Evaluation on contribution rate of each component total salvianolic acids and characterization of apparent oil/water partition coefficient / 中国中药杂志

The difference between three representative components of total salvianolic acids in pharmacodynamic activity were compared by three different pharmacological experiments: HUVECs oxidative damage experiment, 4 items of blood coagulation in vitro experiment in rabbits and experimental myocardial ischemia in rats. And the effects of contribution rate of each component were calculated by multi index comprehensive evaluation method based on CRITIC weights. The contribution rates of salvianolic acid B, rosmarinic acid and Danshensu were 28.85%, 30.11%, 41.04%. Apparent oil/water partition coefficient of each representative components of total salvianolic acids in n-octyl alcohol-buffer was tested and the total salvianolic acid components were characterized based on a combination of the approach of self-defined weighting coefficient with effects of contribution rate. Apparent oil/water partition coefficient of total salvianolic acids was 0.32, 1.06, 0.89, 0.98, 0.90, 0.13, 0.02, 0.20, 0.56 when in octanol-water/pH 1.2 dilute hydrochloric acid solution/ pH 2.0, 2.5, 5.0, 5.8, 6.8, 7.4, 7.8 phosphate buffer solution. It provides a certain reference for the characterization of components.

Solidifying of ginkgo flavones phospholipid complex using colloidal silica / 中草药

Objective: To prepare ginkgo flavones phospholipid complex (GF-PC) and to solidify it using colloidal silica (CS). Methods: CS was used as a carrier to solidify GF-PC. The structures of the phospholipid complex and solidified powder were also characterized by differential scanning calorimetry, X-ray diffractomer, and scanning electron microscope, and dissolution in vitro and fluidity were also investigated. Results: The phase analysis indicated that ginkgo flavones existed in the phospholipid complex and solidified powder as amorphous state. Dissolution in vitro showed that the solidified powder could effectively promote the drug dissolution. Conclusion: The process of the solidified powder is simple and convenient. The powder prepared can significantly improve the fluidity of the GF-PC and promote the dissolution in vitro.

Study on tripterin sustained-release dropping pills / 中草药

Objective: To prepare the Tripterin Sustained-release Dropping Pills (TSRDPs), investigate the disperse state and in vitro release, and optimize the preparation technology. Methods: The TSRDPs were prepared by solid dispersion method with PEG 4000 and glycerol monostearate (GM) as carrier materials. Orthogonal design was conducted to explore the influencing factors of the preparation technology by evaluating the indexes of roundness and weight difference. Results: The ideal condition of TSRDPs: the ratio of tripterin-GM-PEG 4000 was 1:3:7; the temperature of drug mixture was 80 °C; dropping speed was 20 d/min; dropping distance was 5 cm; and the condensate temperature was 15 °C. Tripterin existed as amorphous state in carriers. The maximum cumulative release amount of tripterin was 91.2% at 12 h. Conclusion: The prepared TSRDPs have a good sustained-release effect.

Preparation of self-assembled beads drug delivery system of tripterine based on cyclodextrin and oil as well as its in vitro evaluation / 中草药

Objective: To prepare the self-assembled beads drug delivery system of triptrine based on cyclodextrin and oil, and to carry out its in vitro evaluation. Methods: The beads were prepared by a continuously shaking starting from a mixture of cyclodextrin aqueous solution and oil. The bead diameter and drug distribution were investigated by microscopic observations, and drug disperse state was observed by differential scanning calorimetry (DSC). The drug-loading and entrapment efficiency of tripterine in beads were investigated by HPLC. The in vitro dissolution of tripterine in beads was also determined. Results: The diameter was in the range of (1.49 ± 0.20) mm. The drug-loading and encapsulation efficiency of the prepared beads were (87.21 ± 0.58) μg/g and (80.14 ± 1.24)%, respectively. DSC suggested that tripterine existed as amorphous form in beads. Confocal microcopy showed that the hydrophobic drug was localized inside the beads. The maximum cumulative release amount of tripterine in simulated intestinal fluid was more than 80% at 6 h. Conclusion: The formulation and preparation process are practical and simple, and these beads have great potentialities for carrying hydrophobic drug.

Polybasic research on the biopharmaceutical characteristics of 20 (S)-protopanaxadiol / 药学学报

In this study, the biopharmaceutical properties of 20 (S)-protopanaxadiol (PPD) were studied. Firstly, the equilibrium solubility and apparent oil/water partition coefficient of PPD were used to predict the absorption in vivo. Meanwhile the membrane permeability and absorption window were studied by Caco-2 cell model and single-pass intestinal perfusion model. Furthermore, the bioavailability and metabolism were combined to study the absorption properties and metabolic properties in vivo. All of them were used to provide theoretical and practical foundation for designing PPD preparation. The results showed that PPD is poorly water-soluble, and the equilibrium solubility in water is only 35.24 mg x L(-1). The oil-water partition coefficient is 46.21 (logP = 1.66). By Caco-2 cell model, the results showed PPD uptake in general, and it also has efflux. By in situ intestinal perfusion model, the results showed that the absorption of PPD in the intestine is good, and the effective permeability coefficient were duodenum > jejunum > ileum > colon. The oral bioavailability of PPD was 29.39%. It was not well. Metabolic studies showed PPD in vivo presented a wide spread metabolism. So the main factors that restricted oral bioavailability of PPD were the poor solubility and first-pass effect.

Study on dosage form design for improving oral bioavailability of traditional Chinese medicines / 中国中药杂志

Both chemical drugs and traditional Chinese medicines have the problem of low bioavailability. However, as traditional Chinese medicines are a multi-component complex, their dosage forms are required to be designed in line with their characteristics, in order to improve the bioavailability of traditional Chinese medicines. Traditional Chinese medicines are mostly prepared into pill, powder, paste, elixir and decoction, but with such drawbacks as high administration dose and poor efficacy. With the process of modernization of traditional Chinese medicines, new-type preparations have be developed and made outstanding achievements. However, they fail to make an organic integration between traditional Chinese medicine theories and modern preparation theories. Characteristics of traditional Chinese medicines are required to be taken into account during the development of traditional Chinese medicines. In the article, multi-component preparation technology was adopted to establish a multi-component drug release system of traditional Chinese medicines on the basis of multiple components of traditional Chinese medicines.

Establishment of modern multi-component sustained-release preparations of oral traditional Chinese medicines / 中国中药杂志

Traditional Chinese medicines have a long history, with a large quantity of efficient traditional Chinese medicines and prescriptions. However, the vast majority of pharmaceutical dose forms remain common preparations, with very few efficient, long-lasting and low-dose preparations. The sustain-release preparation allows sustained drug release in a longer period of time, maintains blood drug concentration, reduces the toxic effect and medication frequency, and improves medication compliance. Unlike monomer drugs, the material base of traditional Chinese medicine and compounds is multi-component, instead of single or several active monomers. Therefore, under the guidance of the Chinese medicine theories, modern multi-component sustained-release preparations were developed for oral traditional Chinese medicines, with the aim of finally improving the clinical efficacy of traditional Chinese medicines.

The imaging study on the value of ~1H-MR spectroscopy in diffuse axonal injury / 中华放射学杂志

Objective To investigate the value of ~1H-MRS in the diagnosis and prognosis of diffuse axonal injury(DAI).Methods A prospective imaging study was performed in 63 patients with craniocerebral injury admitted from October 2002 to April 2004.Sixty-three patients were divided into DAI group(27 cases)and Non-DAI group(36 cases)according to the result of the MRI.Then,the ratio of NAA/Cr,Cho/Cr,mINs/Cr,and GIx/Cr at basal ganglia and genu and splenium of corpus callosum was quantified using ~1H-MRS and compared between DAI group and Non-DAI group.Twenty healthy persons were served as control group.The relation between ~1H-MRS indexes and period of primary uneonciousness post-injury was analyzed.Results The results of NAA/Cr and Cho/Cr at genu and splenium of corpus callosum and basal ganglia of control group were 1.19?0.18,1.21?0.24;1.89?0.17,1.84?0.14; 1.57?0.16,1.85?0.25,which of DAI group were 0.83?0.24,2.92?0.78;1.25?0.35,2.54? 0.42;1.33?0.17,2.38?0.44,and those of Non-DAI group were 1.11?0.23,1.61?0.33;1.61? 0.22,1.93?0.26;1.49?0.23,1.89?0.29.The differences between them were statistically significant (P