Study on Integral Dissolution Model Based on Biological Potency for Compound Chinese Materia Medica / 中草药·英文版

Objective: To investigate the integral dissolution model based on biological potency in order to evaluate the dissolution of Compound Chinese materia medica (CCMM) in vitro. Methods: The contents of paeoniflorin, phillyrin, ginsenoside Rg1, and adenosine of ten batches of Compound Biejia Ruangan Tablet (CBRT) were determined at different times. The self-defined weighting coefficient based on the contents has been created to establish the integral dissolution model. In addition, the biological potency of CBRT was measured by MTT assay. Then, the f2 similar factor was used to evaluate the similarity of the batches. Results: Compared with batch a, some batches' f2 values of paeoniflorin and adenosine were less than 50, while f2 values of ginsenoside Rg1, phillyrin, and integral component were more than 50. Likewise, ginsenoside Rg1, phillyrin, and integral component were all in good correlation with biological dissolution. Conclusion: The results of the integral dissolution based on biological test of CBRT demonstrate that the bioassay method may be a promising supplement for its quality evaluation.

Preparation and characterization of cucurbitacin B sodium deoxycholate/phospholipid-mixed oral fast dissolving film and antitumor activity study / 中国中药杂志

A novel drug delivery system combining oral fast dissolving film with sodium deoxycholate/phospholipid mixed micelles was prepared to increase the absorption of cucurbitacin B that is a poor aqueous solubility substance. Encapsulation efficiency, particle size, zeta potential, polydispersity coefficient, investigated the morphology, disintegration time of oral fast dissolving film and the pharmacodynamic properties of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles before and after solidified in mice were evaluated and compared. The oral fast dissolving film prepared in this study showed a homogeneous pale yellow and could completely disintegrated in the 30 s. It could meet the requirements of rapidly disintegrating fully. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles loaded in oral fast dissolving film were (43.36 +/- 2.12)%, (108.82 +/- 5.2) nm, (-34.18 +/- 1.07) mV, 0.088 +/- 0.012, respectively. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles in solution were (41.26 +/- 2.22)%, (181.82 +/- 4.48) nm, (-30.67 +/- 0.81) mV, 0.092 +/- 0.012, respectively. The difference of pharmacodynamics among film of cucurbitacin B-loaded micelles, cucurbitacin B-loaded micelles and free cucurbitacin B in vivo was compared. Solubility of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles has also been greatly improved. The tumor inhibition rate of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles was significantly improved and did not change significantly before and after solidified. These showed that the sodium deoxycholate/phospholipid-mixed micelles could enhance the antitumor activities of cucurbitacin B and the stability of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles was improved significantly after solidified by oral fast dissolving film technology without pharmacodynamic properties changed significantly.

Spectrum-activity relationship on anti-hepatic fibrosis efficacy of Trionycis Carapax / 中草药

Objective: To investigate the spectrum-activity relationship between HPLC of Trionycis Carapax from different regions and its anti-hepatic fibrosis efficacy, in order to reveal the "active component group" for anti-hepatic fibrosis efficacy of Trionycis Carapax. Methods: The samples from 12 regions were determined with the HPLC-DAD method. The representative standard fingerprint was calculated using the Similarity Evaluation System for Chromatographic Fingerprint of Traditional Chinese Medicine (Version 2004A). The common patten and the principal component analysis (PCA) were established. Using the LX-2 hepatic stellate cell as a hepatic fibrosis model of Trionycis Carapax to study its inhibition on the hepatic fibrosis cells. The spectrum-effect relationship was studied by SPSS 19.0 software. Results: Seven common peaks in the HPLC-fingerprint of Trionycis Carapax were obtained. It was tentatively concluded that peaks 2 and 5 related better to the inhibitory effect of LX-2 cells (OD value) in the seven characteristic peaks. Peak 4 had the strongest correlation. And the quality of Trionycis Carapax was influenced by the concentration of peak 4 obtained by PCA. Conclusion: All the samples could inhibit the proliferation of LX-2 hepatic stellate cell in some extent. There may be a certain relationship between HPLC fingerprint and anti-hepatic fibrosis efficacy. In addition, the research could be used as the quality control method of Trionycis Carapax.

Effects of different pulverization fineness on in vitro dissolution rate of Compound Biejia Ruangan Tablet based on biological value evaluation / 中草药

Objective: To explore the effects of different pulverization fineness of solid preparations of Chinese materia medica on their in vitro dissolution, using MTT method combined with HPLC. Methods: Compound Biejia Ruangan Tablet (CBRT) was used as model drug, and MTT method was used to obtain the characteristic cell inhibitory rate by different pulverization fineness of dissolving solutions in the dissolution medium (phosphate buffer, pH value 7.4) at different time points. From these results, the cumulative dissolution of CBRT based on cell inhibitory rate was obtained. The dissolution rates of paeoniflorin was determined by HPLC method. Using f2 similar factor, the relevance of these two methods was evaluated. Results: Dissolution of paeoniflorin is changed with the change of pulverization fineness, the accumulative dissolutions of 200 and 300 meshes in vitro were higher than those of other meshes. The results showed that f2 values of 200 and 300 meshes were more than 50, indicating that there was a good correlation between the two methods of measuring the dissolution rate. Conclusion: The results show that the biological potency detection could be used to screen the particle size of CBRT. Considering the production cost of CBRT, 200 mesh is the best particle size.