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A newly developed and fully validated HPLC method for simultenous determination of in-situ single pass intestinal permeability of domperidone, metoprolol tartarate and phenol red 建立了同时测定多潘立酮、酒石酸美托洛尔和酚红原位单通肠通透性的高效液相色谱方法
IF 0.8 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.29228/jrp.376
Saniye Özcan, E. Çağlar, M. Kaynak, N. Okur
: One of the most popular methods for figuring out a drug’s intestinal permeability is the intestinal perfusion (SPIP) approach. Metoprolol as tartrate and phenol red are frequently utilized as reference compounds in perfusion tests to assess the permeability coefficient of the study’s focus component, Domperidone maleate. Our study’s goal was to create and validate a reversed-phase liquid chromatographic technique for the simultaneous detection of Domperidone maleate, metoprolol, and phenol red for use in intestinal perfusion studies. The analysis was performed on a C18 column 150 × 1.5 mm, 5.0 µm using a mobile phase consisting of methanol: 20 mM potassium dihydrogen phosphate buffer 43:57, v/v ; pH 3.1. The procedure was validated using the FDA’s standards for stability, linearity, precision, and accuracy. All calibration curves were linear r 2 > 0.99. The system suitability parameters of the method are the required limits all analytes. The in situ intestinal permeability experiments can easily be standardized with the help of this newly created and proven approach.
肠灌注法(SPIP)是测定药物肠通透性最常用的方法之一。美托洛尔作为酒石酸盐和酚红经常被用作灌注试验的参比化合物,以评估本研究的重点成分马来酸多潘立酮的渗透系数。本研究的目的是建立并验证一种同时检测马来酸多潘立酮、美托洛尔和酚红的反相液相色谱技术,用于肠道灌注研究。色谱柱为C18,色谱柱为150 × 1.5 mm, 5.0µm,流动相为甲醇:20 mm磷酸二氢钾缓冲液43:57,v/v;pH值3.1。该方法使用FDA的稳定性、线性度、精密度和准确度标准进行验证。所有的校准曲线均为线性r 2 bb0 0.99。该方法的系统适宜性参数是所有分析物的要求限值。在这种新方法的帮助下,原位肠通透性实验可以很容易地标准化。
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引用次数: 0
THE ROLE OF METABOLOMICS IN MEDICINAL PLANT SCIENCE 代谢组学在药用植物科学中的作用
IF 0.8 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.29228/jrp.380
E. Nemutlu
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引用次数: 0
Diffusion and Lipolysis Test on Forskolin Microemulsion Gel 福斯克林微乳凝胶的扩散及脂解试验
IF 0.8 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.29228/jrp.431
Rahma NAFI’AH, Y. Sumirtapura, S. T. Darijanto, M. Iwo
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引用次数: 0
Definition and prevalence over the years of polypharmacy in Turkey: A systematic review 定义和流行多年的多种药房在土耳其:一个系统的回顾
IF 0.8 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.29228/jrp.434
Cansu Goncuoglu, Nesligul Ozdemir, Emre Kara, Aygin Bayraktarekincioglu
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引用次数: 0
Chemometrics-assisted UV-spectroscopy for simultaneous determination of curcumin and piperine in solid dispersion-based microparticles containing Curcuma longa and Piper nigrum extracts 化学计量学辅助紫外光谱法同时测定含有姜黄和黑椒提取物的固体分散微颗粒中的姜黄素和胡椒碱
IF 0.8 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.29228/jrp.423
Dewi Setyaningsih, Y. Hartini, D. Notario
: Piperine and curcumin can be combined in a mixture as piperine has been known as a bioenhancer. The piperine-curcumin combination was formulated in a solid dispersion-based microparticle containing Piper nigrum and Curcuma longa extracts. The aim of the study was to simultaneously determine piperine and curcumin concentrations in a combined dosage form of solid dispersion-based microparticles using UV-Vis spectrophotometry. A UV-Vis spectrophotometry was combined with a partial least square (PLS) approach with a central composite design (CCD) to develop a calibration series consisting of 36 standard mixtures of piperine and curcumin at concentrations ranging from 0 to 6 g/mL. The model of the calibration series was validated for determination coefficient ( R 2 ), root means square of error prediction/cross-validation (RMSEP/RMSECV) dan predicted residual sum of square (PRESS). Accuracy and precision were determined as per ICH guidelines. The PLS model was successfully validated and applied for resolving overlaid spectra of piperine and curcumin at 206 – 408 nm. Accuracy and precision studies of prepared samples containing a mixture of piperine and curcumin at low, medium, and high concentrations conducted on different days were met with the AOAC International requirements. The limit of detection (LOD) was determined using a pseudo-variates model, and the limit was found to be 0.25 µ g/mL and 0.33 µ g/mL for piperine and curcumin, respectively. The proposed method is suitable for simultaneously determining piperine and curcumin that appeared in a mixture of P. nigrum and C. longa extracts in the solid dispersion-based microparticle samples.
胡椒碱和姜黄素可以混合在一起,因为胡椒碱是一种生物增强剂。将胡椒-姜黄素组合制成含有胡椒和姜黄提取物的固体分散微颗粒。本研究的目的是利用紫外可见分光光度法同时测定基于固体分散的微颗粒中胡椒碱和姜黄素的组合剂型。采用紫外-可见分光光度法结合偏最小二乘(PLS)方法和中心复合设计(CCD),建立了由36种胡椒碱和姜黄素标准混合物组成的校准系列,浓度范围为0至6 g/mL。对校准系列模型进行决定系数(r2)、误差预测均方根/交叉验证(RMSEP/RMSECV)和预测残差平方和(PRESS)的验证。准确度和精密度根据ICH指南确定。验证了PLS模型的有效性,并将其应用于辣椒碱和姜黄素在206 ~ 408 nm的重叠光谱中。对低、中、高浓度胡椒碱和姜黄素混合物制备的样品在不同日期进行的准确度和精密度研究均符合AOAC国际要求。采用伪变量模型确定了辣椒碱和姜黄素的检出限(LOD),检出限分别为0.25µg/mL和0.33µg/mL。该方法适用于同时测定固体分散微颗粒样品中黑姜和龙骨提取物混合物中的胡椒碱和姜黄素。
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引用次数: 0
Determination of Vitamin D3 Loaded Selfnanoemulsifying Drug Delivery Systems (SNEDDS) Based Hydrogel 基于水凝胶的维生素D3自纳米乳化给药系统(SNEDDS)的测定
IF 0.8 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.29228/jrp.410
Adeltrudis Adelsa DANIMAYOSTU, E. Lukitaningsih, R. Martien, Retno Danarti
: High Performance Liquid Chromatography (HPLC) was used to determine vitamin D3 content from the topical dosage form. Self-nanoemulsifying drug delivery systems (SNEDDS) based hydrogel was aimed to optimize the delivery of vitamin D3 through the skin due to its high lipophilicity. Quantifying vitamin D3 was performed using the internal standard, vitamin D2, on LiChrocart C18 125-4 reverse phase column. Several characteristics of validation were referred including specificity, linearity, range, accuracy, precision, limits of detection, and quantification. The mobile phase was optimized as a mixture of acetonitrile-methanol-water for injection 94:3:3 v/v, and the flow rate was optimized at 0.8 mL/min at 25°C. Vitamin D3 detection and quantification were observed at a wavelength of 266 nm using an ultra-violet (UV) detector. The analysis method performed no excipient interference, including separating vitamin D3 from its matrix. Extraction of vitamin D3 from its matrix was observed using the dialysis membrane, with agitation (vortex) and no agitation (immersion). The drug content determination was found to be 108.22 % ± 14.77% for the immersion method and 72.04% ± 33.37% for the vortex method. Further, the high variability of the results indicated the dialysis membrane was not a suitable method for determining lipophilic drug content from the colloidal polymer matrix. The other techniques with negligible variation, such as reverse dialysis or subsequent solvent addition, are preferred.
采用高效液相色谱法测定外用剂型中维生素D3的含量。基于水凝胶的自纳米乳化药物递送系统(SNEDDS)旨在优化维生素D3通过皮肤的递送,因为它具有高亲脂性。采用内标维生素D2,在LiChrocart C18 125-4反相柱上定量。包括特异性、线性度、范围、准确度、精密度、检出限和定量在内的几个验证特性被提及。流动相优化为乙腈-甲醇-注射用水94:3:3 v/v,流速优化为0.8 mL/min,温度25℃。采用紫外(UV)检测器在266 nm波长下对维生素D3进行检测和定量。该分析方法无辅料干扰,包括将维生素D3从基质中分离出来。用透析膜从基质中提取维生素D3,有搅拌(涡流)和无搅拌(浸泡)。浸渍法和涡流法分别为108.22%±14.77%和72.04%±33.37%。此外,结果的高度可变性表明透析膜不是测定胶体聚合物基质中亲脂性药物含量的合适方法。其他变化可忽略不计的技术,如反透析或随后的溶剂添加,是优选的。
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引用次数: 0
The in vivo Activity of Fraxinus angustifolia in Pain and Inflammation- Examination of the Biological Activities of the Sub-extracts in Mice 黄曲霉抗疼痛和抗炎症的体内活性——亚提取物在小鼠体内的生物活性研究
IF 0.8 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.29228/jrp.414
Yeşim Kaya Yaşar, S. Sevgi, Gülin Renda, İrem Çavuşoğlu Nalbantoğlu, M. Duman, Feride Sena Sezen
: Fraxinus species (Oleaceae) are commonly used in the treatment of several inflammatory conditions with pain, such as rheumatism, arthritis, and gout in folk medicine. We aimed to evaluate this ethnobotanical claim through in vivo experiments. The n-hexane, dichloromethane, ethyl acetate and water subextracts were obtained from the methanolic extract, which was prepared from the bark of Fraxinus angustifolia Vahl. The antinociceptive and anti-inflammatory activities of extracts were evaluated in mice by hot plate and formalin-induced edema assays, respectively. Mice were treated with 5-100 mg/kg methanol crude extract and 100 mg/kg subextracts intraperitoneally. Administration of methanol extract decreased paw thickness in doses of 25 and 100 mg/kg. Water and ethyl acetate subextracts decreased paw thickness while water subextract also decreased paw volume compared with the control. Paw thickness values in the dichloromethane and n-hexane subextract groups and paw volume values in the ethyl acetate, dichloromethane, and n-hexane subextract groups were comparable to those in the control group. The latency values were higher in the groups treated with the dichloromethane and n-hexane subextracts than in the control group while the other subextracts did not change the latency values compared to the control group in the hot plate test. In conclusion, the cortex of Fraxinus angustifolia exhibited a significant in vivo anti-inflammatory and antinociceptive activity.
:曲霉属(油棕科)常用于治疗几种炎症性疼痛,如风湿病、关节炎和痛风等民间医学。我们的目的是通过体内实验来评估这一民族植物学主张。以白蜡树皮为原料制备甲醇提取物,得到正己烷、二氯甲烷、乙酸乙酯和水亚提取物。采用热板法和福尔马林致水肿法分别评价提取物的抗炎活性和抗炎活性。小鼠腹腔注射5 ~ 100 mg/kg甲醇粗提物和100 mg/kg甲醇亚提物。25和100 mg/kg剂量的甲醇提取物可降低脚爪厚度。水提物和乙酸乙酯提物均能降低足跖厚度,而水提物也能降低足跖体积。二氯甲烷和正己烷亚提取物组的脚爪厚度值和乙酸乙酯、二氯甲烷和正己烷亚提取物组的脚爪体积值与对照组相当。热板试验中,二氯甲烷和正己烷亚提取物处理组的潜伏期值高于对照组,而其他亚提取物处理组的潜伏期值与对照组相比没有变化。综上所述,白蜡叶皮层具有明显的体内抗炎和抗伤活性。
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引用次数: 0
DISCOVERY OF NOVEL HCV NS5B POLYMERASE INHIBITORS BY IN SILICO APPROACHES 用计算机方法发现新型HCV ns5b聚合酶抑制剂
IF 0.8 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.29228/jrp.456
Berin Karaman Mayack
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引用次数: 0
Effect of riboflavin on rat bladder contractility and oxidant damage following ischemia/reperfusion 核黄素对大鼠缺血再灌注后膀胱收缩性及氧化损伤的影响
IF 0.8 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.29228/jrp.468
Büşra Ertaş
: Ischemia/reperfusion (IR) encompasses the processes of organ function damage and oxidative injury depending on the successive blood flow obstruction and removal of the obstruction. Known as a vitamin, riboflavin (Rb) is known to be protective against tissue damage with its antioxidant and anti-inflammatory properties. The aim of this study is to investigate the effect of Rb treatment on bladder contraction dysfunction and tissue damage due to IR. The study was conducted with forty Sprague-Dawley rats. The abdominal aorta of anaesthetized rats was occluded to induce ischemia (60 min) and then allowed reperfusion (60 min). Rb (25 mg/kg), n-acetylcysteine NAC (100 mg/kg) or saline was administered orally 15 min before the IR model immediately. The bladder was assessed by biochemical and histological analysis, and the contractility of the I/R-related bladder was detected by organ bath. Compared to the control group, MDA, MPO and caspase-3 activities increased in the IR group, while GSH levels decreased. MDA, GSH and caspase-3 activities were reversed with Rb treatment, but there was no change in MPO level. Healing of IR-induced edema and oxidant damage with Rb and NAC treatment resulted in improvement of the thinning of the bladder wall. According to these results, it can be said that Rb therapy can regulate IR-induced bladder dysfunction by improving antioxidant properties and tissue damage.
缺血/再灌注(IR)包括器官功能损伤和氧化损伤的过程,这取决于连续的血流阻塞和阻塞的清除。作为一种维生素,核黄素(Rb)具有抗氧化和抗炎的特性,可以防止组织损伤。本研究的目的是探讨Rb治疗对膀胱收缩功能障碍和IR引起的组织损伤的影响。这项研究是用40只Sprague-Dawley大鼠进行的。麻醉大鼠腹主动脉闭塞致缺血(60 min),再灌注(60 min)。IR模型建立前15分钟立即口服Rb (25 mg/kg)、n-乙酰半胱氨酸NAC (100 mg/kg)或生理盐水。通过生化和组织学分析评估膀胱,并通过器官浴检测I/ r相关膀胱的收缩性。与对照组相比,IR组MDA、MPO和caspase-3活性升高,GSH水平降低。MDA、GSH和caspase-3活性随Rb处理而逆转,但MPO水平无变化。Rb和NAC治疗ir诱导的水肿和氧化损伤后,膀胱壁变薄的情况得到改善。根据这些结果,Rb治疗可以通过改善抗氧化性能和组织损伤来调节ir诱导的膀胱功能障碍。
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引用次数: 0
A NEW APPROACH IN DRUG DISCOVERY: NETWORK PHARMACOLOGY 药物发现的新途径:网络药理学
IF 0.8 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.29228/jrp.454
Neziha Yagmur DİKER, Vahap Murat Kutluay
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引用次数: 0
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Journal of Research in Pharmacy
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