Effect of acidity of drugs on the prediction of human oral absorption by biopartitioning micellar chromatography

Biopartitioning micellar chromatography (BMC) is a potentially high throughput and low cost alternative for in vitro prediction of drug absorption, which can mimic the drug partitioning process in biological systems. In this paper, a data set of 56 compounds representing acidic, basic, neutral and amphoteric drugs from various structure classes with human oral absorption (HOA) data available were employed to show the effect of acidity of drugs in oral absorption prediction. HOA was reciprocally correlated to the negative value of the capacity factor (kBMC) determined by BMC at pH 7.4 and 6.5. The relationships between kBMC and the corresponding HOA values of all compounds were rather poor, but the correlations were improved when the acidity of drugs was taken into consideration. Moreover, the proposed models allowed obtaining of good predictive values for both highly and poorly absorbed compounds. It is demonstrated that the constructed models derived from compounds with the same kind of charge property are of more practically meaningful and rigorous.     

Preliminary study on Salvia miltiorrhiza bung endophytic fungus

Objective To select the strains which can produce tanshinone ⅡA like its host plant Salvia miltiorrhiza bung. Methods A total of 50 strains of endophytic fungi were isolated from healthy, living and symptomless tissues of Salvia miltiorrhiza bung, among which 29 strains were obtained from the root, 14 from the stem, 3 from the leaf, 3 from the flower and 1 from the seed. Their antimicrobial activities against nine different bacteria, including both Gram-negative and Gram-positive bacteria, were measured by Oxford plate agar diffusion bioassay. Results Our data showed that all but four strains had significant antibacterial activities on at least one indicator bacterium to some extent, and five strains (DR1, DR4, DR16, DR18 and DF2) manifested quite prominent antibacterial activities against certain pathogenic bacteria. In some degree, it might indicate that this endophytic fungus isolated from the tissues of Salvia miltiorrhiza bung has a potential value as a natural antibacterial medicine as well. Thin layer chromatography (TLC) and high-performance liquid chromatography (HPLC) were carried out to test selected strains, both inside and outside of the cell to see if any strain can produce tanshinone ⅡA. The result showed that extracts from three strains, labeled as DR12 (outside cell), DR21 (inside cell) and DF3 (inside cell), had a component with the same Rf value in TLC assay as that of authentic tanshinone ⅡA. The extract from DR12 (outside cell) and DR21 (inside cell) had a peak at retention time identical to that of authentic tanshinone ⅡA in HPLC. Conclusion The fungi appear to produce the bioactive compound tanshinone ⅡA, and they could be used to produce tanshinone ⅡA by fermentation. It provides a new way to synthesize this natural medicine.     

老年人与药物不良反应

文章针对老年人生理和脏器功能的逐年衰退，对药物的吸收，分布，代谢和排泄也逐渐减慢。为了保障老年人的用药安全，避免药物不良反应，列举了部分合理用药的方法和注意要点。     

锰中毒治疗的研究

慢性锰中毒治疗以驱锰、DA替代疗法为主，物理治疗为辅。CaNa2EDTA仅适用于早期轻症锰中毒的治疗，L-dopa对具有肌肉僵直及肌张力障碍的锰中毒治疗有效，但这2药易出现副作用。PAS-Na治疗锰中毒有一定的近期疗效，远期疗效未见报道。辅助治疗的一些药物、保健品和物理疗法尚属探讨性研究，有待进一步验证。     

高压氧对小鼠S—180肉瘤化学治疗增效作用的研究（论著）

目的：探讨高压氧（ＨＢＯ）对荷Ｓ－１８０肉瘤小鼠在化学治疗中的增效作用及其机理。方法：２４０只荷Ｓ－１８０肉瘤的ＩＣＲ小鼠被随机等分为不治疗对照组、高压氮氧组、ＨＢＯ组、ＳＯＤ－ＨＢＯ组、ＨＢＯ－平阳霉素组、ＨＢＯ－环磷酰胺组、平阳霉素组和环磷酰胺组共８个组。分别使用化学治疗结合ＨＢＯ疗法，采用电子自旋共振（ＥＳＲ）技术直接检测Ｓ－１８０肉瘤组织中的氧自由基（ＯＦＲ）含量，并应用分光光度计法测定其     

2008～2010年我院烧伤科抗菌药物利用分析

对2008～2010年我院烧伤科抗菌药物的用药数据进行调查分析,结果表明抗菌药物用药频率排序前3位的分别是头孢哌酮-舒巴坦、头孢他啶、替硝唑,日均用药金额排序前3位的分别是亚胺培南-西司他丁、美罗培南、氨曲南。我院烧伤科抗菌药物的使用基本合理,日均用药金额呈不同程度的下降,但需进一步加强监督和管理。