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  • Author or Editor: G. Bettinetti x
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Differential scanning calorimetry DSC has been applied to the analysis of drugcyclodextrin binary systems in order to gain experimental evidence of the interaction and determine the stoichiometry of the inclusion compound. Two model systems, paracetamolbetacyclodextrin and vinburnineg-ammacyclodextrin were tested through the comparison of thermal behaviors of interacted and non-interacted mixtures containing excess drug. DSC allowed a confirmation of both interaction and stoichiometry of the inclusion compounds.

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Journal of Thermal Analysis and Calorimetry
Authors: M. Sorrenti, L. Catenacci, M. Bonferoni, G. Sandri, C. Caramella, and G. Bettinetti

Abstract  

Interactions between diltiazem hydrochloride (DTZ), an orally active calcium antagonist used in the treatment of angina and hypertension, and lambda carrageenan (λCRG), which has been successfully used in matrix formulations to obtain constant and pH-independent release of basic drugs, were investigated in solid state using differential scanning calorimetry (DSC) and thermogravimetric analysis (TG). The effect of particle size on thermal behaviour of the drug and the polymer was assessed, and the result used to select the most suitable granulometric fractions for the study. Physical mixtures ranging in composition from 3:1 to 0.6:1 (by weight) drug-to-polymer ratios were analyzed as such and after kneading. A stoichiometric ratio of interaction of 1.6:1 (w/w) DTZ:λCRG was found, in agreement with that obtained from dialysis equilibrium studies. All the examined granulometric fractions (<45 μm, 45–75 μm, 75–105 μm and >105 μm) of the interaction product showed similar thermal behaviour.

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Journal of Thermal Analysis and Calorimetry
Authors: M. Kónya, M. Sorrenti, F. Ferrari, S. Rossi, I. Csóka, C. Caramella, G. Bettinetti, and I. Erős

Abstract  

Thermogravimetric and rheological investigations of oil/water (o/w) creams prepared with different types of surface-active agents (non-ionic, non-ionic POE-free, ionic) were carried out. Thermogravimetry was aimed at the indirect study of the water bond mechanism in o/w creams and the influence of the composition, type and concentration of the mixed emulsifier on the binding of water incorporated in the structure (interlamellar, bulk) and on the binding proportions. The microstructural changes during application were studied with respect to the stability of the lamellar bilayer.

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Abstract  

Sugar esters (SEs) have a wide range of hydrophilic-lipophilic balance (HLB) values (1–16) and hence can be applied as surfactants or as solubility or penetration enhancers. They can be used for hot melt technology and solvent method which are frequently applied techniques to preparation of solid dispersions. In this study drug-SE products were prepared by physical mixing, melt technology and solvent methods. The products were investigated by DSC, X-ray powder diffraction and dissolution tests. Diclofenac sodium (DS) as model drug and two SEs, P1670 (HLB=16) and S970 (HLB=9) were used for the preparation of the products. DSC curves revealed considerable melting range and enthalpy decreases for the DS-SE products. The dissolved drug molecules broke down the structures of the SEs but were not built into the crystalline phase of the carrier. The melt technology led to a solid dispersion while in the case of the solvent methods the DS was in molecularly dispersed form which resulted in faster dissolution. The drug release was influenced by the structures resulting from the various treatments, by the HLB and by the gel-forming behaviour of the SEs.

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Abstract  

Isostructural solvates of the 1:1 molecular complex between the antibacterial drugs tetroxoprim (TXP) and sulfametrole (SMTR) with formulae TXPSMTRCH3OH (I), TXPSMTRC2H5OH (II) and TXPSMTRH2O (III), were investigated to establish their propensity for guest exchange. Separate exposure of powdered (I), (II) and (III) to a saturated atmosphere of each solvent of the complementary solvate pair at ambient temperature resulted in reversible solvent exchange in all cases. DSC and TG were the methods of choice for monitoring the exchange processes since (I)-(III) have distinct onset temperatures of desolvation and characteristic mass losses. Interpretation of the results in terms of the known locations of the solvent molecules in crystals of (I)-(III) led to the conclusion that solvent exchange probably proceeds by a co-operative mechanism involving material transport through channels while the common host framework is maintained.

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Journal of Thermal Analysis and Calorimetry
Authors: G. P. Bettinetti, C. Caramella, F. Giordano, A. La Manna, C. Margheritis, and C. Sinistri

Thermal analysis of the binary system benzoic acid (BA) and trimethoprim (TMP) provided evidence of the formation of two molecular compounds. BA-TMP and two crystalline forms of (BA)2-TMP were characterized on the basis of their thermodynamic parameters as well as of crystallographic and spectroscopic properties. The availability of these compounds (by recrystallization) allowed interpretation of thermal effects in the DSC curves of the mixtures and the theoretical phase diagrams could be drawn. The results are consistent with the model of a very slight dissociation of the molecular compounds in the melt.

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Abstract

In view of the poor aqueous solubility of nifluminic acid (NIF), the aim of this article was to improve its solubility and dissolution rate through the preparation of formulations based on hydroxypropyl β-cyclodextrin (HPβCD) and polyvinylpyrrolidone K25 (PVP K25), a combination of carriers which has been advantageously used for a similar purpose with various hydrophobic drugs. Ternary systems of NIF, HPβCD, and PVP K25 were prepared in different drug to CD to PVP ratios by physical mixing, kneading, microwave irradiation, and co-evaporation. Differential scanning calorimetry, thermogravimetric analysis, hot stage microscopy, Fourier transform infrared spectroscopy, and X-ray powder diffractometry were used to investigate the resulting solid-state interactions. The results showed that the solid state of the drug in the amorphous or crystalline ternary combinations influenced both the solubility and the dissolution rate of NIF.

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