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Mapping multiple phases in curcumin binary solid dispersions by fluorescence contrasting

Chinese Chemical Letters 2024年第9期35卷 266-272页

作者： Ying Xu chengying shen Hailong Yuan Wei Wu Key Laboratory of Smart Drug Delivery of MOE School of PharmacyFudan UniversityShanghai 201203China Center for Medical Research and Innovation Shanghai Pudong HospitalFudan University Pudong Medical CenterShanghai 201399China Department of Pharmacy Air Force Medical CenterPLABeijing 100142China Jiangxi Provincial People’s Hospital The First Affiliated Hospital of Nanchang Medical CollegeNanchang 330006China

The microphases and miscibility in binary curcumin(Cur)solid dispersions(SDs)with amorphous polyvinylpyrrolidone K30(PVP K30)and semi-crystalline poloxamer(P407)and poly(ethylene glycol)6000(PEG6000)as carriers were investigated by fluorescence contrasting utilizing confocal laser scanning microscopy.A super sensitive fluorophore P4 with typical aggregation-caused quenching properties was employed to stain the continuous polymer phases and contrasted with the autofluorescence of the model drug *** addition,differential scanning calorimetry(DSC)and powder X-ray diffraction(PXRD)were utilized to assist in explanation of the fluorescence *** all three SD systems,there is always a homogenous polymer phase stained by P4 and it is difficult to adulterate Cur crystals by ***-enriched rather than polymer-enriched domains could be *** the Cur-PVP K30 system,Cur exists in an amorphous form at a Cur loading level of 50%and below,while Cur crystallines phase out and continuously grow with the increase of Cur loading from 60%to 90%.The phase behaviors in the Cur-P407 and Cur-PEG 6000 systems are similar but with minor *** both systems,Cur phases out as clusters of drug-enriched domains at a loading level of 20%and below,which however cannot be correlated with crystallization,as evidenced by both DSC and *** is a transition from an amorphous to a crystalline state from 20%to 30%Cur loading,above which Cur crystallines can be *** is interesting that a co-mix phase of both Cur-and PEG 6000-enriched domains can be identified at Cur loading levels of 10%and *** together,it is concluded that contrasting Cur autofluorescence with the signals of P4 proves to be a functional strategy to reveal multiple phases in the binary SD systems investigated.

关键词： Solid dispersion Curcumin PEG PVP Poloxamer Fluorescence Environment-responsive Confocal laser scanning microscopy

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The contribution of absorption of integral nanocrystals to enhancement of oral bioavailability of quercetin

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Acta Pharmaceutica Sinica B 2021年第4期11卷 978-988页

作者： Baode shen chengying shen Weifeng Zhu Hailong Yuan Department of Pharmacy Air Force Medical CenterPLABeijing 100142China Key Lab of Modern Preparation of Traditional Chinese Medicine(TCM) Ministry of EducationJiangxi University of TCMNanchang 330004China

In this study,self-discriminating hybrid nanocrystals was utilized to explore the biological fate of quercetin hybrid nanocrystals(QT-HNCs)with diameter around 280 nm(QT-HNCs-280)and550 nm(QT-HNCs-550)following oral and intravenous administration and the contribution of integral nanocrystals to oral bioavailability enhancement of QT was estimated by comparing the absolute exposure of integral QT-HNCs and total QT in the *** showed that QT-HNCs could reside in vivo as intact nanocrystals for as long as 48 h following oral and intravenous administration.A higher accumulation of integral QT-HNCs in liver and lung was observed for both oral and intravenous administration of *** particle size affects the absorption and biodistribution of integral QT-HNCs and total *** compared to QT-HNCs-550,QT-HNCs-280 with smaller particle size is more easily absorbed,but dissolves faster in vivo,leading to higher distribution of QT(146.90 vs.117.91 h·mg/mL)but lower accumulation of integral nanocrystals(6.82 e10 vs.15.27 e10 h·[p/s]/[μW/cm2])in liver following oral *** to its slower dissolution and enhanced recognition by RES,QT-HNCs-550 with larger diameter shows higher liver distribution for both of QT(1015.80 h·mg/mL)and integral nanocrystals(259.63 e10 h·[p/s]/[μW/cm2])than those of QT-HNCs-280(673.82&77.66 e10 h·[p/s]/[μW/cm2])following intravenous *** absolute exposure of integral QT-HNCs in liver following oral administration of QT-HNCs are 8.78%for QT-HNCs-280 and 5.88%for QT-HNCs-550,while the absolute exposure of total QT for QT-HNCs-280 and QT-HNCs-550 are 21.80%and 11.61%,*** to imprecise quantifcation method,a surprisingly high contribution of integral QT-HNCs to oral bioavailability enhancement of QT(40.27%for QT-HNCs-280 and 50.65%for QT-HNCs-550)was *** results revealed signifcant difference in absorption and biodistrbution between integral nanocrystals and overall drugs following oral and intr

关键词： Nanocrystals Biological fate Quercetin Pharmacokinetics Biodistribution Oral bioavailability Contribution Drug delivery

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Insight into the in vivo fate of intravenous herpetrione amorphous nanosuspensions by aggregation-caused quenching probes

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Chinese Chemical Letters 2022年第11期33卷 4948-4951页

作者： Lingyu Hang chengying shen Baode shen Hailong Yuan Department of Pharmacy Air Force Medical CenterPLABeijing 100142China College of Pharmacy Jiangxi University of Chinese MedicineNanchang 330004China Department of Pharmacy Jiangxi Provincial People's HospitalNanchang 330006China

Intravenous nanosuspensions are attracted growing attention as a viable strategy for development of intravenous formulations of poorly water-soluble ***,only few information about the biological fate of intravenous nanosuspensions is currently known,especially amorphous nanosuspensions are not reported *** this study,the in vivo fate of herpetrione(HPE)amorphous nanosuspensions following intravenous administration was explored by using an aggregation-caused quenching(ACQ)probe and HPLC *** ACQ probe is physically embedded into HPE nanoparticles via anti-solvent method to form HPE hybrid nanosuspensions(HPE-HNSs)for ***-HNSs emit strong and stable fluorescence,but fluorescence quenches immediately upon the dissolution of HPE-HNSs,confirming the selfdiscrimination of *** intravenous administration of HPE-HNSs,integral HPE-HNSs and HPE show similar degradation and biodistribution,with rapid clearance from blood circulation and obvious accumulation in liver and *** to the slower dissolution and enhanced recognition by reticuloendothelial system,450 nm HPE-HNSs accumulate more in liver,lung and spleen than that of 200 nm *** results demonstrate that integral HPE-HNSs determine the in vivo performance of *** study provides insight into the in vivo fate of intravenous amorphous nanosuspensions.

关键词： Amorphous nanosuspensions Herpetrione In vivo fate Intravenous delivery Aggregation-caused quenching

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黄芩汤的抗须癣毛癣菌活性及作用机制研究

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中国药房 2024年第3期35卷 311-315页

作者：沈成英罗忠章佩邓冯沂申宝德胡建新江西省人民医院(南昌医学院第一附属医院)药学部南昌330006 南昌大学药学院南昌330006 江西省人民医院(南昌医学院第一附属医院)临床医学研究所南昌330006 江西中医药大学现代中药制剂教育部重点实验室南昌330004

研究黄芩汤(HQD)的抗须癣毛癣菌活性及作用机制。方法通过测定最小抑菌浓度(MIC)、最小杀菌浓度(MFC)、菌丝长度、孢子萌发率、生物量和观察菌丝超微结构评价HQD的抗须癣毛癣菌活性;通过山梨醇保护实验检测HQD对须癣毛癣菌细胞壁的影响... 详细信息

研究黄芩汤(HQD)的抗须癣毛癣菌活性及作用机制。方法通过测定最小抑菌浓度(MIC)、最小杀菌浓度(MFC)、菌丝长度、孢子萌发率、生物量和观察菌丝超微结构评价HQD的抗须癣毛癣菌活性;通过山梨醇保护实验检测HQD对须癣毛癣菌细胞壁的影响;通过测定麦角固醇含量和角鲨烯环氧酶(SE)、羊毛甾醇14α-去甲基化酶(CYP51)的活性考察HQD对须癣毛癣菌细胞膜的影响;通过测定线粒体中苹果酸脱氢酶(MDH)、琥珀酸脱氢酶(SDH)及ATP酶(包括钠钾ATP酶、钙镁ATP酶和总ATP酶)的活性考察HQD对须癣毛癣菌线粒体的影响。结果 HQD对须癣毛癣菌具有显著的抑菌活性,MIC、MFC值分别为3.13、25 mg/mL。经HQD干预后,须癣毛癣菌菌丝长度均显著缩短(P<0.05);孢子萌发率、生物量、细胞膜中麦角固醇含量和SE、CYP51活性以及线粒体中MDH、SDH、各种ATP酶的活性均显著降低(P<0.05);细胞结构受到了一定程度的破坏,但细胞壁的完整性没有受影响。结论 HQD具有显著的抗须癣毛癣菌活性,其作用机制与降低细胞膜中麦角固醇含量和SE、CYP51活性以及线粒体相关酶活性有关。

关键词：黄芩汤须癣毛癣菌抗真菌活性作用机制细胞膜线粒体

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Daily administration times of Canhuang tablet based on a pharmacodynamic/pharmacokinetic model in jaundiced rats

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Journal of Traditional Chinese Medicine 2015年第1期35卷 84-89页

作者： Bai Jinxia Han Jin Chen Hongge shen Baode Xu He Dai Ling shen chengying Yuan Hailong Department of Pharmacy 302 Hospital of PLA Pharmacy College Chengdu University of Traditional Chinese Medicine

OBJECTIVE: To study the daily administration times of Canhuang tablet(CHT) for treating jaundice in rats based on a pharmacodynamic/ pharmacokinetic ***: Rats were modeled by 4% 1-Naphthylisothiocyanate(75 mg/kg, p.o.). After 48 h, CHT was given(p.o.) at 0.75 g/kg once a day, 0.375 g/kg twice a day, and 0.25 g/kg three times a day. Blood was collected from the orbital sinus at different intervals. Levels of liver enzymes and bilirubin were detected using these blood samples. Bile was collected and determined after the first administration of CHT. High-performance liquid chromatography was used to determine the concentration of berberine in bile simultaneously. Time-effect and time-dose curves were then ***: Compared with rats taking CHT twiceand three times a day, the total amount of bile within 10 h of rats taking CHT once a day were 1.32-and 1.47-fold higher, respectively. There was good consistency between the pharmacokinetics of berberine and the pharmacodynamics of the effect on liver enzymes and bilirubin in vivo. The pharmacokinetic analyses showed that rats administered CHT once daily maintained a higher concentration of berberine in bile for a longer period than rats administered CHT two- and three-times ***: In jaundiced rats, taking CHT once a day is better than taking CHT twice or three times a day. These data may provide a reference for the clinical application of CHT.

关键词： Jaundice 1-Naphthylisothiocyanate Pharmacokinetics Berberine Pharmacology Can-huang tablet

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Effects of novel Fufang Biejia Ruangan Tablets with sheep placenta as substitute for Hominis Placenta on CCl4-induced liver fibrosis

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Chinese Herbal Medicines 2022年第1期14卷 104-110页

作者： Baode shen Li Deng Yuan Liu Ruisheng Li chengying shen Xiao Liu Yinchao Li Hailong Yuan Department of Pharmacy Air Force Medical CenterPLABeijing 100142China College of Pharmaceutical Sciences Zhengzhou UniversityZhengzhou 450001China Research Center for Clinical and Translational Medicine The Fifth Medical Center of ChinesePLA General HospitalBeijing 100039China School of Chemistry Biology and Material ScienceEast China University of TechnologyNanchang 330013China

Objective:Fufang Biejia Ruangan Tablet(FBRT) is widely used for the treatment of liver ***,Hominis Placenta(HP),as an important adjuvant of FBRT,has been restricted for medicinal using due to the limited availability,ethical controversy and safety *** present study aimed to investigate the therapeutic effects of novel FBRT(N-FBRT) with sheep placenta(SP) as substitute for HP on liver fibrosis and explore its possible *** dosages of SP in N-FBRT were also ***:Rats were subcutaneously injected with CCl_(4)to induce liver fibrosis and then treated with NFBRT and *** anti-hepatic fibrosis effect was determined based on biomarkers analysis of liver function and hepatic fibrosis,and the liver pathology was visualized by H&E staining and Masson *** oxidative stress and inflammatory cytokines were also *** staining of a-SMA,real time PCR and Western blotting were performed to evaluate hepatic stellate cells(HSCs)activation and TGF-β1/Smad signaling ***:N-FBRT and FBRT could ameliorate CCl_(4)-induced liver fibrosis and improve liver function,as evidenced by lowering serum biomarkers levels of liver function and hepatic fibrosis,and decreasing hepatic Hyp content and collagen deposition,and improving the hepatic morphology and architecture ***,the anti-liver fibrosis effect was better when the dosage of SP used in N-FBRT was 1/2 of HP in *** of N-FBRT markedly alleviated oxidative stress and inflammatory cytokines,and inhibited a-SMA ***,the mRNA expression of Col Ⅰ,Col Ⅲ,a-SMA and TGF-β1,and proteins expression of a-SMA,TGF-β1,Smad2/3 and p-Smad2/3 were significantly down-regulated by N-FBRT ***:SP can be used as substitute for HP to prepare N-FBRT for the treatment of liver fibrosis and the anti-liver fibrosis effect of N-FBRT is achieved by eliminating oxidative stress and inflammation,and inhibiting HSCs ac

关键词： Fufang Biejia Ruangan Tablet Hominis Placenta liver fibrosis sheep placenta substitute TGF-β1/Smad signaling pathway

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In vivo dissolution of poorly water-soluble drugs:Proof of concept based on fluorescence bioimaging

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Acta Pharmaceutica Sinica B 2021年第4期11卷 1056-1068页

作者： Yinqian Yang Yongjiu Lv chengying shen Tingting Shi Haisheng He Jianping Qi Xiaochun Dong Weili Zhao Yi Lu Wei Wu Key Laboratory of Smart Drug Delivery of MOE School of PharmacyFudan UniversityShanghai 201203China Center for Medical Research and Innovation Shanghai Pudong HospitalFudan University Pudong Medical CenterShanghai 201399China

In vitro-in vivo correlation(IVIVC)of solid dosage forms should be established basically between in vitro and in vivo dissolution of active pharmaceutical ***,in vivo dissolution profles have never been accurately *** current practice of IVIVC has to resort to in vivo absorption fractions(Fa).In this proof-of-concept study,in vivo dissolution of a model poorly watersoluble drug fenofbrate(FNB)was investigated by fuorescence *** crystals were frst labeled by near-infrared fuorophores with aggregation-caused quenching *** dyes illuminated FNB crystals but quenched immediately and absolutely once been released into aqueous media,enabling accurate monitoring of residual drug *** linearity established between fuorescence and crystal concentration justifed reliable quantifcation of FNB *** vitro dissolution was frst measured following pharmacopoeia monograph protocols with well-documented *** synchronicity between fuorescence and in vitro dissolution of FNB supported using fuorescence as a measure for determination of *** vitro dissolution correlated well with in vivo dissolution,acquired by either live or ex vivo *** newly established IVIVC was further validated by correlating both in vitro and in vivo dissolution with Faobtained from pharmacokinetic data.

关键词： In vivo dissolution Fenofibrate Fluorescence Aggregation-caused quenching Bioimaging IVIVC

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The Construction of the Major Clusters in Higher Vocational Colleges from the Perspective of Industrial Cluster

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International Journal of Technology Management 2015年第9期 14-16页

作者： Qingtang ZHANG chengying shen Jiangyin Polytechnic College Jiangyin 214405 Jiangsu China

The development of industrial cluster plays a significant influence on the major construction of higher vocational colleges. In this paper, in combination with the practice of Jiangyin Polytechnic College, the interaction relationship between the construction of the major clusters in higher vocational colleges and the development of the regional industry clusters is analyzed, and then the significance and idea of constructing the maior clusters are introduced from the perspective of industrial cluster.

关键词： Industrial Cluster Higher Vocational Colleges the Construction of Major Clusters

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化工专业顶岗实习的实践

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中国职业技术教育 2006年第36期22卷 33-34页

作者：沈澄英江阴职业技术学院江苏江阴214433

严格实施顶岗实习的过程管理、制定考核细则．可确保实习的质量与效果．

关键词：顶岗实习过程管理考核细则化工专业

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Rational Daily Administration Times of Canhuang Tablet Based on PD/PK Model in Rats with Jaundice

Rational Daily Administration Times of Canhuang Tablet Based...

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第十四届全国中药和天然药物学术研讨会

作者： Jinxia Bai Jin Han Hongge Chen Baode shen He Xu Ling Dai chengying shen Hailong Yuan 302 Hospital of PLA

Objective To study the rational daily administration times of Canhuang Tablet(CHT) for treating jaundice in rats based on pharmacodynamics/ pharmacokinetics *** Rats were mbdeled by orally administrating 4%1-Naphthylisothiocyanate(75mg/kg).After48 h,CHT was orally administrated with a dose of 0.75g/kg once a day,0.375 g/kg twice a day and 0.25 g/kg three times a day,*** was collected from the orbital sinus at different intervals,then we investigated the levels of liver enzymes and bilirubins using these processed blood *** was collected and determined after first administration,and HPLC were used to determine the concentration of berberine in the bile at the same ***,we obtained the time-effect curve and time-dose *** Compared with the groups of rats taking CHT twice and thrice a day,the total bile within 10 h of the rats taking CHT once a day were 1.32 and 1.47 times higher,*** results also showed that there was good consistency between pharmacokinetics of berberine and the pharmacodynamics of the effect on liver enzymes and bilirubins in *** of berberine and the cholaneresis and retro-jaundice kinectics when administrated once a day were significantly higher than that of administrated 2 and 3 times a *** It is reasonable to take CHT one time a day in the treatment of experimental jaundice,which may provide a reference for clinical application of CHT.

关键词： daily administration times Canhuang Tablet berberine Bile pharmacokinetics jaundice

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