Tadalafil

In the present work Tadalafil fast disintegrating tablets were prepared with poloxamer as carrier to enhance the solubility of Tadalafil and in order to disperse at faster rate in the mouth. Chemically Tadalafil is (6R,12aR)-6-(1,3-Benzodioxol-yl) 2,3,6,7,12,12a hexahydro-2-methylpyrazino[10,20:1,6] pyrido [3,4-b]indole-1,4-dione used in erectile dysfunction. In this current work Tadalafil fast disintegrating tablets were formulated from F1-F12 by direct compression method by taking 1:1, 1:2 and 1:3 ratio of poloxamer as a water soluble polymer and super disintegrating agents such as crospovidine, croscarmellose sodium, sodium starch glycolate and kryon. There after FT-IR studies were performed and it was observed that there were no incompatible reactions found between the Tadalafil and excipients used in formulations. Then all the formulations of Tadalafil fast disintegrating tablets F1-F12 were evaluated for pre and post compressional parameters including in-vitro dissolution studies. In which formulation F-12, containing (1:3) ratio of drug-poloxamer and kryon as super disintegrating agent was shown significant changes in wetting time (13±2.09sec), dispersion time (36±3.605sec) and fastest percentage drug release of 99.27±2.78 within 30 minutes was observed.

Simple, accurate and precise and economical UV–spectroscopy method have been developed and validated for the estimation of Tadalafil and Fluoxetine HCl in a synthetic mixture. Tadalafil is used in treatment of Erectile Dysfunction and Fluoxetine HCl is used in depression. The Tadalafil and Fluoxetine HCl stock solutions are prepared in methanol solution. At zero crossing point (ZCP) of Tadalafil (230nm) Fluoxetine HCl showed a measurable derivative absorbance, whereas at zero crossing point (ZCP) of Fluoxetine HCl (235nm) Tadalafil showed a appreciable derivative absorbance value. The Tadalafil and Fluoxetine HCl are linear in concentration range of 5-25 μg/ml. Developed method was validated according to the ICH Q2 (R1) guidelines. The precision were found within limits (RSD< 2%). Accuracy were determined by recovery studies and showed % recovery between 97 to 100 % for both the drugs Tadalafil and Fluoxetine HCl. The LOD and LOQ values of Tadalafil at ZCP 230 nm were found to be 0.24 and 0.74 correspondingly and for Fluoxetine HCl at ZCP235nm were found to be 0.29 and 0.89 correspondingly.

This study is aimed at Developing and validating an UPLC method for determination of Sildenafil and tadalafil content in API and formulations. A chromatographic system consisting Waters  Acquity UPLC BEH C8(1.8 µm)column, mobile phase of  0.2 M ammonium acetate and Acetonitrile with gradient elution at flow of 0.3 mL/min and UV detector set at 245 nm has shown a good chromatographic separation for Sildenafil tadalafil. The developed method was validated as per ICH Guidelines, the developed UPLC method has run time of only 10 minutes making the method productive and tested by spiking all the impurities of sildenafil and tadalafil. It may be applied for Quality control Testing.

  A simple and sensitive high performance thin layer chromatography (HPTLC) method has been developed for the quantitative estimation of Tadalafil in its single component tablet formulation (20 mg). Tadalafil was chromatographed on silica gel 60 F254 TLC plate using chloroform: methanol (9:1, v/v) as mobile phase. Tadalafil showed Rf value 0.78 + 0.008 and scanned at 285 nm using a camag TLC scanner 3. The method was validated in terms of linearity (100 – 800 ng/spot), precision (intra-day variation, 0.38 to 0.81% and inter-day variation, 0.45 to 1.90%), accuracy (100.3 ± 0.76) and specificity. The limit of detection and limit of quantification for Tadalafil were found to be 28.11 ng/spot and 93.45 ng/spot, respectively. The developed method was successfully used for the assay of Tadalafil tablet formulation. The method was found to be simple, sensitive, specific, accurate and precise and can be used for the routine quality control testing of Tadalafil in tablet dosage form.