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Formulation and in vitro /in vivo Evaluation of Silymarin Solid Dispersion- Based Topical Gel for Wound Healing 水飞蓟素固体分散体外用伤口愈合凝胶的配方及体外/体内评价
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-01 DOI: 10.31351/vol32isssuppl.pp42-53
Bushra Malik, Eman Bekir
Silybum marianum, from which silymarin (SM) is extracted, is a medicinal herb. In the Biopharmaceutics Classification System, it is of the class II type, meaning it is almost completely insoluble in water. It has a number of therapeutic properties, including anti-inflammatory as well as properties that promote wound healing. This research target is to promote the dissolution and solubility of SM by employing a technique called solid dispersion and then incorporating the formula of solid dispersion into a topical gel that can be used for wound healing. Solid dispersion is a technique used to enhance solubility and dissolve pharmaceuticals that are not water-soluble. This method is widely used because of its low cost and high efficiency. Because of its capacity to repair skin, the hydrophilic carrier nicotinamide (NA) was selected in this investigation as the carrier. Kneading, solvent evaporation and fusion with a consistent drug-to-carrier ratio were the three separate processes utilized in the preparation of solid dispersion (1:1, 1:3, and 1:5). In addition, the products were examined to determine their physical characteristics and the degree of crystallinity. The selected formula was combined into a hyaluronic acid base gel using the cold method. This gel was then evaluated in vitro for physical qualities and put to an in vivo (animal) examination to determine how it healed wounds. The study found that the solvent evaporation made SM 25 times more soluble and caused all of it to be released in 20 minutes for a 1:3 ratio. Additional research using DSC and XRD demonstrated the amorphous nature of the result. According to FTIR, there was no evidence of interaction between the two. The gel formula had good qualities, like a pH of 6.6, good spreadability, and drug release within three hours. It also contributed to the rapid healing of wounds.
水飞蓟(Silybum marianum)是一种草药,从其中提取水飞蓟素(SM)。在生物制药分类系统中,它属于II类,这意味着它几乎完全不溶于水。它有许多治疗特性,包括抗炎和促进伤口愈合的特性。本研究的目标是通过采用固体分散技术促进SM的溶解和溶解度,然后将固体分散配方纳入可用于伤口愈合的局部凝胶中。固体分散是一种用于提高溶解度和溶解非水溶性药物的技术。该方法成本低、效率高,得到了广泛的应用。由于其修复皮肤的能力,本研究选择亲水性载体烟酰胺(NA)作为载体。混合、溶剂蒸发和药载比一致的融合是制备固体分散体(1:1、1:3和1:5)的三个独立工艺。此外,对产品进行了检测,以确定其物理特性和结晶度。将选定的配方用冷法制成透明质酸基凝胶。然后在体外评估这种凝胶的物理特性,并进行体内(动物)检查,以确定它如何愈合伤口。研究发现,溶剂蒸发使SM的可溶性提高25倍,并使其在20分钟内以1:3的比例全部释放。进一步的DSC和XRD研究证明了结果的无定形性质。根据FTIR,没有证据表明两者之间存在相互作用。凝胶配方pH值为6.6,涂抹性好,3小时内释药。它也有助于伤口的快速愈合。
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引用次数: 0
Protective Effect of Cafestol on Doxorubicin-induced Genotoxicity in Rats 咖啡醇对阿霉素致大鼠遗传毒性的保护作用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-01 DOI: 10.31351/vol32isssuppl.pp16-25
None Sara A. Al-Kenany, Nada N. Al-Shawi
Doxorubicin is an efficient antineoplastic agent that has a broad antitumour spectrum; however, its genotoxic adverse effects on normal cells can be produced through oxidative damage, and this limits its clinical application. Cafestol is a naturally-occurring diterpene in unfiltered coffee with noteworthy antioxidant, antimutagenic and anti-inflammatory activities. The present study aimed to investigate the possible protective effect of cafestol against doxorubicin-induced chromosomal and DNA damage in rat bone marrow cells. Wistar Albino rats of both sexes were administered cafestol (5mg/kg body weight once daily for 14 consecutive days) by oral gavage alone or with doxorubicin which was injected as a single dose (90 mg/kg intraperitoneally at day 14) to induce toxicity. The bone marrow was harvested 24 hours after doxorubicin’s injection in all groups for the assessment of structural chromosomal aberration, micronucleus, and comet assays. The result showed that rats in the doxorubicin-only group exhibited a significant decrease (P<0.05) in mitotic index with a significant elevation (P<0.05) in the % DNA in Tail, micronucleus appearance and total structural chromosomal aberrations compared to those of the negative control group; while oral administration of cafestol 14 days prior to doxorubicin, significantly-reduced the % DNA in Tail, micronucleus appearance, and the total number of chromosomal aberrations (P<0.05), and improved the mitotic index compared to rats intraperitoneally-injected with doxorubicin alone. This study revealed that cafestol has protective effects against the genotoxicity induced by doxorubicin.
阿霉素是一种有效的抗肿瘤药物,具有广泛的抗肿瘤谱;然而,其可通过氧化损伤对正常细胞产生遗传毒性不良反应,这限制了其临床应用。咖啡醇是未经过滤的咖啡中天然存在的二萜,具有显著的抗氧化、抗诱变和抗炎活性。本研究旨在探讨咖啡醇对阿霉素诱导的大鼠骨髓细胞染色体和DNA损伤的保护作用。纯种# x0D;用咖啡醇(5mg/kg体重,每天1次,连续14天)单独灌胃或与阿霉素(90 mg/kg,第14天腹腔注射)联合诱导毒性。各组注射阿霉素24小时后采集骨髓,进行染色体畸变、微核和彗星检测。结果表明,与阴性对照组相比,阿霉素组大鼠有丝分裂指数显著降低(P<0.05),尾区% DNA、微核外观和总染色体结构畸变显著升高(P<0.05);与单独腹腔注射阿霉素相比,口服咖啡醇可显著降低小鼠尾部% DNA、微核外观和染色体畸变总数(P<0.05),并提高有丝分裂指数。& # x0D;本研究表明,咖啡醇对阿霉素的遗传毒性具有保护作用。
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引用次数: 0
Possible Effects of Vitamin D3 and Levofloxacin on Selected Hematology Parameter of Rats 维生素D3和左氧氟沙星对大鼠血液学参数的可能影响
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-01 DOI: 10.31351/vol32isssuppl.pp74-84
Abbas Muslim Mhaibes, Farah Kais Abdul- Wahab2
Vitamin D is a fat-soluble vitamin with antioxidant and DNA protecting properties , Levofloxacin is a member of the fluoroquinolone drug class, Its broad-spectrum bactericidal effect affects both Gram-positive and Gram-negative bacteria. The goal of the study is to analyze the haematology analysis in rats received levofloxacin and show the preventive impact of vitamin D3 by analyzing the haematology parameters: packed cell volume (PCV), mean corpuscular hemoglobin concentration(MCHC),haemoglobin (HB), red blood cell (RBC), mean corpuscular volume (MCV),meancorpuscular haemoglobin(MCH), WBC ,differential WBC, and Platelets. The study included 42 rats divided into 6 groups each group 7 rats. group I negative control : healthy animals received normal saline 0.9%, group II: received levofloxacin LFX dose of 50mg/kg/day (IP) for fourteen days, group III : received LFX 100mg/kg/day (IP) for fourteen days, group IV : received vitamin D3 500 IU/day orally by oral gavage for twenty one days, group V received vitamin D3 500 IU/day orally for twenty one days and levofloxacin 50 mg/kg/day IP injected at day 8 for fourteen days, group VI received vitaminD3 500IU/day for twenty one days orally and levofloxacin 100 mg/kg/day IP injected at day 8 for fourteen days. Blood samples taken from rats treated with levofloxacin, showed a decrease in the values of RBC, HB, PCV, MCH, MCHC, as well as a decrease in total white blood cells, then returned approximately to normal levels in the groups IV ,group V and group VI . from the result of the study conclude that some haematological changes caused by levofloxacin ameliorated by vitamin D3 may be due to indirect effect of vitamin D3 on haematology parameters.
维生素D是一种脂溶性维生素,具有抗氧化和保护DNA的特性,左氧氟沙星是氟喹诺酮类药物中的一员,它对革兰氏阳性菌和革兰氏阴性菌都有广谱杀菌作用。 本研究的目的是分析左氧氟沙星治疗大鼠的血液学分析,并通过分析血液学参数:堆积细胞体积(PCV)、平均红细胞血红蛋白浓度(MCHC)、血红蛋白(HB)、红细胞(RBC)、平均红细胞体积(MCV)、平均红细胞血红蛋白(MCH)、白细胞计数、差异白细胞计数和血小板计数来显示维生素D3的预防作用。实验选用大鼠42只,分为6组,每组7只。ⅰ组阴性对照:健康动物给予生理盐水0.9%,ⅱ组:给予左氧氟沙星LFX剂量50mg/kg/天(IP)连用14天,ⅲ组:给予LFX 100mg/kg/天(IP)连用14天,ⅳ组:给予维生素D3 500IU/天口服灌胃,连续21天,V组给予维生素D3 500IU/天口服21天,第8天注射左氧氟沙星50 mg/kg/天IP,连续14天,VI组给予维生素D3 500IU/天口服21天,第8天注射左氧氟沙星100 mg/kg/天IP,连续14天。 左氧氟沙星处理后大鼠血液中RBC、HB、PCV、MCH、MCHC值降低,白细胞总数减少,但在IV、V、VI组近似恢复到正常水平。 从研究结果得出,维生素D3改善左氧氟沙星引起的一些血液学变化可能是由于维生素D3对血液学参数的间接影响。
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引用次数: 0
Synthesis, Characterization, and Preliminary Evaluation of Antimicrobial activity of Imines derived from Vanillic Acid Conjugated to Heterocyclic 香草酸偶联杂环亚胺的合成、表征及抗菌活性初步评价
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-01 DOI: 10.31351/vol32isssuppl.pp8-15
Noor Ali Sabzi, May Mohammed Jawad
The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(substituted amino)-5-mercapto-4H-1,2,4-1triazol-3-yl)-2-methoxy phenol derivatives (5-8). These compounds were characterized spectroscopically by FT-1IR and 1H-1NMR. These imine derivatives (5-8) were tested for their antimicrobial activity and compared with three different standard references (amoxicillin, ciprofloxacin, and fluconazole). Overall, compounds 6 and 8 exhibited varying degrees of inhibitory effects on the growth of the examined bacterial species and fungus. The most active one is compound 6 having pyrrole ring imine derivative showed potent activity against C. 1albicans and moderate activity against all tested bacteria compared to other derivatives but no activity toward P. 1aeruginosa and P. 1mirabilis.
本研究的目的是制备新的1,2,4-三唑-3-硫醇杂环香草酸衍生物,并对其抗菌活性进行初步评价。建立了一种新的香草酸-三唑缀合物的多步合成方法。4-(4-氨基-5-巯基- 4h -1,2,4-三唑-3-基)-2-甲氧基苯酚中间体(4)在含有少量乙酸的乙醇中与不同的杂环醛(噻吩-2-甲醛、吡咯-2-甲醛、噻吩-3-甲醛和糠醛)反应,生成相应的4-(4-(取代氨基)-5-巯基- 4h -1,2,4-1三唑-3-基)-2-甲氧基苯酚衍生物(5-8)。这些化合物通过FT-1IR和1H-1NMR进行了光谱表征。对这些亚胺衍生物(5-8)进行了抗菌活性测试,并与三种不同的标准参比(阿莫西林、环丙沙星和氟康唑)进行了比较。总的来说,化合物6和8对所检测的细菌和真菌的生长表现出不同程度的抑制作用。活性最高的是含有吡咯环亚胺衍生物的化合物6,与其他衍生物相比,对白色念珠菌有较强的活性,对所有被试细菌都有中等的活性,但对铜绿假单胞菌和奇异假单胞菌没有活性。
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引用次数: 0
Assessment of ellagic acid action in 5-fluorouracil induced intestinal mucositis 鞣花酸在5-氟尿嘧啶诱导的肠黏膜炎中的作用评价
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-01 DOI: 10.31351/vol32isssuppl.pp33-41
Dareen Al-hoshary, None Munaf H. Zalzala
The intestinal mucositis define as inflammation and ulceration in the gastrointestinal tract wall and in some case in the oral cavity these cause by treatment with antineoplastic drug like 5-fluorouracil and Irinotecan and other types of chemotherapeutics drugs , 5-Fluorouracil-induced intestinal mucositis (IM) is consider as one of the more common tumor issue .it cause series of undesirables symptoms like severe diarrhea ,abdominal pain , stomach uncomfortable and other. The aim of this current study to see how ellagic acid act to Attenuates 5-FU-Induced Intestinal Mucositis and Diarrhea in Mice . we induced the intestinal mucositis by injected the mice intraperitoneally in 5-fluorouracil about 50mg per kg daily for four days respectively and then assessment the IM by measurement the level of some antioxidant enzymes like SOD , and level of some pro-inflammatory cytokines (IL-6) and lipid peroxidation biomarker (MDA) and we note the difference in the histopathological scoring after administration the ellagic acid to the mice in two different dose (10mg and 5mg per kg) daily for ten days respectively and before the fluorouracil injection in one hour .pretreatment with ellagic acid specialized dose of 10mg per kg significant improvement in the level of antioxidant enzymes ,pro inflammatory cytokines ,lipid peroxidation biomarker and histopathologicaL score compared with 5-FU group, moreover the potential action of ellagic acid was further supported by histopathological examination. all these data suggest that the ellagic acid effective in protective from 5-FU-induced intestinal mucositis.
5-氟尿嘧啶诱导的肠道黏膜炎(IM)被认为是较为常见的肿瘤疾病之一,可引起严重的腹泻、腹痛、胃部不适等一系列不良症状。5-氟尿嘧啶诱导的肠道黏膜炎是由5-氟尿嘧啶、伊立替康等抗肿瘤药物及其他类型的化疗药物引起的胃肠道壁及部分口腔的炎症和溃疡。本研究的目的是观察鞣花酸如何减轻5- fu诱导的小鼠肠黏膜炎和腹泻。我们分别腹腔注射5-氟尿嘧啶50mg / kg / d,连续4天诱导小鼠肠黏膜炎,然后通过测定SOD等部分抗氧化酶的水平来评估IM。并观察了花鞣花酸给药10天后(10mg / kg和5mg / kg)和注射氟尿嘧啶前1小时(10mg / kg)小鼠抗氧化酶、促炎细胞因子和脂质过氧化生物标志物(MDA)水平的差异生物标志物和组织病理学评分与5-FU组比较,组织病理学检查进一步支持鞣花酸的潜在作用。提示鞣花酸对5- fu诱导的肠黏膜炎具有保护作用。
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引用次数: 0
Possible Anti-Asthmatic Effect of Iraqi Ammi Majus Seeds Extract Against Asthma Induced by Ovalbumin in Mice 伊拉克蜜籽提取物对卵清蛋白诱导小鼠哮喘可能的抗哮喘作用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-01 DOI: 10.31351/vol32isssuppl.pp1-7
None Zainab T. Younis, Shihab H. Mutlag
Asthma is a chronic respiratory disorder of airways characterized by inflammation, hyperresponsiveness, inflammatory cell infiltration, mucous secretion, and remodelling. Ammi majus is medicinal plant belong to family of Apiaceous which has anti-inflammatory and antioxidant activities. This study designed to investigate of anti-asthmatic activity of alcoholic extract of Ammi majus in improvement of asthma. Forty-eight healthy female mice divided to six groups Group I: the negative control group (distal water only), Group II: Positive control group (ovalbumin group), Group III: Ammi majus (64 mg/kg/day) with sensitization, Group IV:Ammi majus (128 mg/kg/day) with sensitization, Group V: Ammi majus (64 mg/kg/day) without sensitization, Group VI: Ammi majus (128mg/kg/day) without sensitization. Mice were sacrificed by diethyl ether and blood samples were collected to prepare of serum samples that used in ELISA kits for measuring of parameter IL-4, IL-5, IL-33, & IgE. Levels of all parameters (IL-4, IL-5, IL-33, & IgE) for mice of treated groups with alcoholic extract of Ammi majus were highly significant reduced (p<0.05) in compared to ovalbumin group.in conclusion, our results demonstrated that alcoholic extract of Ammi majus has a potent anti asthmatic activity that improved ovalbumin-induced asthma.
哮喘是一种慢性呼吸道疾病,以炎症、高反应性、炎症细胞浸润、粘液分泌和气道重塑为特征。麻麻是一种具有抗炎、抗氧化作用的药用植物。本研究旨在探讨麻草醇提物对哮喘的改善作用。48只健康雌性小鼠分为6组:ⅰ组:阴性对照组(仅远端水),ⅱ组:阳性对照组(卵清蛋白组),ⅲ组:致敏的氨水(64 mg/kg/d),ⅳ组:致敏的氨水(128mg/kg/d),ⅴ组:不致敏的氨水(64 mg/kg/d),ⅵ组:不致敏的氨水(128mg/kg/d)。采用乙醚法处死小鼠,采集血样制备血清样品,用于ELISA试剂盒中IL-4、IL-5、IL-33、和amp等参数的测定;IgE。各项参数(IL-4、IL-5、IL-33、&与卵清蛋白组相比,麻豆醇提物处理组小鼠的IgE水平显著降低(p < 0.05)。综上所述,我们的研究结果表明,大鼠酒提取物具有有效的抗哮喘活性,可以改善卵清蛋白诱导的哮喘。
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引用次数: 0
Effectiveness of Myoinositol alone or in Companion with Metformin in Improving Hormonal, Metabolic, and Clinical Features of PCOS Women 肌醇单用或联用二甲双胍改善PCOS女性激素、代谢和临床特征的有效性
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-01 DOI: 10.31351/vol32isssuppl.pp61-73
Zainab Abdulhameed Alnisani, None Manal Khaled Abdulrida
Polycystic ovary syndrome (PCOS) referring to a syndrome that is recognized as a life-course disease and has both metabolic and reproductive signs; main pathophysiological cause includes insulin resistance, hyperandrogenism, and oxidative stress state. The study aimed to assess the impact of combining Myoinositol and Metformin, the main insulin-sensitizing drugs, on improving clinical, metabolic, and hormonal parameters in females with PCOS. A clinical trial that was prospective, randomized, and comparative on 54 patients (aged 18-40 y) are divided into three groups: group1 patients allocated to receive Myo-inositol(4g), group2 patients assigned to receive Metformin(1g) and group3 patients assigned to receive Myo-inositol(4g) + Metformin(1g) all for three months. Baseline and post-intervention fasting blood samples were collected to evaluate hormonal, metabolic parameters, and oxidative stress biomarkers. Metformin and Myoinositol together lead to a significant drop free testosterone (P = 0.002), LH (P 0.003), LH to FSH ratio(P=0.004), FSI (P 0.012), the HOMA IR (p 0.019), hirsutism score (p=<0.001) and acne score (p= 0.003), besides substantial increase in GPX (P 0.02). Meanwhile, Myoinositol supplement causes a substantial drop in free testosterone (p=0.013), FSI (P 0.02), and HOMA – IR (P value=0.025) also a substantial rise in GPX (P=0.005). Combining Myoinositol with metformin results in improving clinical, metabolic, hormonal parameters, as well as oxidative indicators for PCOS females.
多囊卵巢综合征(PCOS)指的是一种被认为是一种终身疾病,同时具有代谢和生殖体征的综合征;主要病理生理原因包括胰岛素抵抗、高雄激素和氧化应激状态。该研究旨在评估肌醇联合二甲双胍(主要的胰岛素增敏药物)对改善PCOS女性患者临床、代谢和激素参数的影响。一项前瞻性、随机和比较的临床试验将54例患者(18-40岁)分为三组:组1患者分配给myo -肌醇(4g),组2患者分配给二甲双胍(1g),组3患者分配给myo -肌醇(4g) +二甲双胍(1g),均为三个月。收集基线和干预后空腹血液样本,评估激素、代谢参数和氧化应激生物标志物。二甲双胍和肌醇联合使用可显著降低游离睾酮(P= 0.002)、LH (P= 0.003)、LH / FSH比值(P=0.004)、FSI (P 0.012)、HOMA IR (P 0.019)、多毛症评分(P= <0.001)和痤疮评分(P= 0.003), GPX显著升高(P 0.02)。同时,肌醇补充使游离睾酮显著降低(p=0.013), FSI显著降低(p= 0.02), HOMA - IR显著降低(p= 0.025), GPX显著升高(p= 0.005)。肌醇联合二甲双胍可改善PCOS女性的临床、代谢、激素参数以及氧化指标。
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引用次数: 0
Preparation and characterization of Posaconazole as a Nano-micelles using d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) d-α-生育酚聚乙二醇1000琥珀酸酯(TPGS)制备泊沙康唑纳米胶束及表征
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-01 DOI: 10.31351/vol32isssuppl.pp26-32
Alaa abdul elah Abdulqader, Nawal A. Rajab Sultan
It is important to note that Posaconazole (POCZ) is a newly developed extended-spectrum triazole that belongs to BCS class II and has a solubility of less than 1µg/ml. In patients with a weakened immune system, POCZ has been shown to be effective as an antifungal treatment for invasive infections caused by candida and aspergillus species. The nano-micelles technique can be used to increase POCZ solubility. In order to increase their apparent solubility in water, nano-micelles are made by combining macromolecules that self-assemble into ordered structures capable of entrapping hydrophobic drug molecules in the interior domain. Dispersed colloidal systems, of which nano-micelles are a subset, are a large and diverse group. Composed of a phase that is itself dispersed throughout a medium (continuous phase). Surfactants form a colloidal solution when their concentration in solution is higher than their critical micelle concentration (CMC). POCZ nano-micelles are made with TPGS and tween 80. In this study, we prepared six different formulations and analyzed their particle size, polydispersity index (PDI), entrapment efficiency (EE), drug loadings (DL), saturation solubility, and in-vitro release. The drug-loaded nano-micelles of the Posaconazole formula (POCZ6) were characterized, and their properties were found to be: Particle size (90.68 nm), PDI (0.27), EE (94%), DL (10.3%), and best solubility factor (1133) are all better in the TPGS: tween80(1:5:3) ratio than in the pure drug. An in-vitro release study was conducted, and the results showed that the chosen formula POCZ6 released the entire dose of drug in 70 minutes, compared to only 23% for pure drug. Fourier transform infrared microscopy and other forms of investigation (FTIR). As can be seen from the data, there are no interactions or changes in the major peaks of Posaconazole when it is combined with polymer and surfactant.
泊沙康唑(Posaconazole, POCZ)是一种新开发的扩展谱三唑,属于BCS II类,溶解度小于1µg/ml。在免疫系统较弱的患者中,POCZ已被证明是一种有效的抗真菌治疗由念珠菌和曲霉引起的侵袭性感染。纳米胶束技术可以提高POCZ的溶解度。为了增加其在水中的表观溶解度,纳米胶束是由大分子组合而成的,这些大分子自组装成有序的结构,能够在内部区域内包裹疏水药物分子。分散胶体系统是一个庞大而多样的群体,纳米胶束是其中的一个子集。由本身分散在介质中的相组成的(连续相)。当表面活性剂在溶液中的浓度高于临界胶束浓度(CMC)时,表面活性剂会形成胶体溶液。用TPGS和t80制备了POCZ纳米胶束。在本研究中,我们制备了6种不同的配方,并分析了它们的粒径、多分散指数(PDI)、包封效率(EE)、载药量(DL)、饱和溶解度和体外释放度。对泊沙康唑配方(POCZ6)的载药纳米胶束进行了表征,结果表明:在TPGS: tween80(1:5:3)比下,其粒径(90.68 nm)、PDI(0.27)、EE(94%)、DL(10.3%)和最佳溶解度(1133)均优于纯药物;体外释放研究结果表明,所选择的配方POCZ6在70分钟内释放全剂量药物,而纯药的释放率仅为23%。傅里叶变换红外显微镜和其他形式的调查(FTIR)。从数据可以看出,泊沙康唑与聚合物和表面活性剂结合时,其主峰没有相互作用,也没有变化。
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引用次数: 0
Protective Effect of Daidzein on Ifosfamide-Induced Neurotoxicity Via Improving Some Selected Oxidative Stress Parameters in Male Rats 大豆苷元通过改善氧化应激参数对异环磷酰胺诱导的雄性大鼠神经毒性的保护作用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-01 DOI: 10.31351/vol32isssuppl.pp53-60
Hiba Zaki Hammodi, Nada Naji Al-Shawi
In this study, the possible protective effects of daidzein on ifosfamide-induced neurotoxicity in male rats were examined by the determination of changes in selected oxidant–antioxidant markers of male rats’ brain tissue. Twenty-eight (28) apparently-healthy Wistar male rats weighing (120-150gm) allocated into 4 groups (n=7) were used in this study. Rats orally-administered 1% tween 20 dissolved in distilled water/Control (Group I); rats were orally-administered daidzein suspension (100mg/kg) for 7 days (Group II); rats intraperitoneally-injected with a single dose of ifosfamide (500 mg/kg) (Group III); rats orally-administered for 7 days with the daidzein (100mg/kg) before a single intraperitoneal dose of ifosfamide (500 mg/kg) at day 7 (Group IV). Twenty-four (24) hours after the end of treatment, determination of the malondialdehyde, reduced glutathione, and superoxide dismutase enzyme activity levels in the rats’ brain tissue homogenate were performed; in addition to the histopathological examination of the brain tissues sections. Results showed that the levels of malondialdehyde in brain tissue were significantly-increased (P<0.05) in (Group III/ifosfamide-only) rats compared to such level in the rats’ brain tissue of controls (Group I). Furthermore, the brain tissue level of the malondialdehyde was significantly-decreased (P<0.05) in rats of Group IV (orally-administered DZN prior to IFO) compared to such tissue level in rats of Group III. Moreover, the brain levels of each of the reduced glutathione and the superoxide dismutase enzyme activity were significantly-decreased (P<0.05) in (Group III) compared to each level in those of Group I. Additionally, the brain levels of each of the antioxidant parameters was significantly-increase (P<0.05) in Group IV rats compared to each of these tissue levels in rats of Group III. As a results, daidzein has a protective effect against ifosfamide-induced neurotoxicity in rats via improving some selected oxidative stress parameters in male rats.
本研究通过测定雄性大鼠脑组织中氧化-抗氧化标记物的变化,探讨大豆苷元对异环磷酰胺诱导的雄性大鼠神经毒性可能的保护作用。本研究选用28只体重(120 ~ 150gm)明显健康的Wistar雄性大鼠,分为4组(n=7)。大鼠口服1% tween 20溶于蒸馏水/对照组(I组);大鼠口服大豆苷元混悬液(100mg/kg) 7 d (II组);大鼠腹腔注射单剂量异环磷酰胺(500 mg/kg) (III组);大鼠口服大豆苷元(100mg/kg) 7天,第7天单次腹腔注射异磷酰胺(500mg /kg) (IV组)。治疗结束24(24)小时后,测定大鼠脑组织匀浆中丙二醛、还原性谷胱甘肽和超氧化物歧化酶活性水平;另外对脑组织切片进行组织病理学检查。结果显示,与对照组(ⅰ组)相比,(ⅲ组/单异磷酰胺组)大鼠脑组织中丙二醛水平显著升高(P<0.05),而IV组(IFO前口服DZN)大鼠脑组织中丙二醛水平显著降低(P<0.05)。此外,III组大鼠脑内还原性谷胱甘肽水平和超氧化物歧化酶活性均较i组显著降低(p < 0.05), IV组大鼠脑内各抗氧化参数水平较III组大鼠脑内各组织水平显著升高(p < 0.05)。 结果表明,大豆苷元通过改善雄性大鼠的氧化应激参数,对异环磷酰胺诱导的大鼠神经毒性具有保护作用。
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引用次数: 0
Evaluation of Anxiety and Depression among a Sample of Hypothyroidism-Treated Iraqi Patients 伊拉克甲状腺功能减退患者焦虑和抑郁的评价
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-01 DOI: 10.31351/vol32iss2pp162-168
Nada Hamid Rasheed, Basma Zuheir Al-Metwali, Mohamed Sadoon Mohsen Al Shamaa
Background: Hypothyroidism is the most prevalent thyroid disorders worldwide. Hypothyroidism manifestations are wide spectrum, affecting various systems in human body including the nervous system. Hypothyroidism can cause neuropsychiatric symptoms such as anxiety, depression and diminishing in attention, memory and executive function. Aim: to investigate the level of anxiety and depression in patients with hypothyroidism receiving levothyroxine treatment. Method: a cross-sectional study was conducted at Baghdad Center for Nuclear Medicine and Radiation Therapy from March to June 2022. The study population included patients of both genders, aged 18-65 years, diagnosed with hypothyroidism, were receiving levothyroxine treatment and have achieved euthyroid state for at least 2 months prior to their enrolment in the study. Based on levothyroxine dose, the enrolled patients were divided into two groups: low dose group < 1.7 µg/kg/day and high dose group ≥ 1.7 µg/kg. Hospital Anxiety and Depression Scale (HADS) was used for the evaluation of anxiety and depression. Result: The mean age of the participants was 40.35 ± 9.5 years with mean body mass index of 30.61 ± 5.72 kg/m2. The mean scores of anxiety and depression for the total sample are 8.72 ±3.46 and 7.80 ±2.83; respectively, there was statistically non-significant difference for anxiety and depression scores between the low dose group and the high dose group. Conclusion: the presence of anxiety and depression symptoms although the patients were in euthyroid state. However, socio-demographic and clinical characteristics did not significantly influence the scores of anxiety and depression.
背景:甲状腺功能减退是世界范围内最常见的甲状腺疾病。甲状腺功能减退症表现广泛,可影响包括神经系统在内的人体各系统。甲状腺功能减退可引起神经精神症状,如焦虑、抑郁和注意力、记忆力和执行功能下降。目的:探讨左旋甲状腺素治疗甲状腺功能减退患者的焦虑、抑郁水平。方法:于2022年3 - 6月在巴格达核医学与放射治疗中心进行横断面研究。研究人群包括年龄在18-65岁、诊断为甲状腺功能减退、正在接受左甲状腺素治疗且在入组研究前已达到甲状腺功能正常状态至少2个月的男女患者。根据左甲状腺素剂量,将入组患者分为低剂量组和低剂量组;1.7µg/kg/天,高剂量组≥1.7µg/kg。采用医院焦虑抑郁量表(HADS)评价患者的焦虑和抑郁。结果:参与者平均年龄为40.35±9.5岁,平均体重指数为30.61±5.72 kg/m2。总样本的焦虑和抑郁平均得分分别为8.72±3.46分和7.80±2.83分;低剂量组与高剂量组的焦虑、抑郁评分差异均无统计学意义。结论:患者甲状腺功能正常,但存在焦虑和抑郁症状。然而,社会人口学和临床特征对焦虑和抑郁得分没有显著影响。
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引用次数: 0
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Iraqi Journal of Pharmaceutical Sciences
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