STABILITY INDICATING RP-HPLC-PDA METHOD FOR DETERMINATION OF ABIRATERONE ACETATE AND CHARACTERIZATION OF ITS BASE CATALYZED DEGRADATION PRODUCT BY LC-MS

Objective: The present work describes stability indicating (SI) RP-HPLC-PDA method for determination of abiraterone acetate (ABA) and characterization of its base catalyzed degradation product by LC-MS.Methods: The separation was achieved by using column Kromasil C18 (250 mm × 4.6 mm, 4.0 µ) using acetonitrile (ACN): ammonium acetate buffer 10 mM, pH adjusted to 3.5 with acetic acid (AA) in the ratio of 10:90 % v/v as eluent. The Mobile phase flow rate was 0.6 ml/min and data integration was achieved at 235 nm.Results: The retention time of ABA was 5.4±0.01 min. Linearity was found to be in the range of 5–30 μg/ml. The limit of detection and quantitation were 0.25 μg/ml and 0.75 μg/ml respectively, and percentage recovery of ABA was found to be 99.52 to 100.13 %. Mass spectral data of base degraded product of ABA shows a prominent molecular ion peak at m/z-391.5. Major fragmentation leads to formation of 10–Methyl 2,3,4,7,8,9,10,11,12,13,14,15-dodecanhydro-1H cyclopenta (α)phenanthren-3-ol as a degradant (D2) at m/z-257.81, due to corresponding loss of C8H12ON. All the analytical validation parameters were determined and found in the limit as per ICH guidelines.Conclusion: The results of the various validation studies showed that the LC method is fast, specific, accurate, reproducible, possessed significant linearity and precision. The drug was found to be stable under all the stress conditions except basic stress. Thus developed method reported first time is novel with a very short run time of 6 min.Â

Synthesis and Biological Assessment of Carbazole Linked Pyrazole Schiff bases and Diarylthiourea Derivatives

In this study, (E)-9-ethyl-N-((1,3-diphenyl-1H-pyrazol-4-ylmethylene)-9H-carbazol-3-amine (3a–f) and 1-(9-ethyl-9H-carbazol-6-yl)-3-phenylthiourea (5a–f) derivatives were synthesized and their in vitro antimicrobial and antimalarial activities were evaluated. The structures of the synthesized compounds were elucidated and confirmed by using IR, 1H NMR, 13C NMR, and mass spectra. This work is licensed under a Creative Commons Attribution 4.0 International License

FORMULATION AND EVALUATION OF RAPIDLY DIS INTEGRATING FILM OF AMLODIPINE BES YLATE

Fast-dissolving drug-delivery systems were first developed in the late 1970s as an alternative to tablets, capsules, and syrups. Fast dissolving oral films (FDOFs) are the most advanced form of  oral solid dosage form due to more flexibility and comfort. It improve the efficacy of APIs by dissolving within minute in oral cavity after the contact with less saliva as compared to fast dissolving tablets, without chewing and no need of water for admin istration. The FDOFs place as an alternative in the market due to the consumer’s preference for a fast dissolving product over conventional tablets / capsules. The oral thin-film technology is still in the beginning stages and has bright future ahead because it fulfils all the need of patients. Eventually, film formulations having drug/s will be commercially launched using the oral film technology. In the present study fast dissolving film of  Amlodipine Besylate was prepared using sodium alginate as film forming polymer. To decrease the disintegration time of formulationssodium starch glycolate was used as disintegrating agent. A full 32factorial design was applied using concentration of polymer and disintegrant as independent variable and disintegration time and % cumulative drug release as dependent variable. Response surface curves were plotted. Batch F6 was found to be the optimized batch as its disintegration was completed within the minimum time as compared to all other batches. The formulation (F6) was also showing sufficient drug release after 6 min. All the nine formulation was showing approximately 70-85% drug release after 6 mi

Enantioselective Synthesis of C-O Axially Chiral Diaryl Ethers via NHC-Catalyzed Atroposelective Desymmetrization

Axially chiral diaryl ethers, a distinguished class of atropisomers possessing unique dual C-O axis, hold immense potential for diverse research domains. In contrast to the catalytic enantioselective synthesis of conventional single axis bearing atropisomers, the atroposelective synthesis of axially chiral ethers containing flexible C-O axis remains a significant challenge. Herein, we demonstrate the first N-heterocyclic carbene (NHC)-catalyzed synthesis of axially chiral diaryl ethers via atroposelective esterification of dialdehyde-containing diaryl ethers. Mechanistically, the reaction proceeds via NHC-catalyzed desymmetrization strategy to afford the corresponding axially chiral diaryl ether atropisomers in good yields and high enantioselectivities under mild conditions. The derivatization of the synthesized product expands the utility of present strategy via access to a library of C-O axially chiral compounds. The temperature dependency and preliminary investigations on the racemization barrier of C-O bonds are also presented

Veterinary World, EISSN: 2231-0916 Available at www.veterinaryworld.org/Vol.7/Jan-2014/2.pdf RESEARCH ARTICLE Open Access

Studies on acute toxicity of synthetic pyrethroid λ-cyhalothrin on freshwater fish Labeo rohit