School of Pharmacy and Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Islamic Republic of Iran.
Pharm Dev Technol. 2011 Jun;16(3):243-9. doi: 10.3109/10837451003610837. Epub 2010 Feb 22.
Spherical crystallization (SC) of carbamazepine (CBZ) was carried out for preparation of the agglomerates using the solvent change method. The potential of the intraagglomerate addition of sodium starch glycolate (SSG) as a disintegrant agent and povidone (PVP) as a hydrophilic polymer was also evaluated. The process of SC involved recrystallization of CBZ and its simultaneous agglomeration with additives. An ethanol:isopropyl acetate:water system was used where isopropyl acetate acted as a bridging liquid and ethanol and water as good and bad solvents, respectively. The agglomerates were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (XRPD), and Scanning electron microscopy and were evaluated for yield, flowability, disintegration time and drug release. CBZ agglomerates exhibited significantly improved micromeritic properties as well as dissolution behavior in comparison to conventional drug crystals. The dissolution rate of drug from agglomerates was enhanced by inclusion of SSG, while addition of PVP to CBZ/SSG agglomerates led to reduction in the release rate of CBZ even below that of the conventional drug crystals. SC process can be considered as a suitable alternative to conventional granulation process to obtain agglomerates of CBZ with excipients with improved micromeritic properties and modified dissolution rate.
采用溶剂变化法进行卡马西平（CBZ）的球晶化（SC），以制备团聚物。还评估了内团聚体添加交联羧甲淀粉钠（SSG）作为崩解剂和共聚维酮（PVP）作为亲水性聚合物的潜力。SC 过程涉及 CBZ 的重结晶及其与添加剂的同时团聚。使用乙醇：异丙基乙酸酯：水体系，其中异丙基乙酸酯作为桥接液体，乙醇和水分别作为良溶剂和不良溶剂。通过差示扫描量热法（DSC）、粉末 X 射线衍射（XRPD）和扫描电子显微镜对团聚物进行了表征，并对其产率、流动性、崩解时间和药物释放进行了评价。与常规药物晶体相比，CBZ 团聚物表现出明显改善的微粉学性质和溶解行为。SSG 的加入提高了药物从团聚物中的释放速率，而 PVP 的加入则导致 CBZ/SSG 团聚物中 CBZ 的释放速率降低，甚至低于常规药物晶体。SC 工艺可以被认为是替代传统制粒工艺的合适方法，以获得具有改善的微粉学性质和改良的溶解速率的 CBZ 团聚物。
