drug , therefore this drug would be a good candidate for bioavailability studies using urine samples. In this study the bioequivalency of two marketed formulations using both urine and plasma samples were investigated. RANITIDINE 150 mg tablets (generic) and Zantac 150 mg tablets were compared in a double blind crossover study using eight healthy male volunteers. A simple and rapid HPLC method was also developed to analyze the drug concentration in both urine and plasma. Double peak phenomenon, observed in plasma samples, was omitted when the urine samples were used. Bioavailability of the two formulations calculated from urinary data were not significantly different, whereas the plasma data were considerably different (based on Cmax, & Tmax but not AUC). Pharmacokinetic parameters resulted from urine regarding the rate of the absorption (Tmax-ud, (dDu/dt) max,Ka-ud) did not correlate well with their respective plasma parameters (Tmax, Cmax, Ka), whereas those of absorption extent and elimination rates (plasma AUC, K and urinary Du∞, K) were well correlated. It is concluded that the urine sampling which has advantages of easy sample collection and extraction could be used for determination of the extent of absorption and rate of the elimination of RANITIDINE, since similar parameters can be obtained with easier sample collection and extraction, whereas for determination of absorption rate, Cmax,& Tmax, plasma data are preferred.