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A NOTE ON THE TOXICITY AND SOLVENT PROPERTIES OF DIMETHYL SULPHOXIDE. 二甲基亚砜的毒性和溶剂性质。
Pub Date : 1964-03-01 DOI: 10.1097/00043764-196403000-00030
V. Brown, J. Robinson, D. E. Stevenson
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引用次数: 19
The neuromuscular blocking action of suxamethonium on the rat diaphragm. 苏曲霉素对大鼠膈肌的神经肌肉阻滞作用。
Pub Date : 1964-02-01 DOI: 10.1097/00132586-196402000-00004
R. Whittaker
Experiments are described using the rat isolated phrenic nerve diaphragm preparation, in which suxamethonium produced a neuromuscular block consisting of an initial phase of fairly sharp onset followed by a prolonged phase, which first remained at a steady level and then slowly decreased in intensity over several hours. Suxamethonium block is antagonised by potassium and intensified by tubocurarine in both phases. It would therefore appear that the depolarising action of suxamethonium is complicated by some measure of competitive inhibition in the isolated nerve-muscle preparation as in the intact animal.
实验描述了使用大鼠分离膈神经隔膜制剂,其中suxamethonium产生神经肌肉阻滞,包括初始阶段相当剧烈的发作,随后是一个延长的阶段,首先保持在稳定的水平,然后在几个小时内强度缓慢下降。Suxamethonium阻滞在两相中均被钾拮抗,并被管碱增强。因此,suxamethonium的去极化作用在孤立的神经-肌肉准备中与在完整的动物中一样,由于某种程度的竞争性抑制而变得复杂。
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引用次数: 3
Infra-red spectroscopy. 红外光谱。
Pub Date : 1956-04-01 DOI: 10.1615/atoz.i.infra-red_spectroscopy
T. Canback
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引用次数: 0
Physiology of alkaloids. 生物碱生理学。
Pub Date : 1955-06-01 DOI: 10.1146/ANNUREV.PP.06.060155.002141
K. Mothes
{"title":"Physiology of alkaloids.","authors":"K. Mothes","doi":"10.1146/ANNUREV.PP.06.060155.002141","DOIUrl":"https://doi.org/10.1146/ANNUREV.PP.06.060155.002141","url":null,"abstract":"","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"64 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1955-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114785713","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 83
Wound healing and dressings. 伤口愈合和敷料。
Pub Date : 1900-01-01 DOI: 10.1002/9781119548935.ch49
J. Scales
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引用次数: 1
Improving glyburide solubility and dissolution by complexation with hydroxybutenyl-beta-cyclodextrin. 羟基丁烯基-环糊精络合改善格列本脲的溶解度和溶出度。
Pub Date : 1900-01-01 DOI: 10.1211/jpp/61.01.0004
S. Klein, M. Wempe, T. Zoeller, N. Buchanan, J. L. Lambert, Michael G. Ramsey, K. Edgar, C. Buchanan
OBJECTIVESGlyburide, an important drug for type 2 diabetes, has extremely poor aqueous solubility and resulting low bioavailability. This study describes the ability of hydroxybutenyl-beta-cyclodextrin (HBenBCD) to form complexes with glyburide, with enhanced solubility and dissolution rate in vitro.METHODGlyburide and glyburide-HBenBCD were evaluated in various test media known to simulate human gastrointestinal conditions in the fasted and fed states, respectively.KEY FINDINGSAt approximately 14 wt% drug load, in the presence of HBenBCD, an almost 400-fold increase in glyburide aqueous solubility was observed. In the presence of HBenBCD, glyburide solubility was also significantly improved in all physiologically relevant test media. Subsequent dissolution experiments confirmed the solubility study results; the dissolution rate and total amount of drug released were significantly increased.CONCLUSIONSComplexation with HBenBCD may be an effective way to increase the bioavailability of glyburide.
目的格列本脲是治疗2型糖尿病的重要药物,其水溶性极差,导致生物利用度低。本研究描述了羟基丁烯基- β -环糊精(HBenBCD)与格列本脲形成配合物的能力,并在体外提高了溶解度和溶出率。方法对格列本脲和格列本脲- hbenbcd分别在各种已知的模拟空腹和进食状态下人体胃肠道状况的试验培养基中进行评价。在HBenBCD存在的情况下,约14wt %的药物负荷下,格列本脲的水溶性增加了近400倍。在HBenBCD存在的情况下,格列本脲在所有生理相关的测试介质中的溶解度也显著提高。随后的溶解实验证实了溶解度研究结果;药物溶出率和总释放量明显增加。结论与HBenBCD络合可能是提高格列本脲生物利用度的有效途径。
{"title":"Improving glyburide solubility and dissolution by complexation with hydroxybutenyl-beta-cyclodextrin.","authors":"S. Klein, M. Wempe, T. Zoeller, N. Buchanan, J. L. Lambert, Michael G. Ramsey, K. Edgar, C. Buchanan","doi":"10.1211/jpp/61.01.0004","DOIUrl":"https://doi.org/10.1211/jpp/61.01.0004","url":null,"abstract":"OBJECTIVES\u0000Glyburide, an important drug for type 2 diabetes, has extremely poor aqueous solubility and resulting low bioavailability. This study describes the ability of hydroxybutenyl-beta-cyclodextrin (HBenBCD) to form complexes with glyburide, with enhanced solubility and dissolution rate in vitro.\u0000\u0000\u0000METHOD\u0000Glyburide and glyburide-HBenBCD were evaluated in various test media known to simulate human gastrointestinal conditions in the fasted and fed states, respectively.\u0000\u0000\u0000KEY FINDINGS\u0000At approximately 14 wt% drug load, in the presence of HBenBCD, an almost 400-fold increase in glyburide aqueous solubility was observed. In the presence of HBenBCD, glyburide solubility was also significantly improved in all physiologically relevant test media. Subsequent dissolution experiments confirmed the solubility study results; the dissolution rate and total amount of drug released were significantly increased.\u0000\u0000\u0000CONCLUSIONS\u0000Complexation with HBenBCD may be an effective way to increase the bioavailability of glyburide.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"112 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128963994","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 15
Fish skin as a model membrane: structure and characteristics. 鱼皮作为模型膜:结构与特性。
Pub Date : 1900-01-01 DOI: 10.1211/jpp/61.01.0017
Fífa Konrádsdóttir, T. Loftsson, S. Sigfússon
OBJECTIVESSynthetic and cell-based membranes are frequently used during drug formulation development for the assessment of drug availability. However, most of the currently used membranes do not mimic mucosal membranes well, especially the aqueous mucous layer of the membranes. In this study we evaluated catfish (Anarichas lupus L) skin as a model membrane.METHODPermeation of hydrocortisone, lidocaine hydrochloride, benzocaine, diethylstilbestrol, naproxen, picric acid and sodium nitrate through skin from a freshly caught catfish was determined in Franz diffusion cells.KEY FINDINGSBoth lipophilic and hydrophilic molecules permeate through catfish skin via hydrated channels or aqueous pores. No correlation was observed between the octanol/water partition coefficient of the permeating molecules and their permeability coefficient through the skin. Permeation through catfish skin was found to be diffusion controlled.CONCLUSIONSThe results suggest that permeation through the fish skin proceeds via a diffusion-controlled process, a process that is similar to drug permeation through the aqueous mucous layer of a mucosal membrane. In addition, the fish skin, with its collagen matrix structure, appears to possess similar properties to the eye sclera.
目的:合成膜和细胞膜在药物处方开发过程中经常用于药物可用性评估。然而,目前使用的大多数膜都不能很好地模拟粘膜,特别是膜的水粘膜层。在这项研究中,我们评估了鲶鱼(Anarichas lupus L)皮肤作为模型膜。方法采用Franz扩散细胞法测定氢化可的松、盐酸利多卡因、苯佐卡因、己烯雌酚、萘普生、苦味酸和硝酸钠在新鲜捕获鲶鱼皮肤中的渗透作用。亲脂和亲水分子都通过水合通道或水孔渗透到鲶鱼皮肤中。渗透分子的辛醇/水分配系数与其通过皮肤的渗透系数无相关性。通过鲶鱼皮肤的渗透被发现是扩散控制的。结论:该药物通过鱼皮的渗透是一个扩散控制的过程,这一过程类似于药物通过粘膜水层的渗透。此外,鱼皮具有胶原蛋白基质结构,似乎具有与眼睛巩膜相似的特性。
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引用次数: 6
Effect of natsudaidain isolated from Citrus plants on TNF-alpha and cyclooxygenase-2 expression in RBL-2H3 cells. 柑桔纳屈苷对RBL-2H3细胞tnf - α和环氧合酶-2表达的影响
Pub Date : 1900-01-01 DOI: 10.1211/jpp/61.01.0015
T. Matsui, C. Ito, M. Itoigawa, T. Okada, H. Furukawa
OBJECTIVESFlavonoids inhibit the activity of chemical mediators released from mast cells. Our aim was to investigate the effects of natsudaidain, a polymethoxyflavone isolated from Citrus plants, on mast cells.METHODSWe investigated the inhibitory effects of natsudaidain, which is a polymethoxyflavone isolated from Citrus plants, on histamine release, tumour necrosis factor-alpha production and cyclooxygenase-2 expression in Ca ionophore-stimulated rat basophilic leukemia cells (A23187-stimulated RBL-2H3 cells) by spectrofluorometric, ELISA and immunoblotting methods.KEY FINDINGSThe percent of histamine release from A23187-stimulated RBL-2H3 cells pretreated with natsudaidain at 5, 25 and 50 microM was not changed as compared with non-treated A23187-stimulated cells. At 100 and 200 microM, natsudaidain pretreatment resulted in slightly reduced histamine release (% histamine release, 89.8+/-3.5% and 71.5+/-5.6% at 100 and 200 microM). Thus, natsudaidain hardly affects histamine release from RBL-2H3 cells, except at high concentrations. On the other hand, natsudaidain dose-dependently inhibited tumour necrosis factor-alpha protein and mRNA levels in A23187-stimulated RBL-2H3 cells; a concentration of 6.8 microM was required for a 50% reduction. In addition, all concentrations of this compound that we tested also inhibited cyclooxygenase-2 protein expression. The mRNA levels of cyclooxygenase-2 in A23187-stimulated RBL-2H3 cells treated with natsudaidain were also markedly decreased. The phosphorylated-p38 MAPK protein levels in A23187-stimulated RBL-2H3 cells treated with natsudaidain were lower than in the non-treated cells.CONCLUSIONSThese findings suggest that natsudaidain inhibits tumour necrosis factor-alpha and cyclooxygenase-2 production by suppressing p38 MAPK phosphorylation but not p65 NFkappaB phosphorylation, and that natsudaidain might alleviate inflammatory diseases.
目的:黄酮类化合物抑制肥大细胞释放的化学介质的活性。我们的目的是研究从柑橘植物中分离的多甲氧基黄酮natsudaidain对肥大细胞的影响。方法采用荧光光谱法、酶联免疫吸附法和免疫印迹法研究了从柑橘类植物中分离的多甲氧基黄酮纳屈苷对Ca离子载体刺激的大鼠嗜碱性白血病细胞(a23187刺激的RBL-2H3细胞)组胺释放、肿瘤坏死因子α产生和环氧化酶-2表达的抑制作用。与未处理a23187刺激的细胞相比,用那舒地丹在5、25和50微米下预处理a23187刺激的RBL-2H3细胞的组胺释放百分比没有变化。在100和200微米时,纳舒地丹预处理导致组胺释放量略有降低(组胺释放%,100和200微米时分别为89.8+/-3.5%和71.5+/-5.6%)。因此,除了高浓度外,那舒地丹几乎不影响RBL-2H3细胞的组胺释放。另一方面,那舒地丹剂量依赖性地抑制a23187刺激的RBL-2H3细胞中的肿瘤坏死因子- α蛋白和mRNA水平;需要6.8微米的浓度才能减少50%。此外,我们测试的所有浓度的化合物也抑制环氧化酶-2蛋白的表达。纳舒地丹对a23187刺激RBL-2H3细胞的环氧化酶-2 mRNA水平也显著降低。在a23187刺激的RBL-2H3细胞中,纳苏地丹处理的磷酸化p38 MAPK蛋白水平低于未处理的细胞。结论纳他丹通过抑制p38 MAPK磷酸化而非p65 NFkappaB磷酸化抑制肿瘤坏死因子- α和环氧化酶-2的产生,提示纳他丹可能具有减轻炎性疾病的作用。
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引用次数: 6
Determination of barbituric acid derivatives as mercury complexes. 巴比妥酸衍生物汞配合物的测定。
Pub Date : 1900-01-01 DOI: 10.3891/ACTA.CHEM.SCAND.12-1149
C. O. Bjorling, A. Berggren, B. Willman-Johnson
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引用次数: 9
An improved long-acting delivery system for narcotic antagonists. 一种改进的麻醉拮抗剂长效给药系统。
Pub Date : 1900-01-01 DOI: 10.1016/B978-0-08-023768-8.50918-X
A. Misra, R. Pontani
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引用次数: 4
期刊
The Journal of pharmacy and pharmacology
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