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1.
Giampiero Bettinetti Milena Sorrenti Laura Catenacci Franca Ferrari Silvia Rossi Ilaria Salvadeo Paolo Carraro 《Journal of inclusion phenomena and macrocyclic chemistry》2007,57(1-4):329-332
Triacetyl α-cyclodextrin, triacetyl β-cyclodextrin and triacetyl γ-cyclodextrin were tested as possible hydrophobic carriers
to prolong the release of hydrophilic teicoplanin (TCP). Physical–chemical characterization of individual components, drug-carrier
physical mixtures at 0.5, 0.67 and 0.75 mass fraction of carrier, and the respective interaction products by kneading or evaporative
crystallization under microwave irradiation was carried out using differential scanning calorimetry (DSC) and thermogravimetric
analysis (TGA). In vitro drug release in pH 7.4 phosphate buffer at 37 °C was determined by intrinsic dissolution rate (IDR)
measurements on non disintegrating compressed discs. Solid-state interactions of TCP with triacetyl α-cyclodextrin by evaporative
crystallization and kneading and with triacetyl β-cyclodextrin by evaporative crystallization (probably resulting in carrier
amorphization) were demonstrated. The role of carrier hydrophobicity, carrier mass fraction and preparation method of solid
drug-carrier combinations on solid-state drug-carrier interactions and slowing down of TCP release was assessed. Modulation
of drug release can be achieved using TCP-triacetyl γ-cyclodextrin combinations at 0.5 mass fraction of carrier. 相似文献
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G. P. Bettinetti P. Mura F. Melani M. Rillosi F. Giordano 《Journal of inclusion phenomena and macrocyclic chemistry》1996,25(4):327-338
The crystallinity of naproxen in solid combinations with amorphous maltoheptaose, the non-cyclic analog of -cyclodextrin, was assessed using differential scanning calorimetry supported by X-ray powder diffractometry. Cogrinding induced a decrease in drug crystalinity to an extent which depended on the grinding time, and was most pronounced for the combination of equimolecular composition. Thermal analysis showed that the mechanism behind the conversion of crystalline naproxen into the amorphous state by cogrinding with maltoheptaose differed from that with randomly substituted, amorphous -cyclodextrins. Interactions of naproxen with maltoheptaose in aqueous solution were studied by means of fluorescence spectroscopy, phase-solubility analysis, and computeraided molecular modelling. Maltoheptaose can wrap up naproxen, taking on a cyclic conformation and forming a pseudo inclusion complex (apparent binding constant K1: 1 = 1.0 × 103 (–20%) L mol–1 at 25 °C) which is about as stable as the true inclusion complex with -cyclodextrin in the lowest temperature range (0-100 K). A better complexing ability for naproxen in terms of binding constant values, however, was displayed by both native and derivatized -cyclodextrins, the hosts with covalently-bound cyclic structures. 相似文献
4.
F. Giordano G. P. Bettinetti A. La Manna A. Marini V. Berbenni 《Journal of Thermal Analysis and Calorimetry》1988,34(2):531-536
Differential scanning calorimetry has been applied to the study of the solid system cross-linked polyvinylpyrrolidone/trimethoprim.Different results have been systematically obtained on co-ground and not co-ground mixtures, suggesting some type of interaction to take place between components as a consequence of co-grinding.A simple phenomenological model of the interaction is proposed, which quite satisfactorily agrees with thermal data.
This work has been partially supported by Ministero Pubblica Istruzione (Fondi 60%). 相似文献
Zusammenfassung Das feste System von vernetztem Polyvinyl-pyrolidin/Trimethoprim wurde mittels DSC untersucht. Unterschiedliche Ergebnisse wurden systematisch für zusammen und nicht zusammen verriebene Mischungen gefunden, was auf eine Wechselwirkung zwischen Komponenten beim Verreiben hindeutet. Ein einfaches phänomenologisches Modell dieser Wechselwirkung wird vorgeschlagen, das mit thermischen Daten befriedigend übereinstimmt.
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This work has been partially supported by Ministero Pubblica Istruzione (Fondi 60%). 相似文献
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Paola Mura Gian Piero Bettinetti Maria Teresa Faucci Milena Sorrenti Alessandra Negri 《Supramolecular chemistry》2013,25(4):379-389
Abstract Interactions of naproxen (NAP) with amorphous, randomly methylated β-cyclodextrin at a degree of substitution per anhydroglucose unit of 1.8 (RAMEB) and with crystalline heptakis-(2,6-di-O-methyl)-β-cyclodextrin (DIMEB) were studied in aqueous solution and in the solid state using, respectively, phase-solubility analysis (at 25 °C, 37 °C and 47 °C) and differential scanning calorimetry (DSC) supported by X-ray powder diffractometry. RAMEB and DIMEB displayed similar solubilizing and complexing abilities towards NAP, suggesting analogous inclusion modes of the drug in the host cavity in aqueous solution. Differences were instead observed in interactions in the solid state, where the amorphizing capacity of RAMEB toward NAP (evaluated by DSC) was about twice that of DIMEB at each drug-to-carrier ratio. Assuming that inclusion complexation is also involved in solid-state interactions, molecular modelling accounted for the experimental results in terms of structural features of DIMEB, i.e. the particular inwards orientation of O-6-C-8 groups of three alternate glucoses on the primary hydroxyl side which hampers a deep penetration of NAP in the DIMEB cavity in the solid state. On the contrary, no obstruction of the cavity apparently occurs with RAMEB due its noncrystalline state. The aqueous dissolution rate of NAP from NAP-RAMEB and NAP-DIMEB blends containing 0.59, 0.73, 0.85, and 0.92 mass fraction of carrier linearly increased at decreasing drug-to-carrier ratios. The improvement was 5 to 20 times (from powders) and 50 to 200 times (from discs) the dissolution rate of NAP alone for both carrier. Therefore the choice of the amorphous RAMEB in pharmaceutical formulations can be recommended mainly for economic reasons, though the anhydrous and non-hygroscopic nature of crystalline DIMEB might be of particular advantage in case of moisture sensitive formulations. 相似文献
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α-, β-, and γ-cyclodextrins (CDs) marketed by five different companies were characterized from the thermal and structural
point of view. Three αCD samples showed two-step DSC dehydration profiles and their XRD patterns were characteristic for αCD⋅6H2O form I, whereas one brand with an apparent three-step DSC dehydration behaviour was a mixture of αCD⋅6H2O form I and anhydrous αCD. The differences in the DSC profiles after dehydration and EGA onset decomposition temperatures
recorded for the five βCD brands were attributed to different manufacturing and purification processes. The five γCDs brands
showed a common thermal behaviour and very similar XRD patterns. The patterns did not match the idealized pattern of γCD⋅14.1H2O, indicating the occurrence of two different hydrated crystal structures.
This revised version was published online in August 2006 with corrections to the Cover Date. 相似文献
7.
S. Pietra G. F. Bettinetti A. Albini G. Minoli 《Chemistry of Heterocyclic Compounds》1977,13(12):1263-1274
Data on the electronic structures and spectral characteristics of phenazine 5-oxides and 5, 10-dioxides are correlated. Methods for the synthesis of N-oxides of the phenazine series and their reactions (reduction, electrophilic and nucleophilic substitution, and photochemical transformations) are examined. Data on the natural compounds of this series are presented.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 12, pp. 1587–1599, December, 1977. 相似文献
8.
A. Szűts M. Sorrenti L. Catenacci G. Bettinetti Piroska Szabó-Révész 《Journal of Thermal Analysis and Calorimetry》2009,95(3):885-890
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. 相似文献
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