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Simulation of pharmacokinetic drug-drug interaction and dosage regimens optimization of nelfinavir and cepharanthine as a potential combination against COVID-19 奈非那韦与头孢酞啶联合抗COVID-19药代动力学相互作用模拟及用药方案优化
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.29090/psa.2023.01.22.375
Wichit Nosoongnoen
The pharmacokinetic (PK) drug-drug interactions (DDIs) of nelfinavir and cepharanthine combination is limited information in human. In addition, the dosage regimen of this combination is not available for COVID-19 treatment. The objective of this study was to perform in silico simulations using GastroPlusTM software to predict physicochemical properties, PK parameters using the physiologically based pharmacokinetic (PBPK) model of healthy adults in different dosage regimens. The DDIs analysis of nelfinavir and cepharanthine combination was carried out to optimize the dosage regimens as a potential against COVID-19. The Spatial Data File (SDF) format of nelfinavir and cepharanthine structures obtained from PubChem database were used to carry out in silico predictions for physicochemical properties and PK parameters using several aspects of modules such as ADMET Predictor, Metabolism and Transporter, PBPK model. Subsequently, all data were utilized in the DDIs simulations. The dynamic simulation feature was selected to calculate and investigate the Cmax, AUC0-120, AUC0-inf, Cmax ratio, AUC0-120 ratio, and AUC0-inf ratio. The victim or nelfinavir dosage regimens were used four oral administration regimens of 500 mg and 750 mg in every 8 and 12 hours for simulations. The perpetrator or cepharanthine oral dosage regimens were used in several regimens from 10 mg to 120 mg in every 8, 12, and 24 hours. From all predicted results, the dosage regimen as a potential combination against COVID-19 was nelfinavir 500 mg every 8 hours and cepharanthine 10 mg every 12 hours.Copyright © 2023 by Faculty of Pharmacy, Mahidol University, Thailand is licensed under CC BY-NC-ND 4.0. To view a copy of this license, visit https://www.creativecommons.org/licenses/by-nc-nd/4.0/.
奈非那韦联合头孢酞氨酸在人体内的药代动力学(PK) -药物相互作用(ddi)信息有限。此外,这种组合的给药方案不适用于COVID-19治疗。本研究的目的是利用GastroPlusTM软件进行计算机模拟,利用基于生理的药代动力学(PBPK)模型预测不同给药方案下健康成人的理化性质和药代动力学参数。通过ddi分析奈非那韦与头孢酞氨酸联合用药方案,优化抗COVID-19用药方案。利用PubChem数据库中获取的奈非那韦和头孢酞氨酸结构的空间数据文件(Spatial Data File, SDF)格式,利用ADMET Predictor、Metabolism and Transporter、PBPK模型等几个方面的模块对奈非那韦的理化性质和PK参数进行计算机预测。随后,将所有数据用于ddi模拟。选择动态仿真特征,对Cmax、AUC0-120、AUC0-inf、Cmax比率、AUC0-120比率和AUC0-inf比率进行计算和研究。采用受害者或奈非那韦剂量方案,每8和12小时口服500 mg和750 mg四种给药方案进行模拟。犯罪者或头孢酞菁口服剂量方案在每8、12和24小时从10毫克到120毫克的几个方案中使用。从所有预测结果来看,针对COVID-19的潜在联合用药方案是奈非那韦每8小时500毫克,头孢酞素每12小时10毫克。版权所有©泰国玛希隆大学药学院2023,CC by - nc - nd 4.0授权。要查看此许可证的副本,请访问https://www.creativecommons.org/licenses/by-nc-nd/4.0/。
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引用次数: 0
Assessment of pharmaceutical care services provided to HIV infected patients on antiretroviral therapy in Rivers state, Nigeria 评估尼日利亚河流州向接受抗逆转录病毒治疗的艾滋病毒感染者提供的药物保健服务
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.29090/psa.2023.02.22.332
Arloe ThankGod, I. Suleiman, T. Aremu
Pharmaceutical care of HIV infected persons on antiretroviral therapy is pertinent in optimal management to achieve viral suppression and improve immune status. The objective of the study was to assess pharmaceutical care services provided to HIV infected patients on antiretroviral therapy. A prospective, cross-sectional study was carried out among 217 pharmacists giving pharmaceutical care services to HIV positive patients in Rivers State, Nigeria. Data collection tool was a structured, pre-tested questionnaire used to assess pharmaceutical care services carried out by pharmacists. The data collected were analyzed using SPSS version 20 and Microsoft Excel. Most of the respondents were female (62.8%). More than half (59.9%) of the subjects involved in provision of pharmaceutical care to HIV infected patients were practicing in the hospital setting. Most respondents (77.8%) did not monitor for drug therapy problems (DTPs), while most (89.9%) did not document interventions to identified drug therapy problems. Majority of respondents (90.3%) established rapport with patients to improve adherence. Most respondents (72.5%) had regular supply of antiretroviral drugs in their health facility. Pharmaceutical care services rendered to HIV infected patients on antiretroviral therapy was sub-optimal. Identification of DTPs and respective interventions, involvement in general patient management, and documentation of activities were the most affected.
在抗逆转录病毒治疗中,HIV感染者的药学服务与优化管理有关,以实现病毒抑制和改善免疫状态。本研究的目的是评估向接受抗逆转录病毒治疗的艾滋病毒感染者提供的药学服务。一项前瞻性的横断面研究在217名药剂师中进行,这些药剂师为尼日利亚河流州的艾滋病毒阳性患者提供药物护理服务。数据收集工具是一份结构化的、预先测试的问卷,用于评估药剂师开展的药学服务。收集的数据使用SPSS version 20和Microsoft Excel进行分析。受访者中以女性居多(62.8%)。参与向艾滋病毒感染患者提供药学服务的受试者中,有一半以上(59.9%)在医院执业。大多数受访者(77.8%)没有监测药物治疗问题(dtp),而大多数(89.9%)没有记录干预措施以确定药物治疗问题。大多数应答者(90.3%)与患者建立了良好的关系,以提高依从性。大多数答复者(72.5%)的卫生机构定期提供抗逆转录病毒药物。对接受抗逆转录病毒治疗的艾滋病毒感染者提供的药学服务不够理想。确定dtp和相应的干预措施、参与一般患者管理和记录活动受到的影响最大。
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引用次数: 0
Current advances in nose to brain drug delivery 鼻到脑给药的最新进展
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.29090/psa.2023.03.23.477
Venkatesh Prasad S, P. Sudheer, Kannika Belludi Chandrashekhar Shetty
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引用次数: 0
The use of hydrophilic carrier derived from eggshell and novel gel forming technique in a solid dispersion system 在固体分散体系中使用蛋壳亲水性载体和新型凝胶形成技术
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.29090/psa.2023.01.22.339
Zarni Myint, P. Lawanprasert, S. Puttipipatkhachorn, J. Leanpolchareanchai
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引用次数: 0
Design, synthesis, and evaluation of indoleamin-2,3-dioxygenase 1 inhibition activity of novel 5/6-amino indazole derivatives with amide template 基于酰胺模板的新型5/6-氨基吲哚胺-2,3-双加氧酶1抑制活性的设计、合成及评价
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.29090/psa.2023.01.22.309
Ngo Xuan Hoang, T. Vo, Van-Hai Hoang, T. K. Nguyen, J. Seo, Phuong-Thao Tran
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引用次数: 0
Formulation of topical gel containing Tagetes erecta L. floral extract and its antibacterial activity 万寿菊花提取物外用凝胶的研制及其抑菌活性
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.29090/psa.2023.02.22.369
Papangkorn Meetong, Pattarapol Ananchaiphatthana, Chawalinee Asawahame, Phurit Thanarangsarit, Aranya Jutiviboonsuk
Tagetes erecta L. (marigold) flowers were extracted to obtain crude ethanolic extract (MGE), water insoluble extract (MGP), as well as water soluble extract (MGW). All extracts were determined of total flavonoid content and antibacterial activities against Staphylococcus aureus and Pseudomonas aeruginosa . The results suggested that MGP contained the highest amount of total flavonoids (29.48%w/w quercetin equivalent) with good activity against S. aureus (MIC 6.25 mg/mL and MBC 25.0 mg/mL). This extract was subjected to formulate the topical gels at the concentration of 1 and 2 times of MIC. The gel formulation containing 1.25%w/w MGP with the solvent mixture of propylene glycol and ethanol (1:1) showed good physical properties. Furthermore, it exhibited the most effective antibacterial activity against S. aureus by agar well diffusion method with the inhibition zone of 15.15±0.43 mm. Therefore, the extract of marigold flower could be formulated as topical gel for the treatment of skin infections.
对万寿菊(Tagetes erecta L.)花进行提取,得到粗乙醇提取物(MGE)、水不溶提取物(MGP)和水溶性提取物(MGW)。测定各提取物的总黄酮含量及对金黄色葡萄球菌和铜绿假单胞菌的抑菌活性。结果表明,MGP总黄酮含量最高(槲皮素当量为29.48%w/w),对金黄色葡萄球菌具有良好的抑菌活性(MIC为6.25 mg/mL, MBC为25.0 mg/mL)。将该提取物以MIC的1倍和2倍浓度配制外用凝胶。以丙二醇与乙醇(1:1)为溶剂,含1.25%w/w MGP的凝胶配方具有良好的物理性能。琼脂孔扩散法对金黄色葡萄球菌的抑菌效果最好,抑菌带为15.15±0.43 mm。因此,万寿菊提取物可配制成外用凝胶治疗皮肤感染。
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引用次数: 0
Association of the rs1128503 and rs1045642 polymorphisms in the MDR-1 gene with steroid responsiveness in Iraqi children with idiopathic nephrotic syndrome 伊拉克特发性肾病综合征儿童耐多药1基因rs1128503和rs1045642多态性与类固醇反应性的关系
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.29090/psa.2023.03.23.245
A. M. A. Alridha, D. Kadhim, A. Alkhazrajy
Steroid-resistant nephrotic syndrome (SRNS) is a leading cause of end-stage renal disease in children, with an increasing number of cases. Polymorphisms in the MDR-1 gene were reported to contribute to SRNS development, but with varying results among different ethnicities. Thus, we investigated the association of the MDR-1 rs1128503 (C1236T) and rs1045642 (C3435T) polymorphisms with steroid responsiveness in Iraqi children with idiopathic nephrotic syndrome (INS). This case-control study was conducted at the Babylon Hospital for Maternity and Pediatrics. Children with SRNS (n=32) and steroid-sensitive nephrotic syndrome (SSNS; n=32) were genotyped via the polymerase chain reaction-restriction fragment length polymorphism. The genotypes were subjected to association testing and haplotype analysis. The C1236T TT genotype was associated with a higher risk of developing SRNS compared to the CC and TC genotypes (odds ratio [OR]=10.33, 95% confidence interval [95% CI]=1.208-88.362; p -value=0.026; recessive model). The combination of the two TT genotypes of C1236T and C3435T variants was significantly more frequent ( p -value=0.029) in SRNS (88.9%) than in SSNS (11.1%). The haplotype analysis showed no association between the C1236T and C3435T haplotypes and steroid responsiveness, but the TC haplotype was associated with an age at onset of ≥8 years ( p -value=0.0028). In conclusion, this study revealed that children who have the MRD-1 C1236T TT genotype alone or combined with the C3435T TT genotype may be at increased risk of developing SRNS and in need of other therapeutic strategies. Additional research is required to identify other genetic contributions to steroid responsiveness and further understand their
类固醇抵抗性肾病综合征(SRNS)是儿童终末期肾病的主要原因,病例数量不断增加。据报道,耐多药-1基因的多态性有助于SRNS的发展,但不同种族的结果不同。因此,我们研究了MDR-1 rs1128503 (C1236T)和rs1045642 (C3435T)多态性与伊拉克特发性肾病综合征(INS)儿童类固醇反应性的关系。这项病例对照研究是在巴比伦妇产儿科医院进行的。伴有SRNS (n=32)和类固醇敏感肾病综合征(SSNS;N =32)通过聚合酶链反应-限制性片段长度多态性进行基因分型。基因型进行关联检验和单倍型分析。与CC和TC基因型相比,c1236ttt基因型发生SRNS的风险更高(优势比[OR]=10.33, 95%可信区间[95% CI]=1.208-88.362;p值= 0.026;隐性模型)。C1236T和C3435T两种TT基因型的组合在SRNS(88.9%)中显著高于SSNS (11.1%) (p值=0.029)。单倍型分析显示C1236T和C3435T单倍型与类固醇反应性无相关性,但TC单倍型与发病年龄≥8岁相关(p值=0.0028)。总之,本研究表明,单纯携带MRD-1 c1236ttt基因型或与c3435ttt基因型合并携带MRD-1 c1236ttt基因型的儿童发生SRNS的风险可能增加,需要其他治疗策略。需要进一步的研究来确定其他遗传因素对类固醇反应性的影响,并进一步了解它们
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引用次数: 0
The effect of different sweeteners on the free radical scavenging activities, alcohol contents, sugar reductions, and hedonic properties of green tea kombucha 不同甜味剂对绿茶康普茶自由基清除活性、酒精含量、糖还原和享乐特性的影响
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.29090/psa.2023.01.22.340
Muhammad Shidiq Rukman, Ayu Nala El Muna Haerussana
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引用次数: 1
Study on consequences for interaction of myricetin with canagliflozin: A special attention to pharmacokinetics and pharmacodynamics of drug 杨梅素与卡格列净相互作用的后果研究:特别关注药物的药代动力学和药效学
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-01-01 DOI: 10.29090/psa.2023.01.22.304
Naga Raju Kandukoori, Deepika B, Kiranmai Mandava
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引用次数: 0
Screening for production of amylase and protease by locally-isolated Bacillus spp. from soil collected in Taguig City and Clark Freeport Zone, Philippines 菲律宾塔吉格市和克拉克自由港地区土壤中分离的芽孢杆菌产淀粉酶和蛋白酶的筛选
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-01-01 DOI: 10.29090/psa.2022.02.21.156
John Paul Matthew Guzman, Sheila Mantaring, E. Panerio
Amylase and protease are two of the most commonly used enzymes in the pharmaceutical industry. Particularly, Bacillus spp. is widely regarded as a “factory” of these enzymes. In this study, a total of 40 isolates were collected from four soil samples from different metropolitan sites namely, near Chemicals and Energy Division (CED), and National Metrology Laboratory (NML) oil tankers parking lot inside the Department of Science and Technology (DOST) Compound in Taguig City, and two metropolitan-volcanic sites in Clark Freeport Zone, Pampanga (CRK1, CRK2). Of these, 33 isolates were deemed putative Bacillus spp. via phenotypic assays and were screened for the production of amylase and protease. Results showed that 26 of the screened isolates were able to produce protease and 12 were positive for amylase production. Molecular identification revealed that the enzyme-producing isolates were Bacillus spp., B. cereus, B. aryabhattai, B. amyloliquefaciens, B. firmus , B. velezensis , and Fictibacillus sp. No isolate was able to produce amylase alone. These results show the potential of Bacillus spp. from metropolitan soil as sources of pharmaceutically-important enzymes.
淀粉酶和蛋白酶是制药工业中最常用的两种酶。特别是,芽孢杆菌被广泛认为是这些酶的“工厂”。在本研究中,共从4个不同的大都市站点的土壤样本中收集了40个分离株,这些站点分别是大庆市科技部(DOST)大院内化学和能源部门(CED)和国家计量实验室(NML)油轮停车场附近,以及邦板卡克拉克自由港区(CRK1, CRK2)的两个大都市-火山站点。其中33株菌株经表型鉴定为芽孢杆菌,并进行淀粉酶和蛋白酶的筛选。结果表明,筛选的分离株中有26株能产生蛋白酶,12株淀粉酶产生阳性。分子鉴定结果表明,产酶菌株为芽孢杆菌、蜡样芽孢杆菌、aryabhattai芽孢杆菌、解淀粉芽孢杆菌、B. firmus、B. velezensis和Fictibacillus sp.。这些结果表明,从都市土壤中提取的芽孢杆菌具有作为重要药用酶来源的潜力。
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引用次数: 1
期刊
Pharmaceutical Sciences Asia
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