[Varieties systematization and standards status analysis of fermented Chinese medicine].

Fermented Chinese medicine has long been used. Amid the advance for preservation of experience, the connotation of fermented Chinese medicine has been enriched and improved. However, fermented Chinese medicine prescriptions generally contain a lot of medicinals. The fermentation process is complicated and the conventional fermentation conditions fail to be strictly controlled. In addition, the judgment of the fermentation end point is highly subjective. As a result, quality of fermented Chinese medicine is of great difference among regions and unstable. At the moment, the quality standards of fermented Chinese medicine are generally outdated and different among regions, with simple quality control methods and lacking objective safe fermentation-specific evaluation indictors. It is difficult to comprehensively evaluate and control the quality of fermented medicine. These problems have aroused concern in the industry and also affected the clinical application of fermented Chinese medicine. This article summarized and analyzed the application, quality standards, and the modernization of fermentation technology and quality control methods of fermented Chinese medicine and proposed suggestions for improving the quality standards of the medicine, with a view to improving the overall quality of it.

[Arsenic speciation and valence].

As arsenic widely exists in nature and has been used in the pharmaceutical preparations, the traditional Chinese medicine(TCM) with arsenic include realgar(As_2S_2 or As_4S_4), orpiment(As_2S_3), and white arsenic(As_2O_3). Among the above representative medicine, the TCM compound formulas with realgar are utilized extensively. Just in Chinese Pharmacopoeia(2020 edition), there are 37 Chinese patent medicines including realgar. The traditional element analysis focuses on the detection of the total amount of elements, which neglects the study on the speciation and valence of elements. The activity, toxicity, bioavailability, and metabolic pathways of arsenic in vivo are closely related to the existence of its form, and different forms of arsenic have different effects on organisms. Therefore, the study on the speciation and valence of arsenic is of great importance for arsenic-containing TCMs and their compound formulas. This paper reviewed four aspects of the speciation and valence of arsenic, including property, absorption and metabolism, toxicity, and analytical assay.

Responses of soil phosphorus cycling and bioavailability to plant invasion in river-lake ecotones.

The invasion of exotic plants in the river-lake ecotone has seriously affected the nutrient cycling processes in wetland soil. The South American species Alternanthera philoxeroides (Mart.) Griseb. is rapidly invading the river-lake ecotone in subtropical China, and has become the dominant species in the river-lake ecotone. However, there have been few studies on the effects of A. philoxeroides invasion on soil phosphorus (P) cycling and bioavailability in this ecotone. Here, we measured the bioavailable P fractions, physicochemical properties and nutrient content in the surface soils of the native plant (Zizania latifolia (Griseb.) Turcz and Nelumbo nucifera Gaertn.) communities and the adjacent invasive A. philoxeroides communities in three river-lake ecotones with different nutrient substrates in the subtropical Dongting Lake basin over a 3-year period to reveal the effects of A. philoxeroides invasion on the morphology and concentrations of soil bioavailable P. The principal coordinate analysis results showed that the A. philoxeroides invasion significantly altered the bioavailable P concentrations in the soil of native plant communities in the different river-lake ecotones, and this effect was not disturbed by the heterogeneity of the soil matrix. However, the effects of invasion into different native plant communities on the fractions of soil bioavailable P were different. Compared with native Z. latifolia and N. nucifera communities, A. philoxeroides invasion increased the concentration of inorganic P by 39.5% and 3.7%, respectively, and the concentration of organic P decreased by 32.7% and 31.9%, respectively. In addition, the invasion promoted P cycling and accumulation in the river-lake ecotone, which resulted in average decreases in the soil N:P and C:P ratios of 7.9% and 12.5%, respectively. These results highlight the impact of exotic plant invasions on nutrient cycling in wetland ecosystems in the river-lake ecotone, and this process may be detrimental to the late recovery of native plants.

Sichen Formula Ameliorates Lipopolysaccharide-Induced Acute Lung Injury via Blocking the TLR4 Signaling Pathways.

Purpose: Sichen (SC) formula is a classic prescription of Tibetan medicine. Due to its potential anti-inflammatory effect, the SC formula has been clinically used to treat respiratory diseases for many years in the Chinese Tibet region. The present study aimed to investigate the anti-inflammatory effect of SC and explore the underlying mechanisms. Methods: SC formula was characterized by HPLC analysis. The acute lung injury (ALI) mouse model was induced by direct intratracheal lipopolysaccharide (LPS) instillation, and bronchoalveolar lavage fluid (BALF) and lung tissues were collected. Meanwhile, RAW264.7 macrophages were stimulated by LPS. The contents of inflammatory mediators in the culture medium were determined by ELISA. Protein levels were determined by immunohistochemical staining or Western blotting. Nuclear localization of NF-κB, AP-1, and IRF3 was performed using immunofluorescence and Western blotting. Results: In the LPS-induced ALI mouse model, SC treatment suppressed the secretion of inflammatory mediators (TNF-α, IL-6, IL-1ß, MCP-1, MIP-1α, and RANTES) in BALF. SC treatment hindered the recruitment of macrophages. SC treatment also inhibited the expression of CD68, p-p65, and TLR4 in the lung tissue. In the LPS-exposed RAW264.7 cells, the cell viability was not changed up to 400 µg/mL of SC. SC concentration-dependently suppressed the production of nitric oxide, prostaglandin E2, TNF-α, IL-6, MCP-1, MIP-1α, and RANTES in LPS-challenged RAW264.7 cells. The expression levels of iNOS, COX-2, p-p38, p-JNK, p-ERK, p-TBK1, p-IKKα/ß, p-IκB, p-p65, p-c-Jun, and p-IRF3 were decreased after SC treatment. Moreover, the nuclear translocation of p65, c-Jun, and IRF3 was also blocked by SC treatment. Conclusion: SC treatment inhibited the inflammatory responses in LPS-induced ALI mouse model/RAW264.7 macrophages. The underlying mechanism of this action may be closely associated with the suppression of TLR4 signaling pathways. These research findings provide further pharmacological justifications for the medicinal use of SC in the management of respiratory diseases.

Arsenic speciation and valence / 中国中药杂志

As arsenic widely exists in nature and has been used in the pharmaceutical preparations, the traditional Chinese medicine(TCM) with arsenic include realgar(As_2S_2 or As_4S_4), orpiment(As_2S_3), and white arsenic(As_2O_3). Among the above representative medicine, the TCM compound formulas with realgar are utilized extensively. Just in Chinese Pharmacopoeia(2020 edition), there are 37 Chinese patent medicines including realgar. The traditional element analysis focuses on the detection of the total amount of elements, which neglects the study on the speciation and valence of elements. The activity, toxicity, bioavailability, and metabolic pathways of arsenic in vivo are closely related to the existence of its form, and different forms of arsenic have different effects on organisms. Therefore, the study on the speciation and valence of arsenic is of great importance for arsenic-containing TCMs and their compound formulas. This paper reviewed four aspects of the speciation and valence of arsenic, including property, absorption and metabolism, toxicity, and analytical assay.

Varieties systematization and standards status analysis of fermented Chinese medicine / 中国中药杂志

Fermented Chinese medicine has long been used. Amid the advance for preservation of experience, the connotation of fermented Chinese medicine has been enriched and improved. However, fermented Chinese medicine prescriptions generally contain a lot of medicinals. The fermentation process is complicated and the conventional fermentation conditions fail to be strictly controlled. In addition, the judgment of the fermentation end point is highly subjective. As a result, quality of fermented Chinese medicine is of great difference among regions and unstable. At the moment, the quality standards of fermented Chinese medicine are generally outdated and different among regions, with simple quality control methods and lacking objective safe fermentation-specific evaluation indictors. It is difficult to comprehensively evaluate and control the quality of fermented medicine. These problems have aroused concern in the industry and also affected the clinical application of fermented Chinese medicine. This article summarized and analyzed the application, quality standards, and the modernization of fermentation technology and quality control methods of fermented Chinese medicine and proposed suggestions for improving the quality standards of the medicine, with a view to improving the overall quality of it.

[Preparation regularity of Chinese patent medicine in Chinese Pharmacopoeia (2020 edition, Vol.â )].

Chinese Pharmacopoeia is an important part of drug standards in China, and it is also a legal basis that must be strictly followed in drug development, production, operation, application, and management. The information on prescriptions, preparation methods, properties, identification, inspection, content determination, functions and indications, usage and dosage, precautions, specifications, and storage of Chinese patent medicine preparations included in the Chinese Pharmacopoeia(Vol.Ⅰ) was clarified. The "Preparation Method" section describes the preparation process of Chinese patent medicine from decoction pieces to finished preparations in detail and specifies the preparation production methods and parameters, which has a good guiding and standardizing effect on the production of Chinese patent medicine in China. The present study summarized the preparation methods of Chinese patent medicine preparations and single drug preparations contained in the Chinese Pharmacopoeia(2020 edition, Vol.Ⅰ) in stages and analyzed the common preparation methods and technical parameters of Chinese patent medicine preparations, which is helpful to understand the current situation of Chinese patent medicine production technology in China and can provide references for the development of new Chinese medicine, the transformation of large varieties of Chinese patent medicine, and the optimization of preparation process of Chinese patent medicine in the market.

[Study on characteristic chromatogram and content determination of Wuzhuyu Decoction reference sample].

In this study, the critical quality attributes of Wuzhuyu Decoction reference sample were explored by using characteristic chromatogram, index component content and dry extract rate as indexes.The dissemination relationship of quantity value between medicinal materials-decoction pieces-reference sample was investigated to preliminarily formulate the quality standard of the reference sample.The characteristic chromatogram of 15 batches of Wuzhuyu Decoction was established by high performance liquid chromatography(HPLC) and the similarity analysis was conducted.Common peaks were demarcated and assigned to medicinal materials.Moreover, quantitative determination of limonin, evodiamine, rutaecarpine and ginsenoside Rb_1 of Wuzhuyu Decoction were performed.The dissemination of quantity value was explored combined with dry extract rate, similarity of characteristic chromatogram and transfer rate of index component content.A total of 18 common peaks were identified in the corresponding materials of Wuzhuyu Decoction reference sample, with the similarity of characteristic chromatogram greater than 0.9, and Fructus Evodiae, Radix Ginseng, Rhizoma Zingiberis Recens and Fructus Jujubae contributed 9, 5, 8 and 2 chromatographic peaks, respectively.The index component content of corresponding materials and the transfer rates of medicinal materials-decoction pieces and decoction pieces-reference sample of different batches of Wuzhuyu Decoction reference sample were as follows: the content of limonin was 0.16%-0.51%, and the transfer rates were 83.66%-115.60% and 38.54%-54.58%, respectively; the content of evodiamine was 0.01%-0.11%, the transfer rated were 80.80%-116.15% and 3.23%-12.93%, respectively; the content of rutaecarpine was 0.01%-0.05%, the transfer rates were 84.33%-134.53% and 5.72%-21.24%, respectively; the content of ginsenoside Rb_1 was 0.06%-0.11%, and the transfer rates were 90.00%-96.92% and 32.45%-67.24%, respectively.The dry extract rate of the whole prescription was 22.58%-29.89%.In this experiment, the dissemination of quantity value of Wuzhuyu Decoction reference sample was analyzed by the combination of characteristic chromatogram, index component content and dry extract rate.A scientific and stable quality evaluation method of the reference sample was preliminarily established, which provided basis for the subsequent development of Wuzhuyu Decoction and the quality control of related preparations.

Response of spatio-temporal changes in sediment phosphorus fractions to vegetation restoration in the degraded river-lake ecotone.

Phosphorus (P) is an essential element in the ecosystem and the cause of the eutrophication of rivers and lakes. The river-lake ecotone is the ecological buffer zone between rivers and lakes, which can transfer energy and material between terrestrial and aquatic ecosystems. Vegetation restoration of degraded river-lake ecotone can improve the interception capacity of P pollution. However, the effects of different vegetation restoration types on sediment P cycling and its mechanism remain unclear. Therefore, we seasonally measured the P fractions and physicochemical properties of sediments from different restored vegetation (three native species and one invasive species). The results found that vegetation restoration significantly increased the sediment total P and bioavailable P content, which increased the sediment tolerance to P pollution in river-lake ecotone. In addition, the total P content in sediments was highest in summer and autumn, but lower in spring and winter. The total P and bioavailable P contents in surface sediments were the highest. They decreased with increasing depth, suggesting that sediment P assimilation by vegetation restoration and the resulting litter leads to redistribution of P in different seasons and sediment depths. Microbial biomass-P (MBP), total nitrogen (TN), and sediment organic matter (SOM) are the main factors affecting the change of sediment phosphorus fractions. All four plants' maximum biomass and P storage appeared in the autumn. Although the biomass and P storage of the invasive species Alternanthera philoxeroides were lower, the higher bioavailable P content and MBP values of the surface sediments indicated the utilization efficiency of sediment resources. These results suggest that vegetation restoration affects the distribution and circulation of P in river and lake ecosystems, which further enhances the ecological function of the river-lake ecotone and prevents the eutrophication and erosion of water and sediment in the river-lake ecotone.

UPLC-MS/MS method for the determination of the herb composition of Tangshen formula and the in vivo pharmacokinetics of its metabolites in rat plasma.

INTRODUCTION: Tangshen formula (TSF) is a traditional Chinese medicine composed of seven medicinal herbs including Astragalus membranaceus, Rehmannia glutinosa Libosch, Citrus aurantium L., etc. which is used to treat diabetic nephropathy III, IV qi and yin deficiency and stasis syndrome. Most of the studies on TSF are pharmacological and pharmacodynamic experiments. There are few basic studies on its chemical substances, and the effective constituents are not clear. OBJECTIVE: To analyse the main chemical components of TSF and the absorbed components in rat plasma following oral administration based on liquid chromatography tandem mass spectrometry (LC-MS/MS). Moreover, providing a rapid and valid analytical strategy for simultaneous determination of six components in rat plasma and use it in pharmacokinetic studies. RESULTS: A total of 132 components were identified in TSF, and 44 components were identified in rat plasma after oral TSF, 35 of which were prototype components and nine were metabolic components. A sensitive and reliable LC-MS/MS method was developed for simultaneous determination of six components in rat plasma. The intra-day and inter-day precision relative standard deviation (RSD) was lower than 15%; the accuracy of low, medium and high concentrations ranged from 80% to 120%. The recovery met the requirements and the RSD of the recoveries was less than 15%. CONCLUSION: A total of 132 components were identified in TSF. The LC-MS/MS quantitative method for the simultaneous determination of morroniside, loganin, notoginsenoside R1 , ginsenoside Re, ginsenoside Rb1 and astragaloside IV in rat plasma was established for the first time. The pharmacokinetic parameters are clarified, which can guide the clinical medication of TSF.

Active Components from Traditional Herbal Medicine for the Potential Therapeutics of Idiopathic Pulmonary Fibrosis: A Systemic Review.

Idiopathic pulmonary fibrosis (IPF), a tumor-like disease, is a serious and fatal pulmonary inflammatory condition usually characterized by irreversible destruction of the lung parenchyma, excessive matrix accumulation, and decline in lung function. IPF still remains a great burden to the universe. At the moment, the available therapeutic regimens utilized for IPF such as non-pharmacological therapies (lung transplantation) and pharmacological therapies (drugs, nintedanib, pirfenidone, etc.) are normally accompanied by significant limitations, such as adverse reactions, low bioavailability, poor selectivity, low-tissue distribution, in vivo instability, systemic toxicity, inconveniency and unsafe usage. There is a need for the exploration and discovery of new novel remedies by researchers and scientists globally. Recent numerous preliminary studies have laid significant emphasis and demonstrated the antifibrotic importance, good curative actions (little or no adverse reactions), and multiple target sites of the active components from traditional herbal medicine (THM) against IPF, which could serve as a modern, alternative and potential therapeutics or drug candidates in treating IPF. This paper extensively summarizes the pharmacological actions and signaling pathways or mechanisms of active components obtained from THM for treating IPF. Moreover, the sources and modernization, markets, relevant FDA and CFDA studies (the USA and China), preclinical analysis, and various compositions of THM currently under clinical trials are also highlighted. Additionally, this present analytical data would be instrumental towards further drug progression or advancement of active components from THM for the potential therapeutics of IPF in the future.

Herbal Textual Research of Poria in Famous Classical Formulas / 中国实验方剂学杂志

This review made a systematic textual research on the historical evolution and changes of the origin， producing areas and quality， harvest time and processing methods， and cultivation technique of Poria in famous classical formulas from the Catalogue of Ancient Famous Classical Formulas （the First Batch） by referring to the literature of ancient materia medica and medical books combining with the modern literature in CNKI， Wanfang Data and other databases， which could provide reference for the development and research of the famous classical formulas containing Poria. According to the research， the origin of Poria in ancient times was the dried sclerotia of Poria cocos. The producing area of Poria is widely distributed in China， mainly produced in Anhui， Hubei， Henan and Yunnan provinces. The quality of Poria from Yunnan is better， and the yield is larger in Anhui and Hubei provinces. The quality evaluation of Poria is basically the same from ancient to modern， which has the characteristics of large block， heavy weight， thin and wrinkled skin， and white and delicate cross section. The harvesting period of Poria is usually in August of the lunar calendar. The initial processing has undergone the evolution from drying in shade in the ancient time to drying in shade after sweating in the modern time. From ancient times to the present， Poria has been processed by cutting to prepare the Fuling lumps and Fuling slices. The cultivation technique has experienced the evolution process of "wild Poria-inoculation of live pine root-basswood cultured". At present， Poria is mainly cultivated by artificial basswood with mature technical methods and abundant yields， which can meet the research and development needs of the famous classical formulas.

[Analysis and consideration based on first classical prescriptions].

Classical prescriptions are precious wealth left by ancient Chinese medical scientists. Moreover,they are also the important part of the treasure-house in Chinese medicine. Classical prescriptions have a long and rich history for human-use in China and play an important role in keeping people healthy. The state administration of traditional medicine of China published the Catalogue of Classical Prescriptions(first batch) in 2018. This measure has inspired the enthusiasm of Chinese medicine manufacturers to study ancient classical prescriptions and develop classical compound prescriptions. Based on the first batch of classical prescriptions, the dosage forms, sources, prescription components, decocting degree, use of toxic drugs and processing methods of classical prescriptions. The results showed that most of the classical prescriptions in the first batch were decoction and boiled powder,while only four of them were powder and paste forms,all of which were originated from representative classics in the past dynasties. The dosage and decocting degree of decoction were greater than those of boiled powder. The dosage and decocting degree of decoction in Han and Tang Dynasties was close to that in Ming and Qing Dynasties,higher than that in Song and Jin Dynasties. Moreover,the average number of herbs in the prescriptions in Han Dynasty was the smallest. The use of toxic traditional Chinese medicine was the most frequent in Han Dynasty, and Pinellia ternata was the most common toxic medicine. There were various processing methods, including cleansing, cutting, stir-frying, roasting and so on. In this paper, the dosage forms of traditional paste, the time concept of decoction in the ancient times, the traditional roasting method and the processing method of toxic drugs were summarized to provide ideas and reference for further development of classical prescriptions.

Analysis and consideration based on first classical prescriptions / 中国中药杂志

Classical prescriptions are precious wealth left by ancient Chinese medical scientists. Moreover,they are also the important part of the treasure-house in Chinese medicine. Classical prescriptions have a long and rich history for human-use in China and play an important role in keeping people healthy. The state administration of traditional medicine of China published the Catalogue of Classical Prescriptions(first batch) in 2018. This measure has inspired the enthusiasm of Chinese medicine manufacturers to study ancient classical prescriptions and develop classical compound prescriptions. Based on the first batch of classical prescriptions, the dosage forms, sources, prescription components, decocting degree, use of toxic drugs and processing methods of classical prescriptions. The results showed that most of the classical prescriptions in the first batch were decoction and boiled powder,while only four of them were powder and paste forms,all of which were originated from representative classics in the past dynasties. The dosage and decocting degree of decoction were greater than those of boiled powder. The dosage and decocting degree of decoction in Han and Tang Dynasties was close to that in Ming and Qing Dynasties,higher than that in Song and Jin Dynasties. Moreover,the average number of herbs in the prescriptions in Han Dynasty was the smallest. The use of toxic traditional Chinese medicine was the most frequent in Han Dynasty, and Pinellia ternata was the most common toxic medicine. There were various processing methods, including cleansing, cutting, stir-frying, roasting and so on. In this paper, the dosage forms of traditional paste, the time concept of decoction in the ancient times, the traditional roasting method and the processing method of toxic drugs were summarized to provide ideas and reference for further development of classical prescriptions.

Absorption Characteristics of Combination Medication of Realgar and Indigo Naturalis: In Vitro Transport across MDCK-MDR1 Cells and In Vivo Pharmacokinetics in Mice after Oral Administration.

Realgar and indigo naturalis are clinically combined to treat varieties of leukemia. Exploring the drug-drug interactions might be beneficial to find active substances and develop new targeted drugs. This study aimed at exploring the change of arsenic concentration in mice and across MDCK-MDR1 cells and the cytotoxicity on K562 cells when realgar and indigo naturalis were combined. In the presence or absence of indigo naturalis, pharmacokinetics and cell-based permeability assays were used to evaluate the change of arsenic concentration, and K562 cell line was applied to evaluate the change of cytotoxicity. The drug concentration-time profiles exhibited that the combination medication group generated higher AUC, thalf, and longer MRT for arsenic, compared with the single administration of realgar. The apparent permeability coefficients (Papp) of bidirectional transport in MDCK-MDR1 cell permeability experiments showed that arsenic permeability obviously went up when indigo naturalis was incubated together. The combination medication significantly decreased the cell viability of K562 cells when both the concentration of realgar and the concentration of indigo naturalis were nontoxic. The pharmacokinetic research, the MDCK-MDR1 based permeability study, and the K562 cytotoxicity study were united together to verify the combination medication of realgar and indigo naturalis enhanced the absorption and the permeability across cells for arsenic and effectively inhibited the proliferation of K562 cell line. The molecular binding of As4S4 and indirubin was analyzed by computational study. It is predicted that the formation of the complex [As4S4 …Indirubin] involves noncovalent interaction that changes the concentration of arsenic.

Clinical Study on Middle-late Non-small Cell Lung Cancer Treated with Therapy of Strengthening Qi, Resolving Phlegm and Dissipating Mass / 广州中医药大学学报

Objective To observe the clinical effect of therapy of strengthening Qi, resolving phlegm and dissipating mass for middle-late non-small cell lung cancer. Methods Sixty patients with middle-late non-small cell lung cancer were randomly divided into 3 groups according to the results of intention-to-treat and genetic test. All of the 3 groups were given fundamental supportive and asymptomatic treatment, and additionally Group Ⅰ was mainly given oral use of Jinfuan Decoction with the actions of strengthening Qi, resolving phlegm and dissipating mass based on syndrome differentiation, group Ⅱ was treated with molecular targeted therapy with Gefitinib Tablets and /or Erlotinib Hydrochloride Tablets, and groupⅢ was only given the fundamental supportive and asymptomatic treatment. The 3 groups were treated for 3 cycles(84 days), and then we compared the tumor size, clinical symptoms, quality of life, distant metastasis, and the toxic and adverse effect in each group. Results (1) GroupⅠand group Ⅱhad stronger effect on relieving cough, shortness of breath and lassitude than groupⅢ(P<0.05); groupⅡand groupⅢwere more effective on relieving bloody sputum and chest pain than groupⅠ(P<0.05); groupⅠand groupⅢwere more effective on relieving fever than groupⅡ(P < 0.05). (2) In aspect of quality of life, KPS scores of groupⅠand group Ⅱwere much increased after treatment (P < 0.05), but the scores of group Ⅲ showed no obvious increase (P > 0.05). The improvement of KPS scores in groupⅠand groupⅡwas superior to that in groupⅢ(P<0.05). (3) GroupⅡhad a higher effective rate on stabilizing tumor size, the rate arrived to 65.0％, and was superior to that in groupⅠand groupⅢ(P <0.05) , and the effective rate in group Ⅰ was superior to that in group Ⅲ(P < 0.05). Group Ⅰ and group Ⅱhad a higher stabilizing rate than group Ⅲ(P < 0.05) , but the difference between group Ⅰ and group Ⅱ was insignificant (P>0.05). (4) GroupⅠhad less adverse reaction and higher safety. (5) The distant metastasis rate in groupⅠand groupⅡwas obviously lower than that in groupⅢ(P<0.05), but the difference of distant metastasis rate beetween group Ⅰ and group Ⅱ was insignificant (P > 0.05). Conclusion Therapy of strengthening Qi , resolving phlegm and dissipating mass is effective on relieving tumor-related symptoms , improving the quality of life, stabilizing the tumor, and controlling the distant metastasis in middle-late non-small cell lung cancer patients.

Preparation and physicochemical characterization of T-OA PLGA microspheres.

As the carrier of water-insoluble drugs, microspheres can play a role in increasing solubility and delaying releasing essence. The objective of this study was to improve the solubility and to delay the release of a newly discovered antitumor compound 3ß-hydroxyolea-12-en-28-oic acid-3, 5, 6-trimethylpyrazin-2-methyl ester (T-OA). Early-stage preparation discovery concept (EPDC) was employed in the present study. The preparation, physicochemical characterization, and drug release properties of PLGA microspheres were evaluated. T-OA-loaded PLGA microspheres were prepared by an oil-in-water (O/W) emulsification solvent evaporation method. Characterization and release behaviors of the T-OA PLGA microspheres were evaluated by X-ray diffract (XRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and high performance liquid chromatography (HPLC). The results demonstrated that T-OA-loaded PLGA microspheres could be successfully obtained through solvent evaporation method with appropriate morphologic characteristics and high encapsulation efficiency. The XRD analysis showed that T-OA would be either molecularly dispersed in the polymer or distributed in an amorphous form. The DSC and FTIR analysis proved that there were interactions between T-OA and PLGA polymer. SEM observations displayed the morphology of the microspheres was homogeneous and the majority of the spheres ranged between 50 and 150 µm. The drug release behavior of the microspheres in the phosphate buffered saline medium exhibited a sustained release and the duration of the release lasted for more than 23 days, which was fit with zero-order release pattern with r2 = 0.9947. In conclusion, TOA-loaded PLGA microspheres might hold great promise for using as a drug-delivery system in biomedical applications.

[Modified Shengma Biejia Decoction Combined with CAG Program for Elderly Acute Myeloid Leuke- mia Patients with Yin Deficiency Toxin Stasis Syndrome].

OBJECTIVE: To observe the efficacy and safety of modified Shengma Biejia Decoction (MSBD) combined with CAG program in treating elderly acute myeloid leukemia (AML) patients with yin deficiency toxin stasis syndrome (YDTSS). METHODS: Totally 46 elderly AML patients were assigned to the treatment group (24 cases; treated with MSBD + CAG) and the control group (22 cases; treated with CAG + placebos of Chinese medicine) according to random digit table. The therapeutic course of CM placebo or MSBD was 21 days. The clinical efficacy and adverse reactions were observed. Meanwhile, physical state (ECOG Score), transfusion dependency, and TCM syndrome score were compared before and after treatment. RESULTS: (1) The complete remission rate was 54% (13/24) and the objective response rate (ORR) was 71% (17/24) in the treatment group, obviously higher than those of the control group [36% (8/22); 54% (13/24)], with statistical difference (P = 0.036, 0.042). When comparing the efficacy based on risk level, the moderate and poor ORR was 71% (10/14) and 67% (6/9) in the treatment group, and 57% (8/14) and 33% (2/6) in the control group, with statistical difference between the two groups (P = 0.048; P = 0.010). (2) Compared with before treatment in the same group, the ECOG score significantly decreased, the average infusion time of red cells and platelets were markedly prolonged in the treatment group after treatment (P < 0.05). ECOG score, the average infusion time of red cells and platelets were significantly better in the treatment group than in the control group after treatment (P < 0.05). (3) Compared with before treatment in the same group, scores of fever, hemorrhage, and bone pain were markedly reduced in the control group (P < 0.05); scores of fever, fatigue, hemorrhage, dry mouth, and bone pain were markedly reduced in the treatment group (P < 0.05). Better effect in relief of fever, fatigue, hemorrhage, dry mouth, and so on was obtained in the treatment group than in the control group (P < 0.05). (4) In aspect of hematotoxicity, the incidence of neutropenia, anemia, thrombocytopenia was obviously lower in the treatment group than in the control group [29.2% (7/24) vs 54.5% (12/22); 16.7% (4/ 24) vs 45.5% (10/22); 33.3% (8/24) vs 63.6% (14/22); P < 0.05]. The incidence of fatigue and anorexia was obviously lower in the treatment group than in the control group [37.5% (9/24) vs 63.6% (14/22), 37.5% (9/24) vs 81.8% (18/22); P < 0.05]. CONCLUSION: MSBD combined with CAG program in treating elderly AML patients with YDTSS, with efficacy enhancing toxicity reducing effect, had distinct advantages in improving physical condition and clinical symptoms, and reducing transfusion dependency.

[Experience of Professor SUN Xue-mei in Treatment of Primary Thrombocythemia].

There is no radical cure for essential thrombocythemia currently. Professor SUN Xue-mei has extensive clinical experience in treating it by combined therapy of Chinese and Western medicine. In this paper, authors tried to summarize her experience from guiding ideology and therapeutic points. Authors insisted on the direction of integrative medicine on the basis of syndrome differentiation, paying attention to psychological counseling,and applied individual treatment in clinics.

[Thinking on Treatment of Severe Aplastic Anemia by Detoxication, Blood Activating, and Yin Nourishing Method].

Chinese medicine therapy has advantages in treating aplastic anemia (AA) in depart- ments of Chinese medicine (CM) blood diseases. But there is no unified syndrome typing standard of CM for severe AA. Heat-toxin induced yin deficiency syndrome is one of severe AA syndrome types com- monly seen in authors' long-term clinical practice. This syndrome type has the features of asthenia in ori- gin and asthenia in superficiality. Therefore, authors put forward that detoxication, blood activating, and yin nourishing (DBAYN) method, taking detoxication as superficiality and Shen supplementing as origin. Meanwhile, blood activating and stasis removing was assisted. Detoxication aimed to eliminating evils and purifying blood, blood activating aimed to getting rid of evils and generating new blood, and yin nour- ishing aimed to strengthening vital qi and nourishing blood. Classical recipes such as Xijiao Dihuang De- coction and Erzhi Pill could be modified. This theory was of great significance in complementing and per- fecting CM theoretical systems of AA, which provided beneficial ideas and methods for clinical treatment of severe AA.