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Formulation, Characterization, and Optimization of a Topical Gel Containing Tranexamic Acid to Prevent Superficial Bleeding: In Vivo and In Vitro Evaluations. 含有氨甲环酸的局部凝胶预防表面出血的配方、表征和优化:体内和体外评估。
IF 1.7 Pub Date : 2023-08-22 DOI: 10.4274/tjps.galenos.2022.60687
Farideh Shiehzadeh, Daryosh Mohebi, Omid Chavoshian, Sara Daneshmand

Objectives: Tranexamic acid (TXA) is used systemically to stop bleeding, but it can lead to thromboembolism. Trials have revealed the efficacy of topical TXA on local hemorrhages. However, there is a need for an efficient delivery system that can keep the drug at the site of action.

Materials and methods: To develop a gel containing TXA (3%) optimized in terms of viscosity and dispersibility, the central composite design based on two factors-three levels [carbopol 940 and hydroxypropyl methylcellulose (HPMC), 1-1.5% and 1-2%, respectively] was applied. The spreadability and viscosity were assessed using glass slide and rheometer, respectively. To confirm the compatibility of TXA with the gel, fourier transform-infrared (FTIR) spectroscopy was performed. Drug content uniformity was analyzed by a spectroscopy method. An ex vivo mice model using Franz cells was applied to evaluate the permeation of TXA through the skin. To investigate the effect of topical TXA gel on bleeding time, IVY human method was performed.

Results: HPMC/carbopol 940 (1:1, w/w) gel showed the highest quality in terms of viscosity and dispersibility (3.982 ± 17.6 and 6.052 ± 3.562, respectively). FTIR absorption spectrum showed that all the TXA index peaks appeared without displacement. The complete-encapsulated TXA content was uniformly dispersed throughout the gel. In vitro TXA cumulative release reached 90% in 4 h. The bleeding time determined in vivo for TXA gel was significantly lower than that for TXA solution and control.

Conclusion: The results confirm the importance of further studies on this formulation as a potential medication to stop acute superficial bleeding.

目的:氨甲环酸(TXA)用于全身止血,但它可导致血栓栓塞。试验表明局部使用TXA对局部出血有效。然而,需要一种有效的递送系统,使药物保持在作用部位。材料与方法:采用卡波醇940和羟丙基甲基纤维素(HPMC)分别为1-1.5%和1-2%的2因素- 3水平的中心复合设计,制备了一种粘度和分散性优化的含TXA(3%)凝胶。分别用玻片法和流变仪测定涂敷性和粘度。为了确定TXA与凝胶的相容性,傅里叶变换红外光谱(FTIR)进行了测试。用光谱学方法分析药物含量均匀性。采用体外小鼠Franz细胞模型评价TXA在皮肤中的渗透作用。采用IVY人用法研究外用TXA凝胶对出血时间的影响。结果:HPMC/carbopol 940凝胶(1:1,w/w)的粘度和分散性最高(分别为3.982±17.6和6.052±3.562)。FTIR吸收光谱显示,所有TXA指数峰均无位移。完全包封的TXA含量均匀地分散在凝胶中。体外4 h TXA累积释放量达到90%,体内测定的出血时间明显低于TXA溶液和对照组。结论:结果证实了进一步研究该制剂作为一种潜在的治疗急性浅表出血的药物的重要性。
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引用次数: 2
Validated Stability-Indicating RP-HPLC Method for Daclatasvir in Tablets. 经验证的稳定性指示反相高效液相色谱法测定Daclatasvir片中的含量。
IF 1.7 Pub Date : 2023-08-22 DOI: 10.4274/tjps.galenos.2022.87393
Hemlata M Nimje, Smita J Pawar, Meenakshi N Deodhar

Objectives: The current study goal was to create a precise, sensitive, and validated reverse phase-high performance liquid chromatography (RP-HPLC) method for assessing the direct-acting antiviral daclatasvir (DCV) as well as to evaluate the stability of DCV in both drug and tablet formulations. The current investigation was to display stability indicating methods under different stress conditions, including hydrolysis (acidic, basic, and neutral), oxidation, and photolysis.

Materials and methods: All experiments were performed on HPLC Agilent 1100 with a stainless steel Hypersil C18 column having a particle size of 5 μm and a dimension of 4.6 x 250 mm. The mobile phase chosen was acetonitrile: 0.05% o-phosphoric acid (50:50 v/v) in isocratic mode with 0.7 mL/min flow rate and wavelength 315 nm was selected for detection.

Results: This method was validated for linearity and range, accuracy, precision, limit of detection, limit of quantification, and robustness in accordance with International Council for Harmonisation (ICH) requirements. The results were satisfactory. It was observed that retention time (tR) was 3.760 ± 0.01 min. In acidic conditions, DCV degradans show tR at 3.863, 4.121, and 4.783 min and tandem mass spectrometry (MS/MS) spectra scans had m/z 339.1, 561.2 fragment ions. In basic condition, DCV degradans show tR at 5.188, 5.469 min and MS/MS spectra scans having m/z 294.1, 339.1, 505.2, 527.2 fragment ions. In oxidation conditions, DCV degradans shows tR at 4.038 min and MS/MS spectra scans having m/z 301.1 and 339.1 fragment ions were observed.

Conclusion: All the mass fragments exhibited additional degradation observed for different stress conditions. This will help to identify the structure of the degradant and its pathways. No degradation was observed in neutral and photolytic conditions.

目的:建立一种精确、灵敏、有效的反相高效液相色谱(RP-HPLC)方法来评估直接作用抗病毒药物daclatasvir (DCV),并评估DCV在药物和片剂制剂中的稳定性。目前的研究是在不同的应激条件下显示稳定性,包括水解(酸性、碱性和中性)、氧化和光解。材料和方法:所有实验均在Agilent 1100高效液相色谱仪上进行,柱柱为不锈钢Hypersil C18,粒径为5 μm,尺寸为4.6 x 250 mm。流动相为乙腈:0.05% o-磷酸(50:50 v/v),流速0.7 mL/min,检测波长315 nm。结果:该方法的线性和范围、准确度、精密度、检出限、定量限和鲁棒性符合国际统一委员会(ICH)的要求。结果令人满意。在酸性条件下,DCV降解产物的停留时间(tR)分别为3.863、4.121和4.783 min,串联质谱(MS/MS)扫描结果为m/z 339.1、561.2个片段离子。在基本条件下,DCV降解物的tR值分别为5.188、5.469 min, MS/MS扫描的m/z值分别为294.1、339.1、505.2、527.2个碎片离子。在氧化条件下,DCV降解产物的tR值为4.038 min, MS/MS扫描结果显示m/z为301.1和339.1。结论:在不同的应力条件下,所有的质量碎片都表现出额外的降解。这将有助于确定降解物的结构及其途径。在中性和光解条件下未观察到降解。
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引用次数: 1
Exploration of Structure-Activity Relationship Using Integrated Structure and Ligand Based Approach: Hydroxamic Acid-Based HDAC Inhibitors and Cytotoxic Agents. 基于集成结构和配体方法的构效关系探索:基于羟肟酸的HDAC抑制剂和细胞毒性药物。
IF 1.7 Pub Date : 2023-08-22 DOI: 10.4274/tjps.galenos.2022.12269
Ekta Shirbhate, Jaiprakash Pandey, Vijay Kumar Patel, Ravichandran Veerasamy, Harish Rajak

The present study aimed to establish significant and validated quantitative structure-activity relationship (QSAR) models for histone deacetylase (HDAC) inhibitors and correlate their physicochemical, steric, and electrostatic properties with their anticancer activity. We have selected a dataset from earlier research findings. The target and ligand molecules were procured from recognized databases and incorporated into pivotal findings such as molecular docking (XP glide), e-pharmacophore study and 3D QSAR model designing study (phase). Docking revealed molecule 39 with better docking score and well binding contact with the protein. 3D QSAR analysis, which was performed for partial least squares factor 5 reported good 0.9877 and 0.7142 as R2 and Q2 values and low standard of deviation: 0.1049 for hypothesis AADRR.139. Based on the computational outcome, it has been concluded that molecule 39 is an effective and relevant candidate for inhibition of HDAC activity. Moreover, these computational approaches motivate to discover novel drug candidates in pharmacological and healthcare sectors.

本研究旨在建立有意义且有效的组蛋白去乙酰化酶(HDAC)抑制剂的定量构效关系(QSAR)模型,并将其理化、位阻和静电特性与抗癌活性联系起来。我们从早期的研究成果中选择了一个数据集。靶标和配体分子从公认的数据库中获取,并纳入关键发现,如分子对接(XP滑翔),电子药效团研究和3D QSAR模型设计研究(阶段)。对接发现分子39对接得分较高,与蛋白结合良好。对偏最小二乘因子5进行三维QSAR分析,R2和Q2值分别为0.9877和0.7142,假设AADRR.139的标准偏差较低,为0.1049。基于计算结果,我们得出结论,分子39是抑制HDAC活性的有效候选物。此外,这些计算方法激励在药理学和医疗保健部门发现新的候选药物。
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引用次数: 1
LC-MS/MS Method Development and Validation for Determination of Favipiravir Pure and Tablet Dosage Forms. 法匹拉韦纯剂型和片剂的LC-MS/MS方法建立与验证。
IF 1.7 Pub Date : 2023-08-22 DOI: 10.4274/tjps.galenos.2022.75470
Nandeesha Itigimath, Hadagali Ashoka, Basappa C Yallur, Manjunatha Devagondanahalli Hadagali

Objectives: Analytical method development and validation for determination of favipiravir (FVPR) in pure and tablet dosage forms by liquid chromatography with tandem mass spectrometry/mass spectrometry (LC-MS/MS) technique.

Materials and methods: A simple LC-MS/MS method was developed for determination of a new antiviral drug, FVPR in pharmaceutical formulations. The stationary phase employed was a Shim pack GISS, C18 (100 mm × 2.1 mm, 1.9 μm) column and mobile phase used in pump A was 10.0 mM ammonium acetate and in pump B methanol was used. The gradient program was used with fixed mobile phase flow rate at 0.4 mL min-1. Total run time was 5.0 min. The proposed method was validated according to International Conference on Harmonization (ICH) guidelines. The established method found better outcomes.

Results: The linearity graph was found in the range of 50-200 μg/mL and the correlation coefficient value (R2) obtained was found to be 1.0. The limit of detection (LOD) and limit of quantification (LOQ) were 4.044 μg/mL and 12.253 μg/mL, respectively. Tremendous recovery outcomes were observed and found to be 101%, 99.0%, and 99.5% for FVPR at 150% upper, 100% middle, and 50% lower concentrations, respectively.

Conclusion: All outcomes obtained comply with ICH guidelines. The developed method was simple, unique, accurate, robust, precise, and reproducible for determination of FVPR in tablet formulation. The method is novel and could be adopted in formulation industry.

目的:建立液相色谱-串联质谱/质谱(LC-MS/MS)技术测定法匹拉韦(FVPR)纯剂型和片剂剂型的分析方法并进行验证。材料与方法:建立了一种新型抗病毒药物制剂中FVPR含量测定的LC-MS/MS方法。固定相为Shim pack GISS, C18 (100 mm × 2.1 mm, 1.9 μm)色谱柱,流动相为10.0 mm乙酸铵,B泵为甲醇。采用梯度程序,固定流动相流速为0.4 mL min-1。总运行时间为5.0 min。根据国际协调会议(ICH)指南验证了所提出的方法。既定方法的效果更好。结果:在50 ~ 200 μg/mL范围内线性关系良好,相关系数(R2)为1.0。检测限和定量限分别为4.044 μg/mL和12.253 μg/mL。在150%高浓度、100%中浓度和50%低浓度条件下,FVPR的回收率分别为101%、99.0%和99.5%。结论:所有结果均符合ICH指南。该方法简便、准确、可靠、精密度高、重复性好,可用于片剂中FVPR的测定。该方法新颖,可应用于制剂行业。
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引用次数: 1
Medication Reconciliation Service in Hospitalized Patients with Infectious Diseases During Coronavirus Disease-2019 Pandemic: An Observational Study. 冠状病毒病-2019大流行期间住院传染病患者的药物和解服务:一项观察性研究
IF 1.7 Pub Date : 2023-08-22 DOI: 10.4274/tjps.galenos.2022.08455
Cüneyd Enver, Buket Ertürk Şengel, Mesut Sancar, Volkan Korten, Betul Okuyan

Objectives: To determine the prevalence and type of medication discrepancies and factors associated with unintentional discrepancies and identify the rate of hospital readmission and emergency service visit within 30 days after discharge among hospitalized patients with infectious diseases and receiving clinical pharmacist-led medication reconciliation during the coronavirus disease-2019 (COVID-19) pandemic.

Materials and methods: This observational study was conducted in the internal medicine and infectious diseases wards of a tertiary university hospital between July 2020 and February 2021 among hospitalized adult patients with infectious diseases. Medication reconciliation service (including patient counseling) was provided in person or by telephone. The number and type of medication discrepancies detected during the medication reconciliation services, the acceptance rate of pharmacists' recommendation, and factors associated with having at least one unintentional medication discrepancy at admission were evaluated. At follow-up, hospital readmission and emergency service visit within 30 days after discharge were assessed by telephone.

Results: Among 146 patients, 84 (57.5%) had at least one unintentional discrepancy at admission. Only three unintentional discrepancies were determined in three patients at hospital discharge. All the pharmacists' recommendations for medication discrepancies were accepted by the physicians. Having COVID-19 [odds ratio (OR): 2.25, 95% confidence interval (CI): 1.15-4.40; p<0.05], being at a high risk for medication error (OR: 2.01, 95% CI: 1.03-3.92; p<0.05), and higher number of medications used at home (OR: 1.41, 95% CI: 1.23-1.61; p<0.001) were associated with having at least one unintentional discrepancy at admission. The rates of 30 day hospital readmission and admission to the emergency medical service were 12.3% and 15.8%, respectively.

Conclusion: Medication reconciliation service provided by in-person or by telephone was useful for detecting and solving unintentional medication discrepancies during the COVID-19 pandemic.

目的:了解2019冠状病毒病(COVID-19)大流行期间接受临床药师主导的住院感染性疾病患者用药差异的发生率、类型及非故意用药差异的相关因素,确定出院后30 d内再入院率和急诊就诊率。材料与方法:本观察性研究于2020年7月至2021年2月在某三级大学附属医院内科及传染病病房对住院的成人传染病患者进行研究。亲自或电话提供药物调解服务(包括患者咨询)。评估在药物调解服务中发现的药物差异的数量和类型、药师推荐的接受率以及入院时至少有一次非故意药物差异的相关因素。随访时,通过电话评估出院后30天内的再入院和急诊就诊情况。结果:146例患者中,84例(57.5%)在入院时至少有一次非故意差异。在3例出院患者中,仅确定了3个非故意差异。药师对用药差异的建议均被医师接受。患有COVID-19[优势比(OR): 2.25, 95%可信区间(CI): 1.15-4.40;结论:在新冠肺炎疫情期间,通过上门或电话提供药物调解服务,有助于发现和解决非故意用药差异。
{"title":"Medication Reconciliation Service in Hospitalized Patients with Infectious Diseases During Coronavirus Disease-2019 Pandemic: An Observational Study.","authors":"Cüneyd Enver,&nbsp;Buket Ertürk Şengel,&nbsp;Mesut Sancar,&nbsp;Volkan Korten,&nbsp;Betul Okuyan","doi":"10.4274/tjps.galenos.2022.08455","DOIUrl":"https://doi.org/10.4274/tjps.galenos.2022.08455","url":null,"abstract":"<p><strong>Objectives: </strong>To determine the prevalence and type of medication discrepancies and factors associated with unintentional discrepancies and identify the rate of hospital readmission and emergency service visit within 30 days after discharge among hospitalized patients with infectious diseases and receiving clinical pharmacist-led medication reconciliation during the coronavirus disease-2019 (COVID-19) pandemic.</p><p><strong>Materials and methods: </strong>This observational study was conducted in the internal medicine and infectious diseases wards of a tertiary university hospital between July 2020 and February 2021 among hospitalized adult patients with infectious diseases. Medication reconciliation service (including patient counseling) was provided in person or by telephone. The number and type of medication discrepancies detected during the medication reconciliation services, the acceptance rate of pharmacists' recommendation, and factors associated with having at least one unintentional medication discrepancy at admission were evaluated. At follow-up, hospital readmission and emergency service visit within 30 days after discharge were assessed by telephone.</p><p><strong>Results: </strong>Among 146 patients, 84 (57.5%) had at least one unintentional discrepancy at admission. Only three unintentional discrepancies were determined in three patients at hospital discharge. All the pharmacists' recommendations for medication discrepancies were accepted by the physicians. Having COVID-19 [odds ratio (OR): 2.25, 95% confidence interval (CI): 1.15-4.40; <i>p</i><0.05], being at a high risk for medication error (OR: 2.01, 95% CI: 1.03-3.92; <i>p</i><0.05), and higher number of medications used at home (OR: 1.41, 95% CI: 1.23-1.61; <i>p</i><0.001) were associated with having at least one unintentional discrepancy at admission. The rates of 30 day hospital readmission and admission to the emergency medical service were 12.3% and 15.8%, respectively.</p><p><strong>Conclusion: </strong>Medication reconciliation service provided by in-person or by telephone was useful for detecting and solving unintentional medication discrepancies during the COVID-19 pandemic.</p>","PeriodicalId":23378,"journal":{"name":"Turkish Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2023-08-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10445224/pdf/TJPS-20-210.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10442021","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Thermoreversible Gel Formulation for the Intranasal Delivery of Salmon Calcitonin and Comparison Studies of In Vivo Bioavailability. 用于鲑鱼降钙素鼻内给药的热可逆凝胶制剂及体内生物利用度的比较研究。
IF 1.7 Pub Date : 2023-07-07 DOI: 10.4274/tjps.galenos.2022.09482
Abdullah Levent Alparslan, Gülbeyaz Yıldız Türkyılmaz, Leyla Didem Kozacı, Ercüment Karasulu

Objectives: We developed original thermoreversible (sol-gel) formulations of salmon calcitonin (sCT) for nasal applications. The sol-gel has been compared with commercial intranasal sprays in vitro and in vivo studies. The aim of studying sol-gel form is to arrange the viscosity of formulations for a reversible adequate fluidity at different temperatures. This situation may facilitate the use of drugs as sprays and increase the bioadhesive ability to mucosa.

Materials and methods: Characterization of optimum formulations was studied. Validated analytical assays determined the number of sCT. An approximately equal number of commercial and sol-gel dosages were sprayed into the nostrils of the rabbits. Blood samples were collected from the ear veins of rabbits and determined by enzyme immunoassay plates. These plates were evaluated by Thermo Labsystem Multiscan Spectrum at 450 nm. Thanks to Winnonlin 5.2, pharmacokinetic data were evaluated by a non-compartmental method.

Results: The absolute bioavailability of the formulation at pH 4 and the commercial product (CP) was compared by evaluating the primary pharmacokinetic data area under the curve 0→tlast. The absolute bioavailability of the commercial intranasal spray was measured 1.88 based on maximum concentration (Cmax) assessment. Cmax of the sol-gel formulation pH 4 was calculated as 0.99 and the relative bioavailability was obtained 53.3%.

Conclusion: In vivo pharmacokinetic data of sol-gel formulation with pH 3 showed significantly higher volume of distribution parameter than the CP (111167>35408). It is thought that the formulation adhered to the nasal mucosa releases sCT slowly and less.

目的:我们开发了原始的热可逆(溶胶-凝胶)配方的鲑鱼降钙素(sCT)鼻腔应用。溶胶-凝胶已在体外和体内研究中与商业鼻内喷雾剂进行了比较。研究溶胶-凝胶形式的目的是为了在不同温度下使配方的粘度达到可逆的充足流动性。这种情况可能有利于药物作为喷雾剂的使用,并增加对粘膜的生物粘附能力。材料与方法:研究了最佳配方的表征。经验证的分析方法确定sCT的数量。将大约等量的商业剂量和溶胶凝胶剂量喷入兔子的鼻孔。取家兔耳静脉血样,采用酶免疫法测定。利用Thermo Labsystem Multiscan Spectrum在450 nm处对这些板进行评估。采用Winnonlin 5.2软件,采用非区室法对药代动力学数据进行评价。结果:通过0→tlast曲线下的初级药代动力学数据面积,比较了制剂在pH 4下与商品(CP)的绝对生物利用度。根据最大浓度(Cmax)评估,商业鼻内喷雾剂的绝对生物利用度为1.88。计算出溶胶-凝胶制剂pH值为4时的Cmax为0.99,相对生物利用度为53.3%。结论:pH为3的溶胶-凝胶制剂的体内药动学数据显示体积分布参数明显高于CP(111167>35408)。认为黏附于鼻黏膜的制剂释放sCT缓慢且较少。
{"title":"Thermoreversible Gel Formulation for the Intranasal Delivery of Salmon Calcitonin and Comparison Studies of <i>In Vivo</i> Bioavailability.","authors":"Abdullah Levent Alparslan,&nbsp;Gülbeyaz Yıldız Türkyılmaz,&nbsp;Leyla Didem Kozacı,&nbsp;Ercüment Karasulu","doi":"10.4274/tjps.galenos.2022.09482","DOIUrl":"https://doi.org/10.4274/tjps.galenos.2022.09482","url":null,"abstract":"<p><strong>Objectives: </strong>We developed original thermoreversible (sol-gel) formulations of salmon calcitonin (sCT) for nasal applications. The sol-gel has been compared with commercial intranasal sprays <i>in vitro</i> and <i>in vivo</i> studies. The aim of studying sol-gel form is to arrange the viscosity of formulations for a reversible adequate fluidity at different temperatures. This situation may facilitate the use of drugs as sprays and increase the bioadhesive ability to mucosa.</p><p><strong>Materials and methods: </strong>Characterization of optimum formulations was studied. Validated analytical assays determined the number of sCT. An approximately equal number of commercial and sol-gel dosages were sprayed into the nostrils of the rabbits. Blood samples were collected from the ear veins of rabbits and determined by enzyme immunoassay plates. These plates were evaluated by Thermo Labsystem Multiscan Spectrum at 450 nm. Thanks to Winnonlin 5.2, pharmacokinetic data were evaluated by a non-compartmental method.</p><p><strong>Results: </strong>The absolute bioavailability of the formulation at pH 4 and the commercial product (CP) was compared by evaluating the primary pharmacokinetic data area under the curve 0→t<sub>last</sub>. The absolute bioavailability of the commercial intranasal spray was measured 1.88 based on maximum concentration (C<sub>max</sub>) assessment. C<sub>max</sub> of the sol-gel formulation pH 4 was calculated as 0.99 and the relative bioavailability was obtained 53.3%.</p><p><strong>Conclusion: </strong><i>In vivo</i> pharmacokinetic data of sol-gel formulation with pH 3 showed significantly higher volume of distribution parameter than the CP (111167>35408). It is thought that the formulation adhered to the nasal mucosa releases sCT slowly and less.</p>","PeriodicalId":23378,"journal":{"name":"Turkish Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2023-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10337020/pdf/TJPS-20-127.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10164627","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Development and Evaluation of In Situ Gel Formation for Treatment of Mouth Ulcer. 原位凝胶法治疗口腔溃疡的研究进展及评价。
IF 1.7 Pub Date : 2023-07-07 DOI: 10.4274/tjps.galenos.2022.25968
Nikita Harekrishna Gurav, Prerana Shantinath Husukale

Objectives: Mouth ulcers are one of the most prevalent conditions that can be caused by a range of circumstances. Many formulations, such as solutions, suspensions, and ointments are available commercially. However, because there is no long-term effect, no medication can be regarded as totally effective for treating mouth ulcers. The use of bioadhesive methods can boost the therapy efficacy. Because it is easier to administer than prepared gel formulations, the phenomenon of the sol-to-gel conversion can be beneficial. The major goal of this study was to develop and test in situ gels for treating mouth ulcers using choline salicylate and borax as model medicines.

Materials and methods: Because a thermosensitive polymer was employed in this formulation, the sol-to-gel change was thermally reversible, and the frequency of administration was reduced by using the mucoadhesive polymer carbopol. Gelation temperature, pH, gel strength, spreadability, in vitro mucoadhesion, and in vitro drug release were all measured in the formulations.

Results: The experimental section indicated that viscosity of sols and gel strength increased with increasing temperature, i.e., gel can be created at the site of application owing to body temperature. When poloxamer 407 was used at a concentration of 14 to 16 percent w/v, the gelling temperature was close to the body temperature (35-38 °C), but when carbopol 934P was added, the gelling temperature was raised. All formulations had pH between 5.5 and 6.8. All formulations had viscosities of less than 1000 cps, allowing for simple administration of the formulation to a mouth ulcer.

Conclusion: As a result, a correctly developed in situ gel for oral ulcers can extend the duration spent at the application site and minimize the frequency of administration. These findings show that the developed technology is a viable alternative to traditional drug delivery systems and can help patients comply.

目的:口腔溃疡是由多种情况引起的最普遍的疾病之一。许多配方,如溶液、悬浮液和软膏在商业上都可以买到。然而,由于没有长期效果,没有任何药物可以被认为是完全有效的治疗口腔溃疡。采用生物黏附的方法可以提高治疗效果。因为它比制备的凝胶制剂更容易施用,所以溶胶-凝胶转化的现象是有益的。本研究的主要目的是开发和测试以水杨酸胆碱和硼砂为模型药物治疗口腔溃疡的原位凝胶。材料和方法:由于在该配方中使用了热敏聚合物,因此从溶胶到凝胶的变化是热可逆的,并且通过使用粘接聚合物carbopol减少了给药频率。测定了凝胶温度、pH值、凝胶强度、涂敷性、体外黏附、体外释药量。结果:实验切片显示,溶胶的粘度和凝胶强度随温度的升高而增加,即由于体温的作用,可以在涂抹部位形成凝胶。当波洛沙姆407浓度为14 ~ 16% w/v时,胶凝温度接近体温(35 ~ 38℃),但当卡波波尔934P加入时,胶凝温度升高。所有配方的pH值在5.5到6.8之间。所有制剂的粘度都小于1000 cps,因此可以简单地给药于口腔溃疡。结论:因此,一种正确研制的口腔溃疡原位凝胶可以延长在应用部位的时间,并尽量减少给药频率。这些发现表明,开发的技术是传统药物输送系统的可行替代方案,可以帮助患者遵守规定。
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引用次数: 0
Applications of Dietary Supplements and Aromatherapy for Prophylactic and Treatment Purposes During COVID-19 Pandemic. 膳食补充剂和芳香疗法在COVID-19大流行期间预防和治疗中的应用
IF 1.7 Pub Date : 2023-07-07 DOI: 10.4274/tjps.galenos.2022.21370
Methiye Mancak, Ufuk Koca Çalışkan

Objectives: The lack of a specific proven treatment for coronavirus disease-2019 (COVID-19) has led individuals to use different treatment options. Although their effects on COVID-19 have not been proven, interest in dietary supplements and aromatherapy has increased during the pandemic period. In this study, use of dietary supplements and aromatherapy was investigated for COVID-19 among individuals living within the borders of Türkiye.

Materials and methods: This cross-sectional survey study was conducted among 310 individuals. The questionnaire was prepared using online Google Forms and communicated to the participants via social media platforms. The data obtained from the study were analyzed with the statistical program.

Results: The analyzes of the survey revealed that participants increased the usage of supplements mostly prophylactic and for treatment purposes during COVID-19 pandemic, 31.9% individuals declared that they consumed herbal tea/products, 38.1% of them used vitamin/mineral supplements (multivitamin-mineral, vitamins B1, B6, B12, C, D, calcium, coenzyme Q10, iron, magnesium, selenium, and zinc), and 18.4% of the individuals applied aromatherapy (meaning treatment with essential oils). As a result of the study, the most commonly used supplement was vitamin D, the most commonly consumed tea was green tea, the essential oil was thyme oil, and the most eaten vegetable was garlic. Moreover, other frequently used herbal products were found to contain ginger and onion as food and peppermint and eucalyptus oils as aromatherapeutics. Participants often reported that they found it safe to use elevated levels of herbs or herbal products against COVID-19.

Conclusion: Among the individuals participating in this study, it has been observed that the use of dietary supplements has increased during the COVID-19 pandemic period. The study revealed that vitamin D is prominent in self-medication use. Moreover, interest in aromatherapy and dietary supplements has increased. Among aromatherapeutics, thyme stood out over the applied essential oils.

由于缺乏针对2019冠状病毒病(COVID-19)的特异性治疗方法,导致个体使用不同的治疗方案。虽然它们对COVID-19的影响尚未得到证实,但在大流行期间,人们对膳食补充剂和芳香疗法的兴趣有所增加。在这项研究中,调查了居住在 rkiye边境内的个体使用膳食补充剂和芳香疗法治疗COVID-19的情况。材料与方法:本研究采用横断面调查法对310名个体进行调查。调查问卷是使用在线谷歌表格编写的,并通过社交媒体平台传达给参与者。用统计程序对研究所得数据进行分析。结果:调查分析显示,参与者在COVID-19大流行期间增加了补充剂的使用,主要是预防和治疗目的,31.9%的人声称他们食用草药茶/产品,38.1%的人使用维生素/矿物质补充剂(多种维生素矿物质,维生素B1, B6, B12, C, D,钙,辅酶Q10,铁,镁,硒和锌),18.4%的人使用芳香疗法(意思是用精油治疗)。研究结果显示,最常用的补充剂是维生素D,最常食用的茶是绿茶,精油是百里香油,最常食用的蔬菜是大蒜。此外,其他常用的草药产品被发现含有生姜和洋葱作为食物,薄荷和桉树油作为芳香疗法。参与者经常报告说,他们发现使用高水平的草药或草药产品来对抗COVID-19是安全的。结论:在参与本研究的个体中,观察到在COVID-19大流行期间膳食补充剂的使用有所增加。研究表明,维生素D在自我用药中起着重要作用。此外,人们对芳香疗法和膳食补充剂的兴趣也在增加。在芳香疗法中,百里香在应用精油中脱颖而出。
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引用次数: 1
Trachystemon orientalis (L.) G. Don as a Valuable Source of Rosmarinic Acid: Biological Activities and HPLC Profiles. 毛茛(Trachystemon orientalis)唐是迷迭香酸的重要来源:生物活性和高效液相色谱分析。
IF 1.7 Pub Date : 2023-07-07 DOI: 10.4274/tjps.galenos.2022.14265
Burak Bıyık, Sezen Yılmaz Sarıaltın, Alper Gökbulut, Tülay Çoban, Maksut Çoşkun

Objectives: Trachystemon orientalis (L.) G. Don, colloquially known in Türkiye as "kaldırık", is an edible plant belonging to the Boraginaceae. This plant has been practiced in traditional medicine for many years for its various therapeutic benefits. The effectiveness and chemical composition of plants can vary depending on their parts, age, and extraction solvent. Therefore, the current study aimed to define the biological activities of various parts and extracts of T. orientalis, which were collected in distinct seasons as young and mature, and investigate the main component responsible for these biological effects.

Material and methods: Plant material was collected in different seasons from the northwest of Türkiye. 2,2'-Azinobis-(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activities were investigated to assess antiradical and antioxidant potential of the extracts. Anti-inflammatory activity of the extracts was also tested using human red blood cell membrane stabilizing method. Folin-Ciocalteu test was conducted to determine the total phenolic content. Reverse phase-high performance liquid chromatography-photodiode array detector (RP-HPLC-PDA) analysis was performed.

Results: Both methanol and aqueous extracts exhibited significant radical scavenging and anti-inflammatory activities compared with control (p<0.05). The highest percentage of inhibition on ABTS and DPPH free radicals was obtained in aqueous extracts of the mature herbs and roots, respectively. Methanol extracts of the mature roots and herbs exhibited the strongest anti-inflammatory capacity. Rosmarinic acid possessed a much higher antioxidant and anti-inflammatory effect than the reference compounds used in each assay in our study. High rosmarinic acid content of the extracts suggests that the compound responsible for the great biological activity potential is rosmarinic acid.

Conclusion: To the best of our knowledge, the presence of rosmarinic acid in herbs and roots of T. orientalis was shown for the first time in our present study. Phytochemical composition and effective biological activities of T. orientalis explain its traditional use and indicate its significant potential in pharmaceutical industry applications.

目的:毛蕊草(Trachystemon orientalis)唐,在基耶语中俗称为“kaldırık”,是一种属于琉璃苣科的可食用植物。这种植物因其多种治疗作用已在传统医学中使用多年。植物的功效和化学成分可能因其部位、年龄和提取溶剂而异。因此,本研究旨在明确不同季节采集的东方桦幼嫩期和成熟期各部位和提取物的生物活性,并探讨产生这些生物效应的主要成分。材料与方法:采用不同季节采集的植物材料,采自云南西北地区。研究了2,2′-氮唑-(3-乙基苯并噻唑-6-磺酸)(ABTS)和2,2-二苯基-1-吡啶酰肼(DPPH)自由基清除能力,以评价其抗自由基和抗氧化能力。采用人红细胞膜稳定法对提取物的抗炎活性进行了测试。采用Folin-Ciocalteu试验测定总酚含量。反相高效液相色谱-光电二极管阵列检测器(RP-HPLC-PDA)分析。结果:与对照相比,甲醇和水提液均表现出明显的自由基清除和抗炎活性(p)结论:本研究首次发现迷迭香酸在东洋中草药和根中存在。东方红的植物化学成分和有效生物活性解释了其传统用途,并表明其在制药工业中的应用潜力巨大。
{"title":"<i>Trachystemon orientalis</i> (L.) G. Don as a Valuable Source of Rosmarinic Acid: Biological Activities and HPLC Profiles.","authors":"Burak Bıyık,&nbsp;Sezen Yılmaz Sarıaltın,&nbsp;Alper Gökbulut,&nbsp;Tülay Çoban,&nbsp;Maksut Çoşkun","doi":"10.4274/tjps.galenos.2022.14265","DOIUrl":"https://doi.org/10.4274/tjps.galenos.2022.14265","url":null,"abstract":"<p><strong>Objectives: </strong><i>Trachystemon orientalis</i> (L.) G. Don, colloquially known in Türkiye as \"kaldırık\", is an edible plant belonging to the Boraginaceae. This plant has been practiced in traditional medicine for many years for its various therapeutic benefits. The effectiveness and chemical composition of plants can vary depending on their parts, age, and extraction solvent. Therefore, the current study aimed to define the biological activities of various parts and extracts of <i>T. orientalis</i>, which were collected in distinct seasons as young and mature, and investigate the main component responsible for these biological effects.</p><p><strong>Material and methods: </strong>Plant material was collected in different seasons from the northwest of Türkiye. 2,2'-Azinobis-(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activities were investigated to assess antiradical and antioxidant potential of the extracts. Anti-inflammatory activity of the extracts was also tested using human red blood cell membrane stabilizing method. Folin-Ciocalteu test was conducted to determine the total phenolic content. Reverse phase-high performance liquid chromatography-photodiode array detector (RP-HPLC-PDA) analysis was performed.</p><p><strong>Results: </strong>Both methanol and aqueous extracts exhibited significant radical scavenging and anti-inflammatory activities compared with control (<i>p</i><0.05). The highest percentage of inhibition on ABTS and DPPH free radicals was obtained in aqueous extracts of the mature herbs and roots, respectively. Methanol extracts of the mature roots and herbs exhibited the strongest anti-inflammatory capacity. Rosmarinic acid possessed a much higher antioxidant and anti-inflammatory effect than the reference compounds used in each assay in our study. High rosmarinic acid content of the extracts suggests that the compound responsible for the great biological activity potential is rosmarinic acid.</p><p><strong>Conclusion: </strong>To the best of our knowledge, the presence of rosmarinic acid in herbs and roots of <i>T. orientalis</i> was shown for the first time in our present study. Phytochemical composition and effective biological activities of <i>T. orientalis</i> explain its traditional use and indicate its significant potential in pharmaceutical industry applications.</p>","PeriodicalId":23378,"journal":{"name":"Turkish Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2023-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10337024/pdf/TJPS-20-141.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10164625","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Analytical Quality by Design Driven Development and Validation of UV-Visible Spectrophotometric Method for Quantification of Xanthohumol in Bulk and Solid Lipid Nanoparticles. 设计驱动的紫外可见分光光度法定量散装和固体脂质纳米颗粒中黄腐酚的分析质量
IF 1.7 Pub Date : 2023-07-07 DOI: 10.4274/tjps.galenos.2022.05335
Harish Vancha, Devesh Tewari, Rajesh Kumar, Pilli Govindaiah, Sharfuddin Mohd, Sachin Kumar Singh, Monica Gulati

Objectives: Xanthohumol (XH) is a prenylated chalcone available naturally and has diverse pharmacological activities. It has some limitations in the physiological environment such as biotransformation and less gastrointestinal tract absorption. To overcome the limitations, we prepared nanoformulations [solid lipid nanoparticles (SLNs)] of XH. Therefore, an analytical method is required for the estimation of XH in the bulk nanoformulations, so we developed and validated a quality by design (QbD)-based ultraviolet (UV)-spectrophotometric method as per the International Conference of Harmonization (ICH) Q2 (R1) guidelines.

Materials and methods: The new analytical Qbd based UV-visible spectrophotometric technique is developed and validated for estimation of XH in bulk and SLNs as per ICH guidelines Q2 (R1). Critical method variables are selected on the basis of risk assessment studies. Optimization of method variables was performed using the a central composite design (CCD) model.

Results: Multiregression ANOVA analysis showed an R2 value of 0.8698, which is nearer to 1, indicating that the model was best fitted. The optimized method by CCD was validated for its linearity, precision, accuracy, repeatability, limit of detection (LOD), limit of quantification (LOQ), and specificity. All validated parameters were found to be within the acceptable limits [% relative standard deviation (RSD) <2]. The method was linear between 2-12 g/mL concentration with R2 value 0.9981. Method was accurate with percent recovery 99.3-100.1%. LOD and LOQ were found to be 0.77 and 2.36 μg/mL, respectively. The precision investigation confirmed that the method was precise with %RSD <2.

Conclusion: The developed and validated method was applied to estimate XH in bulk and SLNs. The developed method was specific to XH, which was confined by the specificity study.

目的:黄腐酚(XH)是一种天然存在的烯丙基查尔酮,具有多种药理活性。它在生理环境中存在一些局限性,如生物转化和胃肠道吸收较少。为了克服这些限制,我们制备了XH的纳米配方[固体脂质纳米颗粒(SLNs)]。因此,需要一种分析方法来估计散装纳米制剂中的XH,因此我们根据国际协调会议(ICH) Q2 (R1)指南开发并验证了基于质量设计(QbD)的紫外(UV)-分光光度法。材料和方法:根据ICH指南Q2 (R1),开发并验证了新的基于分析Qbd的紫外可见分光光度法技术,用于估计散装和sln中的XH。在风险评估研究的基础上选择关键的方法变量。采用中心复合设计(CCD)模型对方法变量进行优化。结果:多元回归方差分析显示,R2值为0.8698,接近于1,表明模型拟合最佳。通过CCD对优化方法的线性度、精密度、准确度、重复性、检出限、定量限和专属性进行验证。结论:所建立并验证的方法可用于预估原料药和单药的XH。所建立的方法对XH具有特异性,受特异性研究的限制。
{"title":"Analytical Quality by Design Driven Development and Validation of UV-Visible Spectrophotometric Method for Quantification of Xanthohumol in Bulk and Solid Lipid Nanoparticles.","authors":"Harish Vancha,&nbsp;Devesh Tewari,&nbsp;Rajesh Kumar,&nbsp;Pilli Govindaiah,&nbsp;Sharfuddin Mohd,&nbsp;Sachin Kumar Singh,&nbsp;Monica Gulati","doi":"10.4274/tjps.galenos.2022.05335","DOIUrl":"https://doi.org/10.4274/tjps.galenos.2022.05335","url":null,"abstract":"<p><strong>Objectives: </strong>Xanthohumol (XH) is a prenylated chalcone available naturally and has diverse pharmacological activities. It has some limitations in the physiological environment such as biotransformation and less gastrointestinal tract absorption. To overcome the limitations, we prepared nanoformulations [solid lipid nanoparticles (SLNs)] of XH. Therefore, an analytical method is required for the estimation of XH in the bulk nanoformulations, so we developed and validated a quality by design (QbD)-based ultraviolet (UV)-spectrophotometric method as <i>per</i> the International Conference of Harmonization (ICH) Q2 (R1) guidelines.</p><p><strong>Materials and methods: </strong>The new analytical Qbd based UV-visible spectrophotometric technique is developed and validated for estimation of XH in bulk and SLNs as <i>per</i> ICH guidelines Q2 (R1). Critical method variables are selected on the basis of risk assessment studies. Optimization of method variables was performed using the a central composite design (CCD) model.</p><p><strong>Results: </strong>Multiregression ANOVA analysis showed an R2 value of 0.8698, which is nearer to 1, indicating that the model was best fitted. The optimized method by CCD was validated for its linearity, precision, accuracy, repeatability, limit of detection (LOD), limit of quantification (LOQ), and specificity. All validated parameters were found to be within the acceptable limits [% relative standard deviation (RSD) <2]. The method was linear between 2-12 g/mL concentration with R2 value 0.9981. Method was accurate with percent recovery 99.3-100.1%. LOD and LOQ were found to be 0.77 and 2.36 μg/mL, respectively. The precision investigation confirmed that the method was precise with %RSD <2.</p><p><strong>Conclusion: </strong>The developed and validated method was applied to estimate XH in bulk and SLNs. The developed method was specific to XH, which was confined by the specificity study.</p>","PeriodicalId":23378,"journal":{"name":"Turkish Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.7,"publicationDate":"2023-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10337025/pdf/TJPS-20-165.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9862696","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
期刊
Turkish Journal of Pharmaceutical Sciences
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