OBJECTIVE To synthesize p-toluenesulfonic acid(PTS) and famotidine(FMT) cocrystal in order to improve thesolubility of famotidine in water and the permeability. OBJECTIVE The cocrystal was prepared by solvent evaporation method combined with ultrasound. The cocrystal was characterized by scanning electron microscopy, differential scanning calorimetry, thermogravimetric analysis, infrared spectroscopy and powder X-ray diffraction. The single crystal structure of FMT-PTS-H₂O(1∶1∶1) was successfully obtained, and the solubility and permeability of the newly synthesized cocrystal were studied. RESULTS After the formation of cocrystal, the water solubility and permeability of FMT increased by 1.54 and 2.29 times, respectively. CONCLUSION Compared with FMT, the solubility and permeability of FMT after the formation of cocrystal were improved. This study provides a method for improving the permeability of biopharmaceutics classification system(BCS)Ⅲ drugs, which will contribute to the development of low permeability drugs.

Cell membrane chromatography is a bioaffinity chromatography method which has been developing rapidly in recent years, where the carriers coated with receptor-containing biomembrane are packed to stationary phase and the bioaffinity between compound and membrane receptor presents in chromatography process. This method has the advantages of biomimetic, high efficiency and low cost, and has been widely used in drug screening and identifying the affinity between membrane receptor and candidate ligand. Mitochondria, a crucial functional intracellular membrane system, with various drug targets residing in membrane. Recently, significant research advancements have been made in mitochondrial membrane chromatography technology. In this paper, the recent progresses and applications of cell membrane chromatography and mitochondria membrane chromatography are reviewed.

In recent years, transdermal delivery has proven to be one of the most favorable methods among novel drug delivery systems due to avoiding the gastrointestinal tract and reducing systemic side effects. Skin is one of the most immunologically active organs due to the presence of immune cells, such as Langerhans cells(LCs), dermal dendritic cells(dDCs), and T cells. Unique immune properties of the skin offer excellent opportunities for transdermal treatment of autoimmune diseases(ADs). This review highlights the pathogenic mechanism of ADs caused by various reasons such as loss of immune self-tolerance and abnormal autoreactive T cells, and the advantages of transdermal drug delivery for the treatment of ADs, as well as expounds on the application of transdermal drug delivery systems(TDDS) in the treatment of several typical ADs. TDDS will provide new ideas and methods for the treatment and research of autoimmune diseases.

OBJECTIVE To study the protective effect of petroleum ether fraction(AERP) and water soluble fraction(AERW) of Arnebia euchroma(Royle) Johnst. on acute liver injury in mice, and to isolate the effective components of petroleum ether fraction with better effect, and to study the antihepatitis B virus effect of its effective components. OBJECTIVE Forty eight C57 mice were randomly divided into 6 groups. After 14 days of administration, lipopolysaccharide/D-galactosamine(LPS/D-Galn) was used to induce acute liver injury with inflammatory infiltration at the last 2 hours. The liver and spleen index, the content of AST and ALT in mouse serum and the content of NO in liver homogenate were measured, and the pathological section of liver tissue was investigated. The petroleum ether extract was separated by normal silica gel, reverse silica gel and thin layer preparation plate, and four active naphthoquinones were obtained. The antihepatitis B virus activity of the four active naphthoquinones on HepG2.2.15 cells was detected by MTT method. RESULTS Both AERW high-dose group and AERP low-dose group can reduce the activity of AST and ALT in serum and the content of NO in liver tissue of mice to varying degrees, and improve the pathological changes of liver tissue to varying degrees. After comparative analysis, AERP has better liver protective and anti-inflammatory effects. The extraction method of AERP was optimized to obtain AERP with more effective components, and four active naphthoquinones were isolated: isovalerylshikonin, acetylshikonin, 2,3-dimethylpentenylshikonin and shikonin. Four active naphthoquinones have good inhibitory effects on HepG2.2.15 cells. CONCLUSION The results show that AERW and AERP have a good protective effect on acute liver injury. The liver protective effect of AERP is better than that of AERW. The four active components of AERP have a good inhibitory effect on HBV. AER extract has a significant liver protective effect, and the active components of AER have a significant inhibitory effect on hepatitis B virus.

Rheumatoid arthritis(RA) is a chronic, systemic, and abnormal inflammatory immune response. It is characterized by the involvement of synovium and multiple organs and the destruction of joints and articular cartilage. In the past 30 years, some promising new compounds and antibodies have been developed to treat RA. The introduction of RA therapeutic drugs and the development of precision medicine have also given rise to several problems related to patients' access to new treatments, choice of the best regimen, cost-effectiveness, prognosis monitoring and efficacy monitoring, especially in terms of low drug response rate, drug resistance and adverse side effects. People attach great importance to the best combination of drugs for the treatment of RA, especially in patients with severe symptoms or early progression. New treatments and mechanisms are needed to solve these problems, and accurate guidelines for drug selection and drug recombination are established. According to the clinical trial database of the National Library of Medicine, this study summarizes the exciting new drugs, and discusses the trends and challenges in the development of RA drugs, which provides a meaningful reference for the accurate treatment and future research direction of RA.

OBJECTIVE To study the chemical constituents of Pinellia ternata(Thunb).Breit.. OBJECTIVE The 60% ethanol extract of Pinellia ternata(Thunb). Breit. was isolated and purified by silica, MCI, ODS and preparative HPLC, and the structures of obtained compounds were identified by physico-chemical properties and MS、NMR data. RESULTS The compound are kaempferol-3-O-β-D-rutinoside(1), inosine(2), lactariolide I(3), (2E,4E,1'S,2'R,4'S,6'R)-dihydrophaseic acid(4), tryptophan(5), 1-oleoyl-3-O-β-D-galactopyranosyl-sn-glycerol(6), 6'-O-linoleylsucrose(7), 6'-O-palmitoylsucrose(8), gingerglycolipid C(9), (2S)-1-O-6'-O-(α-D-galactopyranosyl)-β-D-galactopyranosyl-3-O-palmitoyl glyceride(10), 1-O-hexadecanoyl-3-O-β-D-galatopyranosylglycerol(11), tianshic acid(12), 4-(2-hydroxyethyl)phenol(13), phenylpropionic acid(14), 3-phenyllactic acid(15), trans-cinnamic acid(16). CONCLUSION Compound 1, 2, 3, 4, 6-13, 15-16 are firstly isolated from the genus Pinellia.

OBJECTIVE To investigate the effects of different drying methods on the concentrates of Astragalus membranaceus and provide a basis for the optimization and establishment of their drying processes. METHODS The contents of Astragalus methyloside, Pistil isoflavone glucoside, Pistil isoflavone, Mangiferin, Astragalus polysaccharide, ethanol extract and the clarity index and solubility index were used as evaluation indexes to dry Astragalus concentrate by freeze-drying, vacuum drying, atmospheric pressure drying and microwave drying, and the weights of each index were jointly determined by hierarchical analysis (AHP) and entropy weighting method, and the most suitable drying method was selected by the combination of comprehensive scoring, cluster analysis, fingerprinting and other methods as well as the characteristics of each drying method itself. RESULTS The effects of different drying methods on the concentration of Astragalus membranaceus varied widely, with the highest comprehensive scores for freeze-drying and vacuum-drying and lower scores for atmospheric-pressure drying and microwave drying. According to the analysis of similarity evaluation software, the fingerprint profiles of freeze-dried and vacuum-dried samples were the most similar to those of concentrates, the differences between the samples obtained from the two drying methods were small, and the results were similar to the comprehensive scores. Within the experimental range, the concentrates of Astragalus membranaceus were more stable under freeze-drying and vacuum-drying conditions. CONCLUSION The effect of different drying methods and conditions on Astragalus concentrates varies greatly. Through the study of four drying methods, vacuum drying is finally selected as the most suitable drying method for Astragalus concentrates.

Rectal in situ gel combines the double characteristics of gel and rectal administration, and has become the focus of pharmaceutics research. Rectal in situ gel is a kind of non-chemical crosslinked semi-solid gel which can be transformed from liquid to gel immediately after administration in solution. It has unique reverse hot gel properties, good sustained release effect and high bioavailability. Referring to the relevant literature at domestic and abroad in the past 10 years, the characteristics, preparation technology, quality evaluation methods and application of rectal in situ gel were summarized.By analyzing the research progress of rectal in situ gel new ideas for the research and development of efficient rectal administration preparations are provided.

OBJECTIVE To study the chemical constituents of ethyl acetate extract from Moringa oleifera leaves. METHODS The chemical constituents of ethyl acetate extract from Moringa oleifera leaves were isolated and purified by chromatographic methods. The structures of isolated compounds were identified by MS and NMR data. DPPH and ABTS were used to test the antioxidant activities of the compounds in vitro. RESULTS Fourteen compounds were isolated from ethyl acetate extract of Moringa oleifera leaves and identified as icariside B1 (1), (3S)-O-β-D-glucopyranosyl-6-[3-oxo-(2S)-butenylideny]-1, 1, 5-trimethylcyclohexan-(5R)-ol (2), icariside B2 (3), 9-hydroxy-megastigma-4, 7-dien-3-one-9-O-β-D-glucopyranoside (4), tectorigenin (5), tectoridin (6), iristectorin A (7), iristectorin B (8), 5-hydroxy-2-hydroxymethylpyridine (9), androsin (10), 3, 4, 5-trimethoxyphenyl-1-O-β-D-glucopyranoside (11), 1-O-(4-hydroxymethylphenyl)-α-L-rhamnopyranoside (12), benzyl-O-β-D-glucopyranoside (13) and methyl 2-[4-(α-L-rhamnopyranosyl) phenyl] acetate (14), respectively. Among them, compounds 6, 7 and 8 had certain antioxidant activities, but the activities were weaker than that of vitamin C as positive control. CONCLUSION Compounds 2-11 are isolated from Moringa genus for the first time.

OBJECTIVE To investigate the non-clinical safety and immunogenicity of recombinant group B meningococcal vaccine by repeatedly dose to rats, so as to provide reference for designing dose level and monitoring toxicity and side effects in clinical trials. METHODS SD rats were used to design 4 main toxicity groups including negative control group, adjuvant control group, low dose vaccine group (1 dose each) and high dose vaccine group (3 doses each) and 3 satellite groups. The vaccine was dosed by intramuscular injection at weeks 0, 3, 6, 9 and 12 respectively. During the study, all the animals of the main toxicity group were observed for clinical signs, indicators such as body weights, food consumption, body temperature, blood cells counting, coagulation, serum biochemistry, ophthalmology, T lymphocyte subsets and cytokines were detected. Serum specific IgG antibody and bactericidal antibody were measured for satellite animals. All the animals were observed anatomically, main organs were weighed to the calculate viscera/body ratio and the viscera/brain ratio, and various tissues and organs were examined pathologically. RESULTS It could produce high-leveled binding antibodies and bactericidal antibodies with strong activity in immune serum that rats injected the low and high doses of recombinant group B meningococcal vaccines. Both the low and high dose vaccines caused the increases in neutrophils, monocytes and lymphocytes significantly, the decreases in hemoglobin and RBC significantly. Other dose-related changes involved the increase in serum globulin and decrease in albumin, with concomitant decrease in A/G, which basically returned to normal after 4 weeks of recovery period. The histopathological findings associated with adjuvant and vaccine were mild or moderate granulomatous inflammation, acute inflammation in injection site, infiltration and proliferation of mononuclear cells/mixed cells in the sciatic membrane, and increased number of myeloid plasma cells and granulocytes in lymph nodes. CONCLUSION Recombinant group B meningococcal vaccine had good immunogenicity and safety profile in SD rats, there is no immune toxicity reaction. It is obvious that adjuvant and vaccine-related changes in indicators of peripheral blood and the inflammation response in injection site. Under the dose levels of this study, there is no adverse effect level on recombinant B group meningococcal vaccine for 3 doses/one rat.