Posted by admin on Aug 31, 2019 in |
Benzofuranone is a bicyclic ring where a benzene ring fused with a furanone. Synthetic chemistry plays a major in developing a series of potent anti-cancer agents. Bromophenyl acetonitrile was prepared from phenyl acetonitrile by bromination at an alpha position which yielded bromophenyl acetonitrile which was a lachrymator compound. Benzofuranone was synthesized by reacting benzene diols and triols with bromo phenyl acetonitrile yielded an imine derivative are converted to a ketone with treatment with hydrochloric acid then cyclized with sodium acetate. The compounds identity and purity are confirmed by spectral and analytical methods. Benzofuranone derivatives are screened anti-neoplastic activity was performed against human skin cancer cell line G361 at micro molecular concentrations. The compounds IA, IB, ID, IE, IF, IIB, IIC, IIIA, IVB, IVF, VA, VC, VD, VE was found to be with potent activity. These compounds exhibited an excellent activity while compared to reference standard doxorubicin at different micromolar concentrations as such of the synthesized...
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Posted by admin on Aug 31, 2019 in |
The concept of quality by design (QbD) justifies the saying that, quality is not an act, it is a habit. This innovative and systematic approach to pharmaceutical development based on scientific principles has been a breakthrough in developing quality products with a high level of reproducibility. The process of QbD is based on risk management which leads to a better understanding of the product and its manufacturing process, resulting in products with required quality, safety, and efficacy. As the quality and reliability requirements of today’s world are constantly increasing, QbD serves as an important tool in outperforming the global competition. This paper comprehensively discusses the concept of pharmaceutical quality by design, elements of QbD; quality target product profile (QTPP), critical quality attributes (CQAs), design space, control strategy, and lifecycle management. Application of QbD across various fields of pharmaceutical development including formulation development, analytical method development, phytopharmaceutical & biopharmaceutical product development are encompassed in the...
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Posted by admin on Aug 31, 2019 in |
The current work defines development of a simple, rapid and precise method based on gas chromatography coupled with Flame Ionization Detector (GC-FID) for the quantitative estimation of diphenhydramine (DPH) present in the marketed formulations following the principles of green analytical chemistry. The analysis was performed using Zebron Phase: ZB-DRUG-1 column with Nitrogen as a carrier gas having a flow rate of 1 ml/min. The injection volume was 1 µL and with the split ratio of 1:10. The retention time of the drug was found to be 4.5 minutes. The developed method was validated according to the ICH guidelines, proving the method to be sensitive towards the analyte with accuracy (mean recovery = 98%), linearity in the range of 2-10 µg/ml (r2 0.993), precision (intraday = 1.118% RSD, interday = 1.16 % RSD), LOD 0.2 µg/ml and LOQ 0.5 µg/ml. The degradation study showed that the drug remains stable in acid, base, neutral, oxidation, and photolytic method. The developed method can be effectively employed for the day to day analysis...
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Posted by admin on Aug 31, 2019 in |
Genotoxicity has fully-grown into a serious question for the cause of several cancers. In this article, we discuss the basics of genotoxicity, the chemicals which cause these genetic damages and also their mechanism of action. The discovery of new drug needs a thorough investigation for its safety and efficacy before their release into the market so, the drug development process and drug attrition, regulatory tests to detect compounds with genotoxic and carcinogenic potential are discussed in the article. And also, a brief discussion about the recent advances in genotoxicity testing, pre-clinical investigations generally to obtain the basic fundamental profile of toxicological and new chemical entities (NCE), the integration of the cytogenetic tests into repeated dose toxicity studies can be used to satisfy the in-vivo cytogenetic data requirement in CFR are explained. Finally, a brief account of the drugs being used in present days, and also some plant products which show antimutagenic effects have been emphasized....
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Posted by admin on Aug 31, 2019 in |
Selecting the best possible design is an uphill task considering a lot of criteria which must be scrutinized while choosing any design out of many alternative design options available. The experimental design is often compared and selected based on alphabetical design optimality criteria, like A, D, G or V. Each of them attempts to summarize any one important characteristic of the selected design. G-optimality criteria favor those experimental designs which are having the smallest maximum prediction variance over the entire region of interest. It does not consider the distribution of the magnitude of the prediction variance throughout the region. Graphical methods like variance dispersion graph and the fraction of design space plots can be used to overcome this drawback. These graphical methods are explored extensively for comparing the quality of prediction throughout the design space. It serves as a useful tool to assess the prediction performance of the design and making a comparison between experimental designs. The fraction of the design space plot provides a comprehensive picture of the...
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