Ketoconazole

To evaluate the physicochemical parameter. Anti-Helminthic  activity, Anti-Fungal activity and Anti-bacterial activity by various extracts (petroleum ether, chloroform, acetone, methanol) against various gram positive and gram negative bacteria (E.coli, Staphylococcus aureus and Bacillus subtilis) using a standard as Amoxicillin, Anti-Fungal activity (Candida Albicans, Aspergillus) using Ketoconazole and Anti-Helminthic  activity using a standard as Albendazole. The collected leaves of Rubus Ursinus were dried under shade for 10 days and then powdered into coarse particles in a mechanical grinder for further use, Extracted with petroleum ether, chloroform, acetone, methanol. Antihelmentic activity was evaluated on adult Pheritima Posthuma. Earthworms by subjecting to standard drug albendazole at a dose level of 10mg/ml and to the extracts of petroleum ether, chloroform, acetone, methanol at doses of 10mg/ml, 20mg/ml,25mg/ml 30mg/ml and 35mg/ml respectively. Anti-Fungal activity and Anti-bacterial activity was also performed against different bacteria by using disc diffusion method, the zones of inhibition of the extracts using standard as Amoxicillin and Ketoconazole  were determined. The powder leaves of Rubus Ursinus plant was subjected to extraction with four solvents petroleum ether, chloroform, acetone, methanol. High yield was obtained by methanol extracts of Rubus Ursinus plants. The qualitative test for methanol extraction was given positive tests for alkaloids, proteins & aminoacids,Tannins,Glycosides,FlavonoidsSaponins,Carbohydrates,Steroids& terpenoids and Phenolic compounds The anti-helmintic study and anti- fungal study of BlackBerry leaves was observed by using the extract of  methyl alcohol. The anti-bacterial study of various BlackBerry leaves extracts (petroleum ether, chloroform, acetone, methanol)  were found to be effective against various gram positive and gram negative bacteria. The leave part of plant of RUBUS URSINUS was observed for the Pharmacognostic investigation and Potent Anti-helmentic activity and significant Anti-Microbial activity. . The purified components may have even more potency with respect to inhibition of microbes. Key Words: RUBUS URSINUS, Amoxicillin, Ketoconazole, Albendazole

A simple, precise, and rapid high performance liquid chromatography (HPLC) method for the determination of ketoconazole level in human plasma using itraconazole as an internal standard (IS) was developed and validated. 0.25 ml plasma samples containing ketoconazole were mixed with 15 µg of the IS. After adding 0.25 ml acetonitrile, the mixture was vortexed for two minutes and then centrifuged for 10 minutes at 16000 rpm at room temperature. The clear supernatant was transferred into an auto-sampler vial, and 100 µl was injected into the HPLC system with a run time of 10 min. The compounds of interest were efficiently separated on 4.6 x 150 mm, Symmetry Shield TMRP18 5-µm steel column, using a Guard Pak pre-column module with    Radial-Pak C18 5-µm insert, and detected using Waters 2475 multi λ fluorescence detector with an the excitation and emission wavelengths set at 260 and 375 nm, respectively. The mobile phase consisted of 0.02 M potassium dihydrogen phosphate (pH = 6.0, adjusted with 0.1 M sodium hydroxide) and acetonitrile (40:60, v:v), and was delivered at a flow rate of 1.0 ml/min. No interference from blank plasma or commonly used drugs was observed; and the detection limit of ketoconazole was 0.1 µg/ml. The relationship between ketoconazole concentration in plasma and peak area ratio of ketoconazole /IS was linear (r2 ≥ 0.9979) in the range of 0.1– 20 µg/ml. Intra- and inter-day coefficients of variation (CV) were ≤ 8.1%  and  ≤ 9.7%, respectively, with corresponding biases of ≤ -13% and ≤ 0.9%, respectively. Mean extraction recovery of ketoconazole and IS were ≥ 85% and 92%, respectively. Using the method, ketoconazole was found to be stable for 48 hrs at -20°C (≥ 95%) in processed samples and for 8 weeks at -20°C (100%) in unprocessed samples. Key words: Ketoconazole, Itraconazole, Human plasma, HPL

This research manuscript describes simple, sensitive, accurate, precise and repeatable reverse phase high performance liquid chromatography method for the estimation of Ketoconazole in tablet dosage form. The sample was analyzed by reverse phase ACE 5 C18 column (150 mm × 4.6 mm i.d, 5 μm particle size) as stationary phase; methanol: acidic water  [91:9, v/v] pH 3.0 as a mobile phase at a flow rate of 0.85 ml/min. Quantification was achieved with Photo Diode Array detector at 243 nm. The retention time for Ketoconazole was found to be 2.764 min. The linearity was obtained in the concentration range of 5-40 µg/ml for Ketoconazole. The method was successfully applied to tablet because no chromatographic interferences from formulation excipients were found. The method retained its accuracy and precision when the standard addition technique was applied.