硫酸沙丁胺醇脉冲释药微丸的制备及其体外释药研究

Preparation of Salbutamol Sulfate Pulsatile Release Pellet and study on its release in vitro

目的研究硫酸沙丁胺醇脉冲释药微丸的制备方法及其体外释放。方法用空白丸芯依次进行含药层(SBA),溶胀层(低取代羟丙纤维素)及控释层(乙基纤维素水分散体)包衣制备硫酸沙丁胺醇脉冲释药微丸。采用紫外法和蓝法考察含药层、溶胀层及控释层在生理盐水中药的体外释放。结果含药层在生理盐水中能正常释药,溶胀层和控释层的增重对脉冲释药微丸的释药时滞和释药速率均有明显影响,溶胀层包衣增重15%,控释层包衣增重20%所制成释药微丸,释药时滞时间约为4.1 h时,这正好对应哮喘患者清晨2∶00发作时晨。结论所制备的硫酸沙丁胺醇脉冲释药微丸具有体外脉冲释药特性,适合哮喘患者预防用药。

Objective To investigate the preparing method of Salbutamol Sulfate Pulsatile Release Pellets and its release in vitro. Methods Salbutamol Sulfate Pulsatile Release Pellets were prepared by using black core coated with Salbutamol Sulfate as drug containing layer （SBA）, swelling agent layer （L-HPC） and controlled-release layer （ethylcellulose aqueous dispersion）. The release properties in vitro of drug containing layer, swelling agent layer and controlled-release layer were studied by using UV method and basket method. Results Drug containing layer could release active ingredients normally into normal saline. The increased weight of swelling agent layer and controlled-release layer had obviously influences on lag time and velocity of drug release. Weights of swelling agent layer and controlled release layer were increased by 15% and 20%, respectively. The lag time was about 4.1 h for the prepared drug release pellets, matching with the fact that asthma usually attacked at 2：00 in the morning. Conclusion The prepared Salbutamol Sulfate Pulsatile Release Pellet can release drugs in vitro in pulsatile style, and it is appropriate to be used as preventive drugs for asthma patients.