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Cefpodoxime proxetil (CPDX-PR) is an oral cephalosporin antibiotic with poor aqueous solubility and bioavailability. Effect of -cyclodextrin on aqueous solubility and dissolution rate of cefpodoxime proxetil was evaluated by the formation of solid inclusion complexes in 1:2 molar ratio of drug: cyclodextrin. Phase solubility study was carried out whereby a typical B's type curve was obtained thus, indicating a 1:2 stoichiometric ratio for optimum complex formation. Solid inclusion complexes in 1:2 molar ratios were prepared by using methods such as physical mixture, solvent evaporation and freeze drying. Prepared complexes were characterized by fourier transform infrared spectroscopy (FT-IR) differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD) and scanning electron microscopy (SEM). Results of in vitro studies appraised of an increased solubility and dissolution rate of cefpodoxime proxetil on complexation with -cyclodextrin (P < 0.05) as compared to CPDX-PR alone. Amongst the complexes prepared by different methods, the complex prepared by freeze drying showed the highest dissolution rate (P< 0.01). The in vitro antimicrobial activity of cefpodoxime proxetil and its freeze dried complex (1:2) was studied against both antibiotic-susceptible and antibiotic-resistant clinical isolates of Neisseria gonorrhoeae. The freeze dried complex (1:2) inhibited all penicillin-susceptible strains and penicillinase-producing strains at 0.015 μg/ml concentration. Chromosomally resistant strains which were not responsive to penicillin were inhibited by the complex at 0.125 μg/ml concentration. The study revealed that complexation of cefpodoxime proxetil with -cyclodextrin effectively enhanced the aqueous solubility and in vitro antibacterial activity.

Coronavirus disease 2019 (COVID-19) has become a major challenge affecting almost every corner of the world, with more than five million deaths worldwide. Despite several efforts, no drug or vaccine has shown the potential to check the ever-mutating SARS-COV-2. The emergence of novel variants is a major concern increasing the need for the discovery of novel therapeutics for the management of this pandemic. Out of several potential drug targets such as S protein, human ACE2, TMPRSS2 (transmembrane protease serine 2), 3CLpro, RdRp, and PLpro (papain-like protease), RNA-dependent RNA polymerase (RdRP) is a vital enzyme for viral RNA replication in the mammalian host cell and is one of the legitimate targets for the development of therapeutics against this disease. In this study, we have performed structure-based virtual screening to identify potential hit compounds against RdRp using molecular docking of a commercially available small molecule library of structurally diverse and drug-like molecules. Since non-optimal ADME properties create hurdles in the clinical development of drugs, we performed detailed in silico ADMET prediction to facilitate the selection of compounds for further studies. The results from the ADMET study indicated that most of the hit compounds had optimal properties. Moreover, to explore the conformational dynamics of protein–ligand interaction, we have performed an atomistic molecular dynamics simulation which indicated a stable interaction throughout the simulation period. We believe that the current findings may assist in the discovery of drug candidates against SARS-CoV-2.

Objective: The main aim of the present study was to develop and validate a simple, precise and accurate Reversed-Phase HPLC-PDA method for the quantitative determination of Chrysin in solid lipid nanoparticles (SLNs). Methods: The RP-HPLC-PDA system equipped with a C-18 reversed-phase column (250 × 4.6 mm, particle size 5 μm) was employed in the present study. HPLC grade methanol and water in 85:15 (v/v) ratio was selected as the mobile phase at flow rate of 1 ml/min under an ambient column oven temperature. The detection wavelength was kept at 268 nm. Validation of developed method was performed according to the ICH guidelines. Results: The developed reversed-phase HPLC-PDA method was found to be linear in the concentration range of 0.2-10 µg/ml with a correlation coefficient of 0.999. The method was also observed to be precise with % relative standard deviation (RSD) below 2%. The limit of detection and limit of quantification of this method were found to be 0.05µg/ml and 0.14µg/ml, respectively. The percent recovery of the developed method was estimated to more than 99%. Conclusion: The developed HPLC method can be utilized for the determination of Chrysin with a high degree of accuracy, precision, robustness, specificity in solid lipid nanoparticles in the presence of excipients.

A major percentage of the new chemical entities are reported to have poor aqueous solubility. Several antihypertensive drugs used clinically have either low solubility or high hepatic metabolism, thereby presenting low bioavailability (BA) and high pharmacokinetic variability. Improving the aqueous solubility of drug molecules would assist in overcoming the variability, and several approaches for improving solubility have been reported. Solid dispersion (SD) is known as a potential technique to conquer the problem of poor aqueous solubility and low BA. Drug solubility is improved by increasing the wetting property of drugs. This review is focused on discussing various approaches to improve solubility, classification, and different approaches used for formulation of SDs, along with special emphasis on the application of the SD approach for improving solubility and eventually enhancing dissolution and increasing the BA of antihypertensive drugs. The review leads to the conclusion that the use of more than one polymeric carrier for formulating SDs might help in overcoming storage and stability issues and in increasing the commercial viability and success of SDs.

need to see that the level of NPAs is kept down. In spite of many fold developments, adverse development of accumulation of NPAs to place over the period, several tools / methods of managing NPAs were tried such as Lok Adalats, Debt Recovery Tribunals, SARFAESI Act, Corporate Debt Restructuring and many more. Cleaning up of the Bank Balance Sheets is essential and urgent to boost growth in coming years, independent loan review mechanism and sale of unproductive assets are some of the ways to arrest the rising NPAs. Since the quality of advances in India particularly the corporate stressed advances are quite poor and huge in comparison to other Asian Pacific emerging countries, if the NPAs are not managed properly there is every chance that the capital and reserves of Banks shall not to able to meet the losses arising on account of write off of Bad Loans.

Background and Objective: The present study describes the UPLC-MS/MS method validation for the analysis of ornidazole in solid dispersion. Methods: The proposed UPLC-MS/MS method utilizes BEH Shield RP18 column (2.1 mm 100 mm, 1.7 μm) with a gradient programmed mobile phase composed of water and acetonitrile at a flow rate of 0.4 mL/min which varies with time program. Ornidazole was detected by UPLC-MS/MS with three proton adducts at m/z 82.04, 128.05 as daughter ions and 220.03 as a parent ion in Multiple Reaction Monitoring (MRM) operated in positive mode. Results: Adducts at m/z 128.05 was found to be the most stable and showed higher intensity was selected for quantification of ornidaozle in solid dispersion. In the method, validation linearity was determined at concentration range of 10-100ng/mL and a correlation coefficient was found (r2) ≥0.9994. The limit of detection and limit of quantification were found to be 1.5 and 4 ng/mL, respectively. Inter and Intra-day precision was found within 0.33 and 0.11% and accuracy within 100.08% and 100.04%. Conclusion: A sensitive and selective UPLC-MS/MS method had been validated for the analysis of ornidazole in solid dispersion. The proposed method of analysis of ornidazole in solid dispersion can be used in quality control laboratories.