Structure-activity relationship of coptis alkaloid bitterness inhibited by mPEG-PLLA / 中国中药杂志

Inhibition of bitterness is a significant measure to improve the compliance and clinical efficacy of traditional Chinese medicine(TCM) decoction. According to the characteristics of TCM decoction, such as high dispersion of bitterness components, multi-component bitterness superposition and strong instantaneous stimulation, the research group put forward a new strategy to inhibit bitterness in the early stage based on the self-assembly characteristics of amphiphilic substances in aqueous solution, in order to reduce the distribution of bitterness components in real solution and achieve the purpose of bitter-masking. It was found that the bitter-masking effect of amphiphilic substances was different on the bitter compounds of various structures. Therefore, it was speculated that there might be a certain relationship between the bitter inhibition effect and the substrate structure. In this paper, the interaction between mPEG-PLLA and five bitter alkaloids(bamatine, jatrorrhizine, berberine, epiberberine and coptisine) in Coptidis Rhizoma was studied to explore the effect of substrate structure on the inhibition of bitterness. The sensory test of volunteers was used to determine the bitter-masking effect of mPEG-PLLA on the decoction of Coptidis Rhizoma and its main bitter alkaloids. The molecular docking and molecular force field were applied to locate the bitter groups and the bitter-masking parts. The relationship between the bitter strength and the structure was analyzed by the surface electrostatic potential of the bitter alkaloids, and the correlation between the bitter-masking effect and the structural parameters of the bitter components was explored by factor analysis, so as to clarify the structure-activity relationship of mPEG-PLLA in masking the bitterness of coptis alkaloids. It was found that mPEG-PLLA had significant taste masking effect on the decoction of Coptidis Rhizoma and five alkaloids. The masking effect was obviously related to the structure of different alkaloids: the effect increased with the increase of the number of hydrogen donors, rotatable bonds, molecular weight, and hydrophobicity, and decreased with the increase of surface electrostatic potential, electrophilicity and binding energy with bitter receptors. In this study, the influence of alkaloid structure of Coptidis Rhizoma on the butter-masking effect of mPEG-PLLA was preliminarily elucidated, providing a scientific basis for better exerting the bitter-masking effect of amphiphilic block copolymers.

Optimized model for formulation prescription of traditional Chinese medicine buccal tablets based on temporal dominant description of sensations combined with multivariate statistical analysis:an example of Compound Caoshanhu Buccal Tablets / 中国中药杂志

The taste is the key to the research and design for formulation prescription of traditional Chinese medicine buccal tablets( TCMBTs). TCMBTs are dissolved in the oral cavity in parallel with the release of the drug,providing a sufficient " time window" for the perception of various basic taste,tactile and retention. The overall taste is the result of competitive inhibition,comprehensive superposition and dynamic change of multiple tastes. Traditional evaluation methods rely mostly on recalled experience score,difficult to reflect the dynamic changes of taste for buccal tablets. Therefore,it is urgent to establish a new optimized model for taste evaluation and formulation prescription according to the formulation characteristics of TCMBTs. To this end,this paper proposed for the first time to construct a research method for the optimal formulation of TCMBTs based on temporal dominant description of sensations combined with multivariate statistical analysis: the sensory test of volunteers was carried out by temporal dominant description analysis method,and elements separation was conducted for the time and taste in the process of inclusion to form a temporal dominant descriptive score of multi-time points and multi-sensory attributes. Finally,the optimal formulation was obtained by multivariate statistical analysis. Taking the formulation prescription of Compound Caoshanhu Buccal Tablets as an example,the research ideas of this method were explained,and the optimal formulation prescription was obtained as follows,Glabrous Sarcandra Extract of 20. 0 g,mannitol of 24. 0 g,microcrystalline cellulose of 12. 0 g,aspartame of 1. 0%,menthol of 0. 7%,and menthol oil of 0. 7%. This study provides a new method for the taste evaluation and formulation research of TCMBTs,providing a new idea for the fine manufacturing and innovative development of TCM buccal tablets in the new era.

Preparation and characterization of SiO2 solid dispersions of Curcumae longae Rhizoma extract / 中成药

AIM To prepare and characterize SiO2 solid dispersions of Curcumae longae Rhizoma extract.METHODS For the solid dispersions prepared by solvent evaporation method,its ratio of extract to carrier (SiO2) was screened by in vitro dissolution test,and the characterization was achieved by determination of particle size,specific surface area,porosity,micromorphology observation,infrared spectroscopy and X-ray.RESULTS When the ratio of extract to carfer was 1:8,three main components (bisdemethoxycurcumin,demethoxycurcumin and curcumin) in the extract reached the highest accumulative dissolution rates.Compared with physical mixture,the solid dispersions demonstrated lower particle size,specific surface area and porosity.Extract was dispensed in the carrier in an amorphous state.CONCLUSION SiO2 solid dispersions can obviously improve the dissolution rates of the main components in Curcumae longae Rhizoma extract.

Solubilization of self-emulsifying drug delivery system (SEDDS) for curcumin components / 中草药

Objective: To explore the feasibility of self-emulsifying drug delivery system (SEDDS) for multicomponents simuitaneous solubilization. Methods: The curcumin (Cur) components were used as model drug, D-optimal mixture design was used to optimize SEDDS prescription, and the contents of bisdemethoxycurcumin (BDMC), demethoxycurcumin (DMC), and Cur, SEDDS particle size, and emulsifying time were made as indicators to select and evaluate SEDDS, so as to explore the feasibility of SEDDS for the multicomponents simuitaneous solubilization. Results: The optimal SEDDS prescription was Obleique CC497-Tween 20-Transcutol P (0.21:0.50:0.29), SEDDS particle size was (248.8 ± 3.4) nm, and emulsifying time was (70 ± 1) s. At 37°C, the maximum loading capacities of SEDDS for BDMC, DMC, and Cur were 2.998, 12.220, and 52.561 mg/g, respectively, and the solubilities in water were 0.107, 0.661, and 1.648 mg/mL. Conclusion: SEDDS can realize the solubilization of multicomponent simultaneously.