Pharmacy and Pharmacology Communications最新文献_第2页

Anti-diabetic Activity of Jussiaea suffruticosa Extract in Rats 柞蚕提取物对大鼠的抗糖尿病作用

Pharmacy and Pharmacology Communications Pub Date : 2000-10-01 DOI: 10.1111/J.2042-7158.2000.TB00219.X

T. Murugesan, B. Rao, S. Sinha, S. Biswas, M. Pal, B. P. Saha

{"title":"Anti-diabetic Activity of Jussiaea suffruticosa Extract in Rats","authors":"T. Murugesan, B. Rao, S. Sinha, S. Biswas, M. Pal, B. P. Saha","doi":"10.1111/J.2042-7158.2000.TB00219.X","DOIUrl":"https://doi.org/10.1111/J.2042-7158.2000.TB00219.X","url":null,"abstract":"The hypoglycaemic and anti-hyperglycaemic potential of a methanolic extract of Jussiaea suffruticosa Linn. (family-Onagraceae) was evaluated in normal and alloxan-diabetic rats. \u0000 \u0000 \u0000 \u0000In normal rats, the methanolic extract of J. suffruticosa Linn. (200 and 400 mg kg−1) exhibited significant hypoglycaemic activity (P < 0.05) within 3 h after oral administration. The plasma glucose concentration was 89.83±6 mg/100 mL (control 115.5±3.6 mg/100 mL) at 3h and 78.16±5.7 mg/100 mL (control 113.2±4.2 mg/100 mL) at 4.5 h after oral administration of 400 mg kg−1 of the methanolic extract. The effect was prolonged up to 24 h and the plasma glucose concentration fell to 75.66±5.5 mg/100 mL (control 112.16±3.7 mg/100 mL). The effect was dose-dependent. In alloxan-diabetic rats, the methanolic extract (400 mg kg−1) showed a significant anti-hyperglycaemic effect (P < 0.05) from 1.5 h after oral administration. This effect was prolonged up to 24 h and the plasma glucose concentration fell to 173.66±6 mg/100 mL (control 296.67±4.9 mg/100 mL) compared with 166.83±6.7 after oral administration of 10 mg kg−1 glibenclamide (standard). \u0000 \u0000 \u0000 \u0000The results indicate that the methanolic extract of whole plants of J. suffruticosa Linn. has potent hypoglycaemic potential in normoglycaemic rats and alloxan-diabetic rats.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79117582","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

Synthesis of Some Unsymmetrical Ester Derivatives of γ-(4-Substituted piperazin-1-yl)-α-phenyl propanols with Antispasmodic Activity 具有抗痉挛活性γ-(4-取代哌嗪-1-基)-α-苯基丙醇不对称酯衍生物的合成

Pharmacy and Pharmacology Communications Pub Date : 2000-10-01 DOI: 10.1211/146080800128735539

P. O. Osadebe, P. Akah, C. O. Okafor, L. Natova

引用次数: 0

Increased γ‐Glutamyl Transpeptidase Activity During Inflammation and its Inhibition by 6‐MFA, a Metabolite Obtained from Aspergillus ochraceus 炎症期间γ‐谷氨酰转肽酶活性的增加及其被6‐MFA抑制，一种从赭曲霉中获得的代谢物

Pharmacy and Pharmacology Communications Pub Date : 2000-10-01 DOI: 10.1211/146080800128735520

J. Dhuley, S. Naik

引用次数: 1

Cyclopiazonic Acid Induces Contractions in Ovine Tracheal Smooth Muscle 环吡唑酸诱导绵羊气管平滑肌收缩

Pharmacy and Pharmacology Communications Pub Date : 2000-10-01 DOI: 10.1211/146080800128735511

S. Mustafa

引用次数: 0

Improvement of Nimesulide Dissolution by a Co‐grinding Method Using Surfactants 表面活性剂共磨法改善尼美舒利的溶出度

Pharmacy and Pharmacology Communications Pub Date : 2000-10-01 DOI: 10.1211/146080800128735476

M. Gohel, L. Patel

{"title":"Improvement of Nimesulide Dissolution by a Co‐grinding Method Using Surfactants","authors":"M. Gohel, L. Patel","doi":"10.1211/146080800128735476","DOIUrl":"https://doi.org/10.1211/146080800128735476","url":null,"abstract":"A co-grinding method was used to improve the dissolution characteristics of nimesulide, a poorly water-soluble non-steroidal anti-inflammatory drug. Nimesulide solubility was studied to determine the solubilization process using different concentrations of Tween 80 at different pH values. \u0000 \u0000 \u0000 \u0000At a 10% Tween 80 concentration, a large proportion (> 90%) of drug was entrapped in micelles when the pH of buffer solution was greater than pKa of nimesulide. A 32 factorial design was adopted using the concentration of Tween 80 and sodium lauryl sulphate as independent variables. Improved drug dissolution was obtained when the drug was mixed first with aqueous surfactant solution and later blended with adjuvant such as lactose and microcrystalline cellulose. Sodium lauryl sulphate was more effective in increasing the drug dissolution compared with Tween 80. The use of a blend of Tween 80 and sodium lauryl sulphate is justified since the interaction term (Tween 80 x sodium lauryl sulphate) for percentage drug release in 45 and 120 min was not significant. Contour plots were obtained for the angle of repose and percentage drug release in 30, 45 and 120 min. \u0000 \u0000 \u0000 \u0000The study revealed that optimum level of surfactants should be used. The granule flow was adversely affected and no further improvement of drug dissolution was observed when the surfactants were used at high levels. The improved drug dissolution may be attributed to improved wetting and micellization due to presence of surfactants or hydrophilic adjuvant. More than two-fold increase in the drug dissolution was obtained by the selected batches.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88218033","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: 14

Antifungal Activity of Diplotaenia damavandica 大黄带绦虫的抗真菌活性

Pharmacy and Pharmacology Communications Pub Date : 2000-10-01 DOI: 10.1211/146080800128735502

S. Sardari, G. Amin, A. Sekhon, R. Micetich, M. Daneshtalab

引用次数: 11

Equilibrium Dialysis in a Stainless Steel Chamber, Measurement of the Free Plasma Fraction of Cyclosporin 不锈钢室平衡透析，环孢素游离血浆组分的测定

Pharmacy and Pharmacology Communications Pub Date : 2000-10-01 DOI: 10.1211/146080800128735494

F. Callejón, J. A. Duran, J. A. Abadín, A. Sánchez

引用次数: 2

Further Evidence of Extensive Pulmonary First‐pass Ester Hydrolysis after Airways Administration in Rats 进一步的证据表明，大鼠气道给药后广泛的肺一过酯水解

Pharmacy and Pharmacology Communications Pub Date : 2000-10-01 DOI: 10.1211/146080800128735485

P. Dickinson, P. Seville, G. Taylor

{"title":"Further Evidence of Extensive Pulmonary First‐pass Ester Hydrolysis after Airways Administration in Rats","authors":"P. Dickinson, P. Seville, G. Taylor","doi":"10.1211/146080800128735485","DOIUrl":"https://doi.org/10.1211/146080800128735485","url":null,"abstract":"The aim of this study was to synthesize an ester with low lipophilicity, and to use this ester to further investigate pre-absorptive pulmonary first-pass metabolism. \u0000 \u0000 \u0000 \u0000Hexanoic acid phenethyl ester was synthesized by reacting 2-phenylethanol with hexanoyl chloride. Pre-absorptive first-pass metabolism was assessed by comparing the areas under the blood concentration-time curves after intra-arterial administration of the hexanoic acid phenethyl ester with those after intratracheal instillation. Hexanoic acid phenethyl ester experienced extensive first-pass metabolism (53% of the absorbed dose) before or during absorption. This and earlier data suggests that the extent of this first-pass extraction is dependent on the physicochemical properties of the ester and in particular whether a compound experiences diffusion-limited absorption. \u0000 \u0000 \u0000 \u0000Pre-absorptive pulmonary first-pass metabolism of compounds whose absorption is diffusion-rate limited may be extensive even when pulmonary enzyme expression is low. This has consequences for the systemic delivery of drugs and in particular esters via the lungs.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84609021","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

Relaxant Action of Azulene‐1‐carboxamidine Derivative N1, N1‐dimethyl‐N2‐(2‐pyridylmethyl)‐5‐isopropyl‐3,8‐dimethylazulene‐1‐carboxamidine (HNS‐32) in Pig Coronary Artery Azulene - 1 - carboxamidine衍生物N1, N1 -二甲基- N2 - (2 - pyridylmethyl) - 5 -异丙基- 3,8 -二甲基- 1 - carboxamidine (HNS - 32)对猪冠状动脉的松弛作用

Pharmacy and Pharmacology Communications Pub Date : 2000-09-01 DOI: 10.1211/146080800128736268

Yoshio Tanaka Makoto Kamibayashi, F. Yamaki, M. Saitoh, T. Nakazawa, Hikaru Tanaka, K. Noguchi, K. Hashimoto, K. Shigenobu

{"title":"Relaxant Action of Azulene‐1‐carboxamidine Derivative N1, N1‐dimethyl‐N2‐(2‐pyridylmethyl)‐5‐isopropyl‐3,8‐dimethylazulene‐1‐carboxamidine (HNS‐32) in Pig Coronary Artery","authors":"Yoshio Tanaka Makoto Kamibayashi, F. Yamaki, M. Saitoh, T. Nakazawa, Hikaru Tanaka, K. Noguchi, K. Hashimoto, K. Shigenobu","doi":"10.1211/146080800128736268","DOIUrl":"https://doi.org/10.1211/146080800128736268","url":null,"abstract":"HNS-32 (N1N1-dimethyl-N2-(2-pyridylmethyl)-5-isopropyl-3,8-dimethylazulene-1-carbox-amidine) (CAS 186086-10-2) is a newly synthesized compound with an azulene structure within the molecule. The coronary relaxant action of HNS-32 was investigated pharmaco-mechanically on isolated pig coronary artery. The effects of HNS-32 were compared with diltiazem, a Ca2+-channel blocker. \u0000 \u0000 \u0000 \u0000HNS-32 inhibited sustained contractions evoked by high KCl, prostaglandin F2α, a thromboxane A2 mimetic (U46619) and endothelin-1 in a concentration-dependent manner. The potency of HNS-32 to inhibit these contractions was 5- to 40-times lower than diltiazem. HNS-32 also diminished phasic contractions induced by acetylcholine, histamine and 5-hydroxytryptamine. Addition of excess Ca2+ counteracted HNS-32-induced inhibition of high KCl-induced contraction only by approximately 10% whereas it restored diltiazem-induced inhibition by about 50%. Suppression of the contractile response to a phorbol ester (phorbol 12,13-dibutyrate) by HNS-32 was approximately 40%. \u0000 \u0000 \u0000 \u0000HNS-32 prevents coronary contractions produced by a wide variety of spasmogens. Although inhibitions of L-type Ca2+ channels and protein kinase C may be partly responsible for HNS-32 action, some direct action on the contractile systems seems to be involved in the coronary relaxation by HNS-32.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91535154","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: 23

The Reason for an Increase in Decomposition of Rifampicin in the Presence of Isoniazid under Acid Conditions 酸条件下异烟肼存在下利福平分解增加的原因

Pharmacy and Pharmacology Communications Pub Date : 2000-09-01 DOI: 10.1211/146080800128736277

Saranjit Singh, T. Mariappan, N. Sharda, Sanjeev Kumar, A. Chakraborti

{"title":"The Reason for an Increase in Decomposition of Rifampicin in the Presence of Isoniazid under Acid Conditions","authors":"Saranjit Singh, T. Mariappan, N. Sharda, Sanjeev Kumar, A. Chakraborti","doi":"10.1211/146080800128736277","DOIUrl":"https://doi.org/10.1211/146080800128736277","url":null,"abstract":"The poor bioavailability of rifampicin from fixed-dose combinations containing isoniazid has been attributed to isoniazid-catalysed degradation under acid conditions in the stomach. The mechanism by which isoniazid enhances rifampicin degradation is not known. The aim of this study was to determine the role of isoniazid in rifampicin decomposition. \u0000 \u0000Degradation studies were performed in 0.1 M HCl at 37°, in absence and presence of isoniazid. Both rifampicin and isoniazid were analysed. The degradation of rifampicin was increased approximately threefold in the presence of isoniazid. Isoniazid itself was degraded to a lesser extent amounting to one-fifth of the fall of rifampicin. HPLC studies revealed that decomposition of rifampicin in acidic conditions in the absence of isoniazid stopped at the formation of 3-formylrifamycin, while the reaction in the presence of isoniazid proceeded to form a hydrazone between 3-formylrifamycin and isoniazid. The existence of hydrazone was confirmed by its isolation on a preparative column and comparison with an authentic sample synthesized from reaction of 3-formylrifamycin with isoniazid. \u0000 \u0000We suggest that once 3-formylrifamycin is formed, it interacts with isoniazid to form the hydrazone, through a fast second-order reaction. As hydrazones are unstable in acid conditions, 3-formylrifamycin and isoniazid are regenerated in a reversible manner through a slower first-order reaction. In this complex reaction process, rifampicin is further degraded, while isoniazid is recovered.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2000-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83601303","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: 82