The Experts below are selected from a list of 18 Experts worldwide ranked by ideXlab platform
T. M. Kalyankar - One of the best experts on this subject based on the ideXlab platform.
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SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUG ATORVASTATIN CALCIUM BY SOLID DISPERSION TECHNIQUE USING NATURAL CARRIER
2016Co-Authors: S. J. Wadher, S. S. Mart, T. M. KalyankarAbstract:Atorvastatin calcium (ATC) is an oral Anticholesteremic Agent. ATC belongs to BCS class II drug having high permeability but low aqueous solubility. In order to get beneficial therapeutic effects, its water solubility needs to be increased. In the present study, attempt was made to improve solubility and dissolution rate of ATC by formulating it into solid dispersion using maltose monohydrate as a highly water soluble carrier. Three methods were used for preparing solid dispersion, namely, physical mixture, kneading and solvent evaporation method in 1:1, 1:3 and 1:5 drug-carrier ratios. The FTIR study of ATC, its combination with the carrier, and of the sold dispersion indicated no interaction between drug, carrier and other excipients used. The prepared solid dispersion showed improved solubility and dissolution rate as compared to pure drug. The improvement in solubility may be attributed to the improved wettability of ATC due to uniform dispersion into the carrier. The optimized batch was K2, which was prepared by kneading method in 1:3 ratios. The optimized batch released 99.59 % drug within 60 min and had solubility almost five folds higher than pure ATC. From the solubility values it was clear that kneading method was more suitable than the other two methods used for preparing solid dispersion. The XRD studies revealed that the crystalline nature of ATC was reduced when formulated into solid dispersion. The optimized batc
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Original Research Paper SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUG ATORVASTATIN CALCIUM BY SOLID DISPERSION TECHNIQUE USING NATURAL CARRIER
2014Co-Authors: S. J. Wadher, S. S. Martande, T. M. KalyankarAbstract:Atorvastatin calcium (ATC) is an oral Anticholesteremic Agent. ATC belongs to BCS class II drug having high permeability but low aqueous solubility. In order to get beneficial therapeutic effects, its water solubility needs to be increased. In the present study, attempt was made to improve solubility and dissolution rate of ATC by formulating it into solid dispersion using maltose monohydrate as a highly water soluble carrier. Three methods were used for preparing solid dispersion, namely, physical mixture, kneading and solvent evaporation method in 1:1, 1:3 and 1:5 drug-carrier ratios. The FTIR study of ATC, its combination with the carrier, and of the sold dispersion indicated no interaction between drug, carrier and other excipients used. The prepared solid dispersion showed improved solubility and dissolution rate as compared to pure drug. The improvement in solubility may be attributed to the improved wettability of ATC due to uniform dispersion into the carrier. The optimized batch was K2, which was prepared by kneading method in 1:3 ratios. The optimized batch released 99.59 % drug within 60 min and had solubility almost five folds higher than pure ATC. From the solubility values it was clear that kneading method was more suitable than the other two methods used for preparing solid dispersion. The XRD studies revealed that the crystalline nature of ATC was reduced when formulated into solid dispersion. The optimized batch of solid dispersion was chosen for formulating immediate release tablet into three batches by direct compression method by varying the concentration of superdisintegrant, crosscarmellose sodium. Tablet prepared with 20% cross carmellose sodium showed 99.41% drug release in 60 min, this drug release was higher compared to the other two batches of tablet prepared.
Stanislav Gobec - One of the best experts on this subject based on the ideXlab platform.
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(Z)-5-(4-Fluorophenyl)pent-4-enoicAcid: A Precursor for Convenient and Efficient Synthesisof the Antihypercholesterolemia Agent Ezetimibe
Synthesis, 2010Co-Authors: Matej Sova, Janez Mravljak, Andreja Kovač, Slavko Pečar, Zdenko Časar, Stanislav GobecAbstract:A convenient and efficient total synthesis of ezetimibe, an intestinal cholesterol absorption inhibitor and useful Anticholesteremic Agent, is described. Based on (Z)-5-(4-fluorophenyl)pent-4-enoic acid as a starting compound, and taking the synthesis through further Z-configured intermediates, the total yield is remarkably increased, compared with the use of the corresponding E-configured starting substances or intermediates.
S. J. Wadher - One of the best experts on this subject based on the ideXlab platform.
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SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUG ATORVASTATIN CALCIUM BY SOLID DISPERSION TECHNIQUE USING NATURAL CARRIER
2016Co-Authors: S. J. Wadher, S. S. Mart, T. M. KalyankarAbstract:Atorvastatin calcium (ATC) is an oral Anticholesteremic Agent. ATC belongs to BCS class II drug having high permeability but low aqueous solubility. In order to get beneficial therapeutic effects, its water solubility needs to be increased. In the present study, attempt was made to improve solubility and dissolution rate of ATC by formulating it into solid dispersion using maltose monohydrate as a highly water soluble carrier. Three methods were used for preparing solid dispersion, namely, physical mixture, kneading and solvent evaporation method in 1:1, 1:3 and 1:5 drug-carrier ratios. The FTIR study of ATC, its combination with the carrier, and of the sold dispersion indicated no interaction between drug, carrier and other excipients used. The prepared solid dispersion showed improved solubility and dissolution rate as compared to pure drug. The improvement in solubility may be attributed to the improved wettability of ATC due to uniform dispersion into the carrier. The optimized batch was K2, which was prepared by kneading method in 1:3 ratios. The optimized batch released 99.59 % drug within 60 min and had solubility almost five folds higher than pure ATC. From the solubility values it was clear that kneading method was more suitable than the other two methods used for preparing solid dispersion. The XRD studies revealed that the crystalline nature of ATC was reduced when formulated into solid dispersion. The optimized batc
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Original Research Paper SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUG ATORVASTATIN CALCIUM BY SOLID DISPERSION TECHNIQUE USING NATURAL CARRIER
2014Co-Authors: S. J. Wadher, S. S. Martande, T. M. KalyankarAbstract:Atorvastatin calcium (ATC) is an oral Anticholesteremic Agent. ATC belongs to BCS class II drug having high permeability but low aqueous solubility. In order to get beneficial therapeutic effects, its water solubility needs to be increased. In the present study, attempt was made to improve solubility and dissolution rate of ATC by formulating it into solid dispersion using maltose monohydrate as a highly water soluble carrier. Three methods were used for preparing solid dispersion, namely, physical mixture, kneading and solvent evaporation method in 1:1, 1:3 and 1:5 drug-carrier ratios. The FTIR study of ATC, its combination with the carrier, and of the sold dispersion indicated no interaction between drug, carrier and other excipients used. The prepared solid dispersion showed improved solubility and dissolution rate as compared to pure drug. The improvement in solubility may be attributed to the improved wettability of ATC due to uniform dispersion into the carrier. The optimized batch was K2, which was prepared by kneading method in 1:3 ratios. The optimized batch released 99.59 % drug within 60 min and had solubility almost five folds higher than pure ATC. From the solubility values it was clear that kneading method was more suitable than the other two methods used for preparing solid dispersion. The XRD studies revealed that the crystalline nature of ATC was reduced when formulated into solid dispersion. The optimized batch of solid dispersion was chosen for formulating immediate release tablet into three batches by direct compression method by varying the concentration of superdisintegrant, crosscarmellose sodium. Tablet prepared with 20% cross carmellose sodium showed 99.41% drug release in 60 min, this drug release was higher compared to the other two batches of tablet prepared.
Matej Sova - One of the best experts on this subject based on the ideXlab platform.
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(Z)-5-(4-Fluorophenyl)pent-4-enoicAcid: A Precursor for Convenient and Efficient Synthesisof the Antihypercholesterolemia Agent Ezetimibe
Synthesis, 2010Co-Authors: Matej Sova, Janez Mravljak, Andreja Kovač, Slavko Pečar, Zdenko Časar, Stanislav GobecAbstract:A convenient and efficient total synthesis of ezetimibe, an intestinal cholesterol absorption inhibitor and useful Anticholesteremic Agent, is described. Based on (Z)-5-(4-fluorophenyl)pent-4-enoic acid as a starting compound, and taking the synthesis through further Z-configured intermediates, the total yield is remarkably increased, compared with the use of the corresponding E-configured starting substances or intermediates.
Janez Mravljak - One of the best experts on this subject based on the ideXlab platform.
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(Z)-5-(4-Fluorophenyl)pent-4-enoicAcid: A Precursor for Convenient and Efficient Synthesisof the Antihypercholesterolemia Agent Ezetimibe
Synthesis, 2010Co-Authors: Matej Sova, Janez Mravljak, Andreja Kovač, Slavko Pečar, Zdenko Časar, Stanislav GobecAbstract:A convenient and efficient total synthesis of ezetimibe, an intestinal cholesterol absorption inhibitor and useful Anticholesteremic Agent, is described. Based on (Z)-5-(4-fluorophenyl)pent-4-enoic acid as a starting compound, and taking the synthesis through further Z-configured intermediates, the total yield is remarkably increased, compared with the use of the corresponding E-configured starting substances or intermediates.