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。

To study the intestinal absorption characters of cefixime (Cef) and the factors affecting Cef absorption. METHODS: A rat intestine loop in situ technique was used to investigate the disappearance rate of Cef from the intestine. Cef concentration in the flux was measured by the reversed phase HPLC. RESULTS: Cef was mainly absorbed from the upper part of the intestine. Its disappearance rate was apparently pH—dependent l(5.8±0.6) nmol•h-1/(g wet tissue)at pH 7.4, (8.9±1.4) nmol•h/(g wet tissue)at pH 5.0, P<0.05) ]. The uptake rate of Cef was curvilinear at 0. 01-0. 5 mmol•L-1. The values of apparent Kt, Jmax, and Kd were 0.114 mmol, 78.41nmol•h-1/(g wet tissue), and 43.70 nmol•h-1•mmol-1/(g wet tissue), respective-ly. Sodium edetate markedly promoted the disappearance rate of Cef from the intestine. CONCLUSION: Cef was transported partly via carrier-mediated transport system and partly via the paracelMar transport system.

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.

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.