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THE STUDY OF PHYSICOCHEMICAL PROPERTIES OF SOLID DISPERSIONS OF IBUPROFEN IN THE PRESENCE OF CHITOSAN

100%
Grimling B., Meler J., Szcześniak M., Pluta J., Górniak A.
Progress on Chemistry and Application of Chitin and its Derivatives
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2015
|
vol. 20
64-72
EN
The aim of the present study was to increase the solubility of ibuprofen. Among the methods to increase the solubility selected solid dispersions of the drug with the polymer. Chitosan was used as the polymer. Solid dispersion obtained. Ibuprofen was incorporated into the chitosan type 652 with molar masse chitosan Mη = 429 kDa. Solid dispersions were prepared by using different ratios of ibuprofen and chitosan (1:9. 3:7 and 5:5). Formulations were tested dissolution rate of the ibuprofen. The highest dissolution of ibuprofen, amounting to 12.59%, was observed after 60 minutes from solid dispersion prepared by the evaporation method and 12.18% from physical mixtures with drug-polymer weight ratio 1:9 in the presence chitosan. The solubility of the drug improved more than 60-fold. XRPD analysis indicates the presence of the ibuprofen in amorphous form in the solid dispersion obtained by the modified solvent evaporation.
2
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PHYSICOCHEMICAL CHARACTERIZATION AND DISSOLUTION STUDIES OF SOLID DISPERSIONS OF CLOTRIMAZOLE WITH CHITOSAN

88%
Grimling B., Jasińska J., Meler J., Szcześniak M., Pluta J. M., Górniak A.
Progress on Chemistry and Application of Chitin and its Derivatives
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2016
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vol. 21
63-72
EN
The aim of the present study was to increase the solubility of clotrimazole. Among the methods to increase the solubility selected solid dispersions of the drug with the polymer. Chitosan was used as the polymer. Clotrimazole was incorporated into the chitosan type 652 with molar masse chitosan Mη = 429 kDa. Solid dispersions were prepared by using different ratios of clotrimazole and chitosan (1:9, 3:7, 5:5, 7:3, 9:1). Formulations were tested dissolution rate of the drug. The highest dissolution of clotrimazole, amounting to 47.95%, was observed after 60 minutes from solid dispersion prepared by grinding method and 42.84% from physical mixtures with drug-polymer weight ratio 1:9 in the presence chitosan. The solubility of the drug improved more than 37-fold. XRPD analysis indicates the presence of the clotrimazole in crystalline form in the solid dispersion obtained by kneading method.
3
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THE INFLUENCE OF A DENTAL FORMULATION PREPARED WITH CHITOSAN ON THE PHARMACEUTICAL AVAILABILITY OF CLOTRIMAZOLE

75%
Grimling B., Meler J., Szcześniak M., Kocoń M., Karolewicz B., Złocińska A., Górniak A.
Progress on Chemistry and Application of Chitin and its Derivatives
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2017
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vol. 22
42-53
EN
The present work involves the development of a dental gel composition obtained on the basis of clotrimazole incorporated into chitosan in order to improve drug solubility. Solid dispersions were prepared by using two methods: grinding and kneading. The solid dispersion varied the ratio of chitosan to drug to increase the volume of the drug; the ratios were 5:5, 3:7, 2:8, 1:9. The mixtures were subjected to the dissolution rate of clotrimazole. The presence of chitosan improved the drug solubility; a better solubility from the solid dispersion prepared by the grinding method was obtained from the ratio of drug to polymer of 1+9. The rate of dissolution of clotrimazole was improved 17 times compared to the pure drug. Fourier transform infrared spectroscopy (both infrared and X-ray diffraction) revealed no new chemical structure of the tested connections and concluded that there was no interaction between the drug and the polymer in the test diffractions. Solid dispersions with the best parameters were used to prepare hydrogels, and the pharmaceutical availability of clotrimazole was analysed. The best properties were characterized by a hydrogel that was composed of the ratio of the amount of drug to polymer 5:5. The study demonstrated the availability of a pharmaceutical drug release at a therapeutic concentration in the first hour of the study. The use of the appropriate balance between clotrimazole and chitosan and the development of the hydrogel composition may affect the improvement of the drug solubility and may create the possibility of obtaining sustained or controlled release of the drug substance.
4
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METHOD VALIDATION AND STABILITY STUDIES OF DIFFERENTIAL ACTIVITY OF HYDROXYPROPYL-β-CYCLODEXTRIN AND HYDROPHILIC CARRIERS OF CARVEDILOL.

75%
Boakye-Yiadom K. O., Kesse S., Korto K., Sarkodie E. K., Baidoo S. A., Filli M. S., Wang B.
Acta Poloniae Pharmaceutica - Drug Research
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2020
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vol. 77
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issue 3
423-430
EN
Stability studies of the formulations of CAR solid dispersions were analyzed at 300C/65%RH for a period of three months. A simple reverse phase HPLC was developed and validated for the quantification of CAR solid dispersions. Chromatographic separation was achieved on Waters Atlantis dC18 (4.6 X 150mm) column with a mobile phase consisting of 0.033M phosphate buffer and methanol (35:65). The mobile phase was filtered using an organic filter paper and sonicated for about 20 min. The flow rate was 1ml/min and 242nm wavelength was used for detection. Force degradation studies were conducted under three conditions namely; acidic, basic and hydroxide peroxide conditions. With the HPLC linearity concentration was in the range of 5-80μg/ml with a correlation coefficient (R2) of 0.9995. There was no interference with drug carriers. The suggested reverse phase HPLC methodology is simple, selective, linear and robust in quantifying the amount of CAR in the various solid dispersion samples. In hydrogen peroxide a degraded product was found on the chromatogram unlike that of the acidic and basic conditions. Degradation occurred more strongly in the acidic condition than in the basic condition. The binary systems were less stable than the ternary system solid dispersions due to the presence of HP-β-CD.
5
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Development of tablets containing solid dispersion of ibuprofen manufactured by Hot Melt Impregnation process.

75%
Garbera K., Woś-Latosi K., Sawicki W.
Acta Poloniae Pharmaceutica - Drug Research
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2019
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vol. 76
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issue 2
341-354
EN
The main assumption of given study was to develop tablets containing amorphous ibuprofen by hot melt extrusion process. However proposed manufacturing procedure demonstrates quite a few differences in comparison to a conventional hot melt extrusion. Accurately the given manufacturing procedure has been called a hot melt impregnation due to the process characteristics. As a product of described process a fine free flowing extrudate is obtained. Four different compositions have been proposed. Materials prepared by hot melt impregnation technique have been extensively examined in terms of physicochemical properties and then were subjected to tablet compression process. Obtained tablets were examined in terms of thermodynamic stability and compared to marketed product containing ibuprofen.
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