Typhoid fever (TF) is an acute systemic infection caused by Salmonella Typhi, Salmonella Para Typhi A and Salmonella Para Typhi B. It is transmitted by the fecal oral route mainly via contaminated food and water. The developing countries have high rate of morbidity and mortality due to Typhoid fever, epidemics take place in developed world also. There are increased incidences of multi drug resistant in S. typhi strains that has further complicated its management and only a few antibiotics are now effective in treatment of typhoid. We report that the aqueous extracts of fruit peel Citrus sinensis (L.) confer anti typhoid activity against Salmonella Typhi, Salmonella Para Typhi A and Salmonella Para Typhi B respectively on comparison with ciprofloxacin.
Key words: Typhoid fever, Salmonella Typhi, Salmonella Para Typhi A , Salmonella Para Typhi B, anti typhoid activity, Citrus sinensis.
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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH AND DEVELOPMENT
The objective of the study is to evaluate the individual main and combined (or interaction) effects of ß cyclodextrin (ßCD) and surfactant (Poloxamer 407) on the solubility and dissolution rate of three BCS class II drugs namely (i) etoricoxib, (ii) nimesulide and (iii) valsartan in a series of 22 factorial experiments. In each case the aqueous solubility of the drug was markedly enhanced by ßCD and Poloxamer 407 alone and in combination. The individual and combined effects of ßCD and Poloxamer 407 in enhancing the solubility of BCS class II drug were highly significant (P < 0.01) in each case. The solubility of etoricoxib was markedly enhanced by ßCD (2.04 fold) and Poloxamer 407 (2.57 fold) individually and combinedly by 1.94 fold. The solubility of nimesulide was markedly enhanced by ßCD (4.12 fold) and Poloxamer 407 (5.37 fold) individually and combinedly by 5.44 fold. The solubility of valsartan was markedly enhanced by ßCD (1.23 fold) and Poloxamer 407 (20.58 fold) individually and combinedly by 9.87 fold. Poloxamer 407 alone gave higher enhancement in the solubility of the three drugs studied.
Solid inclusion complexes of Drug- ßCD were prepared with and without Poloxamer 407 by kneading method as per 22-factorial design in each case. ANOVA indicated that the individual main effects of ßCD and Poloxamer 407 and their combined effects in enhancing the dissolution rate (K1) were highly significant (P < 0.01) with all the three drugs studied. Combination of ßCD and Poloxamer 407 gave markedly higher enhancement in the dissolution rate of (i) etoricoxib and (ii) nimesulide than is possible with them alone. In the case of Valsartan, Poloxamer 407 alone gave higher enhancement in the dissolution rate than ßCD alone and combination of ßCD and Poloxamer 407.
Hence Poloxamer 407 alone is recommended to enhance the aqueous solubility of the three BCS class II drugs studied. A combination of ßCD and Poloxamer 407 is recommended to enhance the dissolution rate of these BCS class II drugs.
Key words: Etoricoxib, Nimesulide, Valsartan, ß Cyclodextrin, Poloxamer 407, Solubility, Dissolution rate, Factorial Study
June 2011 Issue
June - 2011 / Volume - 3/Issue - 04
( Total Articles =30 )
Article No 18
June - 2011 / Volume - 3 / Issue - 04 / / Article No - 18 / Research Article
FACTORIAL STUDIES ON THE EFFECTS OF ß- CYCLODEXTRIN AND POLOXAMER 407 ON THE SOLUBILITY AND DISSOLUTION RATE OF BCS CLASS II DRUGS
Dr. K.P.R. Chowdary*1,
K. Surya Prakasa Rao1
1University College of Pharmaceutical Sciences,
Andhra University, Visakhapatnam - 530 003
Dr. K. P.R. Chawdary