Posted by admin on Jul 31, 2019 in |
Degradation studies are important to know the potentials degradation products and to develop a stability indicating method. Ranolazine active pharmaceutical ingredients subjected to in detailed forced degradation study using several stressing agents (HCl, NaOH, H2O2). Degradation products of Ranolazine under hydrolytic and oxidative stress conditions were identified, and their stabilities were assessed. Three degradation products were formed when the drug was subjected to acid stress and two products were formed in oxidative stress condition. Ranolazine was stable to base hydrolysis. The degradants were separated on a C-8 column employing preparative HPLC using gradient elution. The structures of all the five degradation products (DP-1, DP-2, DP-3, DP-OX1, and DP-OX2) were established by extensive 1D (1H, 13C) and 2D (COSY, HSQC and HMBC) NMR spectroscopic studies and mass spectra. The products were identified as 2-(4-(2-hydroxy-3-(2-hydroxyphenoxy) propyl) piperazine-1-yl) acetic acid (DP-1), 2-(4-(2-hydroxy-3-(2-methoxy phenoxy) propyl) piperazine-1-yl) acetic acid (DP-2), N-(2,6-dimethylphenyl)-2 -(4-(2-hydroxy-3 (2-hydroxyphenoxy) propyl) piperazine-1-yl) acetamide (DP-3), 1-(2-((2,6-dimethylphenyl)amino)-2oxoethyl)-4-(2-hydroxy-3-(2-methoxy phenoxy) propyl) piperazine 1, 4-dioxide (DP-OX1), 4-(2-((2, 6 dimethyl phenyl) amino)-2-oxoethyl)-1-(2-hydroxy-3-(2-methoxy phenoxy) propyl) piperazine 1-oxide (DP-OX2)....
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Posted by admin on Jul 31, 2019 in |
A novel synthesis of N-(2, 4′-dioxo-1, 2-dihydro-3′H-spiro [indole-3, 2′-[1, 3] thiazolidin]-3′-yl)-2 -hydroxybenzamide derivatives were synthesized by cyclization of isatin hydrazones with thioglycolic acid. The synthesized compounds were characterized by spectral data (IR, 1H-NMR, Mass) and evaluated for antibacterial activity against various strains of bacteria at the concentrations of 200 µg/ml. Among the tested compounds X(i) is highly active against E. coli, X(f) is active against B. subtilis, X(h) is active against S. aureus and X(c) is active against S....
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Posted by admin on Jul 31, 2019 in |
Bisphenol-A (BPA), 2,2-bis(4-hydroxyphenyl) propane is an emerging environmental toxicant with endocrine disrupting properties and toxic effects on living organisms. BPA is ubiquitously present in consumer products current in our daily lives. As it is released from consumer products and deposited in the environment, thus creating the potential for human exposure through oral, inhaled, and dermal routes. BPA exposure might be able to cause oxidative damage by disturbing the balance between reactive oxygen species (ROS) and the antioxidant defense system of eukaryotic cells, resulting in the development of oxidative stress-related diseases. From the available information, it can be inferred that a wide variety of BPA intake through any mode results into a generation of reactive oxygen species (ROS), altering the antioxidant balance of eukaryotic cells, induces mitochondrial dysfunction, and affects cell signaling pathways related to oxidative stress. BPA induced oxidative stress might be able to cause sperm damage, mitochondrial dysfunction, and impairment of the structure and function of spermatozoa resulting in male infertility. Here, a review of the current literature...
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Posted by admin on Jul 31, 2019 in |
The scenario of pharmaceutical drug delivery are expeditiously challenging, but conventional pharmaceutical dosage forms are still dominating. Immediate release dosage forms are those wherein ≥85% of labeled amount dissolves within 30 min. Superdisintegrants are used to improve the efficacy of solid dosage forms. The basic approach used in the formulation of the tablet is the use of superdisintegrants like croscarmellose, sodium starch glycolate, and crospovidone, etc. These superdisintegrants provide instantaneous disintegration of the tablet after administration in the stomach. Thus, decreasing the disintegration time which in turn enhances drug dissolution rate. The rapid disintegration may be due to the rapid uptake of water from the medium, swelling, burst effect and thereby promoting bioavailability. Tablets formulations are mostly preferred because of the low cost of manufacture, package, shipment, increased stability. Among various dosage forms used for oral drug delivery, tablets are one of the most successful and marketable drug delivery regimens as it provides several advantages over another form of dosage forms. This article provide an exhaustive account illustrating the...
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Posted by admin on Jul 31, 2019 in |
Garcinia mangostana L. pericarp (GMP) has been known as a traditional medicine in Asian countries. The bioactive from GMP has been recognized to be related to complex phenolic compounds linked with free radical scavenging activity. This research aimed to study the effects of topical formulation types (gel, oil in water cream and water in oil cream) of GMP extract on the in-vitro release and in-vitro shed snake skin penetration. The formulations were evaluated for viscosity and pH. The extent of GMP extracts released and penetrated shed snake skin were evaluated based on stable radical 2, 2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity and expressed by Radical Scavenging activity equivalent GMP Extract concentration (RSGMPE). Mangostin skin penetration was quantified using UV spectrophotometric method. GMP extract exhibited significantly higher DPPH scavenging activity compared to α-mangostin which is known as the major constituent in the GMP extract. RSGMPE released and penetrated through the skin was significantly influenced by the type of formulations. GMP extract loaded gel provided highest RSGMPE amount transported through the skin than...
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