口服缓控释剂型结构对体外释药的影响

目的:综述近年口服缓控释制剂剂型结构对体外释药的影响,为缓释制剂研究提供参考。方法:查阅近年国内外相关文献,对常见的骨架型、包衣型、渗透泵型、微囊型、混合型等口服缓控释制剂的剂型结构及其对体外释药的影响分别加以概述。结果:同一药物,可以考虑制成不同的剂型结构,同一剂型结构又可以根据需求制成不同的剂型。结论:口服缓控释制剂剂型结构对体外释药有较大的影响。

某皮肤病专科门诊外用制剂临床应用及剂型结构分析

目的为专科门诊的临床合理用药和外用制剂的研发提供参考。方法对某皮肤病专科门诊2018年至2020年的外用制剂使用情况进行统计与分析。结果3年间,外用制剂品种数、用药量和销售金额总体稳中有升;药品来源约70%为市售化学药,其用量与金额占比基本同步;医院制剂品种偏少,但用量与市售中成药相差不大,且用药金额占比明显低于中成药;外用制剂销售总额连续3年均超过总销售额的40%(分别占44.07%,47.26%,48.99%);3年间用量排名第一的均为维生素E乳膏,2019年至2020年复方氟米松软膏的用量增加较多;3年间,金额排名第一的均为川百止痒洗剂;3年间,用量排名第一的维生素E乳膏的金额排名均未进入前4;3年间,用量排名前3的乳膏剂、软膏剂、洗剂占外用制剂总用量的(85.84±3.05)%,其用药金额占总用药金额的(84.54±6.76)%;临床用量最大的含激素类制剂以单一激素、激素+抗细菌药物、激素+抗真菌药物、激素+角质化药物等组方为主,占(34.77±2.24)%;其次为中成药制剂,以治疗皮炎、湿疹等瘙痒类疾病的洗剂为主,占(16.58±3.2)%。结论该专科门诊外用制剂种类较集中,剂型结构有偏向;搽剂、散剂、酊剂等剂型品种偏少,价格偏高;祛斑美容外用制剂品种缺乏,建议可作为制剂开发的方向之一。

浅谈固体制剂辅料与剂型结构的关系

浅谈固体制剂辅料与剂型结构的关系黄建敏（广东省珠海市人民医院５１９０００）匡蕾（江西中医学院附属医院３３０００６）关键词固体制剂，辅料，剂型结构固体制剂主要包括片剂、胶囊剂、丸剂和颗粒剂等，由于其具有许多特点，已成为目前发展的主要剂型范畴。因此相对应...

我国农药应用前景

我国人口众多，耕地有限。半个世纪以来，我国以占世界7．2％的耕地供给占全球22％的人口粮食的需要，成就举世瞩目。1998年，我国粮食产量达5．12亿吨，除满足当年约4．8亿吨的需求之外还绰绰有余。惜此后几年粮食总产量一直低于总消费量，粮食安全已经成为国家重大议题。

Oxidation of formic acid on stepped Au(997) surface

The adsorption and reaction of formic acid （HCOOH） on clean and atomic oxygen‐covered Au（997） surfaces were studied by temperature‐programmed desorption/reaction spectroscopy （TPRS） and X‐ray photoelectron spectroscopy （XPS）. At 105 K, HCOOH molecularly adsorbs on clean Au（997） and interacts more strongly with low‐coordinated Au atoms at （111） step sites than with those at （111） terrace sites. On an atomic oxygen‐covered Au（997） surface, HCOOH reacts with oxygen at‐oms to form HCOO and OH at 105 K. Upon subsequent heating, surface reactions occur among ad‐sorbed HCOO, OH, and atomic oxygen and produce CO2, H2O, and HCOOH between 250 and 400 K. The Au（111） steps bind surface adsorbates more strongly than the Au（111） terraces and exhibit larger barriers for HCOO（a） oxidation reactions. The surface reactions also depend on the relative coverages of co‐existing surface species. Our results elucidate the elementary surface reactions between formic acid and oxygen adatoms on Au surfaces and highlight the effects of the coordina‐tion number of the Au atoms on the Au catalysis.

Hydrodeoxygenation of Phenolic Model Compounds over MoS2 Catalysts with Different Structures

Several MoS2 catalysts of different structure, prepared by in situ decomposition of ammonium heptamolybdate （AHM） and molybdenum naphthenate （MoNaph）, and by MoS2 exfoliation （TDM）, were characterized by BET, X-ray diffraction （XRD）, Energy Dispersive X-ray （EDX） and transmission electron microscopy （TEM）. The analysis showed that MoS2 structure was dependant upon the preparation procedure. The activity of the catalysts was determined by measuring the hydrodeoxygenation （HDO） of phenol, 4-methylphenol and 4-methoxyphenol using a batch autoclave reactor operated at 2.8 MPa of hydrogen and temperatures ranging from 320-370℃. By comparing the conversion, the reactivity order of the catalysts was： AHM〉TDM-D〉MoNaph〉thermal〉MoS2 powder〉 TDM-W. Also, the effect of reaction temperature on the HDO conversion was explained in terms of equilibrium of reversible reaction kinetics. The main products of the HDO for phenolic compounds were identified by gas chromatography/mass spectrometry （GC/MS）. The results showed that the product distribution and the HDO selectivity were correlated with the reaction temperature. Two parallel reaction routes, direct hydrogenolysis and combined hydrogenation-hydrogenolysis, were confirmed by the analysis of the product distribution. High temperature favored hydrogenolysis over hydrogenation for HDO of phenol and 4-methoxyphenol, whereas for 4-methylphenol the reverse was true.

Development of a pentaethylenehexamine-modified solid support adsorbent for CO_2 capture from model flue gas

A novel solid support adsorbent for CO2capture was developed by loading pentaethylenehexamine(PEHA)on commercially available mesoporous molecular sieve MCM-41 using wet impregnation method.MCM-41 samples before and after PEHA loading were characterized by X-ray powder diffraction,N2adsorption/desorption,thermal gravimetric analysis and scanning electron microscope to investigate the textural and thermo-physical properties.CO2adsorption performance was evaluated in a fixed bed adsorption system.Results indicated that the structure of MCM-41 was preserved after loading PEHA.Surface area and total pore volume of PEHA loaded MCM-41 decreased with the increase of loading.The working adsorption capacity of CO2could be significantly improved at 60%of PEHA loading and 75°C.The effect of the height of adsorbent bed was investigated and the best working adsorption capacity for MCM-41-PEHA-60 reached 165 mg·(g adsorbent)-1at 75°C.Adsorption/desorption circle showed that the CO2working adsorption capacity of MCM-41-PEHA kept stable.

On the fracture resistance of adhesively jointing structures

The interface toughness of adhesively bonded structural members is one of the critical parameters for adhesive joint design. It is often assumed that the joint toughness is a material constant so that its value can be obtained from fracture tests of simple geometries such as DCB for Mode-Ⅰ, ENF for Mode-Ⅱ, using linear elastic fracture mechanics （LEFM）. However, the LEFM assumption of point-wise crack-tip fracture process is overly simplistic and may cause significant error in interpreting fracture test data. In this paper, the accuracy and applicability of various traditional beam-bending-theory based methods for fracture toughness evaluation, such as simple beam theory （SBT）, corrected beam theory （CBT） and experimental compliance method （ECM）, were assessed using the cohesive zone modelling （CZM） approach. It was demonstrated that the fracture process zone （FPZ） size has profound influence on toughness calculation and unfortunately, all the classic beam-bending theories based methods fail to include this important element and are erroneous especially when the ratio of crack length to FPZ size is relatively small （〈5.0）. It has also been demonstrated that after the FPZ size is incorporated into simple beam formulations, they provide much improved evaluation for fracture toughness. Formulation of first order estimate of FPZ size is aIso given in this paper.

Structure and properties of forming adsorbents prepared from different particle sizes of coal fly ash

In this paper, different particle sizes of coal fly ash FA-R(D50= 15.75 μm), FA-A(D50= 3.61 μm) and FA-B(D50= 1.73 μm) were treated with Na OH solution to prepare the forming adsorbents FFA-R, FFA-A and FFA-B.The structure and adsorption properties of the forming adsorbents for methylene blue(MB) from aqueous solution were examined. The results showed that the specific surface areas and adsorption capacities of the forming adsorbent for MB increased with decreasing particle size of raw coal fly ashes. The adsorption kinetic data of MB on FFA-R, FFA-A and FFA-B fitted the second-order kinetic model very well with the rate constants(k2) of3.15 × 10-2, 3.84 × 10-2and 6.27 × 10-2g·mg-1·min-1, respectively. The adsorption process was not only controlled by intra-particle diffusion. The isotherms of MB on FFA-R, FFA-A and FFA-B can be described by the Langmuir isotherm and the Freundlich isotherm, and the adsorption processes were spontaneous and exothermic.

Design,synthesis and biological evaluation of amino organophosphorus imidazoles as a new type of potential antimicrobial agents

A series of amino organophosphorus imidazoles were designed and synthesized as a novel structural type of antimicrobial agents.Bioactive evaluation in vitro showed that compound 3f exhibited equipotent or superior anti-methicillin-resistant Staphylococcus aureus(anti-MRSA) and anti-S. cerevisiae efficiencies(minimal inhibitory concentration(MIC)=2 μg/mL) to clinical drugs,and the combinations with antibacterial or antifungal drugs enhanced the antimicrobial efficiency. Highly active molecule 3f showed low propensity for bacteria to develop resistance, and the preliminary action mechanism studies demonstrated that 3f was membrane-active, but had no significant intercalation towards MRSA DNA. The computational study on 3f reasonably explained its high antimicrobial activity. Experimental data revealed that ground-state 3f-HSA complexes were formed mainly through hydrophobic interactions and hydrogen bonds with a spontaneous process, and the non-radioactive energy transfer from HSA to 3f occurred beyond F鰎ster resonance energy transfer theory. The participation of metal ions in 3f-HSA supramolucular system could increase the concentration of free compound 3f, and shorten its storage time and half-life in the blood to improve the maximum antimicrobial efficacy.

Construction of smart inorganic nanoparticle-based ultrasound contrast agents and their biomedical applications

Ultrasound(US) imaging in combination with US contrast agents(UCAs) is a powerful tool in the modern biomedical field because of its high spatial resolution, easy access to patients and minimum invasiveness.The microbubble-based UCAs have been widely used in clinical diagnosis; however, they are only limited to the blood pool imaging and not applicable to the tissue-penetrated imaging due to their large particle size and structural instability. Inorganic nanoparticles(NPs), such as silica,gold and Fe x O y, featured with both satisfactory echogenic properties and structural stability have the potential to be used as a new generation of UCAs. In this review, we present the most recent progresses in the tailored construction of inorganic UCAs and their biomedical applications in the US imaging-involved fields. Firstly, the typical inorganic NPs with different structures including solid, hollow and multiple-layer forms will be comprehensively introduced in terms of their structure design,physicochemical property, US imaging mechanism and diverse applications; secondly, the recent progress in exploring the gas-generating inorganic NP system for US imaging purpose will be reviewed, and these intelligent UCAs are multifunctional for simultaneous US imaging and disease therapy; thirdly, several nanocomposite platforms newly constructed by combining inorganic UCAs with other functional components will be presented anddiscussed. These multifunctional NPs are capable of further enhancing the imaging resolution by providing more comprehensive anatomical information simultaneously.Last but not the least, the design criteria for developing promising UCAs to satisfy both clinical demands and optimized US imaging capability will be discussed and summarized in this review.