Research progress, key scientific problems and countermeasures of “green concentration” technology based on membrane and its integration process / 中草药

The energy consumption of Chinese materia medica industry is astonishing. The steam consumption of the heavy concentrating section accounts for about 60% of the whole plant, or even higher. Membrane concentration technology has the important advantages of “low energy consumption and low cost”, but it is restricted by the respective defects caused by the technical principles of different membrane processes. Our research group introduces the international advanced integrated design strategy and method in view of the key technology of “reverse osmosis and membrane distillation integration” which is expected to suitable for the concentrated demand of Chinese medicine pharmaceutical industry. Taking the representative Chinese herbal compound prescription as the experimental system, a three-dimensional model of "time-material rheological characteristics-membrane mass transfer process" was established by using rheological theory and computational fluid dynamics (CFD) as experimental system and dynamic and precise analysis of technological process. The rheological law of traditional Chinese medicine materials and its influence on membrane concentration process were explored by means of multi-disciplinary methods. The mass transfer effect and mechanism of membrane concentration process on traditional Chinese medicine materials were elaborated. The equilibrium points of critical osmotic pressure (RO process) and critical flux (membrane distillation process) were found. The optimal combination schemes of reverse osmosis (RO) and membrane distillation (MD) were explored. In short, we solved the key technical problems of the membrane concentration process, which provided support for the complete set of technical equipment and the technological design, and promoted the theoretical and technological innovation of TCM pharmaceutical engineering.

Network pharmacology-based study on mechanisms of Huanglian Jiedu Decoction impact on macrophage inflammation response / 药学学报

This study was designed to explore the impact of Huanglian Jiedu Decoction (HLJDT) on macrophage inflammation reaction using the network pharmacology method. Glycolysis, sphingolipid metabolism and glutamine metabolism were also investigated for "multi-component, multi-target and multi-pathway", which supports a foundation for drug innovative research. The TCMSP database was used to screen the active components of HLJDT, the target protein predicted by PharmMapper database and the DAVID database for pathways annotation and analysis. The Cytoscape 3.2.1 software was used to construct the active componenttarget-pathway network map and GENEMANIA database for protein interaction analysis. System Dock Database Site is used in verification of molecular docking. The results showed that 84 active ingredients were screened in HLJDT with a total of 111 target targets. Fourteen pathways are affected according to 13 macrophage-related inflammatory proteins, and 8 pathways including 34 target proteins from glycolysis, sphingolipid metabolism and glutamine metabolism. Inflammation-related proteins and metabolism-related proteins can interact with each other through physical correlation, protein co-expression, etc. Berberine, baicalin and geniposide combined well with 5 important targets. Huanglian Jiedu Decoction may act on the glycolysis and sphingolipid pathways to regulate macrophage inflammatory responses.

Study on essential oil separation from Forsythia suspensa oil-bearing water body based on vapor permeation membrane separation technology / 中国中药杂志

To investigate the feasibility of vapor permeation membrane technology in separating essential oil from oil-water extract by taking the Forsythia suspensa as an example. The polydimethylsiloxane/polyvinylidene fluoride (PDMS/PVDF) composite flat membrane and a polyvinylidene fluoride (PVDF) flat membrane was collected as the membrane material respectively. Two kinds of membrane osmotic liquids were collected by self-made vapor permeation device. The yield of essential oil separated and enriched from two kinds of membrane materials was calculated, and the microscopic changes of membrane materials were analyzed and compared. Meanwhile, gas chromatography-mass spectrometry (GC-MS) was used to compare and analyze the differences in chemical compositions of essential oil between traditional steam distillation, PVDF membrane enriched method and PDMS/PVDF membrane enriched method. The results showed that the yield of essential oil enriched by PVDF membrane was significantly higher than that of PDMS/PVDF membrane, and the GC-MS spectrum showed that the content of main compositions was higher than that of PDMS/PVDF membrane; The GC-MS spectra showed that the components of essential oil enriched by PVDF membrane were basically the same as those obtained by traditional steam distillation. The above results showed that vapor permeation membrane separation technology shall be feasible for the separation of Forsythia essential oil-bearing water body, and PVDF membrane was more suitable for separation and enrichment of Forsythia essential oil than PDMS/PVDF membrane.

Preparation and release behaviour of mPEG-PLA α-asarone nanoparticles designed for nasal administration / 中国中药杂志

Taking α-asarone as model drug, mono methoxy polyethylene glycol-polylactic acid copolymer (mPEG-PLA) as the drug carrier material to prepare drug-loading nanoparticles by premix membrane emulsification for nasal administration. The prepared nanoparticles were spherical with smooth surface and average particle size of 360 nm. Polydispersity index (PDI) was 0. 030, average drug loading of (11.5 ± 0.045) % (n = 3), and the encapsulation efficiency of (86.34 ± 0.11) % (n = 3). X-ray diffraction and differential scanning calorimetry results showed that, α-asarone existed in mPEG-PLA carrier in amorphous or molecular state, different from simple physical mixture. In the in vitro release test in simulated human nasal cavity, α-asarone apis can be released quickly at close to 94% at 102 h, in line with the first-order kinetics (R² = 0.981 9). mPEG-PLA drug-loading nanoparticles release only 54%, with slow release effect, in line with Riger-Peppas model (R² = 0.967 9, n = 0.630 2), for non-fick diffusion, released by the spread of drugs and skeleton dissolution dual control. This provided the foundation for nasal drug delivery in vivo pharmacokinetic study.

Studies on preparation by SPG membrane emulsification method and in vitro characterization of tetradrine-tashionone II(A)-PLGA composite microspheres / 中国中药杂志

Tetradrine-tashionone II(A)-PLGA composite microspheres were prepared by the SPG membrane emulsification method, and the characterization of tetradrine-tashionone II(A) -PLGA composite microspheres were studied in this experiment. The results of IR, DSC and XRD showed that teradrine and tashionone II(A) in composite microspheres were highly dispersed in the PLGA with amorphous form. The results of tetradrine-tashionone II(A) -PLGA composite microspheres in vitro release experiment showed that the cumulative release amounts of tetradrine and tashionone II(A) were 6.44% and 3.60% in 24 h, and the cumulative release amounts of tetradrine and tashionone II(A) were 89.02% and 21.24% in 17 d. The process of drug in vitro release accorded with the model of Riger-Peppas. Tetradrine-tashionone II(A) -PLGA composite microspheres had slow-release effect, and it could significantly reduce the burst release, prolong the therapeutic time, decrease the dosage of drugs and provide a new idea and method to prepare traditional Chinese medicine compound.

Preparation and characterization of tetrandrine-loaded PLGA nanocomposite particles by premix membrane emulsification coupled with spray-drying method / 药学学报

For effective inhalable dry-powder drug delivery, tetrandrine-PLGA (polylactic-co-glycolic acid) nanocomposite particles have been developed to overcome the disadvantages of nanoparticles and microparticles. The primary nanoparticles were prepared by using premix membrane emulsification method. To prepare second particles, they were spray dried. The final particles were characterized by scanning electron microscopy (SEM), dry laser particle size analysis, high performance liquid chromatography (HPLC), X-ray diffraction (XRD), differential scanning calorimetry (DSC), infrared analysis (IR) and confocal laser scanning microscope (CLSM). The average size of the primary particles was (337.5 ± 6.2) nm, while that second particles was (3.675 ± 0.16) μm which can be decomposed into primary nanoparticles in water. And the second particles were solid sphere-like with the drug dispersed as armorphous form in them. It is a reference for components delivery to lung in a new form.

In vitro and in vivo study of fluorescent probe PLGA particles prepared by premix membrane emulsification method / 中国中药杂志

Relatively uniform-sized nanoparticles made of poly (lactic-co-glycolic acid) (PLGA) were prepared by premix membrane emulsification method. After the drug loading property was completed, the dynamic tissue distribution of nanoparticles was recorded. With the average particle size and span as indexes, membrane pore size, number of passing membrane times, membrane pressure, volume ratio of oil-water phase and the concentration of poly(vinyl alcohol) (PVA) in external water phase were investigated by single factor test, the optimum preparation technology of blank PLGA nanlparticles was as following: pore size of SPG membrane was 1 μm, membrane pressure was 1. 15 MPa, the number of passing membrane time was 3, the mass fraction of PVA of 2%, volume ratio of oil-water phase of 1 : 5. Prepared nanoparticles were round with smooth surface, the mean diameter was 332.6 nm, span was 0.010, the confocal laser scanning microscope (CLSM) concluded that fluorescent substance is uniform composizion in PLGA nanoparticle, and the in vivo imaging technology in mice include that the nanoparticles show good liver and spleen targeting property.

Optimization theory and practical application of membrane science technology based on resource of traditional Chinese medicine residue / 中国中药杂志

Resource of traditional Chinese medicine residue is an inevitable choice to form new industries characterized of modem, environmental protection and intensive in the Chinese medicine industry. Based on the analysis of source and the main chemical composition of the herb residue, and for the advantages of membrane science and technology used in the pharmaceutical industry, especially membrane separation technology used in improvement technical reserves of traditional extraction and separation process in the pharmaceutical industry, it is proposed that membrane science and technology is one of the most important choices in technological design of traditional Chinese medicine resource industrialization. Traditional Chinese medicine residue is a very complex material system in composition and character, and scientific and effective "separation" process is the key areas of technology to re-use it. Integrated process can improve the productivity of the target product, enhance the purity of the product in the separation process, and solve many tasks which conventional separation is difficult to achieve. As integrated separation technology has the advantages of simplified process and reduced consumption, which are in line with the trend of the modern pharmaceutical industry, the membrane separation technology can provide a broad platform for integrated process, and membrane separation technology with its integrated technology have broad application prospects in achieving resource and industrialization process of traditional Chinese medicine residue. We discuss the principles, methods and applications practice of effective component resources in herb residue using membrane separation and integrated technology, describe the extraction, separation, concentration and purification application of membrane technology in traditional Chinese medicine residue, and systematically discourse suitability and feasibility of membrane technology in the process of traditional Chinese medicine resource industrialization in this paper.

Study on PK/PD model for traditional Chinese medicine biopharmaceutics based on principle of "correspondence of prescriptions and syndromes" / 中国中药杂志

In the principle of "correspondence of prescription and syndrome", this article focuses on key technical issues of traditional Chinese medicine (TCM) biopharmaceutis by using the integrated pharmacokinetic and pharmacodynamic model: (1) As the prescription formulation and compatibility of TCM compounds could be influential to the in vivo pharmacokinetics of chemical components of TCMs, and closely related to therapeutic and adverse effects, how to describe these actions in a biopharmaceutics model? (2) As there are differences between pharmacokinetic processes in the normal and pathological states, how to express characteristic "syndromes" in an animal model? (3) As prescriptions work to reduce and transform syndromes, how o confirm the type and amount of effective substances in case of physiological and pathological indicators and drug distribution in a dynamic corresponding state. In response to the above key issues, we proposed the TCM biopharmaceutic study model based on PK/PD. (1) The integrity of TCMs was better expressed with the effect at the core, supplemented with the component pharmacokinetics; (2) An integrated pharmacokinetic and pharmacodynamic system was established on the basis of pharmacokinetics and pharmacodynamics of many major effective components; (3) AK/PD mathematical function with the three-phase synchronous characterization of "time-concentration-effect" was established by using the data mining techniques, to explore the biopharmaceutic principle of "correspondence of prescriptions and syndromes", in which prescriptions are only required for syndromes, whereas no prescription is required in case of no syndrome.

Studies on bioactive constituents of whole herbs of Vernonia cinerea / 中国中药杂志

<p><b>OBJECTIVE</b>To study the constituents of the whole herbs of Vernonia cinerea. by bio-activity guided isolation with PC-12 model.</p><p><b>METHOD</b>The constituents were separated by column chromatography and the structures were elucidated by spectroscopic methods.</p><p><b>RESULT</b>Four compounds were identified to be (+)-lirioresinol B (1), stigmasterol (2), stigmasterol-3-O-beta-D-glucoside (3), 4-sulfo-benzocyclobutene (4), and their NGF inducing activity were also investigated.</p><p><b>CONCLUSION</b>Compounds 1, 3, 4 were isolated from this genus for the first time, and compound 4 was identified as a new natural product. Compounds 1, 3, 4 showed cytotoxicity on PC-12, and compounds 2, 3, 4 showed inhibition activity. Compound 4 showed a specific effect on the survival of TrkA fibroblasts, and resulted in the inducing NGF activity.</p>