Farmaco (Societa chimica italiana : 1989)最新文献

Mechanistic evaluation of the effect of thermal-treating on Eudragit RS matrices 热处理对Eudragit RS基体影响的机理评价

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-11-01 DOI: 10.1016/j.farmac.2005.07.009

Shirzad Azarmi , Fatemeh Ghaffari , Raimar Löbenberg , Ali Nokhodchi

引用次数: 35

New, simple and validated UV-spectrophotometric methods for the estimation of gatifloxacin in bulk and formulations 新的，简单和有效的紫外分光光度法估计加替沙星原料药和制剂

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-11-01 DOI: 10.1016/j.farmac.2005.08.010

K. Venugopal, Ranendra N. Saha

{"title":"New, simple and validated UV-spectrophotometric methods for the estimation of gatifloxacin in bulk and formulations","authors":"K. Venugopal, Ranendra N. Saha","doi":"10.1016/j.farmac.2005.08.010","DOIUrl":"10.1016/j.farmac.2005.08.010","url":null,"abstract":"<div>New, simple and cost effective UV-spectrophotometric methods were developed for the estimation of gatifloxacin in bulk and pharmaceutical formulations. Gatifloxacin was estimated at 286 nm in 100 mM phosphate buffer (pH 7.4) and 292 nm in 100 mM hydrochloric acid (pH 1.2). Linearity range was found to be 1–18 μg ml–1 (regression equation: absorbance=0.0684×Concentration in μg ml–1  =0.9998) in the phosphate buffer (pH 7.4) and 1–14 μg ml–1 (regression equation: absorbance=0.0864×Concentraion in μg ml–1  =0.9999) in hydrochloric acid medium (pH 1.2). The apparent molar absorptivity was found to be 2.62×104 l mol−1 cm−1 in the phosphate buffer and 3.25×104 l mol−1 cm−1 in hydrochloric acid media. In both the proposed methods sandell's sensitivity was found to be about 0.01 μg cm−2/0.001A. These methods were tested and validated for various parameters according to ICH guidelines and USP. The quantitation limits were found to be 0.312 and 0.3 μg ml–1 in the phosphate buffer and hydrochloric acid medium, respectively. The proposed methods were successfully applied for the determination of gatifloxacin in pharmaceutical formulations (tablets, injection and ophthalmic solution). The results demonstrated that the procedure is accurate, precise and reproducible (relative standard deviation <2%), while being simple, cheap and less time consuming and can be suitably applied for the estimation of gatifloxacin in different dosage forms and dissolution studies.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 11","pages":"Pages 906-912"},"PeriodicalIF":0.0,"publicationDate":"2005-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.08.010","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25637056","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: 55

Feasibility studies of dermal delivery of paclitaxel with binary combinations of ethanol and isopropyl myristate: role of solubility, partitioning and lipid bilayer perturbation 乙醇和肉豆蔻酸异丙酯二元组合给药紫杉醇的可行性研究:溶解度、分配和脂质双分子层扰动的作用

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-11-01 DOI: 10.1016/j.farmac.2005.07.004

Ramesh Panchagnula, Hariraghuram Desu, Amit Jain, Sateesh Khandavilli

{"title":"Feasibility studies of dermal delivery of paclitaxel with binary combinations of ethanol and isopropyl myristate: role of solubility, partitioning and lipid bilayer perturbation","authors":"Ramesh Panchagnula, Hariraghuram Desu, Amit Jain, Sateesh Khandavilli","doi":"10.1016/j.farmac.2005.07.004","DOIUrl":"10.1016/j.farmac.2005.07.004","url":null,"abstract":"<div>In the current investigation, paclitaxel (PCL) delivery into the different layers of skin, vehicle optimization and relationship between vehicle composition and the relative contribution of solubility, partition and diffusion towards drug transport has been outlined. Saturation solubility of PCL was determined in ethanol (EtOH), isopropyl myristate (IPM) and their binary combinations, and partition studies performed to study the probability of skin depot formation. Epidermal and dermal partitioning was carried from PCL saturated vehicles. Skin permeation of PCL was studied using the rat skin. FT-IR has been utilized to study the skin barrier perturbation, and the localization of PCL and isopropyl myristate (IPM) in epidermis. High Kapp value in mineral oil/buffer indicated the tendency of PCL to form a reservoir in skin, and an inverse relationship between PCL solubility in different solvent systems and partitioning into epidermis was found. Maximum Kepidermis for PCL was observed with IPM, while PCL in EtOH/IPM (1:1) showed high partitioning into dermis. Maximum flux of PCL was observed with EtOH/IPM (1:1). For lipophilic drug like PCL modulation of vehicle seems to be effective approach to increase the permeability across the skin. With a binary combination of EtOH/IPM (1:1) higher concentration of PCL can be delivered to deeper layer of skin whereas with IPM higher concentration of PCL could be localized in the epidermis. While engineering the delivery vehicle selection of solvents should be such that one of them is miscible in both hydrophilic and lipophilic phase like ethanol and another should be lipophilic in nature (IPM in this case) so that an optimum balance between ‘push–pull’ and ‘blending’ effect can be achieved.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 11","pages":"Pages 894-899"},"PeriodicalIF":0.0,"publicationDate":"2005-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.07.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25271746","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: 34

Chemical and biochemical transformations of 5-ethoxycarbonyl-5-phenyl-2-isoxazolines 5-乙氧羰基-5-苯基-2-异恶唑啉的化学和生化转化

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-11-01 DOI: 10.1016/j.farmac.2005.07.003

Irmina Zadrożna , Joanna Kurkowska , Hanna Kruszewska

引用次数: 2

INDEX MOTS CLES 2005 指数低于2005年

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-11-01 DOI: 10.1016/S0014-827X(05)00214-4

引用次数: 0

CV2 - Editorial Board CV2 -编辑委员会

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-11-01 DOI: 10.1016/S0014-827X(05)00207-7

引用次数: 0

Nasal administration of heparin-loaded microspheres based on poly(lactic acid) 基于聚乳酸的负载肝素微球鼻腔给药

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-11-01 DOI: 10.1016/j.farmac.2005.08.004

Ayca Yıldız , Alper Okyar , Gül Baktır , Ahmet Araman , Yıldız Özsoy

引用次数: 16

Relationship between lipophilicity of BCS class III and IV drugs and the functional activity of peroral absorption enhancers BCS III类和IV类药物的亲脂性与口服吸收促进剂功能活性的关系

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-11-01 DOI: 10.1016/j.farmac.2005.08.006

Pradeep Sharma, Manthena V.S. Varma, Harmander P.S. Chawla, Ramesh Panchagnula

{"title":"Relationship between lipophilicity of BCS class III and IV drugs and the functional activity of peroral absorption enhancers","authors":"Pradeep Sharma, Manthena V.S. Varma, Harmander P.S. Chawla, Ramesh Panchagnula","doi":"10.1016/j.farmac.2005.08.006","DOIUrl":"10.1016/j.farmac.2005.08.006","url":null,"abstract":"<div>Absorption enhancers (AEs) have been shown to be specific in permeation enhancement capabilities because of which they increase absorption of some drug molecules more than others. Present study was designed to investigate the relationship between lipophilicity of drug molecules and the absorption enhancement potential of AEs. Four drug molecules of different lipophilicity were selected as model compounds, namely, cefotaxime sodium, ceftazidime pentahydrate, lovastatin and cyclosporin A. Their apparent permeability coefficients in the absence and presence of three classes of AEs (fatty acids, cyclodextrins, and bile salts) were determined using in vitro everted rat intestinal sac absorption model. Significant relationship was observed between log P of drug and absorption enhancement ratios by AEs. This relationship was found to be functionally directly or indirectly proportional depending upon nature of AE and explain the mechanism of permeation enhancement.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 11","pages":"Pages 870-873"},"PeriodicalIF":0.0,"publicationDate":"2005-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.08.006","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25602830","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: 30

Synthesis of 3-aryl-5-decapentyl-1,2,4-oxadiazoles possessing antiinflammatory and antitumor properties 具有抗炎和抗肿瘤性质的3-芳基-5-十戊基-1,2,4-恶二唑的合成

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-11-01 DOI: 10.1016/j.farmac.2005.08.003

Natércia M. Miranda Bezerra , Shalom P. De Oliveira, Rajendra M. Srivastava, Joel R. Da Silva

引用次数: 48

A new assay for the discovery of Bcl-XL inhibitors 发现Bcl-XL抑制剂的新方法

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-11-01 DOI: 10.1016/j.farmac.2005.06.017

Cristina Pisoni , Guido Cimoli , Anna Resconi , Daniele Losi , Rolando Lorenzetti , Silvio Parodi , Lucia Carrano

{"title":"A new assay for the discovery of Bcl-XL inhibitors","authors":"Cristina Pisoni , Guido Cimoli , Anna Resconi , Daniele Losi , Rolando Lorenzetti , Silvio Parodi , Lucia Carrano","doi":"10.1016/j.farmac.2005.06.017","DOIUrl":"10.1016/j.farmac.2005.06.017","url":null,"abstract":"<div>The Bcl-2 family of antiapoptotic proteins is commonly over expressed in many types of human cancer and remains one of the few validated targets. Antiapoptotic family proteins such as Bcl-2 and Bcl-XL function, at least in part, by binding proapoptotic members such as Bax and Bak and thereby prevent release of the apoptotic cascade of events. “BH3-only” members of the family disrupt this interaction by binding, via their BH3 domain, to a hydrophobic pocket on the surface of the antiapoptotic members. Disruption of heterodimerization could be used to modulate cell death reinstating apoptosis in cancer cells. An affinity displacement assay based on Bcl-XL/BH3 interaction has been developed. This assay makes use of soluble His-tagged Bcl-XL and fluorescein tagged BH3. Binding is measured as fluorescence associated with magnetic beads. The assay was miniaturized to 96-well microtiter plates and can be employed in high throughput screening (HTS), in addition it is robust enough to be applied to microbial fermentation extracts.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 11","pages":"Pages 938-943"},"PeriodicalIF":0.0,"publicationDate":"2005-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.06.017","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25219278","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