The Journal of pharmacy and pharmacology最新文献_第7页

The Journal of pharmacy and pharmacology Pub Date : 1900-01-01 DOI: 10.1002/9781119548935.ch49

J. Scales

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。

The Journal of pharmacy and pharmacology 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

{"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。

The Journal of pharmacy and pharmacology Pub Date : 1900-01-01 DOI: 10.1211/jpp/61.01.0017

Fífa Konrádsdóttir, T. Loftsson, S. Sigfússon

{"title":"Fish skin as a model membrane: structure and characteristics.","authors":"Fífa Konrádsdóttir, T. Loftsson, S. Sigfússon","doi":"10.1211/jpp/61.01.0017","DOIUrl":"https://doi.org/10.1211/jpp/61.01.0017","url":null,"abstract":"OBJECTIVES\u0000Synthetic 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.\u0000\u0000\u0000METHOD\u0000Permeation 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.\u0000\u0000\u0000KEY FINDINGS\u0000Both 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.\u0000\u0000\u0000CONCLUSIONS\u0000The 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.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"13 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":"126861138","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: 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

The Journal of pharmacy and pharmacology Pub Date : 1900-01-01 DOI: 10.1211/jpp/61.01.0015

T. Matsui, C. Ito, M. Itoigawa, T. Okada, H. Furukawa

{"title":"Effect of natsudaidain isolated from Citrus plants on TNF-alpha and cyclooxygenase-2 expression in RBL-2H3 cells.","authors":"T. Matsui, C. Ito, M. Itoigawa, T. Okada, H. Furukawa","doi":"10.1211/jpp/61.01.0015","DOIUrl":"https://doi.org/10.1211/jpp/61.01.0015","url":null,"abstract":"OBJECTIVES\u0000Flavonoids 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.\u0000\u0000\u0000METHODS\u0000We 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.\u0000\u0000\u0000KEY FINDINGS\u0000The 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.\u0000\u0000\u0000CONCLUSIONS\u0000These 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.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"117 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":"124885693","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: 6

Determination of barbituric acid derivatives as mercury complexes. 巴比妥酸衍生物汞配合物的测定。

The Journal of pharmacy and pharmacology Pub Date : 1900-01-01 DOI: 10.3891/ACTA.CHEM.SCAND.12-1149

C. O. Bjorling, A. Berggren, B. Willman-Johnson

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。

The Journal of pharmacy and pharmacology Pub Date : 1900-01-01 DOI: 10.1016/B978-0-08-023768-8.50918-X

A. Misra, R. Pontani

引用次数: 4

Rat tissue concentrations of chlorimipramine, chlorpromazine and their N-demethylated metabolites after a single oral dose of the parent compounds. 单次口服母体化合物后氯丙咪嗪、氯丙嗪及其n -去甲基化代谢物的大鼠组织浓度。

The Journal of pharmacy and pharmacology Pub Date : 1900-01-01 DOI: 10.1016/1043-6618(95)86446-6

G. Sgaragli, M. Valoti, M. Palmi, M. Frosini, M. Giovannini, L. Bianchi, L. Della Corte

引用次数: 8

In-situ absorption, protein binding and pharmacokinetic studies of S002-853, a novel antidiabetic and antidyslipidaemic flavone derivative in rats. 新型降糖降血脂黄酮衍生物S002-853在大鼠体内的原位吸收、蛋白结合及药代动力学研究。

The Journal of pharmacy and pharmacology Pub Date : 1900-01-01 DOI: 10.1211/jpp/62.05.0007

N. Gautam, H. Kushwaha, R. Pratap, Shio Kumar Singh

{"title":"In-situ absorption, protein binding and pharmacokinetic studies of S002-853, a novel antidiabetic and antidyslipidaemic flavone derivative in rats.","authors":"N. Gautam, H. Kushwaha, R. Pratap, Shio Kumar Singh","doi":"10.1211/jpp/62.05.0007","DOIUrl":"https://doi.org/10.1211/jpp/62.05.0007","url":null,"abstract":"OBJECTIVES\u0000The aim of the study was to investigate the in-situ absorption kinetics, plasma protein binding and pharmacokinetic characteristics of a novel synthetic flavone derivative, S002-853, which shows pronounced antidiabetic and antidyslipidaemic activity.\u0000\u0000\u0000METHODS\u0000Quantification of S002-853 in plasma was performed by the LC-MS/MS method and in-situ sample analysis was carried out by the HPLC-UV method.\u0000\u0000\u0000KEY FINDINGS\u0000The absorption rate constant was 0.274/h in a mild alkaline environment, which S002-853 experiences in the intestine following oral dose administration. Plasma protein binding was found to be 26.37 +/- 2.58% at a concentration of 1 microg/ml. The pharmacokinetic parameters were determined in male rats after administration of a single 40 mg/kg oral dose and 10 mg/kg intravenous dose. The peak plasma concentration (C(max)) was found to be 60.93 ng/ml at 8 h after oral administration. Irregular concentration-time profiles with secondary peaks were observed after oral dose administration. The elimination half-life of the compound was 19.56 h and 16.30 h after oral and intravenous doses, respectively. Comparison of the AUC after oral and intravenous dosing of S002-853 indicates that only about 29.48% (bioavailability) of the oral dose reaches the systemic circulation.\u0000\u0000\u0000CONCLUSIONS\u0000In-situ study of S002-853 shows slow absorption from the gastrointestinal tract. S002-853 also shows low plasma protein binding. The pharmacokinetic parameters after oral and intravenous dose reveal low oral bioavailability and high mean residence time.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"1 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":"134277340","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: 1

Acute withdrawal induced by adenosine A-receptor activation in isolated guinea-pig ileum: role of opioid receptors and effect of cholecystokinin. 腺苷a受体激活诱导离体豚鼠回肠急性戒断:阿片受体的作用和胆囊收缩素的作用。

The Journal of pharmacy and pharmacology Pub Date : 1900-01-01 DOI: 10.1211/jpp/62.05.0010

P. Marini, L. Romanelli, D. Valeri, P. Tucci, P. Valeri, M. Palmery

{"title":"Acute withdrawal induced by adenosine A-receptor activation in isolated guinea-pig ileum: role of opioid receptors and effect of cholecystokinin.","authors":"P. Marini, L. Romanelli, D. Valeri, P. Tucci, P. Valeri, M. Palmery","doi":"10.1211/jpp/62.05.0010","DOIUrl":"https://doi.org/10.1211/jpp/62.05.0010","url":null,"abstract":"OBJECTIVES\u0000In isolated guinea-pig ileum, the mu-opioid acute withdrawal response is under control of several neuronal systems, including the kappa-opioid and the A(1)-adenosine systems, which are involved in the mu-withdrawal response inhibitory control. After mu-opioid system stimulation, indirect activation of both kappa-opioid and A(1)-adenosine systems is prevented by the peptide cholecystokinin-8 (CCk-8). Guinea-pig ileum exposed to A(1)-adenosine agonist (CPA), shows a withdrawal contracture precipitated by the A(1)-adenosine antagonist (CPT). We investigated this response.\u0000\u0000\u0000METHODS\u0000We investigated the involvement of the opioid system in the A(1)-adenosine acute withdrawal response in guinea-pig ileum, the potential induced cross-dependence between the A(1) and the opioid system and also the interaction between the CCk-8 and A(1) systems.\u0000\u0000\u0000KEY FINDINGS\u0000We found that in the guinea-pig ileum preparation exposed to CPA, mu- and kappa-opioid antagonists increased the withdrawal response to CPT. Tissues exposed to CPA showed a contractile response to the opioid receptor antagonist naloxone only after complete removal of the A(1)-agonist. In the presence of CPA, the response to CCk-8 was inhibited while a significant increase in CPT response intensity was observed.\u0000\u0000\u0000CONCLUSIONS\u0000In guinea-pig ileum, stimulation of the A(1) system indirectly activates both mu- and kappa-opioid systems; this indirect activation is significantly, albeit not completely, antagonised by CCk-8. Cross dependence between A(1) and opioid systems was also observed.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"62 5 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":"131294903","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: 3

Potable water. 饮用水。

The Journal of pharmacy and pharmacology Pub Date : 1900-01-01 DOI: 10.4135/9781446247501.n3081

N. Burman, E. Taylor

引用次数: 7