Posted by admin on Dec 1, 2012 in |
Tadalafil (TD), a PDE-5 inhibitor, belongs to BCS class II. It is poorly soluble in water and requires enhancement in solubility and dissolution rate for increasing its oral bioavailability. In the present investigation, solid dispersed systems of tadalafil with poloxamer188 and sodium starch glycolate were prepared using solvent evaporation technique. The dissolution rate of the drug and poloxamer188 based solid dispersion was significantly higher than the sodium starch glycolate (SSG) based preparations and pure drug which reaches closer to the dissolution profile of marketed product. This was due to an increase in surface area of drug available for dissolution. Characterization of binary systems with FTIR studies demonstrated the presence of strong hydrogen bonding interactions, a significant decrease in crystallinity and the possibility of existence of amorphous entities of the drug. In the binary systems tested, 1:0.5 proportion of Tadalafil/poloxamer188 showed rapid dissolution of tadalafil (DE30 56.68 %). In the binary systems, tested (1:0.5) proportion of tadalafil/poloxamer188 showed rapid dissolution of tadalafil. In contrast, higher proportion of polaxmer188 (1:1) offered...
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Posted by admin on Dec 1, 2012 in |
Quinazolinone is a heterocyclic chemical compound. There are two structural isomers, 2-quinazolinone and 4-quinazolinone, with the 4-isomer being the more common. The present survey aims to achieve the synthesis of quinazolinones and their derivatives of specific pharmacological properties. Various novel classes of structurally different quinazolinones have been designed and synthesized depicting potential interventions such as antibacterial, antifungal, antiviral, anticonvulsant, CNS depressant, anti-inflammatory, antihistaminic, anticancer and so on. At present some novel quinazolinone derivatives are synthesized and characterized by IR, H1 NMR, MASS Spectral...
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Posted by admin on Dec 1, 2012 in |
Background: Yerba mate (Ilex paraguariensis) is known to possess many biological activities against diverse tissues among others alimentary tract wall. Correspondence to Author: Dr. Roman Paduch Department of Virology and Immunology, Institute of Microbiology and Biotechnology, Maria Curie-Skłodowska University, Akademicka 19, 20-033 Lublin, Poland E-mail: rpaduch@poczta.umcs.lublin.pl Aim: The aims of the study were to evaluate potential toxic effects of water and ethanol (by Soxhlet extraction and shaking extraction methods) and free radical scavenging properties of Yerba mate extracts on human normal colonic epithelial and human colon carcinoma cells. Materials and methods: NR uptake, MTT, (DPPH.) reduction and ELISA tests were used to test toxicity, anti-proliferative activity, ROS reduction and cytokine level, respectively. Results: Depending on kind of extract, their concentration, kind of cells they influenced on and method of analysis, different toxic and stimulatory of cells viability effects were observed. Yerba mate extracts demonstrated strong free radical scavenging activity. The plant extracts also expressed immunomodulatory effects influencing on IL-6 production by normal and tumor cells. Ilex paraguariensis extracts stimulated...
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Posted by admin on Dec 1, 2012 in |
A novel, safe and sensitive method of spectrophotometric estimation in UV-region has been developed for the assay of paracetamol in its tablet formulation. The method have been developed and validated for the assay of paracetamol using Methanol and water as diluents. Which does not shows any interference in spectrophotometric estimations. All the parameters of the analysis were chosen according to ICH [Q2 (R1)] guideline and validated statistically using RSD and %RSD along with neat chromate...
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Posted by admin on Dec 1, 2012 in |
Cyclodextrin complexes of etoricoxib (poorly water soluble COX-2 inhibitor) were prepared with the β-CD and HPβ-CD by different techniques (physical mixture, kneading and co-evaporation methods) at 1:1 and 1:2 molar ratios. Characterization of the complexes was done in solution by phase solubility analysis and in solid state using FTIR. The stoichiometry and stability constants of ECB-β-CD (1:1-200.4 M-1) and ECB-HPβ-CD (1:1-166.94 M-1) complexes were calculated by phase solubility method. Remarkable improvement in in-vitro drug release profiles in distilled water was observed with all complexes, especially with those prepared by kneading method than with physical and co-evaporation methods. HPβ-CD gave highest enhancement in the dissolution rate of ECB. Thus, it is concluded that stable and dissolution improved CD complexes can be prepared for etoricoxib with β-CD and...
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