Center for Drug Research and Development (CIDEM), Ave 26 No.1605, e/ Boyeros and Puentes Grandes, Plaza de la Revolución, Havana City CP 10400, Cuba.
Institute of Pharmaceutical and Food Sciences (IFAL), University of Havana, Street 23 # 21425 be/214 and 222, La Lisa, Havana City CP 13600, Cuba.
Mar Drugs. 2021 Jun 6;19(6):329. doi: 10.3390/md19060329.
We investigated a spray drying process for preparing water-soluble salts of high molecular weight chitosan (CH) intended for pharmaceutical excipient applications. CH was derived from chitin of marine lobster origin (). The effects of organic acid (acetic or lactic acid) and the ratio (difference) of inlet/outlet air temperature (140/90 °C or 160/100 °C) on spray drying were studied. The yield of spray-dried CH salt powders ranged from 50% to 99% in laboratory and industrial-scale processes. The spray-dried dry powder of CH salts consisted of spherical agglomerated particles with an average diameter of 36.2 ± 7.0 µm (CH acetate) and 108.6 ± 11.5 µm (CH lactate). After dispersing the spray-dried CH salt powder samples in purified water, the mean particle sizes obtained for the CH acetate salts were 31.4 nm (batch A001), 33.0 nm (A002) and 44.2 nm (A003), and for the CH lactate salts 100.8 nm (batch L001), 103.2 nm (L002) and 121.8 nm (L003). The optimum process conditions for spray drying were found: an inlet air temperature of 160 ± 5 °C, an outlet temperature of 100 ± 5 °C and an atomizer disk rotational speed of 18,200 min. The X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) results confirmed the amorphous state of the CH salts. The H nuclear magnetic resonance (NMR) and Fourier transform infrared (FT-IR) spectra of CH acetate and lactate salts verified that the spray drying process does not affect the polymer backbone. In conclusion, both laboratory and industrial-scale spray drying methods for preparing water-soluble acid salts of CH are reproducible, and the physicochemical properties of the corresponding CH acid salts are uniform.
我们研究了一种喷雾干燥工艺，用于制备水溶性高分子量壳聚糖（CH）盐，用作药物赋形剂。CH 由来自海洋龙虾的壳聚糖（）衍生而来。研究了有机酸（乙酸或乳酸）和进出口空气温度比（140/90°C 或 160/100°C）对喷雾干燥的影响。在实验室和工业规模的过程中，喷雾干燥 CH 盐粉末的产率范围为 50%至 99%。CH 盐的喷雾干燥干粉由平均直径为 36.2±7.0μm（CH 乙酸盐）和 108.6±11.5μm（CH 乳酸盐）的球形团聚颗粒组成。将喷雾干燥的 CH 盐粉末样品分散在纯化水中后，CH 乙酸盐的平均粒径分别为 31.4nm（A001 批）、33.0nm（A002 批）和 44.2nm（A003 批），CH 乳酸盐的平均粒径分别为 100.8nm（L001 批）、103.2nm（L002 批）和 121.8nm（L003 批）。喷雾干燥的最佳工艺条件为：进口空气温度 160±5°C，出口温度 100±5°C，雾化器盘转速 18200min。X 射线粉末衍射（XRPD）和差示扫描量热法（DSC）结果证实 CH 盐为无定形状态。CH 乙酸盐和乳酸盐的 H 核磁共振（NMR）和傅里叶变换红外（FT-IR）谱证实，喷雾干燥过程不影响聚合物主链。总之，制备水溶性 CH 酸盐水溶性盐的实验室和工业规模喷雾干燥方法具有重现性，相应 CH 酸盐水溶性盐的物理化学性质均匀。
