Optimum spray congealing conditions for masking the bitter taste of clarithromycin in wax matrix.
Optimum spray congealing conditions for masking the bitter taste of clarithromycin in wax matrix.
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掩盖蜡基质中克拉霉素苦味的最佳喷雾凝结条件。
DOI：
10.1248/cpb.47.220
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发表时间：
1999
影响因子：
1.7
通讯作者：
S. Itai
中科院分区：
文献类型：
--
作者：
T. Yajima;N. Umeki;S. Itai
考察了喷雾-冷冻工艺中操作条件对克拉霉素蜡基质释放度和微粒体性质的影响。用喷雾干燥器在各种雾化器轮速度和液体进料速率下制备含有30%CAM、60%单硬脂酸甘油酯（GM）和10%甲基丙烯酸氨基烷基酯共聚物E（AMCE）的CAM蜡基质。CAM从基质中的释放表现出两相模式，这可能是由于基质表面上破裂的精细部分的溶解。随后释放模式的斜率和外推y轴截距分别定义为CAM从基质中的释放速率和初始释放量。选择这些释放参数以及基质的体积中值直径和比表面积作为响应变量，并进行多元回归分析。对于比表面积和初始释放量，当雾化轮速度恒定且液体进料速率变化时，轮廓曲线上观察到最小点。对于释放速率，在相同条件下在等高线曲线上观察到最大点。认为这些点对于掩蔽CAM制剂的苦味是优选的。显微镜观察表明，在较高的雾化轮转速和最佳的液体进料速率下，可以获得具有光滑表面的小球形基质。该基质还具有优异的掩味性能，具有小的初始释放量和随后的高释放速率。因此，融化液滴的凝结速度是掩盖CAM苦味的主要因素。
The effects of operating conditions in the spray-congealing process on the release and the micromeritic properties of clarithromycin (CAM) wax matrix were evaluated. CAM wax matrix with 30% CAM, 60% glyceryl monostearate (GM) and 10% aminoalkyl methacrylate copolymer E (AMCE) was manufactured at various atomizer wheel speeds and liquid feed rates with a spray dryer. Release of CAM from the matrix exhibited a two-phase pattern, probably due to the dissolution of the fine portions broken on the surface of the matrix. The slope and the extrapolated y-intercept of the subsequent release pattern were defined as the release rate and the initial amount of release of CAM from the matrix, respectively. These release parameters, as well as the volume median diameter and the specific surface area of matrix, were selected as response variables, and multiple regression analysis was performed. For specific surface area and initial amount of release, a minimum point was observed on the contour curve when the atomizer wheel speed was constant and the liquid feed rate was varied. For the release rate, a maximum point was observed on the contour curve under the same conditions. These points were considered preferable for masking the bitter taste of CAM preparation. Microscopic observation revealed that a small spherical matrix with a smooth surface could be obtained with a high atomizer wheel speed and optimum liquid feed rate. This matrix also possessed excellent properties for taste masking, with small initial amount of release and subsequent high rate of release. In conclusion, the congealing speed of melt droplets was the dominant factor in masking the bitter taste of CAM.