Synthesis of some pyrimidine derivatives which plays an important role in the medicinal chemistry because it possesses promising cytotoxic activity. The synthesized compounds were characterized by 13C, 1H NMR spectral data. Some of the new compounds were evaluated for their potential cytotoxicity against different cancer cell lines on the cells MDAMB (breast cancer) using MTT assays. The pyrimidine derivatives 11a, 11b, 11c and 11e serve as good leads for further studies to develop potent cytotoxic agents.
T. Kala Praveen*, Boyapati Veeranjaneyulu, B. Mamatha, K. Komala Devi, S. Theo Mercy, S. K. Naseema, S. Ramya Sri.
A rapid and precise Reverse Phase High Performance Liquid Chromatographic method has been developed for the validated of Pravastatin, in its pure form as well as in tablet dosage form. Chromatography was carried out on Apollo C18 (4.6×150mm, 5µ) column using a mixture of Methanol: water (65:35 v/v) as the mobile phase at a flow rate of 1.0ml/min, the detection was carried out at 235nm. The retention time of the Pravastatin was 2.6 ±0.02min. The method produce linear responses in the concentration range of 20-100µg/ml of Pravastatin. The method precision for the determination of assay was below 2.0%RSD. The method is useful in the quality control of bulk and pharmaceutical formulations.
S. Deepthi*, CH. Viswa Swetha, D.Pushpanjali, D. Amosu, K. Sowjanya, S. Ramya Sri.
A rapid and precise reverse phase high performance liquid chromatographic method has been developed for the validated of Metadoxine, in its pure form as well as in tablet dosage form. Chromatography was carried out on an ODS C18 (4.6 x 150mm, 5µm) column using a mixture of ACN: Water (65:35% v/v) as the mobile phase at a flow rate of 1.0ml/min, the detection was carried out at 305nm. The retention time of the Metadoxine was 3.155 ±0.02min respectively. The method produce linear responses in the concentration range of 10-50µg/ml of Metadoxine. The method precision for the determination of assay was below 2.0%RSD. The method is useful in the quality control of bulk and pharmaceutical formulations.
A. Venu*, K. Sukanya, P. Sowmya Sri, U. Mariya Dasu, V. Kalyani, S. Ramya Sri.
Suaeda maritima is a mangrove plant belonging to family Amaranthaceae. The present investigation is based on chemical and biological aspects of root bark of the plant. Antimicrobial activity was investigated against Bacillus subtilis, Staphylococcus aureus and Gram –ve bacteria Escherichia coli, Proteus vulgaris and Antifungal activity was investigated against Rhizopus oryzae, Aspergillus niger. The extract has shown less antimicrobial activity and significant antifungal activity. Three chemical compounds were isolated and analyzed using H NMR, Mass and IR spectral studies.
K. Neelaveni*, D. K. M. Lakshmi, D. Venkat Rao, B. Gayatri Devi, B. Swapna.
Carbazole is one of the most important nitrogen containing fused heterocyclic moiety in various chronic as well as other diseases. The main objective of molecular docking is to predict the biological activity of given ligand. This work has been focus on the carbazole moiety as anti-microbial agents, present work emphasize the flexible and extra precision docking simulation on eighteen different Carbazole substituted derivatives in order to evaluate their affinity to bacterial proteins for antibacterial and antifungal activity against DNA gyrase (PDB:1KZN) and Lanosterol 14-α-Demethylase (PDB:1EA1) enzymes respectively by Maestro 11.5 Schrodinger software in order to choose the derivatives which shows good interactions with target protein. All the compound shows best docking results compared to Chloramphenicol and Fluconazole as standard drugs. Compound C16 shows -5.373 docking score as standard Chloramphenicol itself shows -5.110 docking score against DNA Gyrase enzyme for anti-bacterial agents. Whereas in anti-fungal study, the compound Ca1 gives -9.869 docking score as standard Fluconazole gives -7.789 docking score against Lanosterol 14-α-Demethylase enzyme. The results may conclude that Carbazole may serve as useful hits in the development of clinically useful anti-microbial agents.
The aim of this study to find out the perfect dose of Berberine Hydrochloride instreptozotocin (STZ) induced diabetic rats by observation of effect of Berberine Hydrochloride on blood glucose, plasma insulin and hemoglobin. Experimental diabetes was induced in rats by a single dose of intraperitonial injection of streptozotocin (40mg/kg b.w). After the 72 hours, diabetic rats treated with Berberine Hydrochloride at different concentrations (25. 50 and 100mg/kg b.w) for 45 days. Berberine Hydrochloride administration significantly declined the levels of blood glucose, glycolated hemoglobin and renal markers whereas elevated the levels of plasma insulin, hemoglobin and body weight in diabetic rats. 50mg/kg b.w of Berberine Hydrochloride showed the prominent effect compared to other two doses. From these results clearly shows the antidiabetic activity of Berberine Hydrochloride.
N. L. Mahammed*, G. Tulja Rani, B. Sravani, A. Mamatha, D. Rupesh, V. Asha Ranjani, K. Jagadeeshwar.
Oral drug delivery system is most common route of administration which is highly accepted by the patients. The reasons behind such popularity is due to its ease of administration. The main objective of' the study is to provide an existing evidence concerning a possible therapeutic effect of sugar free chewing gum for patients. MCG has more potential uses in pharmaceuticals, over the counter medicines and nutraceuticals. Medicated chewing gum (MCGs) is effective locally as well as systemically in dental caries, smoking cessation, pain, obesity, xerostomia, acidity, allergy, nausea, motion sickness, diabetes, anxiety, dyspepsia, osteoporosis, cough, common cold etc. MCGs are not only used by some special population groups who are having swallowing difficulties such as children and the elderly, but also popular among the young generation. Hence it was proven to be an excellent drug delivery system for self-medication. This review article gives detailed information regarding history, advantages, disadvantages, formulation, manufacturing process, limitation of manufacturing process, factors affecting release of active substance, quality control tests for chewing gum, importance, stability studies, future trends and patent filled on MCGs.
K. Ramya*, A. Ankarao, A. Seetha Devi, S. Meraj Sultana.
The present study was focused on formulating and evaluating Capecitabine containing niosomal formulation for in vitro and in vivo pharmacokinetic behavior. Niosomal formulations (drug loaded) were prepared by using different ratio of surfactant span 60, pluronic P85 and cholesterol (1:1:1, 1:2:1 and 1:3:1) by thin film hydration method. Span 60, pluronic P85 and cholesterol ratio 1: 1:1 containing niosomal formulation CF1 displayed highest entrapment efficiency with desired particle size of 240nm. SEM analyses showed that niosomal formulation was spherical in shape. Formulation CF1 displayed higher percentage of drug release after 24 h as compared to other formulations. CF1 formulation was found to be stable at the end of the study on storage condition. Various pharmacokinetic parameters, namely t max, t1/2, AUC, AUMC, and MRT of niosomal formulation, were found to be 2-fold, 2.5-fold, 1-fold, 5-fold and 2.5-fold marketed drug, respectively. The Cmax of the marketed formulation and developed niosomes were found to be and respectively 65.66 and 68.48ng/ml, respectively. The present study suggested that niosomal formulations provide controlled and prolonged delivery of drug with enhance bioavailability.
A simple, particular, fast and exact reversed phase high performance liquid chromatographic technique for analysis of Empagliflozin in API and tablet dosage form has been developed and validated. Chromatography was performed on a Symmetry C18, 250nm×4.6mm and 5µm column with 0.02M phosphate buffer (PH-3.60 adjusted with Orthophosphoric acid): Acetonitrile in the ratio of 40:60 v/v as mobile phase at a flow rate of 1.0ml/min. UV detection was performed at 225nm. The run time was 6.0min. Empagliflozin was eluted with retention time of 2.790min. The method was validated for accuracy, precision, linearity, specificity and sensitivity in accordance with USP and ICH guidelines. Validation acknowledge the method is particular, fast, accurate, precise, predictable and reproducible. Calibration plots were linear over the concentration range 0-35µgm/ml for Empagliflozin. The developed method showed better reproducibility and recovery with RSD <2%. The percentage recovery is within the limits 98-102% of Empagliflozin. The limit of detection (LOD) and the limit of quantification (LOQ) for Empagliflozin were found to be 0.06 and 0.18 µg/ml respectively. The proposed method was found to be simple, linear, precise, accurate and sensitive and can be used for routine quality control analysis for the estimation of Empagliflozin in API and tablet dosage form.
The aim of the present study was to study the in-vitro anti-inflammatory activity of Azadirachta indica (neem) and Basella Alba (Alba) individual extracts and in combination. The powdered plant materials were subjected to maceration processes. The yield was collected and prepared different concentrations (200µg/ml and 400µg/ml). Human red blood cells membrane stabilization method was used as an in-vitro anti-inflammatory method by using diclofenac as a standard drug. Azadirachta indica showed significant inhibition of haemolysis of 77.03%, 82.96% at the concentrations of 200µg/ml, 400µg/ml respectively. Basella Alba showed significant inhibition of haemolysis of 70.3%, 81.4% at 200µg/ml, 400µg/ml respectively. The combined extracts showed significant inhibition of haemolysis of 85.9%, 90.3% at a concentration of 200µg/ml, 400µg/ml respectively.
K. Jagadeeshwar*, G. Tulja Rani, L. M. V. Ramana, Yasmeen Shaik, M. Mahendar, N. Lal Mahammed.