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排序方式: 共有111条查询结果,搜索用时 375 毫秒
91.
E. Yonemochi Y. Yoshioka Y. Yoshihashi K. Terada 《Journal of Thermal Analysis and Calorimetry》2006,85(3):693-697
We have
developed the vacuum dryer attached XRD-DSC system and monitored manufacturing
process of freeze-dried pharmaceutical product. The aim of this study is to
apply the XRD-DSC system for the preformulation of freeze-dried injections.
Gabexate mesilate was used as a model drug. Drug solution was frozen then
heated to annealing temperature according to the process-controlling program.
The XRD-DSC analyses were performed to monitor the crystallized spicies and
their crystallinity of sample. When the solution was cooled slowly, peaks
of gabexate mesilate and mannitol polymorph had been already observed during
the cooling process while those crystallinity were low at fast cooling rate.
As the drying underwent, intensity of ice peaks were getting weaker. At the
cooling rate of 0.1°C min–1, the XRD
profile of final product was revealed that the characteristic peaks of gabexate
mesilate, mannitol δ-form and β-form were appeared. When the cooling
rate was increased, the crystallinity of final products was decreased. From
these results, it was confirmed that the XRD profiles during freeze-drying
process significantly related to the final freeze-dried product. It is obvious
that monitoring by XRD-DSC system is a quite effective way to simulate the
manufacturing process and to optimize the qualified product. 相似文献
92.
Tsugikazu Tomono Etsuo Hasegawa Eishun Tsuchida 《Journal of polymer science. Part A, Polymer chemistry》1974,12(1):167-181
The reaction of a Mannich base type-polyamine polymer with iodine (I2) was studied kinetically and thermodynamically in order to clarify the polymer effects in the formation of triiodide ions (I3?). N,N-Dimethyl-p-(4-methylpiperazinomethyl) aniline and 1,4-dimethylpiperazine were used as low molecular weight donor model compounds. Triiodide ions are produced from the polyamine–I2 system immediately after mixing the two-component solutions, while in the systems with I2 and N,N-dimethyl-p-(4-methyl-piperazinomethyl)aniline and 1,4-dimethylpiperazine they are obtained only when relatively high concentrations of both donor and acceptor solutions were mixed. This is explained by the entropic contributions of the polymer chain such as the stacking effect of donor nitrogen atoms, i.e., the increment of local donor concentration around I2 in the reaction field. The relation between the solution behavior of the reaction systems and the rate of formation of I3? ions also supports this kind of polymer effect. The effects of neighboring groups and dielectric constant on the reaction are also discussed. 相似文献
93.
Kumon M Machida S Suzuki M Kusai A Yonemochi E Terada K 《Chemical & pharmaceutical bulletin》2008,56(5):617-625
In our previous paper, we reported the inhalation properties of dry powder inhaler (DPI) formulations containing Compound A and mechanofusion-processed lactose carriers. The mechanofusion process with magnesium stearate (Mg-St) on the lactose carrier enhanced the fine particle fraction (FPF) value of the Andersen cascade impactor (ACI) study. The increase of FPF seemed to be associated with the increase of the dispersibility of drug particles. The objectives of this study were (1) to evaluate the applicability of lactose carrier mechanofusion-processed with Mg-St and (2) to examine the mechanism of FPF alteration by the mechanofusion process applied on the lactose carrier with or without additive. The inhalation profiles of DPI formulations containing four different pharmaceutical compounds were evaluated with an ACI. The dispersibility of the formulations was observed by particle size distribution measurement in the air stream and the adhesive force was measured bydirect separation method. It was found that higher FPF was obtained with lactose mechanofusion-processed with Mg-St as compared to control lactose carriers for all four compounds. This suggested that mechanofusion process with Mg-St is widely applicable in DPI formulations. The homogenization of surface adhesiveness was attributed to the increased FPF of the DPI including lactose mechanofusion-processed with Mg-St, as suggested by the combination of several physicochemical characteristics. Combination of different characterization methods would be of help to clarify the whole mechanism which defines the inhalation properties of DPI formulations. 相似文献
94.
95.
Yasuo Yoshihashi Etsuo Yonemochi Youri Maeda Katsuhide Terada 《Journal of Thermal Analysis and Calorimetry》2010,99(1):15-19
The induction period of crystallization of amorphous naproxen in solid dispersion was measured by DSC. Hydroxypropylmethylcellulose
acetate succinate LG (HPMCAS-LG) was selected as a polymer of solid dispersion, because of the excellent inhibitory effect
of crystallization. Naproxen was chosen as a model drug having poor water solubility and poor physical stability of glassy
state. The prediction of crystallization of amorphous naproxen in solid dispersion at the desired storage temperature or the
desired polymer content was carried out. If the storage condition satisfied the requirement that was either more than 90%
of HPMCAS-LG content at 333 K or below storage temperature of 301 K for 50% HPMCAS-LG content, the induction period of crystallization
of naproxen in solid dispersion would be more than 1 year. The storage period of amorphous drug in solid dispersion of desired
storage temperature and desired drug content might be predictable from measurement data of induction period of crystallization. 相似文献
96.
97.
98.
99.
Suzuki T Kikuchi H Yonemochi E Terada K Yamamoto K 《Chemical & pharmaceutical bulletin》2001,49(4):373-378
Microcrystalline cellulose (MCC) granules were prepared by wet granulation using a high-shear mixer. Physical characteristics of the granules were investigated using near IR spectrometry, thermogravimetry and isothermal water vapor adsorption. Near IR spectra of dried MCC granules prepared for various granulation times exhibited different peak intensities at 1428, 1772, and 1920 nm, which were assigned to functional groups of cellulose or water. On isothermogravimetric analysis, the rate of dehydration of water was shown to decrease with granulation time. These results suggest that the physical structure of MCC could change during the granulation process, and the interaction between MCC and water was gradually strengthened. The isothermal water vapor adsorption curves suggested that the amorphous region of MCC would be divided by the strong shear force of the impeller, because the high adsorption ability of intact MCC in the low humidity region was diminished in granules collected following 5 and 10 min of granulation. It was suggested that MCC formed a network which caught water within its structure during the wet granulation process. 相似文献
100.
Tsuneo Okubo Emi Itoh Akira Tsuchida Etsuo Kokufuta 《Colloid and polymer science》2006,285(3):339-349
Drying dissipative structural patterns of the thermosensitive gels of poly(N-isopropyl acrylamide) were studied on a cover glass. As the temperature of suspension and room rose from 25 to 50 °C, the small size of drying pattern area extended to the beautiful flickering spoke-like ones transitionally at the critical temperature ca. 35 °C. The principal patterns at 25 °C were the single or multiple broad rings of the hill accumulated with the gels. At 50 °C, on the other hand, the flickering spoke-like patterns were observed at the inner area of the broad ring especially at the gel concentrations higher than 1 × 10−3 g/ml. These observations support that the extended gels at low temperatures apt to associate weakly to each other, whereas the gels at high temperatures shrink and move rather freely with the convectional flow of water, though the very weak intergel attractions still remain. In the presence of sodium chloride at high temperatures, the cooperative patterns formed between the gel spheres and the salt. The gravitational and Marangoni convectional flow of the gels and the very weak interactions between the gels and substrate (cover glass) are important for the flickering spoke-like pattern formation. 相似文献