School of Pharmacy, Sungkyunkwan University, Suwon, Gyeonggi-do, 16419, Republic of Korea.
Drug Deliv Transl Res. 2018 Jun;8(3):552-564. doi: 10.1007/s13346-018-0477-9.
In this study, using the melt-adsorption method, we developed sustained-release microparticles containing the potent drug, tamsulosin HCl, for use as orally disintegrating tablets. A high-speed kneading granulator was used, enabling temperature modulation and uniform material distribution. A lipid and ethylcellulose suspension (Surelease®) was applied to retard drug release, and magnesium aluminometasilicate (Neusilin®) was used as adsorbent. Among various lipid candidates for melt-adsorption, beeswax and glyceryl behenate were selected due to their high mechanical strength. Hot stage microscopy and powder X-ray diffraction analysis results showed compatibility between tamsulosin HCl and both lipids. Characteristic adsorption behavior was observed depending on the physicochemical properties of each composition. Especially, the specific surface area of Neusilin® decreased with increasing amounts of Surelease®, attributed to the pore-covering effect of Surelease®, which significantly increased the size of the microparticles after the lipid adsorption. For a Surelease®-to-beeswax ratio 1:50, both the desired particle size distribution and low burst release were achieved. Furthermore, the orally disintegrating tablet containing optimized microparticles had acceptable tablet hardness and rapid disintegration. Herein, the feasibility of melt-adsorption for the preparation of sustained-release microparticles was well demonstrated. With its convenience and efficiency, the proposed method is a promising alternative to conventional methods, which are relatively difficult and time consuming.
在这项研究中，我们使用熔融吸附法开发了含有强效药物盐酸坦索罗辛的缓释微球，用作口服崩解片。使用高速捏合造粒机进行了实验，该设备能够实现温度调节和均匀的物料分布。使用脂质和乙基纤维素混悬液（Surelease®）来延缓药物释放，并用硅酸镁铝（Neusilin®）作为吸附剂。在用于熔融吸附的各种脂质候选物中，由于其高机械强度，选择了蜂蜡和氢化蓖麻油酸甘油酯。热台显微镜和粉末 X 射线衍射分析结果表明盐酸坦索罗辛与两种脂质均具有相容性。根据每种成分的物理化学性质，观察到了特征吸附行为。特别是，Neusilin®的比表面积随 Surelease®用量的增加而减小，这归因于 Surelease®的孔覆盖效应，这显著增加了脂质吸附后的微球尺寸。对于 Surelease®与蜂蜡的比例为 1:50，既实现了所需的粒径分布，又实现了低突释。此外，含有优化微球的口服崩解片具有可接受的片剂硬度和快速崩解。本文充分证明了熔融吸附法制备缓释微球的可行性。该方法具有方便、高效的特点，是传统方法的一种有前途的替代方法，传统方法相对困难且耗时。
