Phenoporlamine hydrochloride is a novel compound that is used for the treatment of hypertension. The purpose of this study was to develop a sustained release tablet for phenoporlamine hydrochloride because of its short biological half-life. Three floating matrix formulations of phenoporlamine hydrochloride based on gas forming agent were prepared. Hydroxypropyl methylcellulose K4M and Carbopol 971P NF were used in formulating the hydrogel drug delivery system. Incorporation sodium bicarbonate into matrix resulted in the tablet floating over simulated gastric fluid for more than 6 h. The dissolution profiles of all tablets showed non-Fickian diffusion in simulated gastric fluid. Moreover, release of the drug from these tablets was pH-dependent. In vivo evaluations of these formulations of phenoporlamine hydrochloride were conducted in six healthy male human volunteers to compare the sustained release tablets with immediate release tablets. Data obtained in these studies demonstrated that the floating matrix tablet containing more Carbopol was capable of sustained delivery of the drug for longer periods with increased bioavailability and the relative bioavailability of formulation (containing 25% Carbopol 971P NF, 8.3% HPMC K4M) showed the best bioequivalency to the reference tablet (the relative bioavailability was 1.11

茵陈蒿含有香豆索类、色原酮和黄酮类等活性成分，除具有利保保肝作用外，还有镇痛、消炎、降血脂、增强免疫、抗肿瘤作用，值得进一步开发研究。

目的介绍差示扫描量热法（DSC）在蛋白质热变性研究中的应用。方法 以大量具有代表性的文献为依据，讨论如何 运用DSC技术研究蛋白质热变性的原因与影响因素及蛋白质热变性与生理活性的关系。结果与结论DSC在蛋白质热变性研究中的应用有广阔的发展前景。

随着人类社会的老年化，骨质疏松症逐渐成为大众所关注的健康问题。相对其他治疗药物，降钙素由于其有效性和安全性，在抗骨质疏松症治疗的药物中越来越受到重视。现对其结构式、已上市品种及最新给药系统的研究情况及其进展进行了综述。

利用大鼠在体回豌模型，在不同的pH条件下，对酚红的小肠吸收进行了研究。发现酚虹虽然为一离子型的药物，在小肠仍有一定的吸收，其吸收速率为：十二指肠>空肠>回肠>结肠。酚红的吸收受小肠内Ca2+浓度的影响。加入EDTA-Na：能够显著促进酚红的小肠吸收和结肠吸收。实验结果证明：酚红不宜用来标示在体小肠吸收试验中回流液的体积变化。

使用Simplex Lattice统计优化方法，对炎痛喜康透皮吸收剂的处方进行了优选。在3因素4水平上．通过7次实验，结合微机编程外推至200次以上的指标响应范围，得出最优化处方。并经实验证明预测的响应指标——剥离牯性、表面粘性、透皮量与实验值吻合性好，这说明SimplexLattice适用于炎痛喜康透皮吸收剂的背材的体外优化。

The aim of this work was to study the influence of the concentration and molecular weight ofpoly (DL-lactide)(PLA)on the characteristics and in vivo biological activ-iry of protein-loaded microspheres. At the same time, an attempt was made to achieve further optimization of the formulation. In the stuay, insulin was choosen as a model of protein drugs. Nine formulations of injectable insulin-loaded PLA microspheres were prepared using all emulsification and solvent evaporation pro-cess according to a factorial design. The trapping efficiency, drug loading, and the drop percentages of blood glucose levels at 24 hr and 72 hr in mice were used to evaluate the foFmulations. The results showed that PLA molecular weig•ht and, especially, PLA concentration exerted influences on the characteristics and in vivo biological activity of insulin. 10aded microspheres. The drug-trapping efficiency in-creased with the increase ofthe polymer concentration. The drug loading decreased with the increase of the polymer concentration and was not obviously affected by PLA molecular weight. The drop percentage of blood glucose level at 24 hr in-creased with the increase of polymer concentration and molecular weight. At 72 hr, the drop percentages of blood glucose levels were slightly increased with the increase of PLA concentration and then significantly decreased after the PLA con-centration was above 150 mg/ml An optimizedformulation was prepared with PLA-

The crystal structure of the title compound, C18H18FN3O4, was published [Li et al. (2005). Acta Cryst. E61, o2235–o2236] with an error in the chemical formula and without location of the carboxyl H atom. This has now been corrected. The missing H atom was located and refined. This H atom is involved in an intramolecular O—HO hydrogen bond with the carbonyl Oatom.

The aim of this study was to Investigate the effect of water. soluble macromolecular components of Artemisia capillaris Thunberg (ACT) on human hepatoma cell line SMMC-7721 (SMMC-7721). The morphological changes of SMMC-7721 were obsem'ed under a light microscope and an elec-tron microscope. Inhibition of proliferation was measured with a color；metric MTT assay, It was discovered that ACT extract-treated. cells exhibit morphological changes typical of apoptosis， including condensed ehromatin and a reduction In volume. ACT extract at 25-200 ug/ml dos-dependently inhibited the proliferation of SMMC-7721. The 50% effective dose, evaluated on day 3 of exposure to the extract. Was 64.52+3.53/ug/ml. Upon gel electrophoresis，the fragmented DNA showed a characteristic ladder pattern•CHI cycle analyses revealed that ACT induced cell cycle arrest at the GJG J phase.

多肽及蛋白质药物口服吸收困难，但最近的一系列研究表明：一些小分子化合物可以大大提高此类活性大分子药物的口服吸收。本文综述了近年来在此方面的研究进展，包括这些小分子化合物的品种、构效关系、作用机制及应用前景。