马钱子巴布剂体外透皮实验及促透剂的筛选

目的:考察不同促透剂对马钱子巴布剂中马钱子碱、士的宁的体外透皮吸收的影响,筛选合适的促透剂。方法:采用改良Franz扩散池对离体大鼠皮肤进行体外透皮实验,RP-HPLC法测定含不同促透剂的马钱子巴布剂中活性成分的累积渗透量(Q_n)和透过率(T)。结果:马钱子巴布剂体外透皮吸收符合零级动力学方程,不同的促透剂对透皮吸收影响的顺序为:DMF>月桂氮芯卓酮(氮酮)>丙二醇>薄荷醇。在给定的范围内(≤5%),氮酮和薄荷醇的促透性能均是随着浓度增大而先升后降,二甲基甲酰胺和丙二醇的促透效果都是随着浓度增大而增强。结论:不同浓度的促透剂均能一定程度促进马钱子巴布剂活性成分的透皮吸收,其中以5%DMF的促渗效果最好。     

骨愈搽剂中总黄酮及其单体成分的体外透皮行为研究

目的:研究骨愈搽剂中总黄酮及其单体成分的体外透皮行为。方法:采用垂直式Franz扩散池法,以离体小鼠皮肤为透皮屏障进行试验。采用紫外分光光度法测定总黄酮含量,高效液相色谱法测定单体黄酮羟基红花黄色素A(HSYA)含量,考察二者12 h内的体外透皮情况。结果:骨愈搽剂中总黄酮和HSYA的累积渗透量Q均随时间t的增加而增加,并与t1/2有显著相关性,透皮吸收过程均符合Higuchi方程(r=0.995 6、0.999 5),透过速率分别为126.24、47.516μg/(cm2·h)。结论:骨愈搽剂中总黄酮的透皮行为与HSYA的透皮行为具有相似性,均属于骨架扩散型透皮给药系统,具有长效缓释的特点。     

不同骨架型乌头总生物碱贴片的经皮渗透性比较研究

目的:对比研究4种不同骨架型乌头总碱贴片的透皮吸收行为,筛选最佳贴片并对其进行体外释放度实验。方法:采用改良的Franz扩散池,以生理氯化钠溶液为接收介质,以大鼠离体背部皮肤为透皮屏障,计算4种骨架型贴片中乌头总碱及新乌头碱的稳态流量及滞后时间。结果:4种经皮给药制剂(TDS)中,黏胶剂骨架型贴片(P-3)稳态流量最高,其中乌头总碱的稳态流量9.2μg.cm-2.h-1,滞后时间1.413 h;新乌头碱的稳态流量0.243 6μg.cm-2.h-1,滞后时间1.172 h。该贴片体外释放符合回归方程,Higuchi方程为S(t)=13.32t1/2 18.428,r=0.980 1,体外释药机制为药物扩散和骨架溶蚀的综合效应。结论:黏胶剂骨架型是乌头总碱经皮给药制剂的理想设计模型。     

马钱子碱与士的宁体外经皮渗透性质的考察

目的:考察马钱子碱、士的宁游离药物体外经皮渗透性质及相互影响.方法:测定马钱子碱及士的宁在pH值7.4的磷酸盐缓冲液(PBS)、含10%乙醇的PBS、含20%乙醇的PBS及含20%乙醇的生理氯化钠溶液中的溶解度.用改良的Franz扩散池法考察马钱子碱溶液、士的宁溶液以及混合溶液中马钱子碱与士的宁体外透皮渗透性质.结果:根据溶解度实验结果选择含20%乙醇的PBS作为溶剂;以含20%乙醇的生理氯化钠溶液为接受液.马钱子碱与士的宁混合溶液中马钱子碱的体外经皮渗透速率比单用马钱子碱显著提高了近1.5倍(P<0.05),累积透过百分率也明显提高(P<0.01);而士的宁没有显著变化.结论:士的宁可显著促进马钱子碱的体外经皮渗透速度和程度.     

乌头生物碱类成分透皮吸收的研究进展

目的:探讨乌头生物碱类成分经皮给药的研究进展,为其达到减毒增效的效果及透皮制剂的开发和研究提供理论参考。方法:基于乌头生物碱类成分药理、毒理的不断研究和发现,对国内外学者的相关研究进行归纳、分析,总结从透皮给药的选择、影响透皮吸收的因素、改善其透皮行为的方法等方面,对乌头生物碱类成分的透皮吸收研究状况进行简要综述。结果:乌头生物碱类成分具有一定透皮性能。鉴于其具有的毒理性能,需考虑其炮制工艺与制剂工艺的联合;有必要采用一些传统方法来改善其经皮通透性。结论:选择将乌头生物碱类成分制备成透皮制剂在改善其毒性及发挥治疗作用方面具有广阔的发展前景。     

黄连膏体外透皮吸收及抗炎活性研究

目的：采用改良的Franz透皮扩散池考察黄连膏中主要活性成分的体外透皮吸收情况,同时对黄连膏的抗炎活性进行初步研究。方法：选用改良Franz透皮扩散池,接收液为30%乙醇生理盐水,以小鼠背部皮肤为透皮材料,采用紫外分光光度法及高效液相色谱法测定透皮接收液中盐酸小檗碱、芝麻酚、芝麻素及总生物碱的含量,计算透皮吸收动力学参数,考察黄连膏中抗炎活性成分的累计透过量及吸收规律;取30只SPF级小鼠,随机分为5组,即模型组、醋酸地塞米松乳膏组（100 mg·kg^-1）、黄连膏高剂量组0.075 g·g^-1（生药/膏）、黄连膏中剂量组0.15 g ·g^-1（生药/膏）、黄连膏低剂量组0.3g ·g^-1（生药/膏）,每组6只。阳性对照组为醋酸地塞米松乳膏组,进行2,4-二硝基氯苯（DNCB）致小鼠耳肿胀实验,观察黄连膏对炎症的抑制作用。结果：黄连膏中芝麻酚、盐酸小檗碱、芝麻素及总生物碱在24 h内的累积透过量分别为2.82,4.10,0.78,16.54 μg·cm^-2;稳态透皮速率（J_s）分别为0.125 2,0.181 4,0.034 2,0.745 7 μg·cm^-2·h^-1;与阳性对照组比较,黄连膏高剂量组显著抑制DNCB所致小鼠耳肿胀。结论：黄连膏具有良好的体外透皮性能及抗炎活性,24 h内单位面积累积透过量随药物中主要有效成分含量升高而增加,经皮渗透行为符合零级动力学方程。     

水杨酸及其衍生物透皮吸收的研究

目的研究水杨酸及其衍生物的透皮吸收.方法用丙二醇作促透剂,用改良的Franz扩散池进行离体大鼠皮体外释放试验,紫外法测定累积释放量,计算平均透皮速率.结果含丙二醇乳膏中各药物的透皮速率分别为水杨酸38.722 5μg·cm2·h-1,赖氨匹林16.882 1μg·cm2·h-1,阿司匹林10.121 5 μg·cm2·h;不含丙二醇乳膏各药物透皮速率分别为水杨酸29.765 7μg·cm2·h-1,赖氨匹林10.690 0μg·cm2·h-1,阿司匹林6.965 3 μg·cm2·h-1.结论两种乳膏水杨酸、赖氨匹林、阿司匹林透皮速率差异显著;丙二醇对赖氨匹林和阿司匹林均有显著的促透作用.     

可乐定透皮贴片的量效关系及生物利用度研究

可乐定贴片是新研制的透皮吸收控释膜剂，经过３Ｈ－标记的放射性同位素技术测定，家兔透皮吸收后，血药浓度在１６ｈ内维持在４．６３～９．２６ｎｍｏｌ·Ｌ－１，体内吸收情况与静脉滴注相仿，一次使用维持降压２４ｈ以上，其对数剂量与降压百分率呈良好的线性关系（ｒ＝０．９９０２，Ｐ＜０．０１）。并测得其ＥＤ５０为４０．１μｇ·ｋｇ－１，体内生物利用度为０．４４。     

藏药植物药内源性生物碱类毒性成分的代谢转化及减毒特征研究进展

某些藏药植物药中的活性成分同时也是毒性成分,需要在使用中确切了解其作用机制及代谢途径。毒性较大的藏药植物药,其内源性毒性成分主要为生物碱,如乌头类、甲基牛扁碱等二萜生物碱、莨菪烷类生物碱、马钱子碱、士的宁、罂粟碱和苦马豆素等。藏药植物药中具有代表性的内源性生物碱类毒性成分多存在于根、种子和果实中,多因其剧毒或高毒化学物本质,表现出神经毒性和心脏毒性。一般经去烷基、羟基化和水解等Ⅰ相代谢过程及与葡萄糖醛酸、磺酸结合等Ⅱ相代谢过程,产生多种高极性和毒性减弱的代谢产物,排出体外。多种生物碱的中毒剂量与治疗剂量相近,藏药典籍中常采用炒制、奶制、青稞酒制和诃子配伍等减毒后入药。本文针对包括乌头类二萜双酯、莨菪烷和马钱子碱等在内的5类12种生物碱,着重评述其代谢转化、减毒和安全性评价特点,以期为制定藏药植物药内源性毒性成分限量、临床用药和减毒治疗提供全面参考。     

口疳散穴位贴敷的制备工艺及体外透皮吸收研究

目的:考察不同制备工艺,包括药材粉碎方法、黏合剂以及透皮吸收剂对穴位贴敷有效成分透皮吸收的影响.方法:以裸鼠腹部皮肤为体外透皮实验材料,以吴茱萸碱为指标成分,用改良Franz扩散池法建立透皮吸收试验方法,收集穴位贴敷的透皮接受液,用高效液相色谱法测定其吴茱萸碱的含量,计算其累积透皮量、透皮速率和皮肤滞留量.结果:吴茱萸...     

Nutrient compositions of culinary-medicinal mushroom fruiting bodies and mycelia

Mushrooms (including fruiting bodies and mycelia) are a food with high nutritional value. This article summarizes the results of proximate composition studies of 38 fruiting bodies and 19 mycelia of 32 species of culinary-medicinal mushrooms from genera Agaricus, Agrocybe, Antrodia, Auricularia, Boletus, Clitocybe, Coprinus, Cordyceps, Trametes, Dictyophora, Flammulina, Ganoderma, Grifola, Hericium, Hypsizygus, Inonotus, Lentinus, Morchella, Pleurotus, Sparassis, Termitomyces, Tremella, and Tricholoma. Based on the proximate composition, most fruiting bodies and mycelia are low in fat and rich in protein and dietary fiber (DF); however, some are rich in soluble polysaccharides and others are rich in crude fiber. Due to the high amount of DF present, the energy provided by 100 g of dry fruiting bodies and mycelia is 46.96-292.37 kcal and 195.84-373.22 kcal, respectively. The energy (100 g) is classified into four levels: first level of >300 kcal, second level of 200-300 kcal, third level of 100-200 kcal, and fourth level of <100 kcal. Most fruiting bodies are listed in the third level; nine mycelia are listed in the first level and ten in the second level. Overall, the information about the proximate composition and energy are of great interest for fruiting bodies and mycelia to be used as foods or food-flavoring materials or in the formulation of health foods.     

Isolation and characterization of a lethal hemolysin in the sea anemone Parasicyonis actinostoloides

Four species of sea anemones in the coastal waters of Japan were surveyed for hemolysins. Powerful hemolysins were detected in Parasicyonis actinostoloides and Anthopleura japonica, whereas extracts of A. fuscoviridis showed much weaker hemolytic activity and those of of Haliplanella luciae no activity. Among the animal erythrocytes tested sheep were most sensitive to the hemolysins of the three positive species. The major hemolysin (parasitoxin) in whole bodies of P. actinostoloides was isolated by ion exchange chromatography, gel filtration and chromatofocusing. In addition to hemolytic activity (119900 HU/mg) it exhibited lethal activity in mice (LD50 65 micrograms/kg, i.v.) and fish Oryzias latipes (approximate minimum lethal concentration 1.5 micrograms/ml). Parasitoxin was slightly basic (pI 7.9) in nature and its amino acid composition was characterized by the absence of half-cystine. The molecular weight was 19,000 by SDS-polyacrylamide gel electrophoresis or 17,000 by sedimentation equilibrium, indicating that parasitoxin has no subunit structure.     

Stability of ferruginous bodies in human lung tissue following death, embalmment, and burial

The identification of asbestos bodies in tissue sections is an indicator of past exposure to longer asbestos fibers. These structures are formed in lung tissue as a consequence of interactions with pulmonary macrophages resulting in the deposition of a ferroprotein (ferruginous) coating on the fiber. While the process of ferruginous body formation is known to take months in animal tissue, there is no published information on the stability of ferruginous bodies in tissue following death. The material assessed in the present study was obtained from lung material collected from an exhumed body approximately 8(1/2) mo after death, embalmment, and burial. Tissue sections were reviewed for the presence of asbestos bodies. Additional pieces of lung tissue were digested, with the digestate being evaluated by light microscopy for ferruginous bodies and by electron microscopy for uncoated asbestos fibers and core analysis of asbestos bodies. Classical ferruginous (asbestos) bodies were found in abundance in the tissue sections including in areas with fibrosis. The levels of uncoated asbestos fibers and classical appearing ferruginous bodies (asbestos bodies) were consistent with occupational levels of tissue burden. The data from this study indicate that ferruginous bodies remain morphologically stable within the tissue for months following death, embalmment, and burial. Thus the lung tissue from this exhumed individual was usable not only to pathologically confirm asbestosis but also to provide quantitative data of occupational exposure to asbestos.     

Stability of Ferruginous Bodies in Human Lung Tissue Following Death,Embalmment, and Burial

The identification of asbestos bodies in tissue sections is an indicator of past exposure to longer asbestos fibers. These structures are formed in lung tissue as a consequence of interactions with pulmonary macrophages resulting in the deposition of a ferroprotein (ferruginous) coating on the fiber. While the process of ferruginous body formation is known to take months in animal tissue, there is no published information on the stability of ferruginous bodies in tissue following death. The material assessed in the present study was obtained from lung material collected from an exhumed body approximately 8½ mo after death, embalmment, and burial. Tissue sections were reviewed for the presence of asbestos bodies. Additional pieces of lung tissue were digested, with the digestate being evaluated by light microscopy for ferruginous bodies and by electron microscopy for uncoated asbestos fibers and core analysis of asbestos bodies. Classical ferruginous (asbestos) bodies were found in abundance in the tissue sections including in areas with fibrosis. The levels of uncoated asbestos fibers and classical appearing ferruginous bodies (asbestos bodies) were consistent with occupational levels of tissue burden. The data from this study indicate that ferruginous bodies remain morphologically stable within the tissue for months following death, embalmment, and burial. Thus the lung tissue from this exhumed individual was usable not only to pathologically confirm asbestosis but also to provide quantitative data of occupational exposure to asbestos.     

Evaluation of modified methods for determining skin irritation

The premarket testing of household cleaning products for dermal irritancy is best achieved via human testing. Animal dermal irritation testing is generally limited to screening for possible dermal hazard of totally new or unique products or ingredients prior to human testing or to meeting regulatory requirements of government bodies. Alternatives to animal tests are being sought; however, until such time that these alternatives are identified, validated, and accepted by government bodies, the judicious use of animal testing remains a necessity. Modifications to standard animal skin irritation test procedures have been evaluated against human skin irritation results with the objective of defining one method that could be used in place of current standard procedures that differ slightly from one another, and thereby avoid excessive and redundant use of animals. Hill Top Chambers (19 mm) and standard gauze patches (U.S. Department of Transportation procedure) were used to obtain comparative irritation responses for 24 cleaning products, common caustics, and acids in rabbits and humans. Exposure times were 1 or 4 hr, and responses were graded over a 72-hr period. Results indicate that use of the Chamber offers the potential to (1) reduce the number of animals used for skin irritation screening (smaller group size and up to eight test substances/concentrations per animal); (2) eliminate the need for conducting multiple tests to satisfy different governmental requirements; and (3) reduce animal stress by reducing exposure times without compromising the value of the irritancy patch test as a screening tool. When animal data are required, it is suggested that the use of a Chamber and other modifications of traditional test procedures offers advantages that could result in using fewer animals and/or have less potential for producing unnecessarily severe responses in animals.     

Lipid bodies in innate immune response to bacterial and parasite infections

Lipid bodies (also known as lipid droplets, adiposomes) are dynamic organelles with key roles in regulating storage and turnover of lipids in different cells and organisms. The emerging role of lipid bodies as inflammatory organelles raises lipid body status to critical regulators of different inflammatory and infectious diseases and key markers of cell activation. Notably, lipid body biogenesis is highly regulated and is cell and stimuli specific. Lipid body structural features, including lipid and protein composition may vary according to the cell type, activation state and inflammatory environment and thus may determine different cellular functions for lipid bodies. Here we will review the morphological and structural aspects of lipid bodies, the regulated mechanisms of formation, as well as lipid body functions in cells involved in the innate immune response during bacterial and parasite infections.     

Animal Venom for Medical Usage in Pharmacopuncture in Korean Medicine: Current Status and Clinical Implication

Animal venoms, widespread throughout the world, are complex mixtures, the composition of which depends on the venom-producing species. The objective of this study was to contribute to the development of animal venom-based medicines by investigating the use of animal venom pharmacopuncture in Korean medicine (KM) institutions. We surveyed 256 public health centers from 1 through 31 October 2019 as guided by the Ministry of Health and Welfare (MoHW). A questionnaire developed by an expert group was distributed and collected for statistical analysis. The survey identified three types of animal venom-based pharmacopuncture: bee, snake, and toad venoms. The medications are based on a single animal venom ingredient and produced in 11 external herbal dispensaries (EHDs). Each animal venom is processed, refined, and freeze-dried in a cleanroom to produce a powder formulation that is later measured, diluted, filtered, filled, sealed, sterilized, and packaged as pharmacopuncture injections used in KM institutions. Bee venom therapy is effective in treating musculoskeletal pain, snake venom therapy is effective in controlling bleeding during surgery, and toad venom therapy is effective in cancer treatment. The study suggests that bee, snake, and toad venoms could be used in medical institutions and have the potential for drug development.     

胃镜治疗上消化道外源性异物53例临床分析

目的:探讨胃镜在上消化道外源性异物取出中的应用效果.方法:收集1998～2010年上消化道异物患者53例,均于胃镜下安全取出.对其发病年龄、异物种类、部位及取出方法进行分析.结果:53例患者取出异物53件,常规胃镜下取出42例,无痛胃镜下取出11例,包括儿童9例和贩毒嫌疑人2例.病例均未发生出血、穿孔等并发症.结论:上消化道外源性异物经胃镜直视下取出是一种便捷、经济、安全的治疗方法.     

日本鹌鹑睾丸组织学年龄性变化

本文是研究日本鹌鹁(Coturnix coturnix Japonica)睾丸组织不同日龄的生长发育。精细胞的生长发育可分为六期。初级精母细胞于11天龄出现;36天龄出现精于细胞;46天龄可见已成形的精子。鹌鹑的精子细胞与家畜及鸡的精子细胞在结构与染色特点上有所不同。睾丸间质细胞5天龄前已出现,始终明显地存在于睾丸间质组织中,这与鸡的间质细胞在年龄性变化上存有差异。在21天龄后的曲精细管管腔中,可见数量不等的退化细胞及由数个胞质强嗜酸性的细胞组成的嗜酸小体。小体可见有双核,三核或多核的。     

Regulating pesticides in the UK: a case study of risk management problems relating to the organophosphate diazinon.

OBJECTIVES: (1) To assess aspects of occupational and related environmental health risk assessment and risk management decisions of UK regulatory bodies on diazinon used in sheep dip; and (2) to benchmark those decisions against 'the public health precautionary approach'. METHODS: Analysis of diazinon health and safety data available within Government Departments, industry and from users in animal husbandry practice. RESULTS: (1) Data on diazinon produced by the manufacturing companies for the UK pesticide regulatory agencies are not fully transparent; (2) UK regulatory health and safety processes assume accuracy of manufacturer's data and information provided on personal protective equipment (PPE) and application effectiveness; (3) data available reveal gaps and problems with diazinon toxicity, PPE and application methods; and (4) little published evidence shows that industry followed up the health of dippers after product registration or that government departments adopted a public health approach to regulation. CONCLUSIONS: Diazinon sheep dip illustrates the need for the application of a rigorous precautionary principle in both initial registration and later monitoring of chemicals.