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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 drugs.However,only few information about the biological fate of intravenous nanosuspensions is currently known,especially amorphous nanosuspensions are not reported yet.In 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 methods.The ACQ probe is physically embedded into HPE nanoparticles via anti-solvent method to form HPE hybrid nanosuspensions(HPE-HNSs)for bioimaging.HPE-HNSs emit strong and stable fluorescence,but fluorescence quenches immediately upon the dissolution of HPE-HNSs,confirming the selfdiscrimination of HPE-HNSs.Following 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 lung.Due 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 HPE-HNSs.These results demonstrate that integral HPE-HNSs determine the in vivo performance of HPEHNSs.This 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

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 fibrosis.However,Hominis Placenta(HP),as an important adjuvant of FBRT,has been restricted for medicinal using due to the limited availability,ethical controversy and safety issues.The 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 mechanisms.Different dosages of SP in N-FBRT were also evaluated.Methods:Rats were subcutaneously injected with CCl_(4)to induce liver fibrosis and then treated with NFBRT and FBRT.The 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 staining.The oxidative stress and inflammatory cytokines were also detected.Immunohistochemical staining of a-SMA,real time PCR and Western blotting were performed to evaluate hepatic stellate cells(HSCs)activation and TGF-β1/Smad signaling pathway.Results: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 changes.Moreover,the anti-liver fibrosis effect was better when the dosage of SP used in N-FBRT was 1/2 of HP in FBRT.Administration of N-FBRT markedly alleviated oxidative stress and inflammatory cytokines,and inhibited a-SMA expression.Furthermore,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 treatment.Conclusion: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 activation and ECM production by blocking TGF-β1/S

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

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 liver.Results 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 QT-HNCs.The particle size affects the absorption and biodistribution of integral QT-HNCs and total QT.As 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 administration.Due 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 administration.The 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%,respectively.Owing 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 obtained.These results revealed signifcant difference in absorption and biodistrbution between integral nanocrystals and overall drugs following oral and intravenous administration of QT-HNCs,and provided a

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

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黄芩汤的抗须癣毛癣菌活性及作用机制研究

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

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 model.METHODS: 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 obtained.RESULTS: 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 daily.CONCLUSION: 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：动力学模型时间间隔日常管理药效学大鼠黄疸平板电脑高效液相色谱法

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

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Rational Daily Administration Times of Canhuang Tablet Based...

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 model.Methods 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,respectively.Blood was collected from the orbital sinus at different intervals,then we investigated the levels of liver enzymes and bilirubins using these processed blood sample.Bile was collected and determined after first administration,and HPLC were used to determine the concentration of berberine in the bile at the same time.Finally,we obtained the time-effect curve and time-dose curve.Results 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,respectively.The results also showed that there was good consistency between pharmacokinetics of berberine and the pharmacodynamics of the effect on liver enzymes and bilirubins in vivo.AUC 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 day.Conclusions 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

Nanosuspensions of Poorly Water Soluble Drugs Prepared by Precipitation-Combined Homogenization Technology based on Acid-Base Neutralization Reactions

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Nanosuspensions of Poorly Water Soluble Drugs Prepared by Pr...

2015年中国药学大会暨第十五届中国药师周

作者： Gang shen Ling Cheng Lihong Zhang baode shen Juanjuan Li Juan Zhen Rong Xu Hailong Yuan Pharmacy College Chengdu University of Traditional Chinese Medicine Department of Pharmacy Air Force General Hospital of PLA

Herpetospermum caudigerum lignans（HTL）, one of the potential drugs with the treatment of anti-hepatitis B virus and hepatoprotective effects, have been limited in clinical applications because of poor saturation solubility, resulting in low bioavailability. Both herpetrione（HPE） and herpetin（HPN） are considered as the most abundant ingredient in HTL and exhibit weak acidity. The purpose of this study was to produce dried preparations of HTL（composed of HPE and HPN） nosuspensions with high redispersibility using lyophilization. The HTL-NS was prepared by utilizing precipitation-combined homogenization technology based on acid-base neutralization reactions, and variously critical formulation and process parameters affecting the characteristics of HTL-NS were optimized. The resultant products were characterized by particle size analysis, SEM, XRD, physical stability, solubility, dissolution and bioavailability. The dried preparations with a mean redispersed particle size of 286 nm was produced by using 4%（w/v） mannitol as cryoprotectants and possessed good physical stability at 4 oC or 25 oC for two months. Meanwhile, in vitro evaluation showed dried preparations could significantly increase saturation solubility and dissolution rate along with improving in vivo oral bioavailability, when compared with raw drug. This study provides a feasible drug delivery system for poorly water-soluble ingredients with pH-dependent solubility.

关键词： Herpetospermum caudigerum lignans nanosuspensions acid–base neutralization saturation solubility dissolution oral bioavailability

Development and characterization of mucoadhesive buccal films containing phospholipid-bile salts-mixed micelles for Cucurbitacin B delivery

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Development and characterization of mucoadhesive buccal film...

2013年中国药学大会暨第十三届中国药师周

作者： Qingyuan Lv Chengying shen Xianyi Li baode shen Chao Yu Pinghua Xu He Xu Jin Han Hailong Yuan Department of Pharmacy 302 Military Hospital Institute for Drug and Instrument Control Health Department GLD of PLA

Cucurbitacin B （Cu B）, a potent anti-cancer agents, suffers with the problems of gastrointestinal side effects and non-specific toxicity via oral administration and drawbacks in patients compliance and acceptance through injections. An integration of nanoscopic carriers with mucoadhesive buccal films drug delivery system would resolve these issues effectively with greater therapeutic benefits and clinical significance. Thus, the drug loaded mucoadhesive buccal film was developed and characterized in this study and the carboxymethyl chitosan （CCS） was choosed as a bioadhesive polymer, glycerol was choosed as a plasticizer and phospholipid-bile salts-mixed micelles （PL-BS-MMs） was selected as the nanoscopic carriers. The CCS-films containing Cu B loaded PL/SDC-MMs was evaluted for the mechanical properties, mucoadhesion properties, in vitro water-uptake, in vitro release and morphological properties, respectively. The optimal CCS-films containing Cu B loaded PL/SDC-MMs was easily reconstituted in a transparent and clear solution giving back a colloidal system with spherical micelles in the submicron range and presenting the good characteristics after reconstituting into micelles solution compared with corresponding results of initial Cu B-PL/SDC-MMs solution. The in vivo study revealed a greater and more extended release of Cu B from nanoscopic CCS-films compared to that from a conventional CCS films （C-CCS-films） and oral marketed tablet （Hulusupian）. The AUC 0-36h for CCS-films containing Cu B loaded PL/SDC-MMs was found to be 46.43±5.11 μg/mL/h in comparison to 4.44±1.21 μg/mL/h and 17.23±3.46 μg/mL/h for C-CCS-films and oral tablet, respectively. The absorption of Cu B from CCS-films containing Cu B loaded PL/SDC-MMs resulted in 2.69-fold increased in bioavailability as compared to conventional tablet formulation and 10.46 times with reference to the C-CCS-films formulation. Thus, this kind of mucoadhesive buccal film might be an alternative safe route for delivery of Cu B avoiding gastrointestinal side effects

关键词： Cucurbitacin B phospholipid-bile salts-mixed micelles film carboxymethyl chitosan bioavailability

Phospholipid-bile salts-mixed micelles incorporated in oral fast dissolving films for improving the oral bioavailability of poorly water soluble drugs

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Phospholipid-bile salts-mixed micelles incorporated in oral ...

“好医生杯”中药制剂创新与发展论坛

作者： Qingyuan Lv Minggui Lin Chao Yu baode shen He Xu Chengying shen Ling Dai Hailong Yuan Jin Han Department of Pharmacy 302 Military Hospital Institute of Tuberculosis 309 Military Hospital

The phospholipid-bile salts-mixed micelles(PL-BS-MMs)are potent carriers used for oral absorption of drugs that are poorly soluble in water;however,there are many limitations associated with liquid formulations.In the current study,the feasibility of preparing a solid PL-BS-MMs by incorporating liquid PL/SDC-MMs with solid fast dissolving oral films(FDOFs)carriers was examined.FDOFs incorporated with Cucurbitacin B(Cu B)loaded PL-BS-MMs have been developed and characterised.FDOFs were produced by solvent casting method.The formulation presenting the best characteristics before solidifying and after reconstitution.FDOFs containing Cu B loaded PL/SDC-MMs was easily reconstituted in a transparent and clear solution giving back a colloidal system with spherical micelles in the submicron range.The pharmacokinetics study showed that the FDOFs containing PL/SDC-MMs not only kept the absorption properties as same as liquid PL/SDC-MMs,but also significantly increased the oral bioavailability of Cu B compared to the Cu B solution(p<0.05).This study showed that the solid PL/SDC-MMs based on FDOFs could represent a novel platform for the delivery of poorly water soluble drugs via oral administration.Furthermore,the integration with the FDOFs could also provide a simple and cost-effective manner for the solidification of PL/SDC-MMs.

关键词： Cucurbitacin B phospholipid-bile salts-mixed micelles fast dissolving oral films oral bioavailability poorly water soluble drugs

芍药甘草汤中自组装纳米粒形成对甘草主要成分体外释放和肠吸收的影响

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中国药房 2022年第3期33卷 338-343页

作者：沈成英李小芳朱君君申宝德袁海龙胡建新江西省人民医院药学部南昌330006 成都中医药大学药学院成都611137 空军特色医学中心药剂科北京100142 江西中医药大学现代中药制剂教育部重点实验室南昌330004

目的研究芍药甘草汤中自组装纳米粒(SGD-SAN)形成对甘草主要成分体外释放和肠吸收的影响。方法制备甘草单煎液(GSD)、芍药单煎液(SSD)、芍药-甘草单煎混合液(MSSGD)和SGD(即芍药、甘草合煎液),并对其中的SAN进行表征。采用高效液相色谱... 详细信息

目的研究芍药甘草汤中自组装纳米粒(SGD-SAN)形成对甘草主要成分体外释放和肠吸收的影响。方法制备甘草单煎液(GSD)、芍药单煎液(SSD)、芍药-甘草单煎混合液(MSSGD)和SGD(即芍药、甘草合煎液),并对其中的SAN进行表征。采用高效液相色谱法测定甘草中7种主要成分(芹糖甘草苷、甘草苷、芹糖异甘草苷、异甘草苷、甘草素、甘草酸、异甘草素)的含量。采用透析袋法,以pH1.2 HCl溶液和p H6.8磷酸盐缓冲液(PBS)为释放介质,考察SGD-SAN形成对甘草中7种主要成分体外释放的影响;采用在体单向肠灌流实验考察SGD-SAN形成对甘草中7种主要成分在大鼠肠段吸收的影响。结果 GSD、MSSGD和SGD中存在粒径为200~300 nm、多分散性指数为0.3~0.5的SAN;透射电镜观察结果显示,GSD-SAN、MSSGD-SAN呈棒状,SGD-SAN呈不规则球形。体外释放实验结果显示,在p H1.2 HCl溶液中,SGD-SAN形成能显著增加甘草素、异甘草素和甘草酸的体外释放,对其他成分的释放无明显影响;在p H6.8 PBS中,SGD-SAN形成对甘草中各成分的释放均没有明显影响。在体单向肠灌流实验结果显示,SGD-SAN形成能显著促进甘草中各成分在回肠的吸收。结论 SGD-SAN形成能显著改善甘草中难溶性成分的体外释放、促进甘草中主要成分的肠吸收,是芍药、甘草配伍增效的物理结构基础。

关键词：自组装纳米粒芍药甘草汤甘草难溶性成分体外释放肠吸收