1.Study on the in vivo intestinal absorption and tissue distribution of silybin nanocrystals prepared by two methods
Mengyan WANG ; Ying SUN ; Sirui HUANG ; Yabo REN ; Jinhua CHANG ; Xigang LIU
China Pharmacy 2025;36(11):1335-1339
OBJECTIVE To investigate the absorption characteristics and tissue distribution of silybin (Sy) nanocrystals prepared by two methods in different intestinal segments of rats. METHODS Sy nanocrystals (i.e. Sy-NS-G and Sy-NS-F) with comparable particle sizes were prepared using high-pressure homogenization and anti-solvent precipitation methods, respectively. Rats were randomly divided into three groups: Sy raw drug group, Sy-NS-G group, and Sy-NS-F group. Each group was further divided into three subgroups with low, medium, and high (60, 120, 180 μg/mL) mass concentrations (calculated based on Sy), with 3 rats in each subgroup. The absorption rate constant (Ka) and apparent absorption coefficient (Papp) of Sy raw drug, Sy-NS-G and Sy-NS-F in different intestinal segments were investigated by using the in vivo one-way intestinal perfusion experiment. Additionally, the rats were divided into three groups: Sy raw drug group, Sy-NS-G group, and Sy-NS-F group, with 20 rats in each group. Rats in each group were administered a single intragastric dose of 50 mg/kg (calculated based on Sy). They were sacrificed at 0.3, 1, 4, 10, and 24 hours post-administration respectively, to investigate the tissue distribution of Sy raw drug, Sy- NS-G, and Sy-NS-F in the heart, liver, spleen, lungs, kidneys, brain and intestines. RESULTS In duodenum and jejunum, the Ka and Papp of the nanocrystals prepared by the two methods remained unchanged with the increase of Sy concentration, and there was no significant difference (P>0.05); the absorption of Sy-NS-F in the duodenum was greater than that of Sy-NS-G; the absorption sites of Sy-NS-G and Sy raw drug were mainly in the ileum, while those of Sy-NS-F were mainly in the duodenum and ileum. The concentrations of Sy-NS-G and Sy-NS-F in different tissues of rats were different; Sy-NS-G peaked in most tissues at 1 h, and the distribution concentration was as follows: intestine>spleen>heart>lungs>liver≈brain>kidneys. Sy-NS-F reached its peak at 1 h, and the distribution concentration was in the order of intestine>spleen>kidney>lung>heart≈liver>brain. CONCLUSIONS The absorption mode of Sy nanocrystals in the duodenum and ileum is mainly passive diffusion. In the duodenum, the absorption of Sy-NS-F is greater than that of Sy-NS-G; there are significant differences in the tissue distribution of Sy-NS-G and Sy-NS-F in rats.
2.Preparation,characterization and in vitro anti-inflammatory activity of tetrandrine-loaded chitosan-stearic acid nano micelles modified with folic acid
Fei XUE ; Lan YANG ; Jinhua CHANG ; Pei LIU ; Ruxing WANG
China Pharmacy 2024;35(8):925-930
OBJECTIVE To prepare tetrandrine (TET)-loaded chitosan(CS)-stearic acid (SA) nano micelles modified with folic acid (FA)( FA-CS-SA/TET nano micelles), characterize them and study the anti-inflammatory effect in vitro. METHODS FA- CS-SA/TET nano micelles were prepared by ultrasonic method; the preparation technology was optimized by orthogonal test and validation test was also performed with the mass ratio of FA-CS-SA to TET, ultrasound power and ultrasound times as the factors, using the comprehensive score of entrapment efficiency (EE), drug loading (DL) and particle size as evaluation index. FA-CS-SA/ TET nano micelles prepared by the optimal technology were characterized, and their release performance in vitro was investigated. RAW264.7 cells were used as subjects to investigate their anti-inflammatory activity in vitro. RESULTS The optimal preparation technology included that the mass ratio of FA-CS-SA to TET was 2∶1, ultrasonic power was 200 W, and the ultrasonic frequency was 200 times. The parameters of FA-CS-SA/TET nano micelles prepared by optimized technology included that EE was (98.86± 0.30)%, DL was (28.57±0.34)%, the average particle size was (227.0±9.4) nm, polydispersity index was 0.42±0.04, and the Zeta potential was(12.6±2.3)mV, respectively. The nano micelles were uniform in appearance and round in shape. The nano micelles were released quickly in 0.5% sodium dodecyl sulfate solution, with a cumulative release rate of (79.49±3.43)% within 72 hours, and its anti-inflammatory effect was stronger than that of TET raw materials. CONCLUSIONS FA-CS-SA/TET nano micelles are prepared successfully in the study, with good drug loading performance, uniform particle size, and good in vitro anti-inflammatory activity.
3.Correlation between nociceptin/orphanin FQ(N/OFQ)and perioperative myocardial injury in elderly patients with coronary heart disease
Danyan ZHU ; Chang XIONG ; Wenyong PENG ; Duojia XU ; Zhijian LAN
China Modern Doctor 2024;62(11):7-10,14
Objective To evaluate the relationship between perioperative myocardial injury(PMI)and serum N/OFQ levels in elderly patients with coronary heart disease.Methods Totally 120 elderly patients who underwent hip fracture surgery under general anesthesia from January 2022 to May 2023 were included,including 60 patients with coronary heart disease(CHD group)and 60 patients without coronary heart disease(control group).The venous blood of patients was collected 10 minutes before anesthesia induction(T0),12 hours after surgery(T1)and 24 hours after surgery(T2)to detect the content of N/OFQ and high-sensitivity myocardial troponin I(hs-cTnI)in serum.Record perioperative adverse cardiovascular events(PACE)and the use of vasoactive drugs during surgery.Results Compared with the control group,the N/OFQ and hs cTnI levels at T0 and T1 in the CHD group were significantly increased(P<0.05).There was a positive correlation between N/OFQ and hs-cTnI levels at T1 and T2 in CHD and control group(P<0.05).The use of PACE and intraoperative vasoactive drugs in the CHD group was higher than that in the control group(P<0.05).Conclusion There is a correlation between the increased N/OFQ content and PMI in elderly patients with coronary heart disease after surgery,which may become an early predictive indicator of PMI.
4.Study on in vitro dissolution and in vivo pharmacokinetics of Luteolin solid dispersion
Ziting HUANG ; Mengyan WANG ; Jinhua CHANG ; Pei LIU ; Ruxing WANG ; Xigang LIU
China Pharmacy 2024;35(10):1215-1219
OBJECTIVE To explore in vitro dissolution and in vivo pharmacokinetics of Luteolin solid dispersion in Beagle dogs. METHODS The dissolution of Luteolin solid dispersion was investigated according to the second method (paddle method) of the “dissolution determination method” in the 2020 edition of Chinese Pharmacopoeia (Part Ⅳ). UPLC-MS/MS method was established to determine the concentration of luteolin in the plasma of Beagle dogs. Twelve Beagle dogs were randomly divided into luteolin group and Luteolin solid dispersion group, with 6 dogs in each group. They were given relevant medicine orally at the dose of 10 mg/kg luteolin. Blood was collected before medication (0 h), at 5, 10, 15, 30, 45 min and 1, 2, 4, 6, 8, 10, 12, 24, 48 h after administration. After protein precipitation with acetonitrile, the blood concentration of luteolin in Beagle dogs was determined by UPLC-MS/MS and the major pharmacokinetic parameters were calculated with non-compartmental models by using DAS 3.2.8 pharmacokinetic software. RESULTS The dissolutions of Luteolin solid dispersion in purified water and 0.1% sodium dodecyl sulfate solution was significantly higher than those of luteolin; the dissolution rate reached 95% in 0.1% sodium dodecyl sulfate solution for 120 minutes. The peak concentration (cmax) of luteolin in the Luteolin solid dispersion group of Beagle dogs was 5.62 times higher than the luteolin group, and the relative bioavailability was 348%. Compared with luteolin group, cmax and the area under the drug time curve of luteolin in the Luteolin solid dispersion group of Beagle dogs were significantly increased, while the apparent distribution volume was significantly reduced (P<0.05). CONCLUSIONS Luteolin solid dispersion can improve in vitro dissolution and bioavailability of luteolin in Beagle dogs.
5.Association rules between personality traits and health-promoting lifestyle in patients with glaucoma
Tingting XIE ; Hong SUN ; Jinhua XU ; Yongqing WU ; Wan WEI ; Cheng CHANG ; Hang LYU
Chinese Journal of Behavioral Medicine and Brain Science 2022;31(5):420-424
Objective:To explore the association rules of personality traits and health-promoting lifestyle in patients with primary angle closure glaucoma, so as to provide advice for the synthetical treatment.Methods:From July to November 2021, a total of 117 primary angle closure glaucoma patients(acute patients n=89, chronic patients n=28) in ophthalmology department of five hospitals in Nanjing were investigated with type A behavior pattern scale, health-promoting lifestyle scale Ⅱ and general information questionnaire.Based on Weka 3.8.5, algorithm of Apriori was used to mine its association relationship. Results:(1) The total scores of type A behavior pattern scale for patients with acute and chronic types of primary angle closure glaucoma were (32.48±6.43) and (27.54±6.49) respectively.The total scores of health-promoting lifestyle scale Ⅱ were (101.69±11.83) and (97.79±7.78) respectively.(2) There were positive associations among patients with acute primary angle closure glaucoma, type A/A-personality (including impatience and hostility) and health-promoting lifestyle (including stress management disorder, interpersonal relationship management disorder, well sense of health responsibility and adequate dietary nutrition intake)(all support>0.1, confidence >0.6, lift >1.0). And patients with chronic primary angle closure glaucoma were associated with B/B-personality (including patience and mild), health-promoting lifestyle (including stress management disorder, interpersonal relationship management disorder, well sense of health responsibility and adequate dietary nutrition intake)(all support>0.1, confidence >0.6, lift >1.0).Conclusion:Primary angle closure glaucoma is strongly related with personality traits and health-promoting lifestyle.Its synthetical treatment plan should take both physical and mental measures, and classified health management for patients with different disease types.
6.Mandibular angle osteotomy combined with chin augmentation with high-density polyethylene for one stage lower facial recontouring
Jinhua HUANG ; Jie BIAN ; Zhibing MENG ; Caiwang CHANG ; Qiang ZHANG ; Miaomiao SHAO ; Jun GUO
Chinese Journal of Medical Aesthetics and Cosmetology 2020;26(4):265-267
Objective:To investigate the feasibility of mandibular angle osteotomy combined with high-density polyethylene (MEDPOR) prosthesis implantation for one-time lower facial contouring of the protuberance and related surgical precautions.Methods:A total of 18 patients who were treated in the oral and maxillofacial surgery of Yangzhou First People's Hospital from June 2010 to August 2016 were selected to complete the mandibular angle osteotomy combined with MEDPOR prosthesis implantation in the lower part of the prosthetic plane. The patients were followed up regularly and the effect of surgery was observed.Results:All 18 patients were operated successfully with an average time of 2 hours. The effect of operation was satisfactory. Except for one patient whose hematoma caused local bruise to subside completely in 2 weeks, all the others were discharged smoothly in one week after operation. After 2 months to 3 years of follow-up, the effect was satisfactory.Conclusions:Mandibular angle osteotomy combined with MEDPOR prosthesis is safe and effective.
7.Comparison of ultrasound radiomics with conventional imaging models :diagnosis of central cervical lymph node metastasis in papillary thyroid carcinoma
Yunxia HUANG ; Jin ZHOU ; Tongtong LIU ; Yi GUO ; Yuyang TONG ; Jinhua YU ; Yuanyuan WANG ; Min CHEN ; Shichong ZHOU ; Cai CHANG
Chinese Journal of Ultrasonography 2019;28(10):882-887
Objective To compare the difference of diagnostic ability between ultrasound radiomics ( USR) and different conventional imaging models of central neck ( Ⅵ ) lymph node metastasis in papillary thyroid carcinoma ( PTC) . Methods A training set of 609 cases was set up . USR features were extracted and screened by USR method . A weighted formula was established to calculate the USR score of each patient by ultrasound image . T he USR score of the best diagnostic ability was obtained by statistical method and set as the diagnostic criterion . A test set of 326 cases was established to compare the diagnostic ability of USR score with ultrasound ( US ) ,computed tomography ( CT ) and US combined CT . Results T he accuracy ,sensitivity ,specificity ,area under ROC curve and Youden index of USR score in test set were 0 .804 ,0 .867 ,0 .770 ,0 .766 ,0 .533 ,respectively ,which were significantly higher than the corresponding values of US ,CT and US combined CT ( all P = 0 .000 ) . Conclusions USR score obtained with USR method can effectively predict lymph node metastasis in Ⅵ region of PTC . T he diagnostic efficiency and clinical value of USR score were significantly higher than those of conventional medical imaging models .
8. Comparison of ultrasound radiomics with conventional imaging models: diagnosis of central cervical lymph node metastasis in papillary thyroid carcinoma
Yunxia HUANG ; Jin ZHOU ; Tongtong LIU ; Yi GUO ; Yuyang TONG ; Jinhua YU ; Yuanyuan WANG ; Min CHEN ; Shichong ZHOU ; Cai CHANG
Chinese Journal of Ultrasonography 2019;28(10):882-887
Objective:
To compare the difference of diagnostic ability between ultrasound radiomics (USR) and different conventional imaging models of central neck (Ⅵ) lymph node metastasis in papillary thyroid carcinoma (PTC).
Methods:
A training set of 609 cases was set up. USR features were extracted and screened by USR method. A weighted formula was established to calculate the USR score of each patient by ultrasound image. The USR score of the best diagnostic ability was obtained by statistical method and set as the diagnostic criterion. A test set of 326 cases was established to compare the diagnostic ability of USR score with ultrasound (US), computed tomography (CT) and US combined CT.
Results:
The accuracy, sensitivity, specificity, area under ROC curve and Youden index of USR score in test set were 0.804, 0.867, 0.770, 0.766, 0.533, respectively, which were significantly higher than the corresponding values of US, CT and US combined CT(all
9.The association between molecular biomarkers and ultrasonographic radiomics features for triple negative invasive breast carcinoma
Jiawei LI ; Zhou FANG ; Jin ZHOU ; Yuyang TONG ; Zhaoting SHI ; Cai CHANG ; Yi GUO ; Jinhua YU ; Yuanyuan WANG
Chinese Journal of Ultrasonography 2019;28(2):137-143
Objective To evaluate the association between quantitative ultrasonographic features and clinical ,pathological and immunohistochemical features of triple negative invasive breast carcinoma( TNBC) . Methods With the ethical approval , 96 patients who were pathologically confirmed as TNBC were retrospectively reviewed . All patients were sub-grouped according to age ,tumor size ,pathological grade , Ki67 expression level and human epidermal growth factor receptor 2 ( HER-2) score .Ultrasound images were segmented for the breast carcinoma mass using a phase-based active contour model . The high-throughput radiomics features were extracted based on the two-dimensional sonographic features . There were 460 features extracted from each ultrasound image . A series of computer aided algorithms including K-svd algorithm ,sparse representation ,support vector machine ( SVM ) and radial basis function were used to determine the high-throughput sonographic features that were highly correlated to clinical ,pathological and immunohistochemical features of TNBC . The performance efficacy was expressed by accuracy and area under curve ( AUC) of the ROC curve . Results The high-throughput ultrasonographic features of invasive TNBC could predict its pathological grade ,Ki67 level and HER-2 score with the accuracy 92 .2% -96 .9%and AUC 98 .7% -99 .9% . There were 82 radiomics features selected for predicting the pathological grade of TNBC , the feature with the maximum weight was the elliptic-normalized eccentricity based on morphological features . There were 100 features selected for predicting the Ki67 expression level ,the feature with the maximum weight was the standard deviation of the annular region based on the boundary texture features . There were 85 features selected for the prediction of HER-2 score ,the most powerful parameter was the intensity based on NGTDM texture features . Conclusions Quantitative high-throughput ultrasonographic features are correlated with the pathological and immunohistochemical characteristics of invasive TNBC . High-throughput ultrasonographic features are valuable in predicting biological behavior of TNBC .
10.Simultaneous Determination of 7 Components in Zhizi Jinhua Dispersible Tablets by HPLC
Ya XIAO ; Jing LI ; Jinhua CHANG ; Wei CHEN ; Cuizhe LIU ; Xigang LIU
China Pharmacy 2017;28(18):2549-2553
OBJECTIVE:To develop a method for simultaneous determination of geniposide,baicalin,aloe-emodin,rhein, emodin,chrysophanol and physcion in Zhizi jinhua dispersible tablets. METHODS:HPLC method was adopted. The determination was performed on Dimonsil C18 column with mobile phase consisted of methanol-0.05%phosphoric acid(gradient elution)at the flow rate of 0.8 mL/min. The detection wavelength was set at 254 nm,and the column temperature was 25℃. The sample size was 20 μL. RESULTS:The linear ranges of geniposide,baicalin,aloe-emodin,rhein,emodin,chrysophanol and physcion were 0.0323-0.323 μg (r=0.9998),0.1374-1.374μg(r=0.9999),0.00372-0.0372μg(r=0.9997),0.0069-0.069μg(r=0.9995),0.00332-0.0332μg (r=0.9997),0.00864-0.0864 μg(r=0.9997) and 0.00122-0.0122 μg(r=0.9995),respectively. The limits of quantitation were 0.0321,0.1374,0.00372,0.0067,0.00330,0.00864,0.00122 μg,respectively. The limits of detection were 0.0095, 0.0041,0.0012,0.0020,0.0010,0.0026,0.0003 μg,respectively. RSDs of precision,stability and reproducibility tests were all lower than 3%. The average recoveries were 96.54%-99.52%(RSD=1.17%,n=6),97.23%-101.23%(RSD=1.36%,n=6), 97.22%-101.25%(RSD=1.83%,n=6),97.32%-100.23%(RSD=1.09%,n=6),97.99%-102.71%(RSD=1.73%,n=6), 96.99%-100.23%(RSD=1.21%,n=6),96.99%-103.01%(RSD=2.31%,n=6),respectively. CONCLUSIONS:The methods is simple and reproducible. It can be used for the content determination of 7 components in Zhizi jinhua dispersible tablets.

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