Cocrystallization of Loratadine With Succinic Acid Using Neat Grinding Method
Cocrystallization of Loratadine With Succinic Acid Using Neat Grinding Method
复制标题
纯磨法共结晶氯雷他定与琥珀酸
DOI：
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发表时间：
2019
期刊：
影响因子：
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通讯作者：
D. P. Paramita
中科院分区：
文献类型：
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作者：
D. Setyawan;E.R.D. Pravianti;K. D. Pratiwi;D. Isadiartuti;D. P. Paramita
为了改善氯雷他定（L）水溶性差的问题，采用丁二酸（SA）制备了氯雷他定（L）共晶。采用净研磨法，以1：1（CC 1）和1：2（CC 2）的摩尔比制备，因此，在游离CO2水溶液中表征了两者的理化性质和体外溶出度。CC 1的DSC热谱图在116.8°C处显示单一吸热峰，CC 2在90.2和152.2°C处观察到两个峰，L在137.5°C处观察到一个峰。此外，XRPD的结果显示，在2θ 21.93°和21.88°处分别出现了一个新峰，而在两种制剂的FTIR光谱中均发现了C=O和-OH带位移。SEM显微照片显示，与氯雷他定相比，氯雷他定的粒径减小，但习性没有改变，而物理化学表征证实了氯雷他定与琥珀酸的不完全共晶形成，这有助于提高溶出效率（DE 15）。
Cocrystal of loratadine (L) was produced using succinic acid (SA), in order to improve the poor aqueous solubility profile. This was prepared in molar ratio of 1:1 (CC1) and 1:2 (CC2), applying the neat grinding method, therefore, the physicochemical properties and in vitro dissolution of both were characterized in free CO2 aquadest. The thermogram DSC of CC1 exhibited single endothermic peak at 116.8°C, two peaks were seen in CC2, at 90.2 and 152.2°C, and L had one, at 137.5°C. In addition, the results of XRPD showed a new peak at 2θ 21.93° and 21.88°, respectively, while C=O and –OH band shifts were identified in the FTIR spectra of both preparations. SEM photomicrographs revealed particle size reduction without habit alteration, while physicochemical characterization confirmed the incomplete cocrystal formation of loratadine with succinic acid, which promotes efficiency dissolution (DE15), in contrast with loratadine.