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aceclofenac-induced hepatotoxicity:An ameliorative effect of Terminalia bellirica fruit and ellagic acid

World Journal of Hepatology 2020年第11期12卷 949-964页

作者： Ashutosh Gupta Abhay K Pandey Department of Biochemistry University of AllahabadPrayagraj 211002Uttar PradeshIndia

BACKGROUND aceclofenac(ACF),a widely used nonsteroidal anti-inflammatory drug,has been associated with a number of severe cases of clinical *** bellirica,an evergreen tree,is known to have several ethnomedicinal uses including antioxidant and hepatoprotective *** *** fruit extracts and its phytoconstituent ellagic acid(EA)are expected to provide protection against oxidative stress and liver damage produced by long-term use of *** To evaluate the antioxidant and hepatoprotective activities of *** fruit extracts and EA against ACF-induced toxicity in albino Wistar *** The in vitro antioxidant activities of *** fruit ethyl acetate and aqueous extracts were measured by metal ion chelation and nitric oxide radical scavenging *** in vivo antioxidant and hepatoprotective effects of *** extracts(200 mg/kg)and EA(40 mg/kg)in ACF-induced hepatotoxic rats were assessed in serum and liver tissue after oral administration for 21 ***(40 mg/kg)was used as a standard *** stress markers in the blood(ferric reducing ability of plasma and lipid peroxidation inhibition)and liver tissues(superoxide dismutase,catalase and malondialdehyde)were analyzed using standard *** function markers such as alkaline phosphatase,glutamic pyruvic transaminase,glutamic oxaloacetic transaminase,lactate dehydrogenase,γ-glutamyl transferase,creatinine,total protein,and uric acid were evaluated in rat *** The *** fruit ethyl acetate extract exhibited superior metal ion chelating and nitric oxide radical scavenging abilities during in vitro antioxidant assays as compared to aqueous *** administration of ACF in rats(15 mg/kg)for 21 d produced oxidative stress and adversely affected liver function suggesting liver *** with extracts(ethyl acetate and aqueous),EA and silymarin accounted for a significant reduction in the adverse effects of ACF on oxidative

关键词： Terminalia bellirica Ellagic acid aceclofenac Hepatotoxicity Antioxidant Histopathology

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aceclofenac-Soluplus&reg Nanocomposites for Increased Bioavailability

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Soft Nanoscience Letters 2015年第2期5卷 13-20页

作者： Sandeep Patnaik Sai Kiran Aditha Tanu Rattan Venkataramaniah Kamisetti Department of Physics Sri SathyaSai Institute of Higher Learning Prasanthi Nilayam India

aceclofenac is a new generational Non-Steroidal Anti-Inflammatory Drug (NSAID), and is considered a better alternative to the popular pain-killer diclofenac, as it overcomes some of the adverse gastrointestinal and cardiac side effects associated with the latter. However, the bioavailability of the drug remains limited due to low aqueous solubility (0.058 μg/mL) and poor dissolution characteristics. Hence, improving its dissolution characteristics is of prime significance in order to establish its optimal therapeutic efficacy. In an effort to tackle this issue, we report the use of novel Soluplus®-based nanocomposites, prepared from emulsion templates, as effective drug loading agent for aceclofenac. Nanoemulsion templates were prepared by high-shear homogenization using a probe sonicator. The emulsions were subsequently lyophilized to obtain free flowing powders. The amorphization of the drug with increasing polymer content was clearly observed from powder X-ray diffractogram, while the drug-polymer interaction was explored by FTIR spectroscopy. The phase purity and homogeneity of the formulation was characterized using Differential Scanning Calorimetry. The dissolution profiles of the formulations were established by an USP paddle apparatus. Phase solubility study was conducted to evaluate the effect of polymer concentration on aqueous solubility of aceclofenac. The values of Gibbs-free energy (ΔG°tr) associated with the aqueous solubility of aceclofenac in the presence of Soluplus was used to optimize the polymer content. The in vitro dissolution rates of aceclofenac from the nanoparticles were significantly higher compared to the pure drug. Thus, Soluplus nanoparticles provide promising formulations for the improvement of the dissolution profiles and thus, the bioavailability, of aceclofenac.

关键词： aceclofenac Soluplus Nanocomposites Dissolution Emulsion

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aceclofenac：副作用较少的抗风湿新药

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德国临床用药 1998年第3期1卷 8-8,9页

作者： MarcMaegele 蔡亲福

尽管人们对风湿病的发病机理有新的认识,非甾体抗风湿药仍然是其药物治疗的基础。前不久在德国市场上推出这类新药aceclofenac(Biofenac,UCB),其特点是具有软骨稳定作用,利大于弊。

关键词： aceclofenac 抗风湿药新药

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淀粉微球的制备与均匀设计

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中国医药工业杂志 1997年第9期28卷 22-23页

作者：胡新侯新朴北京医科大学药学院物理化学教研室

淀粉微球的制备与均匀设计ＰＲＥＰＡＲＡＴＩＯＮＯＦＳＴＡＲＣＨＭＩＣＲＯＳＰＨＥＲＥＳＡＮＤＵＮＩＦＯＲＭＤＥＳＩＧＮ胡新侯新朴（北京医科大学药学院物理化学教研室，北京１０００８３）ＨＵＸｉｎ，ＨＯＵＸｉｎｇ－Ｐｕ（... 详细信息

淀粉微球的制备与均匀设计ＰＲＥＰＡＲＡＴＩＯＮＯＦＳＴＡＲＣＨＭＩＣＲＯＳＰＨＥＲＥＳＡＮＤＵＮＩＦＯＲＭＤＥＳＩＧＮ胡新侯新朴（北京医科大学药学院物理化学教研室，北京１０００８３）ＨＵＸｉｎ，ＨＯＵＸｉｎｇ－Ｐｕ（Ｄｅｐｔ．ｏｆＰｈｙｓｉｃａｌＣｈ...

关键词： aceclofenac slow releasing tablets dissolution release kinetics

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Multi-compartmental transdermal patch for simultaneous delivery of multiple drugs:formulation and evaluation of newly developed novel dosage form

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Journal of Coastal Life Medicine 2015年第7期 534-538页

作者： Vijayan Venugopal Jayaraja Kumar Selvadurai Muralidharan P.Vasanth Raj Unit of Pharmaceutical Technology Faculty of PharmacyAIMST UniversityBedong-08100Malaysia

Objective:To evaluate the formulation of multi-compartmental transdermal patches for simultaneous delivery of multiple drugs:aceclofenac and ***:The patch was prepared by simple solvent casting method using hydroxy propyl methyl celluloseK100Mas matrix forming agent and dimethyl sulphoxide as permeation *** prepared transdermal patch was evaluated by physiochemical parameters andin-vitro diffusion ***:The multi-compartmental transdermal patch showed sustained drug release over the period of 12 ***:Multicompartmental transdermal patches shows better bioavailability,therapeutic efficacy and very economic as compared with other dosage forms.

关键词： Multi-compartmental Transdermal patch aceclofenac Serratiopeptidase

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即将在德国上市的新药

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国外新药介绍 1997年第4期 15-16页

作者：蔡亲福

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