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Mucoadhesive Film Forming Spray for Buccal Drug Delivery: A Review 口腔给药用黏附成膜喷雾剂的研究进展
Pub Date : 2023-03-02 DOI: 10.32947/ajps.v23i1.994
Reem Wael Shahadha, Nidhal Khazaal Maraie
Film-forming sprays provide a number of advantages over conventional topical treatments, including equal medication distribution and dosing, increased bioavailability (increase local drug concentration), and less irritability (Dosing frequency). Polymers and excipients that improve the characteristics of preparations and increase the stability of active substances are the building blocks of mucoadhesive film-forming sprays. Films made from diverse combinations of polymer and excipient exhibited a wide range of characteristics. This reveiw examines the many types of polymers and excipients, the different types of sprayers, the different evaluations, as well as the essential criteria that are involved in defining the sprayability and film properties. This comes to the conclusion that natural and synthetic polymers with viscoelastic properties can both be employed to optimize the administration of buccal drugs.
与传统的局部治疗相比,成膜喷雾剂具有许多优点,包括均匀的药物分布和剂量,增加生物利用度(增加局部药物浓度)和更少的刺激性(给药频率)。聚合物和赋形剂改善了制剂的特性,增加了活性物质的稳定性,是粘接成膜喷雾剂的基本组成部分。由聚合物和赋形剂的不同组合制成的薄膜表现出广泛的特性。本文综述了聚合物和赋形剂的多种类型,不同类型的喷雾器,不同的评价方法,以及定义可喷涂性和薄膜性能的基本标准。由此得出结论,具有粘弹性的天然聚合物和合成聚合物都可以用于优化口腔药物的给药。
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引用次数: 0
Severity of Symptoms and Mortality in Diabetic Patients with COVID- 19 Infection. Review 糖尿病合并COVID- 19感染患者的症状严重程度和死亡率审查
Pub Date : 2023-03-01 DOI: 10.32947/ajps.v23i1.991
Zahraa ALBasry, Abeer Abdulhadi Rashid, Shaymaa Hasan Abbas
Background: COVID-19 pneumonia is an illness that was spreading rapidly around the world and causes many deaths. Diabetes, is considered as a risk factor which adds severity and mortality to COVID-19 infected persons. There are many studies aiming to explain the  exact association between diabetes and COVID-19.  This review aims to link between diabetes and COVID-19 risk factors, discuss the  management of patients with diabetes and COVID-19 and  provide perception into the COVID-19 disease complications relevant to diabetes .In this  review, many scientific articles and reports about COVID- 19 and Type 2 DM were collected from different databases (e.g., PubMed, Google Scholar, and Web of Science) using keywords such as SARS-CoV2, COVID-19, TYPE 2 DM, Mortality, and CO-morbidities .The result  from this study found that diabetic patients has poor prognosis, severe symptoms, worsen outcomes, and the mortality rate is higher among COVID-19 patients who have diabetes mellitus. Many complications associated with diabetes like peripheral neuropathy and vascular insufficiency can make patients more susceptible to infections. One of the sever complication of Covid-19 infection is, the cytokine storm, that result in excessive release of inflammatory cytokines (TNF-a, IL-6, IL-10), and this may be aggravated by the inflammatory process together with the hyper-coagulable condition in diabetic patients. In conclusion: Hyperglycemia is established as risk factor for increased morbidity and mortality in covid 19 infection.
背景:COVID-19肺炎是一种在世界范围内迅速传播并导致许多人死亡的疾病。糖尿病被认为是增加COVID-19感染者严重程度和死亡率的一个风险因素。有许多研究旨在解释糖尿病和COVID-19之间的确切联系。本综述旨在将糖尿病与COVID-19的危险因素联系起来,探讨糖尿病和COVID-19患者的管理,并对与糖尿病相关的COVID-19疾病并发症提供认识。本综述收集了不同数据库(如PubMed、谷歌Scholar和Web of Science)中关于COVID-19和2型糖尿病的许多科学文章和报告,关键词为SARS-CoV2、COVID-19、Type 2 DM、死亡率、本研究结果发现,糖尿病患者预后差,症状严重,预后较差,合并糖尿病的COVID-19患者死亡率较高。许多与糖尿病相关的并发症,如周围神经病变和血管功能不全,使患者更容易感染。Covid-19感染的严重并发症之一是细胞因子风暴,导致炎症细胞因子(TNF-a、IL-6、IL-10)的过度释放,而炎症过程和糖尿病患者的高凝状态可能会加剧这种情况。结论:高血糖是covid - 19感染中发病率和死亡率增加的危险因素。
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引用次数: 0
The most common route of administration used during COVID-19 COVID-19期间最常用的给药途径
Pub Date : 2023-03-01 DOI: 10.32947/ajps.v23i1.990
Mena Raid Khalil, Ghaidaa S. Hameed, Dalya Basil Hanna
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), is the virus that caused the COVID-19 pandemic. Initial symptoms include fever, cough, and dyspnea. Symptoms include nausea, vomiting, and abdominal pain, GIT involvement is also possible. The COVID-19 outbreak has increased the need for alternative medicine administration routes, particularly in public places. Buccal, sublingual, and rectal administration are all considered transmucosal methods. They are self-administration options for non-invasive systemic distribution. In addition, they are great for use in palliative and end-of-life care because of their quick onset of action and decreased first-pass metabolism. A mucosal atomization device allows for the intranasal administration of a parenteral formulation through nasal spray. Rectal mucosal absorption is comparable to that of the oral route, making the rectal route an extremely versatile and useful method of drug administration for a wide variety of medications. Covid-19 illness is treated with a variety of drugs, including anti-malaria medication (hydroxychloroquine), glucocorticoids (dexamethasone), antibiotics (azithromycin), and antiviral medications (favipiravir). This article discusses the route of drug administration for COVID-19, as well as symptoms, treatments, and the various ways it can be spread
严重急性呼吸综合征冠状病毒2 (SARS-CoV-2)是导致COVID-19大流行的病毒。最初的症状包括发烧、咳嗽和呼吸困难。症状包括恶心、呕吐和腹痛,也可能累及GIT。COVID-19疫情增加了对替代药物给药途径的需求,特别是在公共场所。口腔、舌下和直肠给药都被认为是经粘膜方法。它们是非侵入性全身分布的自我给药选择。此外,他们是伟大的用于姑息治疗和临终关怀,因为他们的快速开始的行动和减少首过代谢。一种粘膜雾化装置,允许通过鼻喷雾剂在鼻内给药。直肠粘膜吸收与口服途径相当,使直肠途径成为一种非常通用和有用的药物给药方法,适用于各种药物。Covid-19疾病可以用多种药物治疗,包括抗疟疾药物(羟氯喹)、糖皮质激素(地塞米松)、抗生素(阿奇霉素)和抗病毒药物(法匹拉韦)。本文讨论了COVID-19的药物给药途径,以及症状、治疗方法和各种传播途径
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引用次数: 0
Histopathological evaluation of induced pulmonary fibrosis under the effect of montelukast 孟鲁司特作用下诱导肺纤维化的组织病理学评价
Pub Date : 2023-02-28 DOI: 10.32947/ajps.v23i1.982
Mohammed Rabah Mahdi, Wassan Abdul Kareem Abbas, Ghaith Ali Jasim
Pulmonary fibrosis (PF) is an interstitial lung disease leading to scarring of the lung. There are several types of lung fibrosis as familial pulmonary fibrosis, idiopathic pulmonary fibrosis, and others associated with non-specific   interstitial pneumonia. The most common type is idiopathic pulmonary fibrosis which is an unknown cause. Lung fibrosis causes changes in the histology of the lung by the disappearance of the lung parenchyma, replaced by an inflammatory infiltrate, and mild thickening of the pulmonary artery. The management of pulmonary fibrosis included Azathioprine, corticosteroid, and N-acetyl cysteinyl in 2011 but in 2014 this guideline was removed and replaced by nintedanib and pirfenidone. This study used Pirfenidone, as standard therapy for the treatment of pulmonary fibrosis, and montelukast is Cysteinyl leukotrienes (CysLT) antagonist which binds to its receptor (CysLTE4) located on smooth muscle cells of the respiratory airway causing anti-inflammatory effect by inhibition of inflammatory markers as TGFβ1. Sixty male rats were divided into five groups,12 rats for each group where the control group received distilled water by gastric gavage, the induction group received bleomycin intratracheally as a single dose, the pirfenidone group received pirfenidone 50mg/kg, montelukast group received montelukast 20mg/kg and the combination group received a half dose of pirfenidone and montelukast. After twenty-eight days after the treatment with montelukast or pirfenidone sacrifice rats and collect the organ (lungs) from each group were then placed in buffer formalin 10% for histopathological study. After 14 days from bleomycin dose, results show that bleomycin cause massive disappearance of pulmonary parenchyma that was replaced by an inflammatory infiltrate and medial thickening of the pulmonary artery in all groups, but montelukast and pirfenidone show normal lung paranchyma and pulmonary artery after 28 days of treatment in pirfenidone, montelukast, and combination groups. In conclusion, that bleomycin changes the histology of the lung causing induction of lung fibrosis in all groups after 14 days except control group but pirfenidone, montelukast, and combination of half dose of pirfenidone with a half dose of montelukast return the lung to normal architecture after 28 days of treatment.
肺纤维化(PF)是一种导致肺瘢痕形成的间质性肺疾病。肺纤维化有几种类型,如家族性肺纤维化、特发性肺纤维化和其他与非特异性间质性肺炎相关的肺纤维化。最常见的类型是特发性肺纤维化,原因不明。肺纤维化引起肺组织学改变,肺实质消失,取而代之的是炎症浸润,肺动脉轻度增厚。2011年肺纤维化的治疗包括硫唑嘌呤、皮质类固醇和n -乙酰半胱氨酸,但在2014年该指南被尼达尼布和吡非尼酮所取代。本研究使用吡非尼酮作为治疗肺纤维化的标准药物,孟鲁司特是Cysteinyl leukotrienes (CysLT)拮抗剂,与位于呼吸道平滑肌细胞上的受体(CysLTE4)结合,通过抑制炎症标志物tgf - β1产生抗炎作用。将60只雄性大鼠分为5组,每组12只,对照组灌胃蒸馏水,诱导组单次气管内给药博来霉素,吡非尼酮组50mg/kg,孟鲁司特组20mg/kg,联合组半剂量吡非尼酮和孟鲁司特。用孟鲁司特或吡非尼酮治疗28天后,处死大鼠,取各组脏器(肺)置于10%福尔马林缓冲液中进行组织病理学研究。博来霉素给药14天后,结果显示博来霉素各组肺实质大量消失,取而代之的是炎症浸润和肺动脉内侧增厚,而孟鲁司特和吡非尼酮组在治疗28天后肺实质和肺动脉正常。综上所述,除对照组外,博来霉素在14天后改变肺组织组织学,引起肺纤维化,而吡非尼酮、孟鲁司特和半剂量吡非尼酮与半剂量孟鲁司特联合用药28天后肺结构恢复正常。
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引用次数: 0
Serum Matrix Metalloproteinase-2: A Possible Link between COVID-19 and Periodontitis 血清基质金属蛋白酶-2:COVID-19与牙周炎的可能联系
Pub Date : 2023-02-28 DOI: 10.32947/ajps.v23i1.985
Suhad Jumaa Abd-Alkareem, Saad Hikmat Abdullah, Noor Dhia Hasan
Background: Coronavirus disease-19 (COVID-19) is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2).  It is a severe infection primarily targeting the respiratory system. However, many other extrapulmonary body organs are also affected with a varying degree of severity. Some evidence indicated the development of periodontist in patients, although the pathogenesis is not well-defined. Aims: This study aimed to investigate the association of COVID-19 severity and role of matrix metalloproteinase 2 in development of periodontitis. Patients and Methods: This is a cross sectional study which included a total of 160 patients with COVID-19. Patients were categorized into severe and mild-moderated according to World Health Organization criteria. Periodontitis was diagnosed in those patients according to clinical criteria. Serum level of matrix metalloproteinase 2 was estimated in all patients using enzyme linked immunosorbent assay (ELISA). Demographic and laboratory data were obtained from the patients’ records. Results: Forty-two patients (26.25%) had severe COVID-19. Demographically, older ages and the presence of comorbidities were significantly associated with COVID-19 severity. Besides the inflammatory markers, the median serum level of MMP-2 was higher in severe than mild-moderate COVID-19 cases (208.12 ng/ml vs. 196.33 ng/ml) with a significant difference. The PO rate in severe and mild-moderate COVID-19 was 23.81% and 10.17%, respectively, with a significant difference. The median serum MMP-2 in patients with PO was 228.5 ng/ml which was significantly higher than those without PO 193.81 ng/ml. Conclusions: These data indicate the significant association between COVID-19 severity and development of PO. Matrix metalloproteinase-2 could be the possible link between severe COVID-19 and PO.
背景:冠状病毒病-19 (COVID-19)是由严重急性呼吸综合征冠状病毒2 (SARS-CoV-2)引起的。这是一种主要针对呼吸系统的严重感染。然而,许多其他肺外器官也受到不同程度严重程度的影响。一些证据表明,发展牙周病的患者,虽然发病机制不明确。目的:本研究旨在探讨COVID-19严重程度与基质金属蛋白酶2在牙周炎发生中的作用。患者和方法:这是一项横断面研究,共纳入160例COVID-19患者。根据世界卫生组织的标准,将患者分为重度和轻度。根据临床诊断标准诊断为牙周炎。采用酶联免疫吸附试验(ELISA)测定所有患者血清基质金属蛋白酶2水平。从患者记录中获得人口统计和实验室数据。结果:重症病例42例(26.25%)。人口统计学上,年龄较大和合并症的存在与COVID-19严重程度显著相关。除炎症标志物外,重度肺炎患者血清中位数MMP-2水平高于轻中度肺炎患者(208.12 ng/ml vs. 196.33 ng/ml),差异有统计学意义。重症、轻中度患者PO率分别为23.81%、10.17%,差异有统计学意义。PO患者血清MMP-2中位数为228.5 ng/ml,明显高于无PO患者的193.81 ng/ml。结论:这些数据表明COVID-19严重程度与PO的发生有显著相关性。基质金属蛋白酶-2可能是重症COVID-19与PO之间的可能联系。
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引用次数: 1
Insights into medicated films as attractive dosage forms 洞察药物薄膜作为有吸引力的剂型
Pub Date : 2023-02-28 DOI: 10.32947/ajps.v23i1.981
Noor Hameed Alsaide, Nidhal Khazaal Maraie
Different traditional dosage forms available in the market with many drawbacks including patient inconvenience, limited applications to several sites, variable bioavailability in addition to patent expiration. These drawbacks make pharmaceutical companies look for other drug platforms. Thin films loaded with active ingredients which are prepared as flexible polymer layer gaining acceptability in drug industry. They are easily prepared, adapted for administration of drug via different routes (to overcome several barriers) including ocular, dermal, transdermal, vaginal, oral and others. In additions, thin films are free of harmful chemicals and offer good drug stability. This review spotlights on the medicated thin films as alternative dosage forms that require further attention to maximize their performance and application.
市场上不同的传统剂型有许多缺点,包括患者不方便、在几个地点的应用有限、生物利用度可变以及专利到期。这些缺点促使制药公司寻找其他药物平台。负载有效成分的薄膜制备成柔性聚合物层,在制药工业中得到认可。它们易于制备,适合通过不同途径给药(克服若干障碍),包括眼、真皮、透皮、阴道、口服和其他途径。此外,薄膜不含有害化学物质,具有良好的药物稳定性。这篇综述的重点是药物薄膜作为替代剂型,需要进一步关注,以最大限度地发挥其性能和应用。
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引用次数: 0
Tamoxifen Citrate- loaded synthetic high-density lipoproteins: Assessment of cellular toxicity in breast cancer cells 负载柠檬酸他莫昔芬的合成高密度脂蛋白:乳腺癌细胞毒性的评估
Pub Date : 2023-02-28 DOI: 10.32947/ajps.v23i1.987
Ameerah A. Radhi, Wedad K. Ali, Fitua Al-Saedi
Tamoxifen Citrate (TC) is the standard endocrine therapy for estrogen receptor (ER) positive breast cancer. TC is a selective estrogen receptor modulator (SERM) whose estrogenic properties in uterus have been linked to increased side effects like blood clots, endometrial polyps and cancer. Therefore, significant amount of research has been carried out to develop tamoxifen loaded nano-formulations with a preferential accumulation in tumor tissue rather than healthy tissues. Synthetic high-density lipoproteins (sHDL) are novel nanocarriers with inherent active-targeting ability towards tumor cells through the ligand–receptor interaction between apolipoprotein A-I (Apo A-I) and scavenger receptor class B type I (SR-BI) overexpressed in various malignant cells. The current study was carried out to investigate whether encapsulation of TC in sHDL could improve the cytotoxic effect of TC against malignant cells. For this purpose, the cytotoxicity of TC-sHDL was evaluated in MCF-7 cell line in vitro. MTT assay demonstrated the increased cytotoxicity of TC-sHDL against cancer cells as compared with the cytotoxic effect of the free drug.
柠檬酸他莫昔芬(TC)是雌激素受体(ER)阳性乳腺癌的标准内分泌治疗药物。TC是一种选择性雌激素受体调节剂(SERM),其在子宫中的雌激素特性与血凝块、子宫内膜息肉和癌症等副作用增加有关。因此,人们进行了大量的研究,以开发负载他莫昔芬的纳米配方,使其优先在肿瘤组织而不是健康组织中积累。合成高密度脂蛋白(sHDL)是一种新型纳米载体,通过载脂蛋白A-I (Apo A-I)与各种恶性细胞中过表达的清道夫受体B类I型(SR-BI)之间的配体-受体相互作用,具有固有的靶向肿瘤细胞的活性。本研究旨在探讨sHDL包封TC是否能提高TC对恶性细胞的细胞毒作用。为此,我们在体外对MCF-7细胞株进行了细胞毒性评价。MTT试验表明,与游离药物相比,TC-sHDL对癌细胞的细胞毒性增加。
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引用次数: 0
Determination of Cr, Se, Ge, and V in Hypothyroidism Patients by Using Graphite Furnace Atomic Absorption Spectrometry and mixture matrix modification 石墨炉原子吸收光谱法和混合基体改性法测定甲状腺功能减退患者的Cr、Se、Ge和V
Pub Date : 2023-02-28 DOI: 10.32947/ajps.v23i1.986
Halah Hamid Hammadi
A simple, accurate and rapid method was developed for routine determination of trace elements in blood serum. The method based on the direct determination for Cr, Se, Ge, and V in hypothyroidism patients before therapy. By using atomic absorption spectrometry with graphite surface coated and uncoated pyrolysis GF-AAS, and a mixture of palladium nitrate and magnesium nitrate as the matrix modifier, with deuterium background correction and no sample pretreatment except dilution was necessary. This permitted direct determination hence the risk of sample contamination was reduced. Further, the use of graphite surface-coated GF-AAS decreased the ashing and atomization temperatures of Cr, Ge, and V to values that were lesser than the corresponding values obtained using uncoated pyrolysis GF-AAS, by 100°C; in case of Se, the atomization temperature decreased to a value that was 200°C lesser than that obtained using uncoated pyrolysis GF-AAS. A mixture of (3µL) palladium nitrate, and (2µL) magnesium nitrate was successfully applied to improve the sensitivity, reproducibility, recovery, limit of detection and the accuracy of the measurements. The correlation coefficients of the calibration curves of Cr, Se, Ge, and V were found to be (0.9999, 0.9999, 0.9995 and 0.9999) respectively, the relative standard deviation of the measurements for Cr, Se, Ge and V were (0.027, 0.075, 0.054 and 0.068) respectively. The statistical analysis of the acquired data showed acceptable accuracy. The analyses thus performed indicated that the levels of serum trace elements Cr, Se, Ge, and V in hypothyroidism patients were lower than those in the control group.
建立了一种简单、准确、快速的血清微量元素常规测定方法。该方法基于治疗前甲状腺功能减退患者的Cr、Se、Ge、V的直接测定。采用石墨表面包覆和未包覆热解GF-AAS原子吸收光谱法,以硝酸钯和硝酸镁的混合物为基体改性剂,进行氘背景校正,除稀释外无需样品前处理。这允许直接测定,因此降低了样品污染的风险。此外,使用石墨表面包覆的GF-AAS使Cr、Ge和V的灰化和雾化温度比使用未包覆的热解GF-AAS的相应温度低100℃;在Se的情况下,雾化温度下降到比未包覆热解GF-AAS低200℃。(3µL)硝酸钯和(2µL)硝酸镁的混合物被成功地应用于提高灵敏度、重现性、回收率、检出限和测量的准确性。结果表明,Cr、Se、Ge和V的校准曲线相关系数分别为(0.9999、0.9999、0.9995和0.9999),Cr、Se、Ge和V的相对标准偏差分别为(0.027、0.075、0.054和0.068)。对采集数据的统计分析显示出可接受的准确性。结果表明,甲减患者血清微量元素Cr、Se、Ge、V的含量低于对照组。
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引用次数: 0
Impact of antenatal depressive and anxiety symptoms on adverse birth outcomes in Baghdad, Iraq: a prospective cohort study 伊拉克巴格达产前抑郁和焦虑症状对不良分娩结局的影响:一项前瞻性队列研究
Pub Date : 2023-02-28 DOI: 10.32947/ajps.v23i1.988
Ola Ali Nassr, Mohammed Mahmood Mohammed, Hind abdulkhaliq Showman
Background: Psychiatric symptoms are common during pregnancy, potentially leading to an increased risk of adverse birth outcomes. Studies assessing the impact of depression and/or anxiety on adverse birth outcomes in Iraq are currently lacking. This study aims to   determine whether depression and/or anxiety is independently associated with preterm birth (PTB) and low birth weight (LBW). Methods: A prospective cohort study included 352 pregnant women from outpatient clinics of Al-Yarmouk hospital and private clinics in Baghdad, Iraq from March 2021 to February 2022 using a convenience sampling. They were screened for depression using Edinburgh Postnatal Depression Scale (EPDS) during pregnancy and followed up to assess adverse birth outcomes. Multivariable logistic regression was used to determine predictors associated with adverse birth outcomes. Results: The prevalence of PTB and LBW was 7.7% and 11.6%, respectively. After adjustment of all potential sociodemographic, clinical and obstetric confounders, depression was independently associated with giving birth to LBW neonate (odd ratio (OR):3.64; 95% confidence interval (CI) 1.70, 7.79), but not PTB. Prevalence of LBW in depressed was 21.2% compared to 7.7% for non-depressed. LBW was also associated with a history of LBW and PTB. In contrast, anxiety did not seem to affect birth outcomes. Conclusion: Depression during pregnancy, regardless of the trimester, is independently associated with a higher likelihood of giving birth to LBW neonates (OR: 3.64; 95% CI 1.70, 7.79). Effective interventions that target maternal depression are vital to decrease morbidity and mortality associated with LBW.  
背景:精神症状在怀孕期间很常见,可能导致不良出生结局的风险增加。目前缺乏评估伊拉克抑郁和/或焦虑对不良出生结果影响的研究。本研究旨在确定抑郁和/或焦虑是否与早产(PTB)和低出生体重(LBW)独立相关。方法:前瞻性队列研究纳入了2021年3月至2022年2月期间来自伊拉克巴格达Al-Yarmouk医院门诊和私人诊所的352名孕妇。她们在怀孕期间使用爱丁堡产后抑郁量表(EPDS)进行抑郁筛查,并随访评估不良分娩结果。使用多变量逻辑回归来确定与不良出生结局相关的预测因素。结果:PTB和LBW患病率分别为7.7%和11.6%。在对所有潜在的社会人口统计学、临床和产科混杂因素进行调整后,抑郁症与LBW新生儿的出生独立相关(奇数比(OR):3.64;95%置信区间(CI) 1.70, 7.79),但PTB除外。抑郁症患者的LBW患病率为21.2%,而非抑郁症患者为7.7%。LBW还与LBW和PTB病史相关。相比之下,焦虑似乎并不影响分娩结果。结论:妊娠期抑郁与分娩LBW新生儿的可能性较高独立相关(OR: 3.64;95% ci 1.70, 7.79)。针对产妇抑郁症的有效干预措施对于降低与LBW相关的发病率和死亡率至关重要。
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引用次数: 0
In Silico Molecular Docking, Synthesis and Preliminary Evaluation of Antibacterial Activity of Levofloxacin Carboxamides with Certain Amino Acids 含氨基酸左氧氟沙星羧胺类药物的硅分子对接、合成及抗菌活性初步评价
Pub Date : 2023-02-28 DOI: 10.32947/ajps.v23i1.984
Sarah Abdul-Razzaq makki, Shakir M. Alwan, Mayada H. Al-Qaissy
Levofloxacin carboxamides with certain amino acids were prepared through an amide linkage to the amino acid (glycine, histidine, or serine). These carboxamides were subjected to an in silico molecular docking evaluation on   DNA gyrase to predict their antibacterial activity using the GOLD suite. The binding affinities were very significant and encouraged the synthesis of the suggested carboxamides for intensive evaluation. These carboxamides were also subjected to Swiss ADME software to predict their ADME parameters. Levofloxacin carboxamides were prepared in high yield, and their chemical structures were confirmed by spectral analysis, such as 1H-NMR, 13C-NMR and FT-IR spectroscopy. Antibacterial activities were evaluated for the new carboxamides against two G-ve (Klebsiella and P. aeruginosa) and one G+ve (Streptococcus pneumonia) bacteria. When compared to levofloxacin, all of the synthesized carboxamides 1-3 demonstrated good activity against three types of bacteria. These carboxamides showed significant antibacterial activities against S. pneumoniae and lower activities against Klebsiella.
通过与氨基酸(甘氨酸、组氨酸或丝氨酸)的酰胺连接,制备了具有某些氨基酸的左氧氟沙星羧胺。利用GOLD套件对这些羧酰胺进行了DNA旋切酶的硅分子对接评价,以预测其抗菌活性。结合亲和性非常显著,并鼓励合成所建议的羧酰胺进行深入评价。这些carboxamide也受到瑞士ADME软件预测其ADME参数。以高收率制备了左氧氟沙星羧胺类化合物,并通过1H-NMR、13C-NMR和FT-IR等光谱分析对其化学结构进行了证实。研究了新羧酰胺对克雷伯菌和铜绿假单胞菌两种G-ve和肺炎链球菌的抑菌活性。与左氧氟沙星相比,所有合成的羧酰胺1-3对三种细菌都有良好的活性。这些羧胺对肺炎链球菌具有显著的抑菌活性,对克雷伯菌的抑菌活性较低。
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引用次数: 0
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Al Mustansiriyah Journal of Pharmaceutical Sciences
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