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Sinha S.,Jubilant Organosys | Ali M.,Hamdard University | Baboota S.,Hamdard University | Ahuja A.,Hamdard University | And 2 more authors.
AAPS PharmSciTech | Year: 2010

Ritonavir is an antiretroviral drug characterized by low solubility and high permeability which corresponds to BCS class II drug. The purpose of the study was to develop solid dispersion by different methods and investigate them for in vitro and in vivo performance for enhancing dissolution and bioavailability, respectively. Since the drug possesses food-related absorption, the effect of biorelevant media (FaSSIF and FeSSIF state) on dissolution behavior was also studied. The solid dispersion was prepared using Gelucire as carrier in 1:4 ratio by different methods and were characterized for differential scanning calorimetry (DSC), X-ray diffractometry, scanning electron microscopy, and FT-IR. Oral bioavailability of 10 mg of ritonavir in solid dispersion prepared by solvent evaporation (SE1) and melt method (MM1) was compared with pure drug after oral administration of solid dispersion and pure drug to Albino Wistar rats of either sex. The results suggested formation of eutectic solid dispersion. In vitro dissolution studies was performed in 0.1 N HCl and biorelevant media showed enhanced dissolution rate as compared to pure drug in both FeSSIF media and 0.1 N HCl. The apparent rate of absorption of ritonavir from SE1 (Cmax 20221.37 ng/ml, tmax 0.5 h) was higher than that of MM1 (Cmax 2,462.2, tmax 1h) and pure drug (Cmax 1,354.8 ng/ml, tmax 0.5 h). On the basis of the result obtained, it was concluded that solid dispersion is a good approach to enhance solubility and bioavailability of poorly water-soluble ritonavir. © 2010 American Association of Pharmaceutical Scientists.

Virsdoia V.,Dishman Pharmaceuticals and Chemicals Ltd. | Manvar A.,Jubilant Organosys | Desai B.,Beckman Coulter Inc. | Parecha A.,ATRI Pharma. Pvt. Ltd | And 7 more authors.
Chemical Biology and Drug Design | Year: 2010

The resurgence of tuberculosis and the emergence of multidrug-resistant strains of Mycobacteria necessitate the search for new classes of antimycobacterial agents. We have synthesized a small library of 50 analogues of 4-(arylamino)coumarins with various aromatic amines at the C 4-position of the coumarin scaffold. The compounds were evaluated for antimycobacterial activity against Mycobacterium tuberculosis H 37Rv with rifampicin as the standard. Of the molecules synthesized, compound 9 was found to be most potent with a minimum inhibitory concentration >6.25 lg/mL for 100% inhibition. In an effort to develop new and more effective molecules in this series, the relationship between structure and activity was investigated by comparative molecular field analysis. Various models were generated using comparative molecular field analysis alone and comparative molecular field analysis plus a hydropathy field (HINT). In all, eight models were generated with atom-fit and field-fit alignment strategies. The comparative molecular field analysis models (Models 3a and 4a) based on field-fit alignment were the best with statistically good correlation coefficients (r 2) and cross-validated q 2. The values of r 2 pred for the validation set were 0.469 and 0.516. Based on the comparative molecular field analysis contours, some insights into the structure-activity relationship of the compounds could be gained. © 2010 John Wiley & Sons A/S.

Saini G.,Guru Gobind Singh Indraprastha University | Narula A.K.,Guru Gobind Singh Indraprastha University | Choudhary V.,Indian Institute of Technology Delhi | Bhardwaj R.,Jubilant Organosys
Journal of Reinforced Plastics and Composites | Year: 2010

This article evaluates the use of bagasse flour - a waste generated by sugarcane refinery-as a filler in the PVC matrix. The aim of the study is to develop a value-added product from the sugar mills. For this purpose, bagasse powder was obtained after grinding the dried waste from sugar mills having particle sizes of 100-150 μm and <50 μm. In order to evaluate the effect of filler content and alkali treatment of bagasse, several PVC formulations were obtained by dry-mixing PVC compound with filler of varying particle size. The compounds were obtained by blending on a hot roll mill followed by compression molding. The test specimens were punched out from the sheets and the effect of filler content, particle size, and alkali treatment of bagasse powder on the properties of PVC were evaluated. Tensile strength, percent elongation at break, and impact strength of composites decreased whereas stiffness, modulus, and hardness of the composites increased with increasing amount of filler. The particle size had a large effect on the properties of composites, and the filler having particle size <50 μm gave better properties as compared to filler with particle size of 100-150 μm. Some improvement in properties was observed when treated bagasse powder was used as filler. An increase of ĝ̂1/448% in tensile modulus, ∼ 10% in thermal stability, and 14% in impact strength was observed as compared to neat PVC at a filler loading of 30 phr. Morphological characterization was done using a scanning electron microscopy. A uniform dispersion of filler was observed. © 2010 SAGE Publications.

Kumar V.,P.A. College | Kukshal A.,Jubilant Organosys | Rathee P.,P.A. College | Rathee S.,P.A. College | Chaudhary H.,Jamia Hamdard University
Research Journal of Pharmaceutical, Biological and Chemical Sciences | Year: 2010

A number of new 5-substituted-1H-indole-2,3-dione-3-N-(4'-substitutedphenyl) thiosemicarbazone (4a-o) have been synthesized from istain (Indole-2,3-dione) and screened for antibacterial activity.

Kumar A.,Hamdard University | Sinha S.,Jubilant Organosys | Agarwal S.P.,Hamdard University | Ali J.,Hamdard University | And 2 more authors.
Journal of Food and Drug Analysis | Year: 2010

A stability-indicating high performance thin layer chromatographic (HPTLC) method for the densitometric analysis of nadifloxacin in microemulsions was developed and validated according to the guidelines of the International Conference on Harmonization (ICH). The compact spot for nadifloxacin was found at an Rf value of 0.39±0.02 at an absorption wavelength of 288 nm using a mobile phase consisting of chloroform : methanol : formic acid (7.5 : 2.0 : 0.5 v/v). The linear regression data for the calibration plots (r 2= 0.9981) was found with respect to peak area in the concentration range of 50-600 ng/spot. The limit of detection (LOD) and limit of quantification (LOQ) were 9.4 and 20.5 ng respectively. The drug was subjected to acid and alkaline hydrolysis, oxidation, photo degradation and dry heat treatment. The peaks of degradation products were well-resolved from the peak of the standard drug with significantly different Rf values. Statistical analysis revealed that the developed HPTLC method is reproducible, selective and accurate for the determination of nadifloxacin in its formulations. The method can effectively separate the drug from its degradation products and be used for stability-indicating assay.

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