KIMS University and College of Pharmacy, Karad, Maharashtra, India.
Drug Dev Ind Pharm. 2010 Sep;36(9):1036-45. doi: 10.3109/03639041003642065.
Pharmaceutical cocrystallization is a promising alternative for improving the solubility and dissolution rate or manipulating other physical properties of active pharmaceutical ingredients. The objective of this investigation was to study the effect of cocrystallization with different cocrystal formers on physicochemical properties of mefloquine hydrochloride.
Cocrystals were prepared by solution crystallization method--mefloquine hydrochloride (414.8 mg, 1 mmol) and different cocrystal formers (1/2 mmol) were dissolved in 20 mL of ethanol with warming. Solution was cooled in ice bath for 6 hours. The crystals were isolated by filtration through a membrane (0.45 microm) and dried in the air. The pure drug and the prepared cocrystals were characterized in terms of saturation solubility, drug content, infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, in vitro dissolution studies, and stability studies.
The cocrystals showed enhanced solubility and dissolution rate. The cocrystals were found to be stable over the period of 6 months confirmed from stability studies.
Cocrystals resist the conversion of anhydrous form of drug into its hydrate which is responsible for the drugs less solubility and dissolution rate.
药物共晶是一种很有前途的方法，可以用来提高活性药物成分的溶解度和溶解速率，或者控制其他物理性质。本研究的目的是研究与不同共晶形成剂共晶化对盐酸甲氟喹理化性质的影响。
采用溶液结晶法制备共晶——将盐酸甲氟喹（414.8mg，1mmol）和不同的共晶形成剂（1/2mmol）溶于 20mL 加热的乙醇中。将溶液在冰浴中冷却 6 小时。通过膜（0.45μm）过滤分离晶体，并在空气中干燥。采用饱和溶解度、药物含量、红外光谱、差示扫描量热法、粉末 X 射线衍射、扫描电子显微镜、体外溶出度研究和稳定性研究对纯药物和制备的共晶进行了表征。
共晶显示出增强的溶解度和溶解速率。稳定性研究证实，共晶在 6 个月的时间内是稳定的。
共晶抑制了药物无水形式向水合物的转化，这是导致药物溶解度和溶解速率低的原因。
