合成8-氯-10，11-二氢-4-氮杂-5H-二苯并[a，d]-5-环庚酮研究进展

介绍了氯雷他定的重要中间体8-氯-10,11-二氢-4-氮杂-5H-二苯并[a,d]-5-环庚酮的基本性质和用途,叙述了以2-溴-3-甲基吡啶、2-[（叔丁基氨基）]-3-甲基吡啶、3-甲基吡啶甲酸和3-吡啶甲酸乙酯为原料出发的合成方法。     

高效液相色谱法测定氯雷他定片溶出度

目的 采用高效液相色谱法(HPLC)测定氯雷他定片的溶出度.方法 色谱柱:Agilent C18柱(4.6 mm× 150 mm,5 μm)色谱柱;流动相:磷酸盐缓冲液(取磷酸氢二钾2.28 g,加水800 mL溶解,磷酸调pH6.0,加水至1000 mL)-甲醇(20∶80);检测波长247 nm;流速1.0 mL/min;进样量20μL.结果 氯雷他定在0.1～10 μg/mL浓度范围内呈良好的线性关系(R=0.9998),平均回收率99.09％,RSD=0.4％(n=6).结论 此法可排除辅料对溶出度的影响,可用于该制剂的质量控制.     

Continuous nanoparticles production through a combination of a micro electro mechanical system and an electromagnetic resonator cavity

In the present work, a reliable, rapid, and controllable method is developed for the continuous generation of pharmaceutical curcumin and loratadine nanoparticles (NPs). Micro droplets of curcumin and loratadine were generated by atomization of their corresponding solutions by a combination of a micro electro mechanical system and an electromagnetic resonator cavity. After evaporation of the solvent of micro droplets by electromagnetic waves, the NPs were collected by a polytetrafluoroethylene (PTFE) filter. NPs were characterized by scanning electron microscopy. Results showed that this method can be an effective way to produce amorphous NPs with narrow particle size distribution, where particle size can be easily controlled by solution concentration. Particles size varies from 152 to 446?nm and from 116 to 719?nm for loratadine and curcumin, respectively.     

Development of the loratadine gel for enhanced transdermal delivery

Background: The oral administration of loratadine, an antihistamine, can have a variety of adverse side effects, such as headache, fatigue, and nausea, because of the transient high blood concentration. To avoid these effects, loratadine can be administered using a transdermal drug delivery system. Method: This study examined the effects of the drug concentration on drug release from prepared hydroxypropyl methylcellulose gels using a synthetic cellulose membrane at 37°C. The drug concentrations tested were 0.1%, 0.2%, 0.3%, 0.4%, and 0.5% (w/w). The effect of temperature on drug release from the 0.3% loratadine gels was evaluated at 27°C, 32°C, 37°C, and 42°C. Various types of penetration enhancers, such as glycols, glycerides, propylene glycol derivatives, nonionic surfactants, and fatty acids, were incorporated in the gel formulation to increase the level of drug permeation. Results: The rate of drug release increased with increasing drug concentration or temperature. The activation energy for the release of the drug was 5.714 kcal/mol for 0.3% loratadine gel. Among all the enhancers used in this study, polyoxyethylene 2-stearyl ether showed the best enhancing effect. The enhancement factor of the loratadine gel containing the polyoxyethylene 2-stearyl ether was 2.03 compared with that of the loratadine system containing no enhancer. Conclusions: These results suggest that the topical gel formulation of loratadine containing a penetration enhancer could be developed to enhance the penetration of loratadine.     

太赫兹光谱技术在药物定性定量检测上的应用

为判断药物的真伪,检查药物的纯度,以及克服目前化学药物定性定量检测中耗时长、损耗样本、操作繁琐等缺陷,提出了一种基于太赫兹光谱技术的快速且能准确定性和定量药物的检测方法。基于太赫兹吸收光谱,提取了氯雷他定、消旋卡多曲的特征峰频点以及峰下面积差特征,并通过这些信息来对药物进行定性与定量检测。实验结果表明：在定量检测中,太赫兹光谱技术具有高的稳定性及检测精度;质量分数梯度变化的线性拟合相关系数达到99.8%;在结合主成分分析法（principal component analysis,PCA）对其他药物的检测中,太赫兹光谱技术定性检测准确率可达100%,定量检测误差小于0.01。这些结果可为后续药物的快速、准确和无损检测提供参考。