Posted by admin on Jan 31, 2021 in |
Present study was planned to prepare a dorzolamide hydrochloride in-situ gel by using Carbopol 974 and HPMC K4M to reduce dosing frequency by increasing residence time as well as sustained drug release from the formulation in cul-de-sac. The concentration of both polymers was optimized by using 32 factorial designs with correlating its impact on dependent variables as cumulative in-vitro drug diffusion at the end of 8 h and viscosity at pH 7.4. Polymer composite showed a quadratic model for drug diffusion as well as for viscosity. Comparative in-vitro drug release study by using type II dissolution apparatus confirms sustained drug release characteristics of optimized formulation which showed 89.41% drug release at the end of 8 h as compared to a marketed formulation which showed complete drug release at the end of 3 h. Ex-vivo transcorneal permeability study ensured permeability of drug through the cornea. Histological study on goat eye cornea proved non-irritation potential of the prepared formulation. A comparative in-vivo study between optimized formulation and marketed formulation on normotensive...
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Posted by admin on Jan 31, 2021 in |
Introduction: Disorders of hyperpigmentation are difficult to treat, particularly in dark skin individuals. There is a dramatic enhancement of skin permeability of phytoconstituents due to their complexation with phospholipids. Complexation leads to better permeation through the skin, which is otherwise not possible. Research work focused on the development and evaluation of phos-phatidylcholine complexes of arbutin, having the issue of poor skin permeability as skin whitening agents. Materials and Methods: Arbutin, phosphatidylcholine, and petroleum ether have been used for the development of complexes. Authentication of arbutin has been performed by Fourier Transform Infrared study. UV–visible spectrophotometric method has been developed for estimation of arbutin followed by the development of complexes by rotary flask evaporation technique, preliminary trials for selection of dependent and independent variables, optimization of complexes by Box- Behnken reduced surface response design, evaluation of optimized batch by percentage entrapment efficiency, particle size, zeta potential, and in-vitro drug release study by Franz diffusion cell. Result and Discussion: Arbutin sample FTIR data and standard FTIR data are matched. Final polynomial...
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Posted by admin on Jan 31, 2021 in |
The present work evaluates the impact of alterable manufacturing and formulation factors on the physicomechanical properties of Acetaminophen (APAP); a poorly compressible Active Pharmaceutical Ingredient (API). By varying the amount of APAP and particle size of Microcrystalline Cellulose (MCC), six different formulations were prepared. These formulations were compressed into tablets at different compression pressures and speeds. The porosity of the tablets was evaluated through “out-of-die” Heckel analysis. Furthermore, the qualitative and quantitative relationships of (i) Percentage of APAP, (ii) Compression pressures, (iii) Compression speeds, and (iv) Particle size of MCC with tablet porosity were evaluated by principle component analysis (PCA) and principle component regression (PCR). Heckel analysis revealed that increasing the ratio of APAP to MCC in the formulation adds its compressibility when the MCC particle size is similar to that of APAP. While, using large MCC particle size increases the compressibility due to fragmentation of particles, using MCC of small particle size increases the compressibility to a higher extend. The PCA indicated that the percentage of APAP, compression...
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Posted by admin on Jan 31, 2021 in |
Gentisic acid (2, 5-dihydroxybenzoic acid) is a diphenolic compound, present abundantly in natural sources. It possesses several pharmacological activities such as nephroprotective, hepatoprotective, neuroprotective, etc. However, the available literature on oral absorption of gentisic acid is scarce. Thus, the aim of the present study was to determine the pharmacokinetic parameters and bioavailability of gentisic acid. A single dose in-vivo pharmacokinetic study was conducted in rats. Gentisic acid was administered at 50 mg/kg, either orally or by intravenous route. Blood samples were withdrawn at designated time intervals (0.083, 0.25, 0.5, 1, 2, 4, 8, 12, and 24 h post-dose), and plasma was separated. A method for the evaluation of gentisic acid in the plasma was developed and validated. The plasma levels of gentisic acid were determined by HPLC using the validated method. The Cmax for oral administration was 312 µg/mL, and Tmax was at 0.083 h. The plasma exposure AUClast values for oral and i.v route of administration were comparable (Oral: 765 h*µg/mL; I.V.: 770 h*µg/mL), indicating similar bioavailability. The...
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Posted by admin on Jan 31, 2021 in |
Drug resistance mutations M184V and M184I are associated with lamivudine. Y181C and H221Y drug resistance mutations are associated with nevirapine and efavirenz and G190R and M230I drug resistance mutations are associated with efavirenz in the reverse transcriptase gene of HIV-1. In the present study, we attempted to identify the drug resistance mutations and interacting amino acids in the reverse transcriptase gene of HIV-1 through a molecular docking approach. Molecular docking of first-line antiretroviral drugs like lamivudine, nevirapine, and efavirenz with wild and mutant type structures was performed using MTi auto dock to compare the binding behaviour of drugs with amino acids of the reverse transcriptase gene. The receptor structure preparation was performed by the University of California, San Francisco chimera (UCSF Chimera). The Ligplot program was used to plot the 2D interaction diagrams of protein-ligand complexes. The 3D models of the mutant-drugs were generated using PyMOL (PyMOL molecular graphics system). The clear bond interactions were visualized with Discovery Studio 3.5 (BIOVIA, USA). Thus, these findings suggest that mutations in...
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