1.Preparation of ibuprofen/EC-PVP sustained-release composite particles by supercritical CO2 anti-solvent technology.
Jinyuan CAI ; Dechun HUANG ; Zhixiang WANG ; Beilei DANG ; Qiuling WANG ; Xinguang SU
Acta Pharmaceutica Sinica 2012;47(6):791-6
Ibuprofen/ethyl-cellulose (EC)-polyvinylpyrrolidone (PVP) sustained-release composite particles were prepared by using supercritical CO2 anti-solvent technology. With drug loading as the main evaluation index, orthogonal experimental design was used to optimize the preparation process of EC-PVP/ibuprofen composite particles. The experiments such as encapsulation efficiency, particle size distribution, electron microscope analysis, infrared spectrum (IR), differential scanning calorimetry (DSC) and in vitro dissolution were used to analyze the optimal process combination. The orthogonal experimental optimization process conditions were set as follows: crystallization temperature 40 degrees C, crystallization pressure 12 MPa, PVP concentration 4 mgmL(-1), and CO2 velocity 3.5 Lmin(-1). Under the optimal conditions, the drug loading and encapsulation efficiency of ibuprofen/EC-PVP composite particles were 12.14% and 52.21%, and the average particle size of the particles was 27.621 microm. IR and DSC analysis showed that PVP might complex with EC. The experiments of in vitro dissolution showed that ibuprofen/EC-PVP composite particles had good sustained-release effect. Experiment results showed that, ibuprofen/EC-PVP sustained-release composite particles can be prepared by supercritical CO2 anti-solvent technology.
2.Inhibitory effect of small-molecule compound AM679 targeting elongation-factor binding protein 2 on hepatitis B virus in vitro
Huijing FANG ; Jinyuan CAI ; Xiaoxue HOU ; Jiali SONG ; Linya PENG ; Chuanlong ZHU
Chinese Journal of Hepatology 2024;32(4):318-324
Objective:To explore the antiviral activity of the small-molecule compound AM679 in hepatitis B virus (HBV) replication and infection cell models.Methods:The positive regulatory effect of AM679 on EFTUD2 expression was validated by qPCR and Western blotting. HepAD38 and HepG2-NTCP cells were treated with AM679 (0.5, 1, and 2 nmol/L). Negative control, positive control, and AM679 combined with the entecavir group were set up. HBV DNA intra-and extracellularly, as well as the expression levels of intracellular HBV total RNAs and 3.5kb-RNA changes, were detected with qPCR. Hepatitis B surface antigen (HBsAg) and hepatitis B e antigen (HBeAg) levels were measured in the cell supernatant by an enzyme-linked immunosorbent assay (ELISA). The t-test method was used for the statistical analysis of the mean difference between groups.Results:EFTUD2 mRNA and protein expression levels were significantly increased in HepAD38 and HepG2-NTCP cells following AM679 treatment, with a statistically significant difference ( P ?0.001). Intra-and extracellular indicators such as HBV DNA, HBV RNAs, HBV 3.5kb-RNA, HBsAg, and HBeAg were decreased to varying degrees in both cell models, and the decrease in these indicators was more pronounced with the increase in AM679 concentration and prolonged treatment duration, while the combined use of AM679 and entecavir had a more significant antiviral effect. The HBV DNA inhibition rates in the supernatant of HepAD38 cells with the use of 2 nmol/L AM679 were 21% and 48% on days three and nine, respectively. The AM679 combined with the ETV treatment group had the most significant inhibitory effect (62%), with a P ?0.01. More active HBV replication was observed after silencing EFTUD2, while the antiviral activity of AM679 was significantly weakened. Conclusion:AM679 exerts anti-HBV activity in vitro by targeting the regulation of EFTUD2 expression.
3.Thoracoscopic pleural lavage for empyema after liver transplantation
Songwang CAI ; Libao LIU ; Yimin WENG ; Shaohong HUANG ; Jun AN ; Jun LI ; Huiguo CHEN ; Jinyuan HE ; Shen LAO ; Junhang ZHANG ; Hongying LIAO
Chinese Journal of Hepatic Surgery(Electronic Edition) 2015;(2):97-99
ObjectiveTo explore the application value of thoracoscopic pleural lavage for empyema after liver transplantation (LT).MethodsClinical data of 5 patients who underwent thoracoscopic pleural lavage for empyema after LT in the Third Afifliated Hospital of Sun Yat-sen University from October 2002 to October 2013 were analyzed retrospectively. All 5 patients were males with the age ranging from 42 to 56 years old and the median of 51 years old. The informed consents of all patients were obtained and the local ethical committee approval had been received. The patients received thoracoscopic pleural lavage for empyema under endotracheal general anesthesia. The thoracoscope was introduced in the seventh intercostal space on the mid-axillary line. The aspirator was inserted in the third intercostal space on the anterior line to drain the pus. And the pleural ifberboard was peeled off. The intraoperative situation and perioperative recovery of the patients were observed.ResultsFive patients received successful operations and recovered and were discharged from hospital. The median length of operation was 2(1-3) h. The length of respirator assisted ventilation was 26(6-42) h. The intraoperative blood loss was 600(300-1 000) ml. The length of indwelling chest drainage tube was 4(2-6) h. The volume of chest drainage was 680(350-1 200) ml. No mortality, empyema recurrence and other serious complications were observed. The postoperative hospital stay was 7(5-11) d.ConclusionThoracoscopic pleural lavage for empyema after LT is a safe and effective treatment.
4.Synthesis and Quality Evaluation of Mitoxantrone
Mingming WANG ; Jinyuan CAI ; Jing LIU ; Puzhong GU ; Huihui SHI ; Yanjun ZHANG
China Pharmacy 2019;30(13):1769-1774
OBJECTIVE: To synthetize the synthesis of mitoxantrone and evaluate its quality. METHODS: Crude product of mitoxantrone was prepared by slow oxidation of 1,4,5,8-tetrahydro-anthraquinone with N-(2-hydroxyethyl) ethylenediamine in water bath at 50 ℃ for 2 h under argon protection and in dry air for 4 h. The crude product was crystallized by ethanol-n-hexane (4 ∶ 1,V/V) mixture solution, which was cooled overnight and then washed by ethanol-n-hexane mixture for many times. The melting range, pH value of solution, ultraviolet-visible absorption spectrum, infrared structural characteristics, drying weight loss (water loss rate) and critical relative humidity (CRH) of the purified products (4 batches) were investigated. HPLC method was used to determine the contents of mitoxantrone. RESULTS: The mitoxantrone was prepared successfully, and synthetic yield of mitoxantrone was 34.3%; the melting point ranged from 159.1-163.6 ℃. The aqueous solution was alkaline (pH 7.63-9.54); there was a maximum ultraviolet absorption peak at 235-245 nm; there was a maximum absorption peak of visible light at 590-600 nm; the infrared characteristics were consistent with those described of mitoxantrone in the 2015 edition of the Infrared Spectrum Collection of Drugs; water loss rate were -0.83%-2.36%; CRH value was 54.7%, and the average content of the product was 78.1%(n=4) by HPLC method. CONCLUSIONS: The mitoxantrone is synthesized under mild, non-toxic and harmless experiment conditions. The synthesis step is simple, the cost is low and the yield is high. The quality of products meets the quality requirements.