Supervisor(s):Chinese Pharmaceutical Association Sponsor(s):Tianjin Institute of Pharmaceutical Research；Chinese Pharmaceutical Association ISSN:0253-2670 CN:12-1108/R
Chinese Traditional and Herbal Drugs is supervised by Chinese Pharmaceutical Association and sponsored by Tianjin Institute of Pharmaceutical Research and Chinese Pharmaceutical Association. Launched in 1970, the journal is an academic journal with a broad scope in publishing research papers, brief reports, reviews, dissertations, and special treatises on the recent achievements of basic study, production, quality control, and clinic application on traditional Chinese medicine and Chinese materia medica.
The journal is included in CA, JST and CSCD.
Objective To determine the prescription technology of gastrodin starch microsphere and investigate its nasal mucoadhesion and in vitro release characteristics. Methods Gastrodin starch microspheres were prepared by complex emulsion crosslinking method. According to the particle diameter, drug loading efficiency (DLE), and entrapment efficiency (EE), the best prescription technology was selected by using single-factor investigation and uniform design. Using toad palate mucosa as model and average residence time as indicator, mucoadhesion of gastrodin starch microsphere was evaluated. Using gastrodin API as a control, paddle method was applied to in vitro release test of gastrodin starch microspheres. The content of gastrodin was determined to calculate the cumulative release percentage. In addition, the curve of drug release in vitro was fitted with different release models to analyze the in vitro release characteristics of gastrodin starch microsphere in nasal cavity synthetically. Results The optimum prescription and preparation technology of gastrodin starch microsphere were as follows: gastrodin 2.0 g, starch 4.5 g, liquid paraffin 100.0 mL, Span 80 3.5 g, ECH 5.1 mL, preparation temperature 40 ℃, and rotational speed 1000 r/min. The particle diameter of gastrodin starch microsphere was (47.69 ± 1.92) μm, and the DLE and EE of microsphere were (9.78 ± 0.70)% and (35.72 ± 3.28)%, respectively. The average residence time of powder without adhesion was about (176.92 ± 23.25) s in nasal cavity, which translated into human nasal residence time was just 20—30 min, while the average residence time of gastrodin starch microspheres was extended to (944.33 ± 68.29) s, which translated into human nasal residence time was about 3 h. The cumulative release percentage of gastrodin starch microspheres was more than 90% in 3 h. Compared with other in vitro release models, Weibull model was the fittest model to gastrodin starch microspheres, the t50 of gastrodin starch microspheres was 40.08 min, and t90 was 245.73 min. Conclusion Gastrodin starch microspheres prepared with optimum prescription technology have uniform particle diameter, high DLE and EE. Microspheres have good mucoadhesion and sustained release, ensuring that gastrodin releases gently and completely during the nasal retention period.
Objective To improve the absorption of trifolirhizin (Tri) isolated from Sophora flavescensthrough preparing it to be phospholipid complex self-microemulsion. Methods In this study, we used the silica gel column chromatography and recrystallization technology to separate and prepare trifolirhizin; we used physical and chemical properties and spectral data to identify the structure. We used the orthogonal experiment and the central composite design response surface method (CCD-RSM) to optimize the Tri phospholipid complex (TPC), Tri phospholipid composite material self micro-emulsifying drug delivery system (TPC-SMEDDS), and used the Caco-2 model to investigate the transmembrane transport of Tri, TPC, and TPC-SMEDDS, respectively. Results The concentration of the phospholipid complex was 4 mg/mL, the ratio of drug to lecithin was 1:1.5, the reaction time was 3 h, the composite rate was (93.20 ± 2.01)%. The emulsifier was polyoxyethylene castor oil (Cremphor EL40), the auxiliary emulsifier was diethylene glycol ethyl ether (Transcutol HP), and the weight ratio (Km) of phospholipid complex was 7.58. The experiments of Caco-2 cell showed that the Papp of Tri was 2.45 × 10−7 cm/s; The Papp values of TPC and TPC-SMEDDS were 5.13 × 10−6 and 1.847 × 10−5 cm/s, respectively. Conclusion The permeability coefficient of Tri can be obviously improved by using phospholipid complex and self-microemulsion technique, which also can improve the efficiency of drug delivery.
Objective To establish HPLC method for the simultaneous determination of protopine, palmatine hydrochloride, berberine hydrochloride, dehydrocorydaline, tetrahydropalmatine, tetrahydroberberine, and corydaline in Cuyanhusuo Granule. Methods The analysis was performed on Ultimate AQ-C18 column (250 mm × 4.6 mm, 5 μm) by gradient elution of acetonitrile–0.1% phosphoric acid (adjust to pH 6.0 with triethylamine) (10 : 90). The UV detection wavelength was set at 280 nm and the flow rate was 1.0 mL/min. Results The linear ranges of protopine, palmatine hydrochloride, berberine hydrochloride, dehydrocorydaline, tetrahydropalmatine, tetrahydroberberine, and corydaline were 6.8–119.0 (r = 0.999 9), 24.38–426.65 (r = 0.999 9), 8.88–155.40 (r = 0.999 9), 77.66–1 359.05 (r = 0.999 9), 41.4–724.5 (r = 0.999 9), 6.70–117.25 (r = 0.999 9), and 25.50–446.25 ng (r = 0.999 9). The average recovery (n = 6) was 98.2% (RSD = 2.0%), 99.6% (RSD = 2.8%), 100.2% (RSD = 1.3%), 99.0% (RSD = 2.2%), 100.8% (RSD = 2.6%), 98.7% (RSD = 2.5%), and 97.7% (RSD = 2.2%), respectively. Conclusion This method is simple and rapid, and can be used for the quality control of Cuyanhusuo Granule with satisfactory separation and repeatability.
Objective To reveal the variation regularity of chemical components in crude Cyathula officinalis and its processed products(stir-fried with yellow rice wine and salt), and promote the quality control of the herb. Methods Agilent Zorbax Eclipse XDB-C18 column (250 mm × 4.6 mm, 5 μm) was used with acetonitrile and 0.1% phosphoric acid solution in a gradient elution mode. The detection wavelength was 266 nm and the flow rate was 0.5 m L/min. The fingerprints for 24 herbal samples were set up and 25 peaks were recorded with different retention time and peak areas. Three peaks were successfully identified as puerarin, cyasterone, and daidzein by comparing the retention time of reference substances. The vectorial angle method was used to evaluate the similarity between fingerprints. The cluster analysis and principal component analysis were applied to studying the HPLC fingerprint and chemical pattern recognition. Results The two processing techniques, stir-frying with wine and salt, both had significant effect on herbal chemical profiles. The contents of three known active components, puerarin, cyasterone, and daidzein, were not observed except a little increasing of the content of puerarin after the crude herbs were processed with salt. Conclusion More precise active components of the processed products of C. officinalis need to future study to improve the current quality standard of C. officinalis in Chinese Pharmacopoeia. The method provided by this study is a powerful tool to identify and quality control between crude and processed C. officinalis because of its quantificational and visual evaluation system.
Objective To investigate the technology for the separation and purification of extract in Dracocephalum moldevica (EDM) by macroporous resin. Methods Static and dynamic adsorption-desorption were used to select the best one from seven different type macroporous resins; With the content of total flavonoids, tilianin, luteolin-7-O-β-D-glucuronide, and rosmarinic acid as indexes, the purification technology parameters of EDM were optimized. Results HPD600 resin showed the best purifying profile, its optimum technology conditions were as follows: The optimum concentration of the sample liquid was 0.08 g/mL equivalent to raw material, the resin column diameter-height ratio was 1∶9, the amount of used adsorption was 0.32 g dried medicinal herb/m L resin, sample flow rate was 1.5 BV/h, and adsorption time was 12 h. In the course of elution, the resin column chromatography was eluted with 6 BV of 70% ethanol after removing impurities with 4 BV of water by flow rate of 1.5 BV/h. The contents of total flavonoids, tilianin, luteolin-7-O-β-D-glucuronide, and rosmarinic acid were more than 53%, 5.5%, 4.7%, and 2.5%. Conclusion Macroporous resin HPD600 is suitable to separate and purify EDM.
