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Hydrate Forms (hydrate + form)
Selected AbstractsInvestigation of impinging-jet crystallization with a calcium oxalate model systemAICHE JOURNAL, Issue 9 2003Jean M. Hacherl An impinging-jet crystallizer was investigated in this work to assess its operational sensitivity and reproducibility for the production of small, monodisperse crystals using calcium oxalate, a model system capable of forming multiple hydrates. The impinging-jet mixer provides rapid mixing of the reactant solutions through the impingement of two narrow reactant streams at high velocity. Impinging jet linear velocity and postjetting conditions were studied, with the jet operated in nonsubmerged mode. Hydrate form and crystal-size distribution (CSD) were determined using optical microscopy and image analysis techniques. The impinging jet consistently produced small, monodisperse crystals. However, at a high level of supersaturation, slight variations in the CSD were observed for apparently identical conditions, suggesting a degree of sensitivity in the system that could lead to difficulty in its application. An apparent trend between impinging-jet linear velocity and crystal size and number was observed, with more small crystals produced at higher linear velocity. [source] Qualitative in situ analysis of multiple solid-state forms using spectroscopy and partial least squares discriminant modelingJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 7 2007Karin Kogermann Abstract This study used in situ spectroscopy to reveal the multiple solid-state forms that appear during isothermal dehydration. Hydrate forms of piroxicam and carbamazepine (CBZ) were investigated on hot-stage at different temperatures using near-infrared (NIR) and Raman spectroscopy combined with multivariate modeling. Variable temperature X-ray powder diffraction, differential scanning calorimetry, thermogravimetric analysis, and Karl Fisher titrimetry were used as reference methods. Partial least squares discriminant analysis (PLS-DA) was performed to qualitatively evaluate the phase transition. It was shown that the constructed PLS-DA models, where spectral differences were directly correlated to solid-state modifications, enabled differentiation between the multiple forms. Qualitative analysis revealed that during dehydration, hydrates, such as CBZ dihydrate, may go through several solid-state forms, which must be considered in quantitative model construction. This study demonstrates that in situ analysis can be used to monitor the dehydration and reveal associated solid-state forms prior to quantification. The utility of the complementary spectroscopic techniques, NIR and Raman, have been shown. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 96: 1802,1820, 2007 [source] Process-induced phase transformation of berberine chloride hydratesJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 4 2010Henry H.Y. Tong Abstract Berberine is a natural quaternary ammonium alkaloid used clinically in the chloride salt form for the treatment of diarrhea in many Asian countries. Although the hydrate formation of berberine chloride (BCl) is well documented, the associated mechanism and implications in pharmaceutical formulation have not been studied in detail. In this study, pure BCl dihydrate and BCl tetrahydrate were recrystallized from water and their phase transformation behaviors under defined conditions were investigated. Additionally, pharmacopoeial grade BCl material consisting predominantly of the dihydrate form was examined for potential phase changes when being subjected to a conventional wet granulation procedure for tablet production. Results from solubility measurements, thermal analysis, variable temperature-powder X-ray diffraction (VT-PXRD), and variable temperature-Fourier transform infrared spectroscopy (VT-FTIR) confirmed the solid-state interconversions between the tetrahydrate and dihydrate at 30,49°C and between the dihydrate and anhydrate at 70,87°C. Consistent with the observed phase changes of the two pure hydrates, wet massing of the pharmacopoeial grade BCl sample led to a thermodynamics-driven transition to the tetrahydrate form at room temperature while subsequent tray drying at 50°C caused a reversion back to the dihydrate form. The rate and extent of such hydrate conversion depended largely on the water activity of the granulated powder matrix, which in turn was governed by the particular excipients employed. The present findings have important implications in the regulation of the hydrate forms of BCl in the finished products using specific excipients. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99: 1942,1954, 2010 [source] Evaluation of hydrate-screening methodsJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 7 2008Yong Cui Abstract The purpose of this work is to evaluate the effectiveness and reliability of several common hydrate-screening techniques, and to provide guidelines for designing hydrate-screening programs for new drug candidates. Ten hydrate-forming compounds were selected as model compounds and six hydrate-screening approaches were applied to these compounds in an effort to generate their hydrate forms. The results prove that no screening approach is universally effective in finding hydrates for small organic compounds. Rather, a combination of different methods should be used to improve screening reliability. Among the approaches tested, the dynamic water vapor sorption/desorption isotherm (DVI) method and storage under high humidity (HH) yielded 60,70% success ratios, the lowest among all techniques studied. The risk of false negatives arises in particular for nonhygroscopic compounds. On the other hand, both slurry in water (Slurry) and temperature cycling of aqueous suspension (TCS) showed high success rates (90%) with some exceptions. The mixed solvent systems (MSS) procedure also achieved high success rates (90%), and was found to be more suitable for water-insoluble compounds. For water-soluble compounds, MSS may not be the best approach because recrystallization is difficult in solutions with high water activity. Finally, vapor diffusion (VD) yielded a reasonably high success ratio in finding hydrates (80%). However, this method suffers from experimental difficulty and unreliable results for either highly water-soluble or water-insoluble compounds. This study indicates that a reliable hydrate-screening strategy should take into consideration the solubility and hygroscopicity of the compounds studied. A combination of the Slurry or TCS method with the MSS procedure could provide a screening strategy with reasonable reliability. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:2730,2744, 2008 [source] | ||||||||||