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DEVELOPMENT AND VALIDATION OF A SIMPLE AND COST-EFFECTIVE UV SPECTROPHOTOMETRIC METHOD FOR QUANTIFYING LINEZOLID 开发并验证一种简单、经济的紫外分光光度法定量利奈唑胺
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50556
Iti Chauhan, Lubhan Singh
Objective: This study focuses on the development and validation of a sensitive, simple, accurate, precise and cost-effective Ultraviolet-Visible (UV) spectrophotometric method for the quantification of Linezolid, a widely used antibiotic in pharmaceutical formulations.Methods: The analysis utilized a solvent system comprising 80% water and 20% methanol (v/v). The absorbance of standard solutions was measured and a calibration curve was constructed. Various analytical performance parameters, including linearity, range, precision, accuracy, Limit of Detection (LOD), Limit of Quantification (LOQ) and ruggedness, were determined following the International Conference on Harmonization (ICH) Q2 (R1) guidelines.Results: The maximum absorption peak (λmax) of Linezolid was determined to be 251 nm in the selected medium. Beer-Lambert’s law was valid in the concentration range of 0.5–9 μg/ml, with a high correlation coefficient (R2) of 0.9955. The proposed method exhibited a recovery ranging from 99.08 to 100.37% with % Relative Standard Deviation (RSD) value consistently below 2%.Conclusion: The study findings confirm the accuracy, precision and reproducibility of the developed method. Additionally, it is characterized by its simplicity, affordability, and time efficiency. Thus, this method can be effectively employed for the quantification of Linezolid in lipid nanoparticles.
研究目的本研究的重点是开发和验证一种灵敏、简单、准确、精确且经济高效的紫外分光光度法,用于定量检测药物制剂中广泛使用的抗生素利奈唑胺:分析采用的溶剂系统为 80% 的水和 20% 的甲醇(v/v)。测量标准溶液的吸光度并构建校准曲线。根据国际协调会议(ICH)Q2 (R1)指南确定了各种分析性能参数,包括线性、范围、精密度、准确度、检测限(LOD)、定量限(LOQ)和耐用性:结果:在所选培养基中,利奈唑胺的最大吸收峰 (λmax) 被确定为 251 nm。比尔-朗伯定律在 0.5-9 μg/ml 浓度范围内有效,相关系数 (R2) 为 0.9955。该方法的回收率为 99.08% 至 100.37%,相对标准偏差(RSD)始终低于 2%:研究结果证实了所开发方法的准确性、精确性和可重复性。此外,该方法还具有简便、经济、省时的特点。因此,该方法可有效地用于脂质纳米颗粒中利奈唑胺的定量分析。
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引用次数: 0
MOLECULAR DOCKING DYNAMICS OF SELECTED BENZYLIDENE AMINO PHENYL ACETAMIDES AS TMK INHIBITORS USING HIGH THROUGHPUT VIRTUAL SCREENING (HTVS) 利用高通量虚拟筛选(HTVS)对作为 TMK 抑制剂的精选苯亚氨基苯基乙酰胺进行分子对接动力学研究
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50023
Koppula Jayanthi, Syed Suhaib Ahmed, Mohd Abdul Baqi, Mohammed AFZAL AZAM
Objective: Thymidylate kinase (TMK) plays a crucial role in bacterial DNA synthesis by catalyzing the phosphorylation of deoxythymidine monophosphate (dTMP) to form deoxythymidine diphosphate (dTDP). Consequently, this enzyme emerges as a promising target for developing novel antibacterial drugs. However, no antibiotics were reported for this target, especially active against Staphylococcus aureus thymidylate kinase.Methods: Benzylidene acetamide-based ligands were examined for their potency using the in silico method. These novel ligand structures were built using ChemDraw software. The protein was retrieved from the Research Collaboratory for Structural Bioinformatics Protein Data Bank (RCSB PDB) website. The molecular docking and binding free energy calculation by prime Molecular Mechanics in Generalized Bond Surface Area (MM-GBSA) was performed for selected ligands. A 100 ns molecular dynamic simulation was also performed to assess the stability of the potential ligand as TMK inhibitors.Results: All ten molecules have shown good glide scores and hydrophobic and hydrogen hydrophobic hydrogen bonding interactions with Arg48, Arg36, and π-π stacking Phe66 in the TMK enzyme (PDB: 4HLC). Among them, N-(2-ethylphenyl)-2-(4-((4-nitrobenzylidene) amino) phenoxy) acetamide molecule had high XP-docking scores of-3.27 kcal/mol based on extra-precision data. Prime Molecular Mechanics in Generalized Bond Surface Area study (MM-GBSA) studies also showed promising binding affinities that are ΔBind (-65.80), ΔLipo (-28.55), and ΔVdW (-55.10). Phe66 amino acid residue maintained continuous connections with the ligand during MD simulation. This ligand showed promising binding affinity with the SaTMK target.Conclusion: The N-(2-ethylphenyl)-2-(4-((4-nitrobenzylidene) amino) phenoxy) acetamide ligand at the position of the benzene ring displayed nitrogen and oxygen group, thus indicating good potential activity as the inhibitor of TMK to treat antibacterial agents.
目的:胸苷酸激酶(TMK)通过催化单磷酸脱氧胸苷(dTMP)的磷酸化形成二磷酸脱氧胸苷(dTDP),在细菌的 DNA 合成过程中发挥着至关重要的作用。因此,这种酶成为开发新型抗菌药物的一个很有前景的靶点。然而,目前还没有报道针对这一靶点的抗生素,尤其是对金黄色葡萄球菌胸苷酸激酶有活性的抗生素:方法:采用硅学方法研究了苯亚乙酰胺配体的效力。这些新型配体结构是用 ChemDraw 软件构建的。蛋白质是从结构生物信息学研究合作组织蛋白质数据库(RCSB PDB)网站上获取的。通过广义键面面积分子力学(MM-GBSA)对选定配体进行了分子对接和结合自由能计算。此外,还进行了 100 ns 的分子动力学模拟,以评估潜在配体作为 TMK 抑制剂的稳定性:结果:所有十种分子都显示出良好的滑行得分以及与 TMK 酶(PDB:4HLC)中 Arg48、Arg36 和 π-π 堆积 Phe66 的疏水和氢疏水氢键相互作用。其中,N-(2-乙基苯基)-2-(4-((4-硝基亚苄基)氨基)苯氧基)乙酰胺分子的XP-对接得分较高,根据额外精度数据为3.27 kcal/mol。广义键表面积分子力学研究(MM-GBSA)也显示出良好的结合亲和力,分别为ΔBind(-65.80)、ΔLipo(-28.55)和ΔVdW(-55.10)。在 MD 模拟过程中,Phe66 氨基酸残基与配体保持连续连接。该配体与 SaTMK 靶点的结合亲和力良好:N-(2-乙基苯基)-2-(4-((4-硝基亚苄基)氨基)苯氧基)乙酰胺配体在苯环的位置上显示出氮基和氧基,因此表明其作为 TMK 抑制剂治疗抗菌剂具有良好的潜在活性。
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引用次数: 0
REVITALIZING THERAPEUTICS: DRUG REPURPOSING AS A COST-EFFECTIVE STRATEGY FOR DRUG DEVELOPMENT 振兴疗法:药物再利用作为一种具有成本效益的药物开发战略
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.49581
Shivani Makhijani
The process of developing new drugs is known for being drawn-out, expensive, risky, and having a high attrition rate. Drug repurposing has grown in favor recently as a practical way to speed up the development of new medicines while reducing the costs and time constraints associated with traditional drug research. The description of this study's pharmacological repurposing highlights its promise as a practical method to fill gaps in the market and revitalize treatment options. This review provides a full analysis of the ground-breaking tactic of repurposing medications, supported by numerous cases that demonstrate its revolutionary potential. We examine instances of repurposed drugs, such as thalidomide, sildenafil, and metformin, that have performed astoundingly well in a range of therapeutic settings despite being used outside of their original scope.Overall, the paper's main goal-to study pharmacological repurposing as a potentially successful strategy for revitalizing treatments-is, succinctly summarized in this abstract. It highlights the potential benefits of this approach and how it might be used in the pharmaceutical industry's ongoing quest for more inexpensive and effective medicine development.
众所周知,新药研发过程耗时长、成本高、风险大、损耗率高。近来,药物再利用作为一种既能加快新药开发,又能减少传统药物研究成本和时间限制的实用方法,越来越受到人们的青睐。本研究对药物再利用的描述突出了其作为填补市场空白和振兴治疗方案的实用方法的前景。本综述全面分析了药物再利用这一突破性策略,并通过大量案例证明了其革命性潜力。我们研究了沙利度胺、西地那非和二甲双胍等再利用药物的实例,尽管这些药物的使用超出了其原有的范围,但它们在一系列治疗环境中的表现却令人震惊。总之,本文的主要目标--研究药物再利用作为振兴疗法的潜在成功策略--在本摘要中得到了简明扼要的概括。总之,本摘要简明扼要地概括了论文的主要目标--研究药理再利用作为振兴治疗方法的潜在成功策略,强调了这种方法的潜在益处,以及如何将其用于制药业正在进行的寻求更廉价、更有效药物的开发过程中。
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引用次数: 0
FORMULATION DEVELOPMENT AND IN VITRO PENETRATION TEST OF ETHOSOME OF CHROMOLAENA ODORATA LEAVES EXTRACT 香叶乙素的配方开发和体外渗透试验
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.49856
Sofia Rahmi, Julia Reveny, Anayanti Arianto, P. Sitorus
Objective: This study aimed to develop and assess ethosome preparation using extracts derived from the leaves of Chromolaena odorata.Methods: The study started by obtaining Chromolaena odorata leaf extracts. Furthermore, Ethosome formulations were produced using a thermal technique. Ethosome variants were created, each with distinct compositions: Formulation F1, containing 10 ml of ethanol without the extract; Formulation F2, consisting of 0.5 grams of the extract mixed with 10 ml of ethanol; Formulation F3, combining 1 gram of the extract with 20 ml of ethanol; and Formulation F4, incorporating 1.5 grams of the extract with 30 ml of ethanol. The ethosomal systems were thoroughly characterized using various analytical techniques, such as organoleptic analysis, quantification of particle dimensions, zeta potential evaluation, pH metric analysis, transmission electron microscopy (TEM) imaging, and in vitro permeability assessment using the Franz Diffusion Cell apparatus.Results: The findings indicated that the optimized F4 formulation showed 161.2±32.0 nm particle size measurement and a+34.33±0.58 mV zeta potential. All formula possess a pH range of 4.5-6.5, within which the skin can acclimate to preparations. It is evident from all formulations that the pH decreased after the addition of the extract at an acidic pH of 4.11. Following the 12-week storage period, the pH of all treatments exhibited a modest reduction; however, it remained within the acceptable range for skin pH. Furthermore, the F4 formula also had a higher level of penetration activity.Conclusion: The optimized ethosomal formulations of Chromolaena odorata have promising applications in enhancing the permeability and efficacy of plant-derived therapeutic agents.
目的:本研究旨在开发和评估乙素体制剂:本研究旨在开发和评估使用从 Chromolaena odorata 叶子中提取的提取物制备的乙素体:方法:本研究首先获得了 Chromolaena odorata 的叶片提取物。此外,还利用热技术制备了 Ethosome 配方。乙素体变体被制作出来,每种变体都有不同的成分:配方 F1,含 10 毫升乙醇,不含提取物;配方 F2,0.5 克提取物与 10 毫升乙醇混合;配方 F3,1 克提取物与 20 毫升乙醇混合;配方 F4,1.5 克提取物与 30 毫升乙醇混合。利用各种分析技术,如感官分析、颗粒尺寸定量、ZETA电位评估、pH值度量分析、透射电子显微镜(TEM)成像以及使用弗朗兹扩散池仪器进行体外渗透性评估,对乙撑体系统进行了全面的表征:结果表明,优化的 F4 配方的粒度测量值为 161.2±32.0 nm,zeta 电位为+34.33±0.58 mV。所有配方的 pH 值范围均为 4.5-6.5,皮肤可在此范围内适应制剂。从所有配方中可以明显看出,在添加提取物后,pH 值下降到 4.11 的酸性 pH 值。储存 12 周后,所有配方的 pH 值都略有下降,但仍在皮肤 pH 值可接受的范围内。此外,F4 配方的渗透活性也更高:优化后的香茅乙素体配方在提高植物提取治疗剂的渗透性和疗效方面具有广阔的应用前景。
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引用次数: 0
DESIGN, DEVELOPMENT AND IMPROVEMENT OF AN EMULGEL CONTAINING SILVER NANOPARTICLES AND VITAMIN D-3 FOR ITS POTENTIAL TO ACCELERATE THE HEALING OF WOUND 设计、开发和改进含银纳米粒子和维生素 d-3 的凝胶,以提高其加速伤口愈合的潜力
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50344
Rishu Yadav, Narendra Kumar Pandey, Rajiv Kukkar
Objective: The aim of this research work was to prepare a topical emulgel based dosage form incorporated with vitamin D-3 and silver nanoparticles to reduce the wound healing time in any kind of wound.Methods: Central Composite Design (CCD) was applied for the optimization of emulgel by using Design expert software. Three responses (pH, viscosity, and in vitro drug release) and two factors (Carbopol concentration and stirring duration) were chosen, and Statistical Analysis of Variance (ANOVA) revealed that all the factors were significantly affecting the responses. Silver Nanoparticles (SNPs) was prepared with Green Tea Extract (GTE) and evaluated for particle size, Poly Dispersity Index (PDI), zeta potential and Fourier Transform Infra-red (FTIR) spectroscopy and revealed that SNPs of desired range and stability have been synthesized. Here excision wound model was used to evaluate the wound healing activity of formulation in vivo.Results: Maximum in vitro release 88.2±2.1 has shown by the optimized formulation F13, pH and viscosity were also found in optimum range i.e., 6.2±0.4 and 1672±33 respectively, followed by Korsmeyer and Peppas model. Total eight groups were designed for animal study and silver sulphadiazine was used as marketed formulation. F13 formulation was further evaluated for in vivo data, it was revealed that emulgel loaded with high dose of vitamin D-3 along with silver nanoparticles has shown 100.5±1.7% wound contraction, while marketed formulation has shown 103.7±1.1% wound contraction, which was much similar with test formulation. Cytotoxic cell study was done using assay on chicken egg, formulation has not shown any cytotoxic behaviour like haemolysis and cell damage on chick embryo’s blood vessels. Accelerated stability study of the optimized formulation was also performed to check whether the formulation was stable or not and it was revealed that optimized formulation was found stable for the period of six months.Conclusion: It was revealed that emulgel loaded with high dose of vitamin D-3 and SNPs found suitable to accelerate wound healing and showed almost similar response in wound contraction on comparison with marketed formulation. This emulgel promised to controlled the delivery of the drug for the longer duration.
研究目的本研究工作旨在制备一种含有维生素 D-3 和纳米银颗粒的外用乳胶剂型,以缩短各种伤口的愈合时间:方法:利用 Design expert 软件,采用中央复合设计(CCD)对润肤凝胶进行优化。选择了三个响应(pH 值、粘度和体外药物释放)和两个因素(Carbopol 浓度和搅拌持续时间),统计方差分析(ANOVA)显示,所有因素都对响应有显著影响。用绿茶提取物(GTE)制备了银纳米颗粒(SNPs),并对其粒度、聚分散指数(PDI)、ZETA电位和傅立叶变换红外光谱(FTIR)进行了评估,结果表明合成的 SNPs 具有所需的范围和稳定性。在此,使用切除伤口模型来评估制剂在体内的伤口愈合活性:结果:优化配方 F13 的体外最大释放量为 88.2±2.1,pH 值和粘度也在最佳范围内,分别为 6.2±0.4 和 1672±33,其次是 Korsmeyer 和 Peppas 模型。共设计了八组动物实验,磺胺嘧啶银被用作市场上的制剂。对 F13 制剂进行了进一步的体内数据评估,结果显示,含有高剂量维生素 D-3 和银纳米粒子的凝胶显示出 100.5±1.7% 的伤口收缩率,而市售制剂显示出 103.7±1.1% 的伤口收缩率,与试验制剂非常相似。细胞毒性研究是在鸡卵上进行的,配方没有显示出任何细胞毒性行为,如溶血和对鸡胚血管的细胞损伤。此外,还对优化配方进行了加速稳定性研究,以检查配方是否稳定,结果表明优化配方在 6 个月内保持稳定:结论:研究发现,含有高剂量维生素 D-3 和 SNP 的凝胶适合加速伤口愈合,与市场上销售的配方相比,它在伤口收缩方面表现出几乎相似的反应。这种凝胶有望在更长的时间内控制药物的输送。
{"title":"DESIGN, DEVELOPMENT AND IMPROVEMENT OF AN EMULGEL CONTAINING SILVER NANOPARTICLES AND VITAMIN D-3 FOR ITS POTENTIAL TO ACCELERATE THE HEALING OF WOUND","authors":"Rishu Yadav, Narendra Kumar Pandey, Rajiv Kukkar","doi":"10.22159/ijap.2024v16i3.50344","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50344","url":null,"abstract":"Objective: The aim of this research work was to prepare a topical emulgel based dosage form incorporated with vitamin D-3 and silver nanoparticles to reduce the wound healing time in any kind of wound.\u0000Methods: Central Composite Design (CCD) was applied for the optimization of emulgel by using Design expert software. Three responses (pH, viscosity, and in vitro drug release) and two factors (Carbopol concentration and stirring duration) were chosen, and Statistical Analysis of Variance (ANOVA) revealed that all the factors were significantly affecting the responses. Silver Nanoparticles (SNPs) was prepared with Green Tea Extract (GTE) and evaluated for particle size, Poly Dispersity Index (PDI), zeta potential and Fourier Transform Infra-red (FTIR) spectroscopy and revealed that SNPs of desired range and stability have been synthesized. Here excision wound model was used to evaluate the wound healing activity of formulation in vivo.\u0000Results: Maximum in vitro release 88.2±2.1 has shown by the optimized formulation F13, pH and viscosity were also found in optimum range i.e., 6.2±0.4 and 1672±33 respectively, followed by Korsmeyer and Peppas model. Total eight groups were designed for animal study and silver sulphadiazine was used as marketed formulation. F13 formulation was further evaluated for in vivo data, it was revealed that emulgel loaded with high dose of vitamin D-3 along with silver nanoparticles has shown 100.5±1.7% wound contraction, while marketed formulation has shown 103.7±1.1% wound contraction, which was much similar with test formulation. Cytotoxic cell study was done using assay on chicken egg, formulation has not shown any cytotoxic behaviour like haemolysis and cell damage on chick embryo’s blood vessels. Accelerated stability study of the optimized formulation was also performed to check whether the formulation was stable or not and it was revealed that optimized formulation was found stable for the period of six months.\u0000Conclusion: It was revealed that emulgel loaded with high dose of vitamin D-3 and SNPs found suitable to accelerate wound healing and showed almost similar response in wound contraction on comparison with marketed formulation. This emulgel promised to controlled the delivery of the drug for the longer duration.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"24 31","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141004850","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: 0
RP-HPLC METHOD DEVELOPMENT AND VALIDATION FOR SIMULTANEOUS ESTIMATION OF CURCUMIN AND RESVERATROL IN NANO-MICELLE: DUAL DRUG DUAL FORM SIMULTANEOUS ESTIMATION 同时估算纳米胶束中姜黄素和白藜芦醇的 rp-hplc 方法开发与验证:双药双态同时估算
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50276
SK Mosiur Rahaman, Atanu Chandra, Ranu Biswas
Objective: To develop a reverse-phase high-performance liquid chromatography (RP-HPLC) method for simultaneous estimation of conjugated form of Curcumin (CCMN) and free form of Resveratrol (RSV) in nano-micelle.Methods: The conjugation of lipophilic CCMN and hydrophilic Chitosan (CHT) through succinyl linker produce amphipathic molecule that can self-assemble into RSV solution to form micelle. Here RSV exists in micelle core as free form and CCMN with micelle backbone as conjugated form. So it required to estimate conjugated drug and free drug simultaneously from nano-micelle. We developed a RP-HPLC method, utilized C18 column, follow flow rate of mobile phase 1.0 ml/min, which consist of acetonitrile with water (0.5% Ortho Phosphoric acid, pH 4.6) in the ratio of 1:1 for 20 min. Injection volume was 10μl and column temperature 25 ℃. Isosbestic detection of both drugs was at 254 nm.Results: The retention time of RSV and CCMN were at 8.15 min and 11.41 min respectively, completely distinguished sharp peak of CCMN and RSV developed with resolution 7.360±0.117, wide range of linearity with correlation coefficient value (R2) of CCMN and RSV were 0.99987 and 0.99992 respectively and recovery value of CCMN and RSV were 100.041±0.22 % and 100.041±0.21 % respectively. The RSD (relative standard deviation) for accuracy, precision and robustness of the method was found to be less than 2%.Conclusion: The develop method for simultaneous estimation of conjugated CCMN and free form of RSV in the nano-micelle formulation was consider to be accurate, precise, robust and sensitive.
目的建立一种反相高效液相色谱(RP-HPLC)方法,用于同时测定纳米胶束中的共轭型姜黄素(CCMN)和游离型白藜芦醇(RSV):方法:亲油型 CCMN 与亲水性壳聚糖(CHT)通过琥珀酰基连接体共轭,产生两亲分子,可自组装到 RSV 溶液中形成胶束。在这里,RSV 以游离形式存在于胶束核心,而 CCMN 与胶束骨架以共轭形式存在。因此,需要同时估算纳米胶束中的共轭药物和游离药物。我们开发了一种 RP-HPLC 方法,采用 C18 色谱柱,流动相流速为 1.0 ml/min,乙腈与水(0.5% 正磷酸,pH 4.6)的比例为 1:1,流动时间为 20 分钟。进样量为 10 微升,柱温为 25 ℃。两种药物的等光检测波长为 254 nm:RSV和CCMN的保留时间分别为8.15 min和11.41 min;CCMN和RSV的峰形完全不同,分辨率为7.360±0.117;线性范围宽,CCMN和RSV的相关系数(R2)分别为0.99987和0.99992;CCMN和RSV的回收率分别为100.041±0.22 %和100.041±0.21 %。方法的准确度、精密度和稳健性的 RSD(相对标准偏差)均小于 2%:该方法准确、精密、稳健、灵敏,适用于纳米微囊制剂中共轭CCMN和游离型RSV的同时测定。
{"title":"RP-HPLC METHOD DEVELOPMENT AND VALIDATION FOR SIMULTANEOUS ESTIMATION OF CURCUMIN AND RESVERATROL IN NANO-MICELLE: DUAL DRUG DUAL FORM SIMULTANEOUS ESTIMATION","authors":"SK Mosiur Rahaman, Atanu Chandra, Ranu Biswas","doi":"10.22159/ijap.2024v16i3.50276","DOIUrl":"https://doi.org/10.22159/ijap.2024v16i3.50276","url":null,"abstract":"Objective: To develop a reverse-phase high-performance liquid chromatography (RP-HPLC) method for simultaneous estimation of conjugated form of Curcumin (CCMN) and free form of Resveratrol (RSV) in nano-micelle.\u0000Methods: The conjugation of lipophilic CCMN and hydrophilic Chitosan (CHT) through succinyl linker produce amphipathic molecule that can self-assemble into RSV solution to form micelle. Here RSV exists in micelle core as free form and CCMN with micelle backbone as conjugated form. So it required to estimate conjugated drug and free drug simultaneously from nano-micelle. We developed a RP-HPLC method, utilized C18 column, follow flow rate of mobile phase 1.0 ml/min, which consist of acetonitrile with water (0.5% Ortho Phosphoric acid, pH 4.6) in the ratio of 1:1 for 20 min. Injection volume was 10μl and column temperature 25 ℃. Isosbestic detection of both drugs was at 254 nm.\u0000Results: The retention time of RSV and CCMN were at 8.15 min and 11.41 min respectively, completely distinguished sharp peak of CCMN and RSV developed with resolution 7.360±0.117, wide range of linearity with correlation coefficient value (R2) of CCMN and RSV were 0.99987 and 0.99992 respectively and recovery value of CCMN and RSV were 100.041±0.22 % and 100.041±0.21 % respectively. The RSD (relative standard deviation) for accuracy, precision and robustness of the method was found to be less than 2%.\u0000Conclusion: The develop method for simultaneous estimation of conjugated CCMN and free form of RSV in the nano-micelle formulation was consider to be accurate, precise, robust and sensitive.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"87 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141002257","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: 0
DEVELOPMENT OF MYCROCRYSTALLINE CELLULOSE ORIGINATE FROM SAGO (METROXYLON SAGU) STEM BARK BY HYDROLISIS METHODE USING NITRIC ACID 用硝酸水解法开发西米茎皮中的霉晶纤维素
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.49622
Nur Illiyyin Akib, Sriwidodo, Adryan Fristiohady Lubis, Mery Dina SYNTIA SAMANI, Ahmad FAHMI NUR, Rina Andriani, A. Chaerunisaa
Objective: Microcrystalline cellulose (MCC) is an essential excipient in tablet formulation. Mostly MCC was obtained from wooden conifer stem fiber, therefore environment issues had been came up. Alternative sources for MCC which offer friendly conifer wood need to be explored. This study aimed to isolate and determine the characteristics of MCC originated from Sago (Metroxylon sago Rottb.) stem fibers as an promising alternative of MCC.Methods: MCC was prepared through pre-hydrolysis using an acetic acid solution, alkali heating using NaOH solution, and acid hydrolysis using nitric acid 0.3 N using three variations of heating temperature, namely 90, 95 and 100 °C. The characterization carried out were pharmaceutical grade, powder properties, FTIR analysis and powder morphology by SEM.Results: The yields obtained were 66.02; 65.53 and 65.08%, respectively. The characteristics of the MCC sample based on pharmaceutical grade quality were white to yellowish white powder, odorless, tasteless, insoluble in: ether, 96% alcohol, HCl 2N and NaOH 1N. The pH of the MCC suspension were 5.07-5.12, while moisture content were 3.67-4.17%, with loss on drying value as much as 0.37-0.4%, and ash content 1-2.17%. The value of permanganate number were 0.09-0.11, Hausner factor was between 1.05-1.25, and angle of repose were between 11.4-24.8°.Conclusion: Based on the results, it can be concluded that Sago is potent natural resource for MCC. The resulting MCC revealed physicochemical and characteristic of MCC, which almost similar to Avicel PH 102 as standard.
目的:微晶纤维素(MCC)是片剂配方中必不可少的辅料。大多数微晶纤维素是从针叶树茎木纤维中提取的,因此出现了环境问题。因此,需要探索对针叶树木无害的 MCC 替代来源。本研究旨在分离并确定源自西米(Metroxylon sago Rottb.)茎纤维的 MCC 的特性,以此作为一种有前景的 MCC 替代品:方法:使用醋酸溶液进行预水解,使用 NaOH 溶液进行碱加热,使用 0.3 N 硝酸进行酸水解,使用三种不同的加热温度(即 90、95 和 100 °C)制备 MCC。所进行的表征包括制药等级、粉末特性、傅立叶变换红外光谱分析和扫描电镜下的粉末形态:获得的产量分别为 66.02%、65.53% 和 65.08%。基于药用级质量的 MCC 样品特征为白色至黄白色粉末,无臭、无味,不溶于乙醚、96% 酒精、2N HCl 和 1N NaOH。MCC 悬浮液的 pH 值为 5.07-5.12,水分含量为 3.67-4.17%,干燥损失值高达 0.37-0.4%,灰分含量为 1-2.17%。高锰酸盐数为 0.09-0.11,豪斯纳系数在 1.05-1.25 之间,休止角在 11.4-24.8° 之间:根据研究结果,可以得出西米是制造 MCC 的有效自然资源的结论。制得的 MCC 显示了 MCC 的理化特性,几乎与 Avicel PH 102 标准相似。
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引用次数: 0
BIOLOGICAL REACTIONS OF MACROPHAGES TO METAL OXIDE NANOPARTICLES 巨噬细胞对金属氧化物纳米颗粒的生物反应
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.49928
Mohammed Zorah, Hassan Lafta Atiyah, Noor WATHTHAB ALI, R. K. Mohammed Jawad, Fatimah H. Zayed, Mustafa Mudhafar, A. H. A., Saif Ahmed Raheem
In our daily lives, nanomaterials are utilized extensively in paints, textiles, food goods, cosmetics, and medicine. Several investigations aim to deter investigations of the physiological effects in various cell types. The innate immune system's macrophages regulate a wide range of biological functions. Depending on the stimulus, macrophages can be activated toward pro- or anti-inflammatory (M1) phenotypes; however, polarization may change in conditions including cancer, autoimmune illnesses, and bacterial and viral infections. Metal oxide nanoparticles have recently gained significant interest due to their diverse range of unique features with applications in research and industry. The production and usage of nanomaterials will rise significantly as the nanotechnology business grows. As a result, testing the consequences of nanomaterial exposure in biological systems is critical. A comparative analysis is conducted on the toxicities of several metal oxide nanoparticles. The significance of biogenically generated metal oxide nanoparticles has been growing in recent years. However, more research is needed to thoroughly characterize the potential toxicity of these nanoparticles to ensure nanosafety and consider environmental views. To that end, nanotoxicology seeks to assess the toxicity of nanomaterials to physicochemical factors such as size and form. In this review, we focus on the biological reactions of macrophages to metal oxide nanoparticles. Because macrophages are the first cells to engage with nanoparticles when they enter the body, they can absorb them through various processes.
在我们的日常生活中,纳米材料被广泛应用于涂料、纺织品、食品、化妆品和医药中。一些研究旨在阻止对各种细胞类型的生理效应进行调查。先天性免疫系统的巨噬细胞可调节多种生物功能。根据不同的刺激,巨噬细胞可被激活,形成促炎或抗炎(M1)表型;然而,在癌症、自身免疫性疾病、细菌和病毒感染等情况下,极化可能会发生变化。由于金属氧化物纳米粒子具有多种独特功能,可应用于研究和工业领域,因此近来备受关注。随着纳米技术业务的发展,纳米材料的生产和使用将大幅增加。因此,测试生物系统中纳米材料暴露的后果至关重要。本文对几种金属氧化物纳米粒子的毒性进行了比较分析。近年来,生物产生的金属氧化物纳米粒子的重要性不断增加。然而,还需要更多的研究来彻底确定这些纳米粒子的潜在毒性,以确保纳米安全性并考虑环境问题。为此,纳米毒理学试图根据纳米材料的尺寸和形态等物理化学因素来评估其毒性。在本综述中,我们将重点关注巨噬细胞对金属氧化物纳米颗粒的生物反应。由于巨噬细胞是纳米粒子进入人体后最先与之接触的细胞,因此它们可以通过各种过程吸收纳米粒子。
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引用次数: 0
ANTIBIOTICS IN INDONESIA: ACCESS, WATCH, AND RESERVE CLASSIFICATION 印度尼西亚的抗生素:获取、观察和储备分类
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50351
Dirgahayuni Sari Agustina, Ambarita, P. Oktamianti, I. Gusti, Ayu Trisnadewi, Dirgahayuni Sari, Agustina Ambarita
Objective: The objective of this study is to compare antibiotics listed in the National Essential Medicines List (NEML) and national formulary in Indonesia by determining the proportion of antibiotics in the three groups, Access, Watch, and Reserve (AWaRe), along with median data, range values, and time trends from 2013 to 2021.Methods: We obtained the compilation of antibiotics from the NEML and national formulary in Indonesia, covering the period from 2013 to 2021. These antibiotics were evaluated according to the 2021 WHO AWaRe classification database. This analysis involved determining the proportion of antibiotics in the AwaRe groups within each healthcare facility. Median data and range values for these antibiotics were also calculated. Trends in the proportion of AWaRe antibiotics were analyzed and visualized using a line chart.Results: The Indonesian NEML includes 20 antibiotics, categorized into two tiers of healthcare settings. Of these antibiotics, 13 were access, seven were watch, and there was neither a reserve nor a not recommended antibiotic. The Indonesian national formulary includes 42 antibiotics, categorized into three tiers of healthcare settings. Of these antibiotics, 19 were access, 22 were watch, one was not recommended, and there was no reserve antibiotic. The proportion of antibiotics during the pre-and post-establishment of the WHO AWaRe in 2017 showed significant changes in the Indonesian national formulary but not in the NEML.Conclusion: In recent years, the proportions of antibiotics in the Indonesian NEML and national formulary have varied according to the WHO AWaRe classification.
研究目的本研究旨在通过确定印度尼西亚国家基本药物目录(NEML)和国家处方集(AWaRe)三个组别中抗生素的比例,以及中位数数据、范围值和2013年至2021年的时间趋势,对国家基本药物目录(NEML)和国家处方集中列出的抗生素进行比较:我们从印度尼西亚国家药品目录和国家处方集中获得了 2013 年至 2021 年期间的抗生素汇编。根据 2021 年世界卫生组织 AWaRe 分类数据库对这些抗生素进行了评估。这项分析包括确定各医疗机构中AwaRe组抗生素的使用比例。此外,还计算了这些抗生素的中位数数据和范围值。使用折线图分析了AwaRe抗生素比例的变化趋势:印尼 NEML 包括 20 种抗生素,分为两级医疗机构。在这些抗生素中,13 种为可获得抗生素,7 种为观察抗生素,既没有储备抗生素,也没有不推荐抗生素。印尼国家处方集包括 42 种抗生素,分为三级医疗机构。在这些抗生素中,19 种为可获得抗生素,22 种为观察抗生素,1 种为不推荐抗生素,没有储备抗生素。在2017年世卫组织AWaRe建立前后,印尼国家处方集中抗生素的比例发生了显著变化,但在NEML中却没有:近年来,根据世卫组织 AWaRe 的分类,印尼 NEML 和国家处方集中抗生素的比例发生了变化。
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引用次数: 0
IDENTIFICATION, SEPARATION, AND CHARACTERIZATION OF DEGRADATION PRODUCTS OF TRIAMCINOLONE HEXACETONIDE USING LC AND LC-MS/MS 利用 LC 和 LC-MS/MS 对曲安奈德六酮降解产物进行鉴定、分离和表征
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-05-07 DOI: 10.22159/ijap.2024v16i3.50122
Bhavna SUNIL MAHAJAN, P. Miniyar
Objective: The study aimed to separate the forced degradation products of Triamcinolone hexacetonide using HPLC and characterize the degradation product by LC-MS/MS fragmentation pattern.Methods: Triamcinolone hexacetonide (THA) and its primary degradation products were identified using a liquid chromatography-mass spectrometry/Mass spectrometry (LC-MS/MS) approach. The degradation study was based on in-depth stress testing with acid, base, peroxide, heat, and light. A Zorbax SB C18 column and a greener mobile phase composed of methanol and 10 mmol ammonium acetate buffer in water at pH 3 were employed to accomplish separation and quantitation at a flow rate of 0.7 ml/min in an isocratic mode with a 239 nm detection wavelength.Results: A major degradation product of the drug was obtained in acidic and alkaline stress conditions. The drug was found to be stable for all other stress conditions. The LC-MS/MS analysis results of the active pharmaceutical ingredient and resulting product after degradation were interpreted to identify the novel degradation product and fragments. The developed method was validated as per International Council for Harmonization (ICH) guidelines. The square root of the correlation coefficients, which indicated linearity for THA in 50 to 150 % of the workload, was 0.99. Method Precision assay was performed on six different preparations, percentage relative standard deviation (% RSD) of assay value is 0.17 % and system precision is 0.30 %. In accuracy, overall % RSD of 50 %, 100 %, and 150 % in triplicate is 0.95.Conclusion: It is concluded that the drug is stable to all other stress conditions except for acidic and alkaline stress conditions and generates a novel degradation product. The developed LC (Liquid chromatography) method separates and identifies the degradation product.
研究目的该研究旨在利用高效液相色谱法分离曲安奈德六酮的强制降解产物,并通过 LC-MS/MS 片段模式分析降解产物的特征:采用液相色谱-质谱/质谱(LC-MS/MS)方法鉴定了曲安奈德六酮(THA)及其主要降解产物。降解研究基于酸、碱、过氧化物、热和光的深度应力测试。采用 Zorbax SB C18 色谱柱和由 pH 值为 3 的甲醇和 10 mmol 乙酸铵缓冲液组成的绿色流动相进行分离和定量,流速为 0.7 ml/min,检测波长为 239 nm:结果:在酸性和碱性压力条件下,该药物的主要降解产物被分离出来。在所有其他应力条件下,药物均保持稳定。对活性药物成分和降解产物的 LC-MS/MS 分析结果进行了解释,以确定新型降解产物和片段。所开发的方法按照国际协调理事会(ICH)指南进行了验证。相关系数的平方根为 0.99,表明在 50%至 150%的工作量中 THA 具有线性关系。对六种不同制剂进行了方法精密度检测,检测值的相对标准偏差(% RSD)为 0.17%,系统精密度为 0.30%。在准确度方面,一式三份中 50%、100% 和 150%的总体 RSD 为 0.95:结论:除了酸性和碱性应力条件外,该药物对所有其他应力条件都很稳定,并且会产生一种新的降解产物。所开发的 LC(液相色谱)方法可分离和鉴定降解产物。
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引用次数: 0
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International Journal of Applied Pharmaceutics
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