1.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.
2.The role of transoralsonography guiding fine-needle aspiration biopsy in the diagnosis of retropharyngeal or parapharyngeal masses identified on the images of treated patients with malignant carcinoma
Youwang ZHANG ; Yafang HUANG ; Hongmei YING ; Lin KONG ; Yongru WU ; Chengrun DU ; Chaosu HU
Chinese Journal of Radiation Oncology 2015;(4):427-430
Objective To investigate the role of transoralsonography guiding fine?needle aspiration biopsy in the diagnosis of retropharyngeal or parapharyngeal masses identified on the CT, MRI or PET?CT images of treated patients with malignant carcinoma. Methods From 2002 to 2013,this study recruited fifty?five patients with a history of cancer, of which 50 were treated with radiation treatment, including 46 nasopharyngeal carcinoma, 3 esophagus squamous cell carcinoma and1 lung apex carcinoma. There were 4 patients with a history of 1 thyroid papillary carcinoma, 1 buccal mucosa squamous cell carcinoma,1 glottis squamous cell carcinoma and 1 sigmoid colon adenocarcinoma treated with surgery. The rest one patient with nasal olfactory neuroblastoma was treated by postoperative radiation. The enlarged retropharyngeal lymph nodes in 44 cases and parapharyngeal masses in 10 cases were identified on CT or MRI imges. The enlarged retropharyngeal lymph node in the rest case was identified on PET?CT. With transoral ultrasound examination, all lesions were with hypo?intensity echo. Cystic areas were noted on occasion. Biopsy was performed in all cases. Results After cytology examination, carcinoma cells were detected in 37 retropharyngeal lymph nodes, with a detection rate of 82% (37/ 45). In the 10 parapharyngeal masses, carcinoma cells were detected in 3 lesions, with a detection rate of 30%. Conclusions Transor alsonography guiding fine?needle aspiration biopsy can be useful in the cytopathology diagnosis of retropharyngeal or parapharyngeal masses identified on the CT, MRI or PET?CT images of treated patients with malignant carcinoma,which facilitates, early diagnosis and treatment for patients.
3.Predictors for HBeAg negative chronic hepatitis patients with steatosis and its value in diagnosis of hepatic inflammation and fibrosis
Ruidan ZHENG ; Chengrun XU ; Jiarong MENG ; Minfeng ZHANG ; Aixia DOU ; Kun ZHOU ; Lungen LU
Chinese Journal of Digestion 2009;29(9):533-536
Objective To investigate the relationship between clinical presentation and pathological characteristics in HBeAg negative chronic hepatitis B(CHB) patients with steatosis, and to find out the predictors of hepatic inflammation and fibrosis. Methods HgeAg negative CHB patients with (n=56) or without (n=60) steatosis confirmed clinically and pathologically were enrolled in the study. All patients were examined for fasting blood glucose(FBG), fasting insulin (FINS), triglyceride (TG), cholesterol (TC), alanine aminotransferase (ALT), aspartate aminotransferase (AST), gamma-glutamyhransferase (GGT), alkaline phosphatase (ALP) albumin (Alb), globulin(Glb), homeostatic model assessment of insulin resistance (HOMA-IR), HBV-DNA and body mass index(BMI). The association of above parameters with hepatic inflammation, fibrosis and fatty deposition were analyzed statistically. Results It was demonstrated that BMI, FBG, FINS, TG, TC, GGT, ALP , Glb and HOMA-IR were significantly higher in HBeAg negative CHB patients with steatosis than those without steatosis (P<0.05). Whereas the levels of HBV-DNA, Alb, ALT and AST were significantly lower in HBeAg negative CHB patients with steatosis compared with those without steatosis (P<0.05). The hepatic inflammation and fibrosis were aggravated in patients with steatosis. It was implicated that BMI,FBG, FINS, TG, TC, GGT and HOMA-IR(all P values 0.05) were significant predictors for hepatic steatosis, while ALT, AST, Glb and HBV-DNA(all P values <0.05) were significant predictors for hepatic inflammation. And the predictors for hepatic fibrosis were ALT, AST, Alb, Glb and HBV-DNA(all P values <0.05). Conclusions Hepatic steatosis is common in HBeAg negative CHB patients which is positively associated with parameters including BMI, FBG, FINS, TG, TC, GGT, ALP and HOMA-IR. Besides steatosis, the hepatic inflammation and fibrosis are also aggravated in these patients.
4.Preparation and preliminary biological evaluation of domestic 177Lu-PSMA-617
Xinyi ZHANG ; Wenhui FU ; Tingting XU ; Chengrun ZENG ; Yuxiao XIA ; Huipan LIU ; Lin CHEN ; Chi QI ; Yuchuan YANG ; Hongyuan WEI ; Yue CHEN
Chinese Journal of Nuclear Medicine and Molecular Imaging 2021;41(5):296-302
Objective:To synthesize 177Lu-prostate-specific membrane antigen (PSMA)-617 with domestic 177Lu (made in China), and explore its optimal labeling condition, biodistribution, stability, and safety. Methods:177Lu-PSMA-617 was prepared with domestic 177Lu by a manual method. The optimal labeling condition, radiochemical purity, stability ( in vivo and in vitro), lipid-water partition coefficient, and plasma protein binding rate were determined. The uptake rate of 177Lu-PSMA-617 was evaluated by using 22RV1 cells. Biodistribution and SPECT/CT imaging were performed on normal mice with imported 177Lu-PSMA-617 as control group. The blood routine test was performed to evaluate the safety. Results:The best labeling result of domestic 177Lu-PSMA-617 can be obtained under the following conditions: pH=4.5, 100 ℃ for 30 min. And the radiochemical purity was ≥99%. The product was stable in vivo and in vitro, with the radiochemical purity >95% in 72 h. The plasma protein binding rate was (35.3±5.3)%, the lipid-water partition coefficient was -2.27±0.06, and the specific uptake rate of domestic 177Lu-PSMA-617 by 22RV1 cells reached the highest in 1 h ((7.58±0.84)%), which was slightly lower than the imported 177Lu-PSMA-617 ((7.86±0.96)%), but there was no significant difference between them ( t=-0.439, P>0.05). The distribution and SPECT/CT imaging of normal mice showed that domestic and imported 177Lu-PSMA-617 in blood were cleared quite fast, and both of them were excreted mainly through the kidneys. No obvious adverse reactions were found in the toxicity test of domestic and imported 177Lu-PSMA-617. There was no obvious abnormality in blood routine and liver and kidney metabolism. Conclusion:The domestic 177Lu-PSMA-617 has many advantages, such as qualified quality control, good biological properties and safety, which support its potential application value in diagnosis of prostatic neoplasms.
5.Analysis of oral microflora diversity and distribution in patients of long-term survival after liver transplantation
Chengrun ZHANG ; Siyuan WEI ; Shaocheng LYU ; Zuyu WANG ; Chaoran YU ; Dongxue ZHANG ; Haiyan WANG
Chinese Journal of Hepatobiliary Surgery 2024;30(11):824-829
Objective:To explore the composition of oral microbiome in patients of long-term survival after liver transplantation, and compare the diversity and distribution of oral microbiome in liver transplant patients with or without liver cancer.Methods:This is a cross-sectional study. Clinical data of 20 patients of long-term survival after liver transplantation from Beijing Chaoyang Hospital Affiliated to Capital Medical University from July 2023 to October 2023 were continuously collected, including 13 males and 7 females, aged 55 (48, 60) years. There were eight patients with hepatocellular carcinoma (HCC) undergoing liver transplantation and 12 non-HCC liver transplant patients. Oral microbiome was analyzed by 16S rDNA gene sequencing, and the diversity analysis and LEfSe analysis were performed.Results:The top ten groups of bacteria in the HCC and non-HCC liver transplant patients were both Bacteroidota, Firmicutes, Proteobacteria, Actinobacteria, Fusobacteriota, Patescibacteria, Campylobacterota, Cyanobacteria, spirochaetota, and Aenigmarchaeota. The top ten genus levels of bacteria in the HCC and non-HCC liver transplant patients were both Haemophilus, Porphyromonas, Gemella, Fusobacterium, Actinomyces, Prevotella, Rothia, Streptococcus, Neisseria. By LEfSe analysis, we found the enrichment of Flavobacteriales, Flavobacteriaceae, Capnocytophaga, Mogibacterium_timidum, Capnocytophaga_leadbetteri, Campylobacter_showae in the HCC group, while the enrichment of Veillonella_atypica, Prevotella_histicola in the non-HCC group.Conclusion:The main microbiome was similar between HCC and non-HCC liver transplant patients, but there were also some differences in microbiome communities.
6.Research progress of salivary glands injury secondary to 225Ac/ 177Lu-PSMA-617 in the treatment of prostate cancer and its protection
Wenhui FU ; Tingting XU ; Huipan LIU ; Xinyi ZHANG ; Chengrun ZENG ; Yue CHEN
Chinese Journal of Nuclear Medicine and Molecular Imaging 2022;42(10):628-632
Prostate specific membrane antigen (PSMA) radioligand therapy (RLT) is effective in metastatic castration-resistant prostate cancer (mCRPC). However, PSMA RLT can cause radiation damage to salivary glands, especially 225Ac/ 177Lu-PSMA-617. Radiation-related salivary glands damage can cause xerostomia, reduce the quality of life, and even limit the dose of radiopharmaceuticals and reduce the efficacy of tumor treatment. At present, there are few literatures on PSMA RLT related salivary glands damage in China. In this article, radiation-related salivary glands damage and the related protective measures during 225Ac/ 177Lu-PSMA-617 RLT are reviewed based on domestic and foreign studies.
7.Synthesis and biological evaluation of a series of 2-(((5-akly/aryl-1-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3)-ones as potential HIV-1 inhibitors.
Yumeng WU ; Chengrun TANG ; Ruomei RUI ; Liumeng YANG ; Wei DING ; Jiangyuan WANG ; Yiming LI ; Christopher C LAI ; Yueping WANG ; Ronghua LUO ; Weilie XIAO ; Hongbing ZHANG ; Yongtang ZHENG ; Yanping HE
Acta Pharmaceutica Sinica B 2020;10(3):512-528
A series of 2-(((5-akly/aryl-1-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3)-ones were synthesized and their anti-HIV-1 activities were evaluated. Most of these compounds were highly active against wild-type (WT) HIV-1 strain (IIIB) with EC values in the range of 0.0038-0.4759 μmol/L. Among those compounds, had an EC value of 3.8 nmol/L and SI (selectivity index) of up to 25,468 indicating excellent activity against WT HIV-1. anti-HIV-1 activity and resistance profile studies suggested that compounds and displayed potential anti-HIV-1 activity against laboratory adapted strains and primary isolated strains including different subtypes and tropism strains (ECs range from 4.3 to 63.6 nmol/L and 18.9-219.3 nmol/L, respectively). On the other hand, it was observed that those two compounds were less effective with EC values of 2.77 and 4.87 μmol/L for HIV-1A (K103N + Y181C). The activity against reverse transcriptase (RT) was also evaluated for those compounds. Both and obtained sub-micromolar IC values showing their potential in RT inhibition. The pharmacokinetics examination in rats indicated that compound has acceptable pharmacokinetic properties and bioavailability. Preliminary structure-activity relationships and molecular modeling studies were also discussed.