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PHYSICOCHEMICAL CHARACTERIZATION AND DISSOLUTION STUDIES OF SOLID DISPERSIONS OF CLOTRIMAZOLE WITH CHITOSAN

100%

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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tom 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.

2

THE INFLUENCE OF A DENTAL FORMULATION PREPARED WITH CHITOSAN ON THE PHARMACEUTICAL AVAILABILITY OF CLOTRIMAZOLE

86%

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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tom 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.

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Double blind study of sertaconazole 2% cream vs. clotrimazole 1% cream in treatment of seborrheic dermatitis

86%

Goldust M. , Rezaee E. , Rouhani S.

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nr 1

EN

Treatment of seborrheic dermatitis (SD) is an important issue in dermatology. This study was undertaken to compare efficiency of sertaconazole 2% cream vs. clotrimazole 1% cream for the treatment of seborrheic dermatitis. One hundred twenty eight patients suffering from SD were studied. Patients were randomly divided into two groups. Sixty four patients received local sertoconazole 2% cream and in control group 64 patients received clotrimazole 1% cream. They were recommended to use the cream twice a day for 4 weeks. At the beginning of referring and 2 and 4 weeks after first visit, the patients were examined by a dermatologist to assess improvement of clinical symptoms. The mean age of sertaconazole and clotrimazole group patients was 34.78±13.54 and 38.68±11.88, respectively. The highest level of satisfaction (87.6%) was observed 28 days after sertaconazole administration and in clotrimazole group it was 50%. Relapse of the disease one month after stopping treatment was not observed in groups treated with sertaconazole 2% cream and clotrimazole 1% cream. This study suggests that sertaconazole 2% cream is an effective and welltolerated treatment for moderate to severe facial seborrheic dermatitis.

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The effect of PAMAM dendrimers with amine or hydroxyl terminal groups on the bioadhesive properties of hydrogels with clotrimazole

58%

Sosnowska K. , Szekalska M. , Winnicka K.

Polimery

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2016

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tom T. 61, nr 5

322--326

EN

Polyamidoamine dendrimers (PAMAM) belong to a relatively new class of polymers that are evaluated as efficient systems for drug delivery due to their nanosize range, ability to improve solubility, permeability and pharmacological activity of many drugs. In this study, the influence of PAMAM dendrimers of generation2 (G2) and 3 (G3) with -NH2or -OH terminal groups (PAMAM-NH2 and PAMAM-OH, respectively) on the bioadhesive properties, viscosity and yield stress of polyacrylic acid polymer hydrogels with clotrimazole was investigated. We show that the addition of PAMAM-NH2 dendrimers G2 and G3 into the hydrogel structures caused, in both cases, an about 2-fold decrease in viscosity of the hydrogels and a 1.3 and 1.4-fold decrease in the value of yield stress, respectively. We also found that PAMAM dendrimers with -NH2 terminal groups induced the highest decrease in the work of adhesion between hydrogels and the examined adhesive layers.

PL

Dendrymery poliamidoaminowe (PAMAM) należą do nowej grupy polimerów badanych pod kątem ich zastosowania jako efektywne nośniki leków. Takim zastosowaniom sprzyjają wymiary nano, zdolność do poprawy rozpuszczalności i przenikania przez błony oraz zwiększania aktywności farmakologicznej wielu substancji leczniczych. W ramach pracy oceniano wpływ dendrymerów PAMAM generacji 2 (G2) i 3 (G3) zawierających końcowe grupy -NH2 lub -OH (odpowiednio, PAMAM-NH2 i PAMAM-OH) na właściwości bioadhezyjne, lepkość i granicę płynięcia hydrożeli z klotrimazolem, wykonanych z użyciem pochodnych kwasu poliakrylowego. Wykazano, że dodatek do struktury hydrożelowej dendrymerów PAMAM-NH2 G2 i G3 powoduje około 2-krotne zmniejszenie ich lepkości oraz, odpowiednio, 1,3- i 1,4-krotne zmniejszenie wartości granicy płynięcia. Stwierdzono również, że dendrymery PAMAM z końcowymi grupami -NH2 powodują największy spadek pracy adhezji pomiędzy hydrożelami a badanymi warstwami adhezyjnymi.