Posted by admin on Nov 30, 2019 in |
The main objective of the study was to formulate tablets of Candesartan cilexetil using the crystal agglomerates for the enhancement in flow properties and solubility. The crystal agglomerates were prepared by polymer enriched bridging liquid (PEBL) technique. The process requires three solvent systems, the good solvent for the drug, the bad solvent and the bridging liquid. The hydrophilic polymer PVP K30 was incorporated in the bridging liquid. The addition of hydrophilic polymer increased the hydrophilicity and wettability of Candesartan cilexetil. The saturation solubility analysis, percentage yield, drug content, micromeritic properties, FTIR, DSC, XRD, SEM were carried out for the evaluation of crystal agglomerates. The tablets were prepared by direct compression using the formulated crystal agglomerates and were subjected to various in-vitro evaluations. The crystal agglomerates prepared by the PEBL technique showed 25 folds enhancement in the solubility. The FTIR analysis revealed the absence of incompatibility. The DSC analysis and XRD pattern showed a reduction in crystallinity. The SEM analysis revealed the porous and sphericity of the agglomerates. The tablets...
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Posted by admin on Nov 30, 2019 in |
The liver is a vital organ of the human body. It is responsible for protecting the body from harmful substances and the maintenance of good health. In last few years, various types of liver disorders, such as drug-induced liver disease, hepatomegaly, fatty liver disease, liver cirrhosis, autoimmune hepatitis, chronic viral hepatitis, autoimmune hepatitis, etc. are become a people’s health problem. Recently numbers of ayurvedic polyherbal and herbomineral formulations are available commercially and physician preferring these formulations for the treatment and management of various liver diseases as modern medical treatment available for liver diseases produces systematic toxicity. In this study a herbomineral formulation “Arka Lavana” was prepared in the laboratory by traditional method using fresh leaves of arka (Calotropis procera) and saindhav lavana and experimentally evaluated against hepatotoxicity induced by dexamethasone and alcohol. It is traditionally used in the treatment of liver and spleen anomalies and ascites etc. The study was evaluated by using 60 mg/kg 90 mg/kg and 120 mg/kg of arka lavana and standard silymarin at a dose...
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Posted by admin on Nov 30, 2019 in |
The geometrical structure and conformational energy stability of vinyl halides CH2=CH–X (X = F, Cl, and Br) were examined by using Density Functional Theory calculations (B3LYP method in combination with 6-311G* basis sets). The values of HOMO-LUMO gap (DE) for vinyl halides (fluoride, chloride and bromide) were 7.68 (eV), 7.10 (eV) and 6.55 (eV) respectively. The calculated geometrical parameters were in good agreement with the previously observed results. Both HOMO-LUMO gap and geometrical parameters were found to account for the stability of the molecules. Electron distribution in HOMO-LUMO Frontier molecular orbitals was investigated to show the charge transfer within the molecules. The atomic charges and molecular electrostatic potential were interpreted together to demonstrate the electrophilic -nucleophilic reactivity. The vibrational frequencies were computed, the comparison between the three halides revealed that vinyl chloride and vinyl bromide have strong C-X stretching vibrations bands, but for vinyl fluoride the bands are weaker, the intensity characterization increasing from F to Br...
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Posted by admin on Nov 30, 2019 in |
Quantitative structure relationship techniques (QSRT) is among the most widely used computational technology for analog-based drug design. A molecular modeling approach using theoretical, computational analysis through chem sketch ACD lab online software was done for determination of probable antimicrobial activity. To develop a pharmacophoric model for inhibition, QSRT parameters PCP, ADME, and toxicity has been used. BCF (Bioconcentration factor), adsorption coefficient, log P, log D values, plasma protein binding, P-gp inhibition, AMES test, hERg inhibition, estrogen receptor, and Lipinski’s type properties have been calculated. From a data set of 11 analogs, it has been concluded that all compounds are non-bio-accumulative, non-endocrine disruptors, non hERg inhibitors, genotoxic and within Lipinski’s criteria. None of the compounds are practically ionizable at various body pH values, and all are zwitterionic compounds. From these data and in-vitro antimicrobial data compounds, 5c and 5f can be exploited for the formulation of bactericide and fungicide with a slight modification in their...
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Posted by admin on Nov 30, 2019 in |
Objective: Physically modified forms of BCS class II drug Nabumetone (NBT) was studied for dissolution in water and pharmacopoeial dissolution media (2%w/v sodium lauryl sulfate in water). Characterization was to identify the suitability of physical processing like heating, cooling, grinding, and milling operations anticipated during commercial manufacturing of dosage forms. Materials and Methods: NBT was subjected to melting followed by quench cooling, grinding, and ball milling to alter the physical characteristics. These were subjected to dissolution studies and compared the values with the raw material. Characterization was done with DSC, FTIR, and PXRD. Results: The quench cooled form of NBT exhibited low dissolution in water compared to NBT raw material and size reduced samples. In water, the cumulative percentage release (CPR) of NBT after 120 min was found to be 4.64 ± 0.04, 4.62 ± 0.09, 4.50 ± 0.07 and 4.06 ± 0.04 for NBT raw material, ground NBT, ball-milled NBT and quench cooled NBT respectively. The CPR of NBT after 120 min in 2% SLS was 86.10 ±...
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