Improving compactibility properties of Lonicera Japonica Flos by Plasdone S-630 / 药学学报

To improve the fluidity and compactibility properties of raw powders of traditional Chinese medicine by particle modification technology, Lonicera Japonica Flos was used as a model drug, fluidized bed bottom spray technology was used, and Plasdone S-630 was used as a modifier to prepare modified particles. The powder properties, tablet compactibility parameters, disintegration time and dissolution were measured. The surface morphology of the powder particles before and after modification and compressed tablets were characterized by combining with scanning electron microscopy technology. The results showed that the particle size of Lonicera Japonica powder has been increased after particle modification, the fluidity, compressibility and compactibility of the powder have been improved to some extent, the disintegration time has also been reduced, and the dissolution in vitro is not affected. Therefore, this study can provide reference and ideas for the common problem that raw powder of traditional Chinese medicine that cannot meet the needs of preparation production due to poor powder properties such as fluidity and compressibility.

Influence of MCC on direct pressure properties of powder extracted from Shufeng Jiedu formula / 中草药

Objective: To study the influence of microcrystalline cellulose (MCC) on the direct pressure properties of powder extracted from Shufeng Jiedu formula (SFJDE), and discuss the correlation between the basic physical properties and its functional properties of the powder before compression. Methods: SFJDE and MCC was mixed in different proportions, the physical properties of the mixed powder and the compression parameters under different pressures were determined. The basic physical properties and functional parameters of the powder were processed and analyzed by linear regression and partial least squares (PLS). Results: The addition of MCC in SFJDE showed a good linear relationship with the moisture content (MC), bulk density (ρb), and porosity ratio (ε) of the powder (r2 ≥ 0.991 9), and showed a good positive correlation with Hausner ratio (HR) and Carr’s index (CI) of the powder flow index (r2 ≥ 0.834 2). The parameters of powder compressibility compaction ratio (CR) and yield pressure (Py) gradually decreased, Unit effective work (Esp) and paramter a gradually increased; The powder compaction parameter kA was gradually increased, and kB was gradually decreased. The basic physical properties of MC, ρb, tap density (ρt), true density (ρtrue), and particle size (D0.5) of the powder had the obvious impact on these parameters by PLS analysis, while size distribution (span), HR, CI had little effect on it. However, span, HR, and CI had the obvious influence on the parameters ab and f, which characterized powder breakage and rearrangement. Conclusion: The increase of MCC reduces the fluidity of SFJDE, improves the compressibility and compactibility of the powder, therefore, we should pay attention to the influence of fluidity and pressure sensitivity during the process of use.

Establishment of skin and joint micro-dialysis sampling method of triptolide in vivo by HPLC-MS/MS / 中国中药杂志

To detect the concentration of triptolide in skin and joint after percutaneous administration,an HPLC-MS/MS method and skin and joint micro-dialysis( MD) method of triptolide were established in this study. The separation was achieved on triple quadrupole( AB QTRAP4500) and phenomenex-C18( 4. 6 mm×150 mm,5 μm,luna) column with acetonitrile-water with 0. 1% formic acid( 65 ∶35) as the mobile phase at a flow rate of 0. 7 m L·min-1. An electrospray ionization( ESI) source was applied and operated in the positive multiple reaction monitoring( MRM) mode. The fragment ion for triptolide was m/z 361. 1→145. 0. The effects of different perfusion [Ringer's,PBS( p H 7. 4),30% ethanol saline]drug concentrations and flow rates on the recovery rate,as well as the relationship between the recovery rate and the loss rate were determined by incremental( dialysis) and reduction( retrodialysis) methods.The reduction method was applied in the in vivo study to investigate and determine the stability of the probe recovery rate in 10 h. The results of HPLC-MS/MS detection method conformed to the requirements of biological samples. The perfusion fluid was 30% ethanol saline. The recovery rate of skin and joint probes in vitro of triptolide increased within the flow rate of 0. 5-2. 5 μL·min-1. In order to increase the timeliness of data and the accuracy,the flow rate was determined to be 1 μL·min-1,and the sample interval was determined to be 0. 5 h. The recovery rate of triptolide in skin and joint probes in vitro and the loss rate were stable and equal despite of change of triptolide concentration within 10-200 μg·L-1. This indicated that the effect of drug concentration on the MD probe recovery rate was small,and the recovery rate could be replaced by the loss rate. The loss rate in vivo using MD method was measured at 10 h,indicating that the transfer rate of triptolide was stable within 10 h. The established method of triptolide in MD and HPLC-MS/MS can be applied to investigate the kinetic in skin and joint after percutaneous administration of triptolide.

Effects of Frankincense and Myrrh essential oil on transdermal absorption in vitro of Chuanxiong and penetration mechanism of skin blood flow / 中国中药杂志

The aim of this paper was to explore the effects of Frankincense and Myrrh essential oil on transdermal absorption in vitro of Chuanxiong, and to investigate the possible penetration mechanism of their essential oil from the perspective of skin blood perfusion changes. Transdermal tests were performed in vitro with excised mice skin by improved Franz diffusion cells. The cumulative penetration amounts of ferulic acid in Chuanxiong were determined by HPLC to investigate the effects of Frankincense and Myrrh essential oil on transdermal permeation properties of Chuanxiong. Simultaneously, the skin blood flows were determined by laser flow doppler. The results showed that the cumulative penetration amount of ferulic acid in Chuanxiong was (8.13±0.76) μg•cm⁻² in 24 h, and was (48.91±4.87), (57.80±2.86), (63.34±4.56), (54.17±4.40), (62.52±7.79) μg•cm⁻² respectively in Azone group, Frankincense essential oil group, Myrrh essential oil, frankincense and myrrh singly extracted essential oil mixture group, and frankincense and myrrh mixed extraction essential oil group. The enhancement ratios of each essential oil groups were 7.68, 8.26, 7.26, 8.28, which were slightly greater than 6.55 in Azone group. In addition, as compared with the conditions before treatment, there were significant differences and obvious increasing trend in blood flow of rats in Frankincense essential oil group, Myrrh essential oil group, frankincense and myrrh singly extracted essential oil mixture group, and frankincense and myrrh mixed extraction essential oil group when were dosed at 10, 20, 30, 10 min respectively, indicating that the skin blood flows were increased under the effects of Frankincense and Myrrh essential oil to a certain extent. Thus, Frankincense and Myrrh essential oil had certain effect on promoting permeability of Chuanxiong both before and after drug combination, and may promote the elimination of drugs from epidermis to dermal capillaries through increase of skin blood flow, thus enhancing the transdermal permeation amounts of drugs.