1.Switching to TMF rescue therapy in patients developing low-level viremia with ETV or TAF treatment
Chengrun SONG ; Yujing LI ; Lanqing LI ; Enqiang CHEN
Chinese Journal of Hepatology 2024;32(S1):14-18
Objective:Some patients receiving entecavir (ETV) or tenofovir alafenamide fumarate (TAF) monotherapy may develop low-level viremia. Therefore, this study aims to observe whether switching to tenofovir alafenamide fumarate (TMF) monotherapy can further improve the efficacy of antiviral therapy in patients with chronic hepatitis B with low-level viremia.Methods:Patients with chronic hepatitis B who received ETV or TAF monotherapy for over one year were chosen. The serum HBV DNA of all patients from initiation to end fluctuated between 20-2 000 IU/ml were observed. All patients who voluntarily switched to TMF to continue antiviral treatment and completed a comprehensive examination at least once every six months were selected. The primary outcome measure was the undetectable rate of HBV DNA following six and twelve months of TMF treatment, and the secondary outcome measures were the incidence of renal tubular injury and dyslipidemia. Two independent sample t-tests or U-tests were used to compare the intergroup measurement data. The intergroup comparison of count data was performed using the χ2 test or Fisher's exact probability method. Results:A total of 73 patients were included, of which 47 received ETV and 26 received TAF treatment. Among them, 33 cases were hepatitis B e antigen (HBeAg)-positive and 40 were HBeAg-negative. 69.9% (51/73) and 74.0% (54/73) of patients had HBV DNA<20 IU/ml following switching to TMF treatment for six and twelve months, respectively. Compared with HBeAg-positive patients, HBeAg-negative patients who switched to TMF treatment had a higher proportion of complete virological response (19/33 vs. 32/40, P=0.038; 18/33 vs. 36/40, P<0.001). The abnormal rate of urinary β2-microglobulin was 16.4% (12/73) after twelve months of treatment, and the proportion of patients with urinary 2-microglobulin that exceeded three times the upper limit of normal was 6.8%. The proportion of blood phosphate below the normal lower limit was 19.2% (14/73). The total cholesterol and low-density lipoprotein cholesterol levels rose compared to before therapy; however, the difference was not statistically significant. Conclusion:CHB patients receiving treatment with ETV or TAF develop low-level viremia. Therefore, switching to TMF can help most patients achieve a complete virological response and possesses good patient tolerance.
2.Switching to TMF rescue therapy in patients developing low-level viremia with ETV or TAF treatment
Chengrun SONG ; Yujing LI ; Lanqing LI ; Enqiang CHEN
Chinese Journal of Hepatology 2024;32(S1):14-18
Objective:Some patients receiving entecavir (ETV) or tenofovir alafenamide fumarate (TAF) monotherapy may develop low-level viremia. Therefore, this study aims to observe whether switching to tenofovir alafenamide fumarate (TMF) monotherapy can further improve the efficacy of antiviral therapy in patients with chronic hepatitis B with low-level viremia.Methods:Patients with chronic hepatitis B who received ETV or TAF monotherapy for over one year were chosen. The serum HBV DNA of all patients from initiation to end fluctuated between 20-2 000 IU/ml were observed. All patients who voluntarily switched to TMF to continue antiviral treatment and completed a comprehensive examination at least once every six months were selected. The primary outcome measure was the undetectable rate of HBV DNA following six and twelve months of TMF treatment, and the secondary outcome measures were the incidence of renal tubular injury and dyslipidemia. Two independent sample t-tests or U-tests were used to compare the intergroup measurement data. The intergroup comparison of count data was performed using the χ2 test or Fisher's exact probability method. Results:A total of 73 patients were included, of which 47 received ETV and 26 received TAF treatment. Among them, 33 cases were hepatitis B e antigen (HBeAg)-positive and 40 were HBeAg-negative. 69.9% (51/73) and 74.0% (54/73) of patients had HBV DNA<20 IU/ml following switching to TMF treatment for six and twelve months, respectively. Compared with HBeAg-positive patients, HBeAg-negative patients who switched to TMF treatment had a higher proportion of complete virological response (19/33 vs. 32/40, P=0.038; 18/33 vs. 36/40, P<0.001). The abnormal rate of urinary β2-microglobulin was 16.4% (12/73) after twelve months of treatment, and the proportion of patients with urinary 2-microglobulin that exceeded three times the upper limit of normal was 6.8%. The proportion of blood phosphate below the normal lower limit was 19.2% (14/73). The total cholesterol and low-density lipoprotein cholesterol levels rose compared to before therapy; however, the difference was not statistically significant. Conclusion:CHB patients receiving treatment with ETV or TAF develop low-level viremia. Therefore, switching to TMF can help most patients achieve a complete virological response and possesses good patient tolerance.
3.Preparation and in vitro evaluation of doxorubicin-loaded magnetic iron oxide nanoparticles.
Song SHEN ; Lin WU ; Chengrun WANG ; Xueyong QI ; Yanru GE ; Yi JIN
Acta Pharmaceutica Sinica 2013;48(12):1844-9
PEG-modified magnetic Fe3O4 (Fe3O4-PEG) nanoparticles were sythesized using a solvothermal reaction and characterized with transmission electron microscopy (TEM) and thermo gravimetric analysis (TGA). The photothermal effect and photothermal destruction of cancer cells were evaluated. Then the doxorubicin loaded Fe3O4-PEG (DOX-Fe3O4-PEG) nanoparticles were prepared. The cytotoxicity and combined chemotherapy/photothermal therapy (PTT) effect were investigated. Uniform PEG coated Fe3O4 nanoparticles with particle size of 155 nm were obtained in the experiment. The loading and release of doxorubicin on Fe3O4-PEG were pH-dependent. The drug loading capacity in water was 21%. The results of MTT indicated a good biocompatiblity of Fe3O4-PEG nanoparticles and high cytotoxicity of DOX-Fe3O4-PEG. In combined therapy experiment, photothermal therapy demonstrated unambiguously enhanced chemotherapy efficacy. In conclusion, the obtained Fe3O4-PEG nanoparticles which exhibit good photothermal effect and drug loading capacity can be used for chemotherapy and photothermal therapy. The synergetic anti-tumor activity indicates the potential for the combined application of chemotherapy and photothermal therapy in cancer treatment.
4.Preparation and evaluation of enteric-coated and taste masking clarithromycin granules.
Tian ZHANG ; Chengrun WANG ; Song SHEN ; Yi JIN ; Yanru GE
Acta Pharmaceutica Sinica 2011;46(12):1520-5
The study is to prepare taste masking and enteric-coated clarithromycin granules by melting and fluid bed coating technology. Clarithromycin and matrix materials were melted at a certain temperature, and then made into particles by fluidized bed coating. X-ray powder diffraction and scanning electron microscopy were used to identify the crystal and morphology of drug loading granules. In vitro dissolution method was used for the observation of the drug release behavior. The results showed that the drug particles size range was 0.2 - 0.6 mm; the crystal form of clarithromycin in the granule did not change; enteric-coated granules accumulated release in 0.1 mol L(-1) hydrochloric acid in 2 h was less than 10%, while in pH 6.8 phosphate buffer in 1 h was more than 80%. The taste masking and enteric-coated clarithromycin granules not only have good taste masking effect, but also have a good release behavior. It is expected to have better clinical application.

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