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检索条件"任意字段=2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会"

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Preparation,Characteristics of Large porous Cyclosporine A/Quaternized Chitosan/Hydroxypropyl-β-Cyclodextrin Microspheres for Inhalation

Preparation,Characteristics of Large porous Cyclosporine A/Q...

引用

2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Cui Liu Qinxin Zhao Qianwen Zhang Huanyu Zang Zhongrui Zhang Qihua Sun Zijing Yu Zhanqin Feng Wei Fen Zhang Clinical Undergraduates of Class 18 Grade 2011 Basic College of Weifang Medical University College of Pharmacy and Biological Science Weifang Medical University

Pulmonary sustained delivery is becoming a novel drug delivery system which has attracted much attention in recent ***（Large Porous Particles,LPPs）with the diameter larger than 5 μm,the density less than 0.4 g/cm are considered to have more advantages for pulmonary drug delivery *** this study,inhalable LPPs were designed to reduce side effects,provide drug protection and to sustained release Quaternized Chitosan（HTCC） and Hydroxypropyl-β-cyclodextrin（Hp-β-CD）were applied to develop large porous microspheres for pulmonary delivery by spray drying method,while the cyclosporine A（CsA） was used as a model *** physiochemical characteristics such as morphology,drug loading,and encapsulation efficiency were *** results of Scanning Electron Microscope showed the microspheres were spherical with smooth or wrinkled surface surfaces,and with the diameters between 0.5～7 μm The drug entrapments of microspheres A-I were from5.77%to 7.28%,and encapsulation efficiencies were from 0.89%to 1.85%,*** microspheres possessed low tap densities（< 0.48 g/cm） and could effectively reduce the *** results suggested that Cyclosporine A/Quaternized Chitosan/Hydroxypropyl-P-cyclodextrin microspheres were a promising carrier for pulmonary delivery.

关键词： Quaternized Chitosan Hydro xypropyl-β-cyclodextrin Large Porous Particles Cyclosporine A Spray-drying Pulmonary delivery

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Combination of time-dependent and pH-dependent polymethacrylates as a single coating formulation for pulsatile release of Dexmethylphenidate pellets

Combination of time-dependent and pH-dependent polymethacryl...

引用

2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： LI Yun WANG Yu-li GAO Chun-sheng YANG Mei-yan SHAN Li The institute of pharmacology and toxicology Chinese academy of military medical sciences

Attention-deficit/hyperactivity disorder(ADHD) is an impairing neurobehavioral condition,clinically characterized by inattention,hyperactivity,and *** to have a worldwide pooled prevalence rate of 5.29%in children and 4.4%in adults,ADHD primarily occurs in childhood,although the symptoms persist through adolescence to adulthood in 46-66%of *** racemic mixture of d-threo- and l-threo-enantiomers of methybhenidate hydrochloride(d,l-MPH) has been the mainstay treatment for *** is the more pharmacologically active d-enantiomer of racemic *** objective of this study were:(i) to evaluate the combination of pH-dependent and time-dependent polymers as a single coating for multiparticulate extended release dosage forms;(ii) to investigate the effects of the polymer blend ratio and coating level on the resulting drug release patterns;and(hi) to explain the observed phenomena based on the physicochemical properties of the *** L100 were used as pH-dependent polymers and Eudragit RS was used as a time-dependent *** HCl-toaded pellets were coated in a fluidized bed coater with organic polymer solutions.A statistical full factorial design was used in order to optimize *** studied in design were percent of Eudragit RS in combination with Eudragit L and coating *** studies of pellets in the media with different pH(2.0,6.0 and 6.8) showed that drug release in intestine could be controlled by addition of Eudragit RS to the pH-dependent *** lag time prior to drug release was highly affected by coating level.A broad range of drug release patterns from coated pellets could be achieved by varying the GIT-insoluble:enteric polymer blend *** increasing relative amounts of Eudragit L,the release rates in all media significantly *** combination of two factors,*** percent of Eudragit RS and coating level,the optimum formulation was found t

关键词： Combination of time-dependent and pH-dependent polymethacrylates as a single coating formulation for pulsatile release of Dexmethylphenidate pellets

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Preparation of antigen entrapped calcium carbonate microparticles and polyelectrolyte microcapsules

Preparation of antigen entrapped calcium carbonate micropart...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Jilei Jia Lianyan Wang Qi Liu Xiaoming Chen Weifeng Zhang Guanghui Ma National Key Laboratory of Biochemical Engineering EngineeringInstitute of Process EngineeringChinese Academy of Sciences

Calcium carbonate(CaCO3) is one of the basic inorganic materials,which has been widely used as pharmaceutical excipient with its good *** cakite is the most stable crystal structure among all polymorphs of CaCO3,amorphous calcium carbonate is attracted much attention because of its wonderful properties—porous structure,biocompatibility,high drug loading capacity and high surface ***03 microparticles with different sizes and morphologies were synthesized by a simple precipitation method,mixing equal volumes of CaCl2 and Na2C03 *** spherical,dendritic,cauliflower-like partilces were prepared through regulating the parameters,such as ionic concentration,reaction temperature,reaction time,mixing *** on the intense agitation,the effect of solution concentration played a more significant role in the process than other *** the formation of the rod-like depended on trisodium citrate as *** using the different mixing strategies of mechanical stirring,homogenizing and ultrasonic processing,we have successfully fabricated spherical CaCO3 microparticles with several average diameters ranging from 0.7 μm to 6 μm The results of scanning electron microscopy(SEM) and X-ray diffraction(XRD) showed that they were consist of cakite and vaterite polymorphs with the porous *** zeta-potential was also measured and the positive charge on the external of the microparticles made them easier to toad the oppositely charged antigen—Hepatitis B surface antigen(HBsAg).The entrapment capacity of various CaC03 microspheres for HBsAg was examined by a Coomasie brilliant blue protein assay and the particles with an average size of 1.0 μm had the highest amounts of *** HBsAg entrapped CaCO3 microparticles were used in the subsequent *** one hand,they were directly investigated as vaccine adjuvants to improve the immunology *** the other hand,they were used as the templates to coat polyelectrolytes o

关键词： calcium carbonate polyelectrolyte microcapsules LBL technique vaccine adjuvant

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Multi-subcellular compartment delivery of doxorubicin by one pH-sensitive micelle

Multi-subcellular compartment delivery of doxorubicin by one...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Yan-feng Song Han Cui Bang-le Zhang Si-yuan Zhou Department of Pharmaceutics School of PharmacyFourth Military Medical University

Doxorubicin(DOX) is a widely-used drug for treating a broad range of tumors in ***,its clinical use is hindered by its side effects such as cardbtoxicity and acquired drug *** addition to nucleus,mitochondria are found to be another subcellular targeting of DOX action Dequalinium(DQA) is one of the delocalized lipophilic *** has been reported that DQA can accumulate in the cell mitochondria because of the inner membrane potential of ***(anisamide) is sigma receptor selective *** receptor is over-expressed in a bt of proliferating tumor cells such as melanoma,non-small cell lung carcinoma,breast cancer and prostate *** this paper,a pH-sensitive amphiphilic polymer AA-C6-PEG-hyd-DSPE and mitochondria-specific conjugate DQA-DOX was synthesized,and a new pH-sensitive micelle was prepared by emulsion-solvent evaporation method to deliver DOX to nucleus and mitochondria simultaneously.A series of drug loaded micelle-1,mieelle-2,micelle-3,micelle-4 and micelle-5 were prepared by using DOX and DQA-DOX as antitumor *** released from micelle-1 and micelle-5 showed a pH-dependent ***-DOX showed bwer cytotoxicity than free DOX on A549 cells,HUVEC cells and HEK293 cells,but it showed higher cytotoxicity than free DOX on DOX-resistant MDA-MB-231/ADR *** the five kinds of micelles,micelle-5(baded DOX and DQA-DOX)induced the most extensive apoptosis in A549 cells,HepG2 cells,and MDA-MB-231/ADR cells,and exhibited the highest cytotoxicity against A549 cells,HepG2 cells,Hela cells and MDA-MB-231/ADR *** microscopy confirmed that the AA-containing micelle was uptaken through AA receptor mediated ***-cellular distributbn experiment proved that micelle-5 respectively delivered DQA-DOX and DOX to the mitochondria and nucleus simultaneously,which induced more apoptosis on tumor cells and greatly enhanced the cytotoxicity of DOX on wild type tumor cells and DOX resistant tumor ***,mice

关键词： doxorubicin multiple drug resistance mitochondria dequalinium pH-sensitive micelle

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A novel oral preparation of hydroxysafflor yellow A base on a chitosan complex:a strategy to enhance the oral bioavailability

A novel oral preparation of hydroxysafflor yellow A base on ...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Fang-lin Yu Guan-nan Ma Shan Wang Zhi-ping Li Xiang-yang Xie Xing-guo Mei Department of Pharmaceutics Beijing Institute of Pharmacology and Toxicology School of Chemical Engineering & Pharmacy Wuhan Institute of Technology Faculty of Pharmacy Hubei University of Chinese Medicine

Hydroxysafflor yellow A(HSYA),the main active pharmaceutical ingredient of the saffiower plant(Carthamus tinctorius L.),is a hydrophihc drug with taw oral bioavailability(BA).The objective of the present study was to improve the oral BA of HSYA by formulation *** main reason for the taw oral BA of HSYA is its low liposolubility and high water-solubility,which can hinder its penetration across the epithelial *** pharmaceutical excipients have been shown to enhance the permeability of BCS III drugs,such as sodium caprate(SC),sodium deoxycholate,P-cyclodextrin(p-CD) and Potaxamer 188(PI88).Therefore,the above five excipients were selected to investigate their ability to enhance the oral BA of HSYA through animal ***,chitosan is the only basic polysaccharide in nature that is positive charged,the properties of its bioadhesion and absorption enhancement make it a suitable carrier in mucosal drug delivery *** special properties could be utilized to prepare a HSYA-CS *** optimized the preparation process,the binding rate reached 99.4%.Then,HSYA granules,which contain the HSYA-CS complex and a penetration enhancer,were *** these granules have been administered,a portion of the amino groups of each CS molecule bound with HSYA,and another portion of the amino groups,could adhere to the negatively charged intestinal mucosa by electrostatic ***,many drug release cores will be formed and distributed on the surface of intestinal ***,the action time and intensity between HSYA and the intestinal epithelia would be extended and *** the same time,the tight junctions of the intestinal cell monolayer would be opened or the permeability of intestinal cell would be increased due to the action of the absorption enhancer;thus,HSYA could permeate into the cell membrane,which could significantly enhance the absorption of *** results of the pharmacokinetics in Sprague-Dawley rats sho

关键词： hydroxysafflor yellow A(HSYA) oral bioavailability chitosan absorption enhancer

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Design of a disulfide cross-linked stearyl-peptide for efficient delivery of siRNA

Design of a disulfide cross-linked stearyl-peptide for effic...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Zongguang Tai Xiaoyu Wang Jing Tian Lijuan Zhang Ziyuan Dai Chong Yao Xin Wu Wei Zhang Yuan Gao Quangang Zhu Shen Gao Department of Pharmaceutics Changhai HospitalSecond Military Medical University Department of Pharmaceutics Shanghai First People's HospitalShanghai Jiaotong University School of Medicine Department of Pharmacy Yueyang Hospital of Integrated Traditional Chinese and Western MedicineShanghai University of Traditional Chinese Medicine

For RNA interference(RNAi),developing efficient siRNA dehvery vehicles has become a major *** this study,a series of biodegradable polypeptides containing arginine,histidine,cysteine,stearyl moiety,and disulfide bond with different molecular weight(SHRssl,SHRss2,SHRss3,SHRss4) were synthesized and tested as siRNA dehvery vectors in reporter *** synthesized disulfide cross-linked stearyl-peptides(SHRss) can effectively condense siRNA into polyplexes with a hydrodynamic size of 100-300 nm and zeta potential of 20-40 mV at N/P=*** cytometry and confocal laser scanning microscope studies revealed high cellular uptake and rapid dissociation behavior of SHRss2/siRNA ***-lasting high concentration of siRNA in cytoplasm was observed even after 24 h SHRss2/Cy3-siRNA *** with stearyl-peptide monomer,disulfide cross-linked stearyl-peptides showed much improved siRNA interference efficiency targeting luciferase on Luc-Hela ***2 exhibited higher interference efficiency and slower decay rate on Luc-Hela cells than Lipofectamine 2000 or stearyl-peptide monomer(SHR).Much weaker expression of red fluorescence protein was also observed on SHRss2/simCherry-treated mCherry-HEK293 cells than Lipofectamine2000 and *** polymerization of SHR through disulfide bonds did not increase cytotoxicity at 25-200 nM siRNA under *** study indicated that the disulfide cross-linked stearyl-peptides are promising and efficient non-viral vectors for siRNA delivery.

关键词： arginine disulfide bond histidine peptide siRN A delivery stearyl

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Characterization of thermo-sensitive amphiphilic comb-like copolymer and its application in controlled drug release as self-assembled nanoparticles

Characterization of thermo-sensitive amphiphilic comb-like c...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Xiao-Jiao Tang Yue Ma Ju-Ju Zhang Wei-Fang Ren Ling-Ling Huang Shou-Nan Liu Li-Yang Department of Pharmaceutics Shenyang Pharmaceutical University

An amphiphilic thermo-sensitive comb-like copolymer,poly(D,L-lactide)-graft-pullulan(PL),can disperse and self-assemble into thermo-responsive nanoparticles which is available in controlled drug delivery system.A microwave-assisted solution polymerization was applied to synthetize PL in a monomode microwave *** light scattering technique(DLS),and turbidity measurements using UV-VIS spectrophotometry were adopted to characterize the reversible thermo-sensitive properties of the amphiphilic *** thermo-sensitive copolymer was further applied into loading curcumin,serving as thermo-stimuli nanoparticles prepared by an improved-method,low temperature thin film hydration,and characterized with DLS,fluorescence and UV-VIS *** in vitro drug release behavior was monitored at 25,37 and 42℃ to verify the ability,controlling drug release through thermo-stimuli,of the self-assembled thermo-responsive ***-assisted synthesis shortened the copolymerization of PL to 5 min with higher yield and lactide conversion and obtained PL with thermo-sensitive *** results of DLS and turbidity measurements indicated that the low critical solution temperature(LCST) of PL is around 40 ℃,which is above the mean body temperature and below the denaturation temperature of epidermal *** temperature thin film hydration was successfully applied to preparing curcumin-nanoparticles with the solubility of curcumin improved to 2.8mgmL"*** average size of the self-assembled nanoparticles loaded with curcumin was 71.20±0.83 *** remarkable differences in fluorescence and UV-VIS spectroscopy between curumin-nanoparticles and curcumin solution demonstrated that there is interaction among curcumin molecules and *** vitro drug release behavior at different temperatures confirmed the thermo-responsive property of *** total amount of released curcumin after 12 h reached to 3.09,39.7 and 92.7%from curcumin-n

关键词： Poly(D,L-lactide)-graft-pullulan Microwave Thermo-sensitive Self-assembly Nanoparticles Curcumin

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Immune responses to vaccines involving a combined antigen-nanoparticle mixture and nanoparticle-encapsulated antigen formulation

Immune responses to vaccines involving a combined antigen-na...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Weifeng Zhang Lianyan Wang Xiaoming Chen Qi Liu Jilei Jia Tingyuan Yang Guanghui Ma National Key Laboratory of Biochemical Engineering Institute of Process EngineeringChinese Academy of Sciences

Background and Objective:Biodegradable polymer-based micro/nanoparticles have been extensively investigated as vaccine *** characteristics of particulate vaccines determine vaccine potency,and the exposure kinetics of antigen to immune system is an important *** of this study is to investigate how particle-antigen formulation modes affect the kinetics of antigen exposure to immune system,and to uncover the underlying immunopotentiation ***:Antigen(ovalbumin)-entrapped PLGA(poly(lactic-glycolie acid)) nanoparticle(NPs) was fabricated by emulsion-solvent evaporation method combined with membrane emulsification *** morphology and antigen structure integrity were evaluated by SEM,MALDI-TOF,circular dichroism,and fluorescence spectral *** response,cytokines secretion,splenocytes proliferation,and memory T cell responses were determined to evaluate vaccine *** vitro and in vivo experiments were performed to assess action mechanisms of these *** and Conclusion:PLGA NPs,spherical in shape,had narrow size distribution(mean size 341.6 nm) and negative surface charge(- 11.43 mV).Antigen content in NPs was about60 u.g/*** vivo studies revealed that NPs-entrapped antigen elicited stronger immune responses than soluble antigen Compared to NPs-entrapped antigen or antigen mixed with NPs,the combined formulation induced stronger antibody response,significantly enhanced cytokines secretion by splenocytes,and stronger memory T cell response(Fig.1A).The enhanced immune responses elicited by the combined vaccine formulation might be attributed to the antigen-depot effect at injection site(Fig.1B),effective provision of both adequate initial antigen exposure and long-term antigen persistence(Fig.1C),and efficient induction of DC activation and follicular helper T cell differentiation in draining lymph *** the effect of the antigen-nanoparticle formulations on the resultant immune respons

关键词： nanovaccine nanoparticle adjuvant immune response mechanism of action

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Paclitaxel loaded redox-responsive nanoparticles based on a disulfide-linked poly(ethylene glycol)-drug conjugate for drug delivery

Paclitaxel loaded redox-responsive nanoparticles based on a ...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Xingxing Chuan Qin Song Hua Zhang Wenbing Dai Bing He Xueqing Wang Qiang Zhang State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University

To address the obstacles of cancer chemotherapeutics,including toxicity,side effects,water insolubility,and lack of tumor selectivity,a novel stimuli-responsive drug-delivery system was developed based on paclitaxel-loaded polyethylene glycol)-disulfide-paclitaxel conjugate nanoparticles(PEG-SS-PTX/PTX NPs).The formulation emphasizes several benefits,including polymer-drug conjugates /prodrugs,self-assembled NPs,a high drug content,redox-responsibility,and programed drug *** PTX-loaded,self-assembled NPs,with a uniform size of 103 nm,characterized by DLS,TEM,XRD,DSC and 1H-NMR,exhibited excellent drug-loading capacity(15.7%) and entrapment efficiency(93.3%).PEG-SS-PTX/PTX NPs were relatively stable under normal conditions but disassembled quickly under reductive conditions,indicated by the triggered-aggregation phenomena and drug-release profile in the presence of dithiothreitol(DTT),a reducing ***'s more,by taking advantages of difference in drug releasing rates between physical-loaded and chemical-conjugated drugs,the "programmed drug release" phenomenon was observed,which attributed to higher concentration and longer action-time of *** influence of PEG-SS-PTX/PTX NPs on in vitro cytotoxicity,the cell cycle,and cellular apoptosis was determined in MCF-7 cell lines,and the NPs demonstrated a superior anti-proliferation activity associated with PTX-induced cell arrest in the G2/M phase and apoptosis over their nonresponsive ***,the redox-responsive NPs were more efficacious than both free PTX and the non-redox-responsive formulation at equivalent doses of PTX in the breast cancer xenogratt mouse *** redox-responsive PTX drug delivery system is promising and can be explored in effective intracellular drug delivery.

关键词： PTX Paclitaxel loaded redox-responsive nanoparticles based on a disulfide-linked poly drug conjugate for drug delivery ethylene glycol

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Dry power inhalation of Tetrandrine for improve the efficacy of cisplatin

Dry power inhalation of Tetrandrine for improve the efficacy...

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2014中国药物制剂大会——中国药学会药剂专业委员会年会、第六届亚洲阿登制药技术研讨会暨国际控释协会中国分会年会

作者： Wen-Wen Yang Ting Fan Qing-Ri Cao Jing-Hao Cui College of Pharmaceutical Science Soochow University

In order to evaluate the effect of Tetrandrine(TET) on the anticancer efficacy of cisplatin,dry powder inhalation of TET(DPI-TET) was *** evaluation of DPI was performed using two types of index including physicochemical properties(morphology,particle size and distribution,hygroscopicity,flowability) and aerosolisation performances(fine particles fraction and emitted dose).DPI was formed by micronized TET and carrier to obtain desired *** enhancing mechanism of chemotherapeutic drug in vitro was approached using human lung adenocarcinoma cell lines A549 and drug resistant cell lines A549/DDP In results,the sizes of micronized TET particles were in the range from 1 to 5 urn which might be appropriated for pulmonary *** the same time,lactose was selected as carrier due to it can significantly increase flowability and dispersibility of mixture,the fine particles fraction and emitted dose of DPI were improved from59.4±2.9%and 95.7±0.2%to 78.9±0.8%and 98.1±0.1%,*** IC50 value of cisplatin was reduced from 11.3±0.1 μmol·L-1 to 6.0±0.1 μmol·L-l when combined with micronized TET in A549 *** apoptotic rate induced by combination treatment was 42.4±0.8%,while cisplatin alone showed only 23.8±5.6%,and the percentage of S phase in cell cycle was increased from 16.4±0.7%to 46.4±3.1%compared with cisplatin treatment *** A549/DDP cells,the IC50 value of cisplatin was reduced from52.3±1.2 μmol·L-1 to 9.0±0.3μmolL-1 to add micronized TET,the percentage of S phase in cell cycle was increased from 29.4±3.5%to50.4±2.0%compared with cisplatin treatment *** conclusion,combination use of tetrandrine and cisplatin showed significant chemosensitizing effect in lung cancer cell to cisplatin through prolong the cell cycle in S phase.

关键词： Tetrandrine dry powder inhalation fine particles fraction chemosensitize

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