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1
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FORMULATION AND CHARACTERISATION OF MUCOADHESIVE DENTAL APPLICATIONS CONTAINING BENZYDAMINE HYDROCHLORIDE

100%
Grimling B.
Progress on Chemistry and Application of Chitin and its Derivatives
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2021
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vol. 26
71-79
EN
The aim of this research was to develop a bioadhesive film based on benzydamine hydrochloride incorporated into natural bioadhesive polymers with different quantities of chitosan and guar gum but utilising a plasticiser. The obtained gels were deaerated by sonification, formed and evaporated by hot air drying; then, the properties were evaluated. Guar gum had a great influence on mechanical properties of the films – dynamic viscosity, texture, elasticity, stretching robustness, swelling and blur time. The formulations were used to obtain mucoadhesive films containing 0.3% benzydamine hydrochloride; they were tested for the release of the model drug. The amount of chitosan added to the formulation reduced the quantity of released substance and slowed down the release. Fouriertransform infrared spectroscopy did not reveal the creation of new chemical structures. In conclusion, the ratio of chitosan to guar gum in the medium impacts the mechanical properties and release parameters of the drug. These findings should enable researchers to match the parameter values to receive the most beneficial therapeutic outcome.
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INFLUENCE OF SELECTED POLYMERS ON PHARMACEUTICAL: PROPERTIES OF MUCOSAL SYSTEMS CONTAINING ACYCLOVIR

100%
Grimling B.
Progress on Chemistry and Application of Chitin and its Derivatives
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2022
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vol. 27
106-115
EN
The aim of this paper was to formulate the composition of a bioadhesive film obtained based on acyclovir incorporated into natural bioadhesive polymers (chitosan and guar gum) in different quantitative ratios. To this end, the author developed a technology for preparing films containing various quantitative ratios of chitosan to guar gum: 1:0.25; 1:0.50; 1:0.75; 1:1; and 1.2:0.50. The formulations were used to prepare mucoadhesive films containing 2% acyclovir. The dressings were tested with respect to their physicochemical properties and subjected to dissolution testing. A comparative analysis of Fourier-transform infrared (FT-IR) spectra of pure polymers, acyclovir, and films containing polymers in different quantitative ratios was conducted. The quantitative ratio of chitosan to guar gum significantly impacted the mechanical properties of films: texture, elasticity, tensile strength, swelling, and blur time of the testes carriers. The 1:1 formulation showed the highest mechanical strength and flexibility. The dressing containing 1.2% chitosan and 0.5% guar gum had the longest blur time. An increase in the chitosan content in the formulation significantly affected the drug dissolution parameters, which makes it possible to achieve the desired effect of extended-release time. The FT-IR spectra excluded the formation of drug-polymer interactions. Changes in the quantitative ratios of chitosan and guar game in the carrier’s composition may impact the mechanical properties of the drug formulation and changes in the parameters of active substance release.
3
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THE EFFECT OF CHITOSAN ON THE PHYSICOCHEMICAL PROPERTIES OF DERMATOLOGICAL PREPARATIONS CONTAINING HUMULUS LUPULUS L. EXTRACT BASED ON CELUGEL

100%
Grimling B.
Progress on Chemistry and Application of Chitin and its Derivatives
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2023
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vol. 28
26-33
EN
This study evaluated hydrogels containing Celugel, 3% hop cone extract obtained from Humulus lupulus L. using supercritical carbon dioxide extraction substrate, and 1% and 2% chitosan for dermatological application to treat inflammatory skin conditions. The presence of chitosan significantly affected the rheological properties of the formulations, including their dynamic viscosity, hardness, consistency, cohesiveness, and blurring time. The formulations containing 2% chitosan showed the best application possibilities. The formulations were evaluated for dissolution of cohumulone, which is an analogue of humulone contained in hop cone extract. The concentration of chitosan in the formulations had a significant effect on the dissolution testing parameters of the active ingredient: as the chitosan concentration increased, the desired effect of prolonged release time of the active ingredient was achieved while maintaining the membrane-forming properties of Celugel.
4
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EFFECT OF SELECTED MUCOADHESIVE POLYMERS ON PHARMACEUTICAL PROPERTIES OF CHITOSAN FORMULATIONS

100%
Grimling B.
Progress on Chemistry and Application of Chitin and its Derivatives
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2021
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vol. 26
61-70
EN
The aim of this study was to develop a technical process and composition of mucoadhesive hydrogels containing benzocaine, based on different concentration ratios of the natural polymers chitosan and xanthan gum. For this purpose, lyophilisates of polymeric complexes with the quantitative ratios of 0.5:1, 1:1 and 1:0.5 chitosan to xanthan gum were prepared and subsequently used to prepare hydrogels of various concentrations. The physicochemical properties and pharmaceutical availability of benzocaine were evaluated and diffractograms and Fourier-transform infrared spectra of individual polymers and their polyelectrolyte complexes were compared. The 1:1 formulation exhibited the highest water absorption capacity and the gels showed the highest viscosity and the shortest blurring times. More chitosan increased carrier texture parameters, including hardness, cohesiveness and consistency, whereas more xanthan gum led to the longest gel blurring times and improved carrier stability. The concentration ratio of chitosan to xanthan gum in lyophilisates determined the viscosity, texture, spreadability and blurring time of the gels. Increases in lyophilisate percentage in the gels also affected the physicochemical properties of the carrier. In addition, the proportions of polymers in the mixture did not influence the availability of the drug from the prepared gel; this factor appears to depend more on the lyophilisate content in the carrier. Variations in the ratio of chitosan to xanthan gum in the polymer complex as well as lyophilisate percentage in the gel may impact the properties of the hydrogel and its efficacy as a carrier for therapeutic substances administered to the oral cavity mucosa.
5
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THE INFLUENCE OF SELECTED POLYMERS ON THE RHEOLOGICAL PROPERTIES OF HYDROGELS WITH CHITOSAN APPLIED ON THE SKIN

52%
Szcześniak M., Grimling B., Meler J., Karolewicz B.
Progress on Chemistry and Application of Chitin and its Derivatives
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2017
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vol. 22
201 - 206
EN
The aim of the study was to evaluate the effect of methylcellulose and carboxymethylcellulose on the rheological properties of hydrogels applied to skin on chitosan in the presence of the additives propylene glycol and glycerol. Rheological studies showed that the tested gels are non-newtonian systems, and have thixotropic properties. Substrates made of methylcellulose and chitosan are characterised by higher shear values than those obtained with carboxymethylcellulose. The addition of polymers had a positive influence on the dispersion of hydrogels, and the addition of excipients increased firmness, consistency and cohesiveness of the gels. Larger increases were observed with the addition of 10% of glycol propylene and glycerol contents for methylcellulose and of 20% of carboxymethylcellulose.
6
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STUDIES OF GENTAMYCIN ADSORPTION ON CHITOSAN

52%
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.
7
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THE INFLUENCE OF SUBSTRATE COMPOSITION ON THE PHYSICOCHEMICAL PROPERTIES OF HYDROGELS WITH CHITOSAN

52%
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.
8
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INVESTIGATION OF FENOFIBRATE SOLUBILITY IN THE PRESENCE OF CHITOSAN

52%
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.
9
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IN VITRO STUDIES OF ADSORPTION OF ERYTHROMYCIN ON CHITOSANS FROM DIETARY SUPPLEMENTS

52%
Meler J., Grimling B., Szcześniak M., Biernat P.
Progress on Chemistry and Application of Chitin and its Derivatives
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2014
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vol. 19
119-123
EN
In clinical practice, in the treatment of obesity, a plurality of natural high-molecular compounds are used, the activity of which supports weight loss. During the use of dietary supplements containing chitosan, illness sometimes develops and other therapeutic agents are applied as antibiotics The aim of our study was to determine the binding capacity of the antibiotic erythromycin depending on variable physicochemical factors, in the model of the gastrointestinal tract, by chitosans found in slimming dietary supplements Erythromycin adsorption phenomenon was studied by static and dynamic pharmaceutical model (according to the modified method of the Polish Pharmacopoeia) simulating in vitro conditions. The amount of bound drug was used to calculate the average percentage of the adsorbed dose. The results obtained show that erythromycin is adsorbed by chitosans at various pH ranges, and the binding capacity of the environment depends on the pH, viscosity and concentration of the antibiotic, as well as the chitosan and type and additional substances present in the gastrointestinal tract. The average level of the adsorption of erythromycin in the chitosan-nutrients system depends on the pH of the medium. The highest amount of adsorption was noted above pH 7 (chitosan precipitated polymer forming the emulsion-gel system).
10
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APPLICATION OF CHITOSAN IN THE FORMULATION OF METHYL CELLULOSE-BASED HYDROGELS

52%
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.
11
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STUDIES OF NORFLOXACIN ADSORPTION ON CHITOSAN

52%
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.
12
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THE INVESTIGATION OF PHYSICOCHEMICAL PROPERTIES OF THE SOLID DISPERSIONS IN THE PRESENCE POLYMERIC CARRIER- CHITOSAN

52%
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.
13
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THE INFLUENCE OF THE PHYSICOCHEMICAL FACTORS ON DISSOLUTION OF THE SUBSTANCE OF CLASS II BCS FROM SOLID DISPERSIONS WITH CHITOSAN

52%
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.
14
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TECHNOLOGY OF PREPARATION AND EVALUATION OF KETOPROFEN-CHITOSAN SOLID DISPERSION

52%
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.
15
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INVESTIGATION OF FENOFIBRATE DISSOLUTION RATE INCORPORATED ON SOLID DISPERSIONS INTO CHITOSAN

52%
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.
16
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STUDIES ON ADSORPTION TIAMFENICOL ON CHITOSANS DEGRADED RADIATION IN PHARMACEUTICAL IN VITRO MODEL

52%
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.
17
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ADSORPTION STUDIES OF KETOCONAZOLE WITH CHITOSAN

52%
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.
18
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APPLICATION OF CHITOSAN IN THE FORMULATION OF DERMATOLOGICAL HYDROGELS PREPARED ON THE BASIS OF MACROMOLECULAR COMPOUNDS

52%
Szcześniak M., Grimling B., Meler J., Karolewicz B.
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|
vol. 23
179 - 184
EN
The effect of chitosan concentration on the properties of dermatological preparations prepared with 2% methylcellulose and 10% polyvinylpyrrolidone was studied. As the levels of chitosan, propylene glycol-1,2 and glycerol increased, the hardness, consistency and cohesiveness of the hydrophilic gels increased, while the dissipation capacity decreased. Gels based on methylcellulose and chitosan, compared to formulations containing polyvinylpyrrolidone, have a higher rate of loss of volatile compounds, higher pH values for 1,2-propylene glycol formulation and higher texture parameters. The tested hydrogels have good rheological properties, allowing extrusion from the tube and spreading on the skin.
19
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CHARACTERISATION AND DISSOLUTION PROPERTIES OF KETOPROFEN IN BINARY SOLID DISPERSION WITH CHITOSAN

52%
Grimling B., Górniak A., Meler J., Szcześniak M.
Progress on Chemistry and Application of Chitin and its Derivatives
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2014
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vol. 19
23-31
EN
BCS class II includes drugs with low solubility and high permeability. Ketoprofen is an example of this class of drugs. The aim of the study was to investigate the effect of chitosan with average molecular weights in various formulations on the dissolution of ketoprofen incorporated into this polymer carrier. The study investigated ketoprofen in solid dispersions using a method of the solvent evaporations at the drug to polymer ratios of 1:9. 3:7, and 5:5. The highest dissolution of fenofibrate, amounting to 98.8%, was observed after 60 minutes from solid dispersions with a drug-polymer weight ratio 1:9 in the presence of chitosan B and was 32-times higher in relation to the amount of added polymer in comparison to the solubility of pure drug. DSC and IR investigations showed that ketoprofen remained in its crystalline state in solid dispersion. There was no change in the chemical structure of the drug after the incorporation of the drug onto the polymer. Chitosan has been proposed as a useful excipient for enhancing the bioavailability of poorly water-soluble compounds.
20
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EFFECT OF CHITOSAN ON THE RHEOLOGICAL PROPERTIES OF HYDROGELS BASED ON SODIUM CARBOXYMETHYLCELLULOSE

52%
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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