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1
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STUDIES OF GENTAMYCIN ADSORPTION ON CHITOSAN

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Meler J., Grimling B., Pluta J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2013
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vol. 18
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issue 18
175-179
EN
Chitosan as a dietary supplement has been used in the treatment of obesity due to its capability of binding bioactive compounds. A molecule of a cationic polymer, such as chitosan, may bind gentamycin. The aim of the study was to determine the binding capability of Gentamycin by chitosan’s contained in weight-loss supplements. The Gentamycin absorption was investigated by means of a dynamic method in a biopharmaceutical model imitating in vitro conditions including the required level of nutrients. Mean absorption of gentamycin by chitosan ranged from 2,1% to 34,1% depending on the environmental pH. The highest absorption rate was observed at above pH 6,8. Concluding, the studies confirmed that the investigated gentamycin interact with chitosan, what leads to decrease in their amount and affects the bioavailability of the drugs.
2
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THE INFLUENCE OF SUBSTRATE COMPOSITION ON THE PHYSICOCHEMICAL PROPERTIES OF HYDROGELS WITH CHITOSAN

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Szcześniak M., Grimling B., Meler J., Pluta J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2016
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vol. 21
187-191
EN
The aim of the study was to evaluate the effect of Carbopol 934 P and PVP K 90 on the rheological properties of chitosan gels. Hydrogels were prepared with hydrocortisone containing chitosan, Carbopl 934P, PVP, propylene glycol-1,2 or polyethyleneglycol 400 and glycerol. Addition of polymers had positive influence on the dispersion of hydrogels. The studied gels have thixotropic properties, their viscosity increases with the increase of the concentration of polymers. Increase of the content of polyvinylpyrrolidone K 90 and Carbopol 934 P increases the consistence, gels are more firm and cohesive. Gels with 5 % chitosane, 15% polyvinylpyrrolidone K 90 and Carbopol 934 P in the presence of additives have prolonged half release period of hydrocortisone.
3
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INVESTIGATION OF FENOFIBRATE SOLUBILITY IN THE PRESENCE OF CHITOSAN

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Grimling B., Meler J., Pluta J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2012
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vol. 17
79 - 86
EN
Fenofibrate is an active substance which is well absorbed from the gastrointestinal tract, but it is characterized by limited solubility. Due to a wide spectrum of its pharmacological activity, it would be beneficial to improve its solubility, and thus increase the drug absorption capability. The aim of the study was to investigate the effect of chitosan on the solubility of fenofibrate incorporated into this polymer carrier. The study investigated fenofibrate in solid dispersions at the drug to polymer ratio of 3:7,5:5,7:3. The solubility investigation was performed by means of a dynamic method in a dissolution apparatus; mean amount of dissolved fenofibrate and the drug to polymer quantitative ratio in which the solid dispersion possessed the most beneficial properties improving the drug solubility were calculated. The study revealed a multi-fold increase (from 33 to 50 times) in fenofibrat solubility in the presence of chitosan, which increased with duration of the study and with increasing percentage of the polymer in formulations. The obtained results may help develop new technologies for fenofibrate preparations with chitosan, with better solubility characteristics, and thus increased bioavailability of the drug.
4
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APPLICATION OF CHITOSAN IN THE FORMULATION OF METHYL CELLULOSE-BASED HYDROGELS

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Szcześniak M., Grimling B., Meler J., Pluta J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2014
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vol. 19
139-144
EN
The aim of this work was to study the properties of methylcellulose hydrogels with supplements containing chitosan and 1% hydrocortisone. Depending on the composition of the substrate, gels are characterised by a variety of pharmaceutical availabilities. Increasing the concentration of chitosan has an influence on increasing the viscosity, hardness, and cohesiveness of the tested gels.
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STUDIES OF NORFLOXACIN ADSORPTION ON CHITOSAN

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Meler J., Grimling B., Pluta J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2012
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vol. 17
103 - 110
EN
In clinical practice a lot of natural macromolecular compounds which operation is based on assisting weight loss are used in the obesity treatment. These measures swell in the digestive tract and form the polymer gel system, which has the ability to adsorb up to 5 times more lipids relative to its own weight. When using dietary supplements containing chitosan, sometimes it comes to illness and in the therapy other agents such as chemotherapeutics are used. The aim of our study was to determine the binding capacity of chemotherapeutic norfloxacin present in the digestive tract model by chitosans found in slimming medicines, depending on variable physico-chemical factors. Phenomenon of norrfloxacin adsorption was studied by a dynamic pharmaceutical model simulating in vitro conditions. The amount of adsorbed chemotherapeutic agent by chitosan was calculated by the difference in concentrations of study drug before and after sorption. The results of measurements of quantities bounded norfloxacin were used to calculate the average percentage of adsorbed dose. The results show that norfloxacin is adsorbed by the chitosans in the applicable pH ranges, and the binding capacity depends on the pH, viscosity and concentration of chemotherapeutics, as well as the type of chitosan and additional substances in the gastrointestinal tract. The average amount of chemotherapeutic adsorption in the system chitosan-nutrients, depending on the pH ranged from 80 to 98%. The highest number of adsorption points above pH 7. In conclusion, the addition of dietary supplement such as chitosan reduces the amount of administered uniformly chemotherapeutic and simultaneously has a large impact on the bioavailability. The observed dependence may require changes in therapeutic process.
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THE INVESTIGATION OF PHYSICOCHEMICAL PROPERTIES OF THE SOLID DISPERSIONS IN THE PRESENCE POLYMERIC CARRIER- CHITOSAN

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Grimling B., Meler J., Pluta J., Górniak A.
Progress on Chemistry and Application of Chitin and its Derivatives
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2013
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vol. 18
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issue 18
167-173
EN
The BCS class II includes drugs with low solubility and high permeability.. Fenofibrate is an example of this class drugs. The aim of the study was to investigate the effect of chitosan on the saturation solubility of fenofibrate incorporated into this polymer carrier. The study investigated fenofibrate in solid dispersions using a method of the solvent evaporation and physical mixtures at the drug to polymer ratio of 1:9,3:7,5:5.Solid dispersion of fenofibrate containing different ratio of medium and high molecular weight chitosan showed high saturation solubility compared to pure sample of drug. IR spectroscopy reveals that there was no chemical interaction between drug and the polymer. DSC studies showed that there is no change in the crystal structure of drug during the solid dispersion technique. Chitosan has been proposed as a useful excipient for enhancing the bioavailability of poorly water-soluble compounds.
7
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THE INFLUENCE OF THE PHYSICOCHEMICAL FACTORS ON DISSOLUTION OF THE SUBSTANCE OF CLASS II BCS FROM SOLID DISPERSIONS WITH CHITOSAN

100%
Grimling B., Górniak A., Meler J., Pluta J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2013
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vol. 18
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issue 18
157-165
EN
The BCS class II includes drugs with low solubility and high permeability. Fenofibrate is an example of this class drugs. The aim of the study was to investigate the effect of chitosan about average molecular weight in various formulations on the dissolution of fenofibrate incorporated into this polymer carrier. The study investigated fenofibrate in solid dispersions using a method of the solvent evaporations at the drug to polymer ratio of 1:9;3:7;5:5. The highest dissolution of fenofibrate, amounting to 72.7%, was observed after 60 minutes from solid dispersions with drug-polymer weight ratio 1:9 in the presence chitosan A and was72 times higher in relation to the amount of added polymer in comparison to the solubility of pure drug. Investigations DSC showed that fenofibrate was remained in crystalline state in solid dispersion.
8
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TECHNOLOGY OF PREPARATION AND EVALUATION OF KETOPROFEN-CHITOSAN SOLID DISPERSION

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Grimling B., Szcześniak M., Meler J., Pluta J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2014
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vol. 19
15-22
EN
The aim of the study was to investigate the effect of chitosan on the dissolution of ketoprofen incorporated into this polymer carrier. The study investigated ketoprofen in physical mixtures at the drug to polymer ratios of 1:9, 3:7, and 5:5. The solubility investigation was performed by means of a dynamic method in a dissolution apparatus; the mean amount of dissolved ketoprofen and the drug to polymer quantitative ratio in which the solid dispersion possessed the most beneficial properties improving the drug solubility were calculated. The study revealed a multifold increase (33 times) in ketoprofen solubility in the presence of chitosan, which increased with duration of the study and with increasing percentage of the polymer in formulations. The dissolution rates of ketoprofen in the presence of chitosan at the weight ratio 1:9 increased with the decrease of the molecular weight of the chitosan. The results obtained may help to develop new technologies for ketoprofen preparations with chitosan, with better solubility characteristics, and thus increased bioavailability of the drug.
9
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INVESTIGATION OF FENOFIBRATE DISSOLUTION RATE INCORPORATED ON SOLID DISPERSIONS INTO CHITOSAN

100%
Grimling B., Szcześniak M., Meler J., Pluta J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2013
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vol. 18
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issue 18
149-156
EN
The aim of the study was to investigate the effect of chitosan on the dissolution of fenofibrate incorporated into this polymer carrier. The study investigated fenofibrate in physical mixtures at the drug to polymer ratio of 1:9, 3:7, and 5:5. The solubility investigation was performed by means of a dynamic method in a dissolution apparatus; mean amount of dissolved fenofibrate and the drug to polymer quantitative ratio in which the solid dispersion possessed the most beneficial properties improving the drug solubility were calculated. The study revealed a multi-fold increase (from 13 to 70 times) in fenofibrate solubility in the presence of chitosan, which increased with duration of the study and with increasing percentage of the polymer in formulations. The dissolution rates of fenofibrate in the presence of chitosan at the weight ratio 1:9 increased with the increment of the molecular weight of the chitosan. The obtained results may help develop new technologies for fenofibrate preparations with chitosan, with better solubility characteristics, and thus increased bioavailability of the drug.
10
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STUDIES ON ADSORPTION TIAMFENICOL ON CHITOSANS DEGRADED RADIATION IN PHARMACEUTICAL IN VITRO MODEL

100%
Meler J., Grimling B., Pluta J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2012
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vol. 17
95 - 102
EN
Connections of polymers and biopolymers with biologically active compounds are recently the subject of intensive research. Low molecular weight active ingredient combined with a polymer has, in many cases, the modified action. On the other hand, the use of inappropriate polymers can result in incompatibilities drug-polymer. The phenomenon of adsorption of the antibiotic has been studied by the static method in the concentration range generally taken single dose using a pharmaceutical gastrointestinal tract model. The results of measurements bounded drug quantity were used to determine the average percentage of adsorbed dose. The results show that antibiotic tiamphenicol is adsorbed on chitosan in used pH ranges, and the binding ability depends on the variety of chitosan and directly from the environment reaction. It was observed that the average sorption depending on the type of chitosan was within the limit from 82% to 97%.The fact of the lowest adsorption value at pH 6.4 can be explained by chemical properties of chitosan, which shows the load until the pH > 6.7 and the electrostatic adsorption may be exhibit in relation to weak acid medicinal substance. Thus, the specific polymer surface area and its sorption capacity is increased. Based on the above considerations can be stated that between study drug and the polymer an antagonistic interaction exist by involving the adsorption of drugs from this group on chitosan.
11
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ADSORPTION STUDIES OF KETOCONAZOLE WITH CHITOSAN

100%
Meler J., Szcześniak M., Pluta J., Grimling B.
Progress on Chemistry and Application of Chitin and its Derivatives
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2014
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vol. 19
111-117
EN
Combinations of polymers and biopolymers of biologically active compounds in the last period have been the subject of intensive research. The active substance linked to a polymer often has a modified function and sometimes no action. On the other hand, the use of unsuitable polymers may result in a type of mismatch of drug-polymer. The aim of the study was to examine whether the active substance ketoconazole causes incompatibility with dietary supplements containing chitosan. Antifungal drug adsorption phenomenon was investigated by the static method in the concentration range of the single dose using a pharmaceutical model of the gastrointestinal tract. The test results show that the antifungal agent is adsorbed onto the chitosan in the pH ranges used, and the binding ability of the chitosan depends on the variety, or indirectly from the reaction environment. It was observed that the average sorption, depending on the variety of chitosan, was located in the limit from 94% to 100%. The increase of the size of the adsorption of anti-inflammatory drugs on the polymer with increasing pH from 7.6 to 8.0 can be explained by the swelling properties of chitosan, which grow with increasing pH of the environment in the direction of alkaline pH. Thus, the specific surface area and polymer sorption capacity is increased. Based on the above considerations, it can be concluded that, between the test drug and the polymer, there is antagonistic interaction involving the adsorption of the drug of this group on a polymer which is chitosan.
12
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EFFECT OF CHITOSAN ON THE RHEOLOGICAL PROPERTIES OF HYDROGELS BASED ON SODIUM CARBOXYMETHYLCELLULOSE

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Szcześniak M., Grimling B., Pluta J., Meler J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2015
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vol. 20
254-259
EN
The aim of the study was to evaluate the effect of changing the concentrations of chitosan on the rheological properties of the obtained formulation. Hydrogels were prepared with 1% hydrocortisone containing 4% sodium carboxymethylcellulose with the addition of chitosan, propylene glycol-1,2 or polyethylene glycol 400 and glycerol or paraffin. The concentration of chitosan and excipients affects the rheological properties of gels and the pharmaceutical availability of hydrocortisone. Increasing the concentration of chitosan have influence on increasing the viscosity, hardness, and cohesiveness of the tested gels.
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EVALUATION OF PHYSICOCHEMICAL PROPERTIES OF SOLID DISPERSIONS OF BCS CLASS II SUBSTANCES WITH CHITOSAN

100%
Grimling B., Górniak A., Meler J., Pluta J.
Progress on Chemistry and Application of Chitin and its Derivatives
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2012
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vol. 17
87 - 94
EN
The BCS class II includes drugs with low solubility and high permeability. The substances require modification to increase their solubility in the upper part of the digestive system. Fenofibrate is an example of this class drugs. The aim of the study was to investigate the effect of chitosan on the solubility of fenofibrate incorporated into this polymer carrier. The study investigated fenofibrate in solid dispersions using a method of the solvent evaporation by means of freeze-drying at the drug to polymer ratio of 3:7,5:5,7:3. The study revealed a multi-fold increase (from 33 to 57 times) in fenofibrat solubility in the presence of chitosan, which increased with duration of the study and with increasing percentage of the polymer in formulations. DSC examination revealed a possible physical interaction between the drug and the polymer. The degree of lowering of temperature and increased heat effects is correlated with increased solubility of the drug in all the formulations. DSC studies confirmed that fenofibrate is present in solid dispersions in a crystalline form.
14
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STUDIES ON ADSORPTION CHlORAMFENICOL ON CHITOSANS IN PHARMACEUTICAL “IN VITRO” MODEL

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Meler J., Grimling B., Biernat P., Pluta J.
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EN
In clinical practice in the treatment of obesity, uses several natural macromolecular compounds, whose functioning is based on supporting the weight loss. In use of dietary supplements containing chitosan, sometimes reaches the illness and in the treatment, which the other therapeutic agents are chemotherapeutic drugs. The aim of our study was to determine the binding capacity of chloramphenicol chemotherapeutic depending on variable factors physico-chemical properties, present in the intestinal tract model of chitosans present in the drugs. The phenomenon of adsorption of chloramphenicol was examined by a dynamic model simulating the conditions of the pharmaceutical in vitro. the amount of adsorbed chemotherapy. The obtained results show that chloramphenicol is adsorbed by chitosans at pH ranges used, and the binding capacity depends on the pH of the environment and the viscosity and concentration of the chemotherapeutic agent as well as the type of chitosan and the additional substances present in the gastrointestinal tract. The average size of the adsorption system chemotherapeutic chitosan-nutrients depending on the pH of the medium ranged from 22.3 to 100.0%. Maximum number of adsorption points above pH 7 (chitosan precipitated polymer forming the emulsion-gel system).
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EVALUATION OF PREPARATIONS PHARMACEUTICAL SALAZOSULFAPIRIDIN DEPENDING USED FOOD SUPPLEMENTS CONTAINING CHITOSAN IN MODEL “IN VITRO”

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Meler J., Grimling B., Pluta J.
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16
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THE ADSORPTION OF SIMVASTATIN ON CHITOSANS IN AN IN VITRO PHARMACEUTICAL MODEL

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Meler J., Grimling B., Szcześniak M., Pluta J., Biernat P.
Progress on Chemistry and Application of Chitin and its Derivatives
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2017
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vol. 22
151-158
EN
In clinical practice for the treatment of obesity, several natural macromolecular compounds are used, whose operation is based on supporting weight loss. During the use of dietary supplements containing chitosan, disease sometimes occurs and treatment for this often comprises different therapeutic agents and antibiotics. The aim of our study was to determine the binding capacity of simvastatin to chitosan, which is found in dietary supplements promoting weight loss, depending on variable physicochemical factors in the gastrointestinal tract model. The phenomenon of adsorption of simvastatin was investigated by a static and dynamic pharmaceutical model (according to the Modified method of Polish Pharmacopoeia IX) simulating the conditions in vitro. The amount of bound drug is used to calculate the average percentage of the adsorbed dose. The obtained results showed that simvastatin is adsorbed by chitosan in the used pH ranges, and the binding capacity is dependent on the environmental pH, viscosity, the concentration of the drug, the type of chitosan and additional substances present in the gastrointestinal tract. The average adsorption of simvastatin in the system of chitosan-nutrients, depending on the pH of the medium, was in the range of 27 to 95%. The highest amount of adsorption was noted above pH 7 (chitosan precipitated polymer forming the emulsion-gel system), when the bioavailability of dietary supplement using chitosan was almost zero.
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THE STUDY OF PHYSICOCHEMICAL PROPERTIES OF SOLID DISPERSIONS OF IBUPROFEN IN THE PRESENCE OF CHITOSAN

88%
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
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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.
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