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Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)最新文献

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Isolation of beta-sitosterol and evaluation of antioxidant Activity of Iraqi Campsis grandiflora flowers. 伊拉克桔梗花β -谷甾醇的分离及抗氧化活性评价。
Sara Saad Hassoon, Ibrahim Saleh Abbas, Bahir Abdul Razzaq Mshimesh
Campsis grandiflora (Bignoniaceae) is a fast growing deciduous climber, the dried flowers have been used as a carminative, blood tonic, and febrifuge in Chinese traditional medicine. This plant has an anti-inflammatory, anti-oxidant, anti-depressant, and anti-bacterial effect; with a beneficial role in stagnant blood and endometriosis conditions. In this study, the detection of beta-sitosterol in the hexane extract of Iraqi C.grandiflora flowers was performed using thin layer chromatography (TLC) and high performance liquid chromatography(HPLC); while the isolation done by preparative layer chromatography then structure elucidation of isolated compound was done by FTIR and 1HNMR. Furthermore, assessment of the anti-oxidant activity of the ethyl acetate extract of Iraqi C.grandiflora flowers using three different methods and total flavonoid content, then measuring the pearson’s correlation coefficient between these methods. The results showed that the hexane extract of Iraqi C.grandiflora flowers contain beta-sitosterol compound and the ethyl acetate extract of this plant possesses an excellent anti-oxidant effect using the single-electron transfer (SET) pathway in scavenging the free radicals, and this activity attributed to the potent antioxidant i.e. polyphenols.
山茱萸是一种生长迅速的落叶攀援植物,其干花在中药中被用作泻药、补血和退热剂。这种植物具有抗炎、抗氧化、抗抑郁和抗菌的作用;对瘀血和子宫内膜异位症有有益作用。采用薄层色谱(TLC)和高效液相色谱(HPLC)相结合的方法,对伊拉克桔梗花己烷提取物中β -谷甾醇的含量进行检测;采用制备层析法对化合物进行分离,并用FTIR和1HNMR对化合物进行结构分析。在此基础上,采用三种不同的提取方法对桔梗花乙酸乙酯提取物的抗氧化活性和总黄酮含量进行了评价,并测定了三种提取方法之间的pearson相关系数。结果表明,桔梗花正己烷提取物中含有β -谷甾醇化合物,而桔梗花乙酸乙酯提取物具有良好的抗氧化作用,通过单电子转移(SET)途径清除自由基,这种活性归因于其强抗氧化剂多酚类物质。
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引用次数: 1
Factors Impacting Hypertension Awareness among Hypertensive Population: A Quantitative Study in a Tertiary Care Hospital in Malaysia 影响高血压人群高血压意识的因素:马来西亚一家三级保健医院的定量研究
A. H. Mohammed, Bassam Abdul Rasool Hassan, Azyyati Mohd Suhaimi, A. Blebil, J. Dujaili, Abdulrasool M. Wayyes
 There are obstacles to high levels of hypertension awareness that are embedded in gender, income and lifestyle habits which need to be addressed leading to high levels of undiagnosed and uncontrolled hypertension. This study aimed to explore the various factors which affect hypertension awareness among a hypertensive population in a tertiary care hospital. A quantitative study was conducted among hypertensive patients at a tertiary care hospital in Selangor, Malaysia. A validated and translated questionnaire was utilised as a data collection tool. Descriptive and inferential statistical analysis was done using SPSS version 25.A thousand participants (female n=621, male n= 379) were recruited, and their mean age is 48± 11.09 years old. Approximately half of respondents were not informed by their doctor that they have hypertension. More than half of respondents were unaware about the normal range of systolic and diastolic. Female gender, Chinese race, urban resident, older adults, and tertiary education level are the most significant factors that have a great influence on the level of awareness among hypertensive population. Hypertension awareness needs to be addressed from systemic point of view to solve the growing barriers to accessing correct information about the disease. Health care providers and authorities need to regulate the manner in which information on mortal diseases is presented to the public to reduce incidence of malpractice.
要实现高水平的高血压意识,存在着性别、收入和生活习惯方面的障碍,这些障碍需要加以解决,从而导致高水平的未确诊和未控制的高血压。本研究旨在探讨影响三级医院高血压人群高血压认知的各种因素。在马来西亚雪兰莪州的一家三级保健医院对高血压患者进行了定量研究。一份经过验证和翻译的问卷被用作数据收集工具。描述性和推断性统计分析采用SPSS版本25。共招募受试者1000人,其中女性621人,男性379人,平均年龄48±11.09岁。大约一半的受访者没有被医生告知他们患有高血压。超过一半的受访者不知道收缩压和舒张压的正常范围。女性、华人种族、城市居民、老年人和高等教育程度是影响高血压人群认知水平的最显著因素。高血压意识需要从系统的角度来解决越来越多的障碍,以获得正确的信息有关的疾病。卫生保健提供者和当局需要规范向公众提供致命疾病信息的方式,以减少医疗事故的发生率。
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引用次数: 0
Anti-Angiogenic Screening of Moringa Oleifera Leaves Extract Using Chorioallantonic Membrane Assay 用毛尿囊膜法筛选辣木叶提取物抗血管生成
Nisha Shri Chengama Raju, Wong Wing Kei
Background: Angiogenesis is defined as the formation of new blood vessels. However, angiogenesis in cancer will lead to tumour growth and metastasis. Therefore, anti-angiogenesis is one of the ways to slow down growth and spreading of tumour. Moringa oleifera is also known as a “Miracle tree” which has high nutritive value and various therapeutics effect in different parts of the plant. This study aims to determine the anti-angiogenic property of Moringa oleifera leaves extract by using chick chorioallantoic membrane (CAM) assay. Materials and Methods: The extracts were prepared by decoction method using methanol and water. The qualitative phytochemical screening was carried out for both methanol and aqueous extracts. The fertilised chicken eggs were divided into six groups which include negative control group (phosphate-buffer saline with pH 7.4), positive control group (sunitinib), 50% and 100% methanol extract, 50% and 100% aqueous extract. The anti-angiogenic effect of Moringa oleifera leaves extract was determined by calculating the number and percentage decrease in blood vessels in post-24 and post-48 hours of treatment. Results: Statistical analysis by one-way ANOVA has shown significant (p<0.05) percentage reduction in the blood vessels between each treatment group after 48 hours of treatment. Among all the extracts, 100% aqueous extract of Moringa oleifera was found to have highest anti-angiogenic effect with the greater percentage decrease in blood vessels (81.33%) in post-48 hours of treatment. Furthermore, the anti-angiogenic effect of Moringa oleifera leaves was found to increased when the concentration of the Moringa oleifera extract was increased. Conclusion: Moringa oleifera leaves with various phytochemicals was found to possess anti-angiogenic potential.
背景:血管生成被定义为新血管的形成。然而,肿瘤中的血管生成会导致肿瘤的生长和转移。因此,抗血管生成是减缓肿瘤生长和扩散的途径之一。辣木也被称为“奇迹树”,在植物的不同部位具有很高的营养价值和各种治疗效果。采用鸡绒毛膜法(CAM)研究辣木叶提取物的抗血管生成作用。材料与方法:采用甲醇和水煎法制备提取物。对甲醇提取物和水提取物进行了定性植物化学筛选。将受精卵分为6组,分别为阴性对照组(pH 7.4的磷酸盐缓冲盐水)、阳性对照组(舒尼替尼)、50%和100%甲醇提取物、50%和100%水提取物。通过计算处理24小时和48小时后血管减少数和百分比来测定辣木叶提取物的抗血管生成作用。结果:单因素方差分析显示,治疗48小时后,各治疗组血管百分比明显减少(p<0.05)。在所有提取物中,100%辣木水提物抗血管生成作用最强,48 h后血管减少率最高(81.33%)。此外,随着辣木提取物浓度的增加,辣木叶的抗血管生成作用增强。结论:辣木叶含有多种植物化学物质,具有抗血管生成潜能。
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引用次数: 1
Effect of Oral Administration of Valerian Extract at Different Doses on Pharmacokinetic Parameters of Carbamazepine in Rabbits 口服不同剂量缬草提取物对卡马西平在家兔体内药动学参数的影响
I. Abushammala
Carbamazepine (CBZ) is a narrow therapeutic index drug used in the treatment of trigeminal neuralgia and psychiatric disorders. Valerian (VAL) is a popular herbal product which should be prescribed to treat insomnia and anxiety. The study was designed to investigate the presence of significant pharmacokinetic (PK) interaction between Valerian (VAL) at different concentrations on Carbamazepine (CBZ) pharmacokinetic parameters in healthy male rabbits. In an in vivo, parallel-randomized controlled trial, the rabbits in three groups "first (control), second and third" were given oral doses of CBZ (50 mg/kg), for "second and third" groups (as test groups) rabbits were given (20 and 40 mg/kg/day) of the VAL respectively, as  suspension in normal saline for eight consecutive days. On the eighth day, CBZ was co-administered an hour after adding the last dose of VAL suspension. Venous blood samples (1.0-1.5 mL) were obtained from rabbits' ears' marginal vein at predetermined different periods. The plasma of this blood separation was done using centrifugation and stored at -80°C, prior to analysis by using CBZ chemiluminescent enzyme immunoassay detection kit. Different PK parameters such as Cmax, tmax, t½,  ke, AUC0-24 and AUC0-∞ were determined for the three groups, applying Statistical testing (ANOVA). The results showed statistical insignificant differences for all PK parameters among the three groups with (p˃0.05). The findings showed that VAL at both concentrations is not likely to interfere with PK parameters related to CBZ, Further confirmation in humans shoud be done before these findings are applied to patient care.
卡马西平(Carbamazepine, CBZ)是一种用于治疗三叉神经痛和精神疾病的窄治疗指数药物。缬草(VAL)是一种流行的草药产品,应该开处方治疗失眠和焦虑。本研究旨在探讨不同浓度缬草(VAL)对卡马西平(CBZ)在健康雄性家兔体内药代动力学参数的相互作用。在体内平行随机对照试验中,第一组(对照组)、第二组和第三组(试验组)分别口服CBZ (50 mg/kg),第二组和第三组(试验组)分别给予VAL(20和40 mg/kg/d)作为悬液,在生理盐水中连续8天。第8天,在加入最后一剂VAL混悬液1小时后,联合给药CBZ。在预定的不同时期从兔耳缘静脉取静脉血(1.0 ~ 1.5 mL)。分离后的血浆经离心处理,-80℃保存,用CBZ化学发光酶免疫测定试剂盒分析。采用统计学检验(ANOVA)确定三组的不同PK参数Cmax、tmax、t½、ke、AUC0-24和AUC0-∞。结果显示,三组患者PK参数差异均无统计学意义(p > 0.05)。研究结果表明,两种浓度的缬氨酸不太可能干扰与CBZ相关的PK参数,在将这些发现应用于患者护理之前,需要在人类中进一步证实。
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引用次数: 0
Some Pro and Anti-Inflammatory Cytokines in Children with Tonsillitis and their Correlations with Vitamin D Deficiency 扁桃体炎患儿部分促炎性因子及抗炎因子与维生素D缺乏的关系
Zainab Alhakeem, Najwan Kaisar Fakree, Ahmed AbdulSamad Muhsen, Nuha Majeed Hashim
Inflammation of the tonsils could be described as acute tonsillitis, mainly due to infection. Recurrent tonsillitis could be defined as 3-7 episodes during the first 3 years of age. Vitamin D, which is a neuro-hormone with pleiotropic biological activities may modulate the immune response by alleviation, and stimulation of Th1 and Th2 cell proliferation, respectively, that influence the stimulation, synthesis, and secretion of both pro and anti-inflammatory cytokines. In this study we aimed to shed light on the levels of vitamin D in children with different episodes of tonsillitis in association with levels of interleukins (TNFα, IL-2, IL-4, IL-10). Blood samples were collected from 48 participants in 3 groups: control, acute tonsillitis (1-2 episodes/year), chronic tonsillitis (more than 7 episodes/year), serum was separated and the levels of Vitamin D, TNFα, IL-2, IL-4 and IL-10 were estimated using ELISA technique. Vitamin D decreased significantly as the episodes of tonsillitis increased, with level of 16.38± 2.41ng/ml in acute and, 14.13± 2.15 ng/ml in chronic tonsillitis as compared to control (30.91± 2.31 ng/ml), while pro-inflammatory cytokines (TNFα and IL-2) significantly increased (46.88± 14.05 and 44.55± 9.24, 1267.25± 111.85 and 1191.72± 121.52 ng/ml, respectively) as compared to control (9.45 and 138.48 ng/ml respectively). Anti-inflammatory (IL-4, IL-10) cytokines in control group were (243.08± 28.72 and 24.27± 1.83 ng/ml, respectively), which increased non-significantly in acute and chronic tonsillitis (302.76± 38.93, 290.12± 44.69 and 28.16± 2.01, 26.29± 1.99 ng/ml, respectively). Significant direct correlation was observed between the levels of vitamin D and anti-inflammatory cytokines in chronic tonsillitis (P<0.05). In conclusion, deficiency of vitamin D may affect the number of episodes of tonsillitis in children by modulation of the secretion of some cytokines.
扁桃体的炎症可称为急性扁桃体炎,主要由感染引起。复发性扁桃体炎可定义为3-7次发作在前3岁。维生素D是一种具有多种生物活性的神经激素,可分别通过减轻和刺激Th1和Th2细胞增殖来调节免疫反应,从而影响促炎性和抗炎性细胞因子的刺激、合成和分泌。在这项研究中,我们旨在阐明不同扁桃体炎发作的儿童维生素D水平与白细胞介素(TNFα, IL-2, IL-4, IL-10)水平的关系。将48例受试者分为对照组、急性扁桃体炎(1-2次/年)、慢性扁桃体炎(7次/年以上)3组,采集血样,分离血清,采用ELISA技术测定维生素D、TNFα、IL-2、IL-4、IL-10水平。随着扁桃体炎发作次数的增加,维生素D水平明显降低,急性扁桃体炎为16.38±2.41ng/ml,慢性扁桃体炎为14.13±2.15 ng/ml(30.91±2.31 ng/ml),促炎细胞因子(TNFα和IL-2)水平显著高于对照组(分别为46.88±14.05和44.55±9.24、1267.25±111.85和1191.72±121.52 ng/ml)(分别为9.45和138.48 ng/ml)。对照组抗炎(IL-4、IL-10)细胞因子含量分别为(243.08±28.72、24.27±1.83)ng/ml,急性、慢性扁桃体炎组IL-4、IL-10细胞因子含量分别为(302.76±38.93、290.12±44.69、28.16±2.01、26.29±1.99)ng/ml,差异无统计学意义。慢性扁桃体炎患者维生素D水平与抗炎细胞因子水平有显著的直接相关性(P<0.05)。综上所述,维生素D缺乏可能通过调节某些细胞因子的分泌而影响儿童扁桃体炎的发作次数。
{"title":"Some Pro and Anti-Inflammatory Cytokines in Children with Tonsillitis and their Correlations with Vitamin D Deficiency","authors":"Zainab Alhakeem, Najwan Kaisar Fakree, Ahmed AbdulSamad Muhsen, Nuha Majeed Hashim","doi":"10.31351/vol31iss1pp194-201","DOIUrl":"https://doi.org/10.31351/vol31iss1pp194-201","url":null,"abstract":"Inflammation of the tonsils could be described as acute tonsillitis, mainly due to infection. Recurrent tonsillitis could be defined as 3-7 episodes during the first 3 years of age. Vitamin D, which is a neuro-hormone with pleiotropic biological activities may modulate the immune response by alleviation, and stimulation of Th1 and Th2 cell proliferation, respectively, that influence the stimulation, synthesis, and secretion of both pro and anti-inflammatory cytokines. In this study we aimed to shed light on the levels of vitamin D in children with different episodes of tonsillitis in association with levels of interleukins (TNFα, IL-2, IL-4, IL-10). Blood samples were collected from 48 participants in 3 groups: control, acute tonsillitis (1-2 episodes/year), chronic tonsillitis (more than 7 episodes/year), serum was separated and the levels of Vitamin D, TNFα, IL-2, IL-4 and IL-10 were estimated using ELISA technique. Vitamin D decreased significantly as the episodes of tonsillitis increased, with level of 16.38± 2.41ng/ml in acute and, 14.13± 2.15 ng/ml in chronic tonsillitis as compared to control (30.91± 2.31 ng/ml), while pro-inflammatory cytokines (TNFα and IL-2) significantly increased (46.88± 14.05 and 44.55± 9.24, 1267.25± 111.85 and 1191.72± 121.52 ng/ml, respectively) as compared to control (9.45 and 138.48 ng/ml respectively). Anti-inflammatory (IL-4, IL-10) cytokines in control group were (243.08± 28.72 and 24.27± 1.83 ng/ml, respectively), which increased non-significantly in acute and chronic tonsillitis (302.76± 38.93, 290.12± 44.69 and 28.16± 2.01, 26.29± 1.99 ng/ml, respectively). Significant direct correlation was observed between the levels of vitamin D and anti-inflammatory cytokines in chronic tonsillitis (P<0.05). In conclusion, deficiency of vitamin D may affect the number of episodes of tonsillitis in children by modulation of the secretion of some cytokines.","PeriodicalId":14509,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)","volume":"21 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81438660","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Anti-Inflammatory Activity of Gingko Biloba Extract in Cotton Pellet-Induced Granuloma in Rats: A comparative Study with Prednisolone and Dexamethasone 银杏叶提取物对棉球致肉芽肿大鼠抗炎作用:与强的松龙、地塞米松的比较研究
Ahmed Azad Kareem, T. Aziz, Zheen Aorahman Ahmed, Hemn Hassan Othman, Saad Abdulrahman Hussain
The current study was designed to evaluate the anti-inflammatory effect of GKB in the rat model of granulomatous inflammation. Thirty rats were distributed into five groups:  The first group served as negative control group that received distilled water (DW) only without inducting inflammation, positive control group; treated with DW with the induction of inflammation and they were assigned to cotton pellet-induced granuloma, ginkgo biloba (GKB) treated group (200mg/kg/day), dexamethasone-treated group (1mg/kg), and Prednisolone treated group (5mg/kg). All the treatments were given orally for seven consecutive days.  On day eight, the rats were anesthetized and the pellets together with granulation tissue were carefully removed and made free from extraneous tissue. The weight and the percent of the exudate and granuloma were determined and samples of the tissues were sent for histopathological examination. Blood samples were collected by cardiac puncture and used for the analysis of the inflammatory markers: TNF-alfa, IL10, VCAM-1, and hs-CRP. The study revealed a significant reduction in the weight and the percent of exudate (p-value = 0.019), (17%) and granuloma (p-value = 0.013), (20%) by GKB which was comparable to that produced by prednisolone. All the treatment groups showed a significant reduction in serum TNF-?, VCAM-1, and hs-CRP concentration compared with the positive control. The histopathological finding revealed pronounced improvement. In the current study, GKB was effective in attenuating the level of inflammation by decreasing the exudate, granuloma, and inflammatory markers. The underlying mechanisms could be the inhibitory effect on the expression of the inflammatory cytokines and endothelial adhesion molecule. These findings suggest GKB as a good contender to be tested in the treatment of inflammatory diseases.  
本研究旨在评价GKB在肉芽肿性炎症大鼠模型中的抗炎作用。将30只大鼠分为5组:第一组为阴性对照组,只注射蒸馏水(DW),不诱导炎症;用DW诱导炎症,分为棉球肉芽肿、银杏叶(GKB)处理组(200mg/kg/d)、地塞米松处理组(1mg/kg)、强的松龙处理组(5mg/kg)。所有治疗均口服,连续7天。第8天,麻醉大鼠,小心地取出颗粒和肉芽组织,去除外部组织。测定出液和肉芽肿的重量和百分比,并将组织样本送去组织病理学检查。通过心脏穿刺采集血液样本,用于分析炎症标志物:tnf - α、il - 10、VCAM-1和hs-CRP。研究显示,GKB与泼尼松龙的效果相当,显著降低了患者的体重和渗出液百分比(p值= 0.019)(17%)和肉芽肿百分比(p值= 0.013)(20%)。所有治疗组血清TNF-?VCAM-1、hs-CRP浓度与阳性对照比较。组织病理学检查显示明显改善。在目前的研究中,GKB通过减少渗出物、肉芽肿和炎症标志物有效地减轻炎症水平。其潜在机制可能是抑制炎症细胞因子和内皮粘附分子的表达。这些发现表明GKB是一个很好的竞争者,可以在炎症性疾病的治疗中进行测试。
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引用次数: 2
Development of novel paracetamol/naproxen co-crystals with an improvement in naproxen solubility. 新型扑热息痛/萘普生共晶的研制及萘普生溶解度的改善。
A. Al-Dulaimi, Myasar Al-kotaji, F. Abachi
Co-crystals are new solid forms of drugs that could resolve more than one problem associated with drugs formulations like solubility, stability, bioavailability, mechanical and tableting properties. A preliminary theoretical study for estimating the possible bonding between the co-crystal components (paracetamol and naproxen) was performed using the ChemOffice program. The results revealed a high possibility for bonding between paracetamol and naproxen and indicated the ability of molecular mechanics study to predict the co-crystal design.        In this work, four different methods were used for the preparation of three different ratios 1:1, 2:1, and 1:2 of paracetamol:naproxen co-crystals. The four methods are liquid-assisted grinding, solvent evaporation method, ultrasonic-assisted co-crystallization, and microwave-assisted co-crystallization. The characterization of the prepared co-crystal was performed by Fourier transform infrared spectroscopy, Thermogravimetric Analysis, Differential scanning calorimetry, Powder X-Ray diffraction, and Field emission scanning electron microscopy.        The results showed that the most successful method for co-crystal production was solvent evaporation methods. The FTIR and DSC results indicated the formation of paracetamol-naproxen co-crystals when prepared by using the solvent evaporation method in the three ratios 1:1 (N1), 2:1 (N2), and 1:2 (N3). Moreover, the PXRD results confirm the previous conclusions.        A solubility study was conducted to compare the water solubility of pure paracetamol and naproxen with co-crystals solubility. The naproxen solubility was improved by more than two times in (1:1) and (1:2) paracetamol/naproxen co-crystals.        To conclude, this work succeeded in formation of new paracetamol/naproxen co-crystals, which can be considered as a new promising technique for formulation of these two drugs with an obvious enhancement in naproxen solubility and crystallinity. This could be exploited in preparation of tablets with possible enhancement in dissolution and bioavailability, however, further work is needed to prove this assumption.
共晶是一种新的固体形式的药物,可以解决与药物配方相关的多个问题,如溶解度、稳定性、生物利用度、机械和片剂性能。使用ChemOffice程序对共晶组分(扑热息痛和萘普生)之间可能的键合进行了初步的理论研究。结果表明,对乙酰氨基酚与萘普生之间存在键合的可能性较大,表明分子力学研究可以预测共晶设计。本文采用四种不同的方法制备了1:1、2:1、1:2三种不同配比的扑热息痛:萘普生共晶。四种方法分别是液体辅助研磨法、溶剂蒸发法、超声辅助共结晶法和微波辅助共结晶法。利用傅里叶变换红外光谱、热重分析、差示扫描量热、粉末x射线衍射和场发射扫描电镜对制备的共晶进行了表征。结果表明,溶剂蒸发法是制备共晶最成功的方法。FTIR和DSC结果表明,以1:1 (N1)、2:1 (N2)和1:2 (N3)的溶剂蒸发法制备对乙酰氨基酚-萘普生共晶。PXRD结果也证实了上述结论。对纯扑热息痛和萘普生的水溶性和共晶溶解度进行了比较。萘普生在(1:1)和(1:2)扑热息痛/萘普生共晶中的溶解度提高了2倍以上。综上所述,本工作成功地形成了新的扑热息痛/萘普生共晶,可以认为这是一种有前景的新技术,可以明显提高萘普生的溶解度和结晶度。这可以用于制备片剂,可能提高溶出度和生物利用度,但需要进一步的工作来证明这一假设。
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引用次数: 0
Lornoxicam-Loaded Cubosomes: - Preparation and In vitro Characterization. 氯诺昔康负载立方体体:制备和体外表征。
Rasha Saadi Younus Alkawak, Nawal A. Rajab
Cubosomes are nanosized structures self-assembled nanostructured materials used for controlling the release of the entrapped drug molecule. Lornoxicam (LXM) is a potent analgesic nonsteroidal anti-inflammatory (NSAID) drug with a short half-life (3-4) hours. The present study aims to prepare LXM-loaded cubosomes with well-defined morphology, particle size, PDI, high entrapment efficiency, sustained drug release, and high zeta potential value, as a transdermal drug delivery system.       Twelve formulas of LXM-loaded cubosomal dispersions were prepared by a solvent dilution method using Glyceryl monooleate ( GMO) as polar lipid with different stabilizers as Pluronic® F127 or tween 80 and different types of hydrotrope as ethanol or propylene glycol. These formulas were evaluated for their particle size analysis & PDI, E.E. %, and in-vitro drug release to select a group of the optimum formulas, that further characterized by transmission electron microscopy (TEM) and zeta potential analyzer to select the optimum dispersion. FTIR study was used to investigate the compatibility of the drug with excipients. The obtained results indicated that F3, composed of GMO, Pluronic® F127, ethanol, drug, and phosphate buffer solution pH 7.4 in the following per cents 7.28%, 1.82%, 8%, 2%, and 80.9% w/w, respectively, prepared in 20min agitation period, as the optimum formula for its high E.E. % (94.30±0.002%), small particle size (16.3±0.19nm), low PDI          (0.06±0.02), and high zeta potential value (-65.9±0.05mV), and well-defined cubic structure. FTIR study indicated no interaction between LXM and other formulas components. This study's conclusion illustrated that LXM-loaded cubosomal dispersion could be considered a promising nano-carrier for transdermal drug delivery.
立方体体是一种纳米级结构的自组装纳米结构材料,用于控制被包裹的药物分子的释放。氯诺昔康(LXM)是一种有效的镇痛非甾体抗炎(NSAID)药物,半衰期短(3-4小时)。本研究旨在制备形态清晰、粒径大小、PDI、包封效率高、药物缓释和zeta电位值高的lxm负载立方体体作为透皮给药系统。采用溶剂稀释法,以单油酸甘油酯(GMO)为极性脂质,不同稳定剂为Pluronic®F127或tween 80,不同类型的水相为乙醇或丙二醇,制备了12种负载lxm的立方体体分散体配方。对各配方进行粒径分析、PDI、E.E. %、体外释放度等评价,优选出一组最佳配方,并通过透射电子显微镜(TEM)和zeta电位分析仪对其进行表征,优选出最佳分散度。用红外光谱研究了该药物与辅料的配伍性。结果表明,由GMO、Pluronic®F127、乙醇、药物和磷酸盐缓冲液组成的F3,其pH分别为7.28%、1.82%、8%、2%和80.9% w/w,搅拌时间为20min,具有较高的e - e %(94.30±0.002%)、较小的粒径(16.3±0.19nm)、较低的PDI(0.06±0.02)、较高的zeta电位值(-65.9±0.05mV)和良好的立方结构。FTIR研究表明,LXM与其他配方成分无交互作用。本研究的结论表明,载lxm的立方体体分散体可以被认为是一种很有前途的经皮给药纳米载体。
{"title":"Lornoxicam-Loaded Cubosomes: - Preparation and In vitro Characterization.","authors":"Rasha Saadi Younus Alkawak, Nawal A. Rajab","doi":"10.31351/vol31iss1pp144-153","DOIUrl":"https://doi.org/10.31351/vol31iss1pp144-153","url":null,"abstract":"Cubosomes are nanosized structures self-assembled nanostructured materials used for controlling the release of the entrapped drug molecule. Lornoxicam (LXM) is a potent analgesic nonsteroidal anti-inflammatory (NSAID) drug with a short half-life (3-4) hours. The present study aims to prepare LXM-loaded cubosomes with well-defined morphology, particle size, PDI, high entrapment efficiency, sustained drug release, and high zeta potential value, as a transdermal drug delivery system. \u0000      Twelve formulas of LXM-loaded cubosomal dispersions were prepared by a solvent dilution method using Glyceryl monooleate ( GMO) as polar lipid with different stabilizers as Pluronic® F127 or tween 80 and different types of hydrotrope as ethanol or propylene glycol. These formulas were evaluated for their particle size analysis & PDI, E.E. %, and in-vitro drug release to select a group of the optimum formulas, that further characterized by transmission electron microscopy (TEM) and zeta potential analyzer to select the optimum dispersion. FTIR study was used to investigate the compatibility of the drug with excipients. \u0000The obtained results indicated that F3, composed of GMO, Pluronic® F127, ethanol, drug, and phosphate buffer solution pH 7.4 in the following per cents 7.28%, 1.82%, 8%, 2%, and 80.9% w/w, respectively, prepared in 20min agitation period, as the optimum formula for its high E.E. % (94.30±0.002%), small particle size (16.3±0.19nm), low PDI          (0.06±0.02), and high zeta potential value (-65.9±0.05mV), and well-defined cubic structure. FTIR study indicated no interaction between LXM and other formulas components. \u0000This study's conclusion illustrated that LXM-loaded cubosomal dispersion could be considered a promising nano-carrier for transdermal drug delivery.","PeriodicalId":14509,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)","volume":"15 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78592885","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 4
Development of 5-FU Loaded poly lactic-co-glycolic acid Nanoparticles for Treatment of Lung Cancer 5-FU负载聚乳酸-羟基乙酸纳米颗粒治疗肺癌的研究进展
Sankha Bhattacharya
Non-Small Cell Lung Cancer (NSCLC) accounts for about 84% of all lung cancer types diagnosed so far. Every year, regardless of gender, the NSCLC targets many communities worldwide. 5-Fluorouracil (5-FU) is a uracil-analog anticancer compound. This drug tends to annihilate multiple tumour cells. But 5-FU's most significant obstacle is that it gets very easily metabolized in the blood, which eventually leads to lower anticancer activity. Therfore a perfect drug delivery system is needed to overcome all the associated challenges.In this experiment, an attempt was made to prepare 5-FU loaded poly lactic-co-glycolic acid  nanoparticles using solvent evaporation method and subsequently observed the effect of molecular weight of poly lactic-co-glycolic acid, loading of poly lactic-co-glycolic acid, sonication period on the cytotoxic effect of 10 % w/w 5-FU loaded PLGA nanoparticles against human A549 Isogenic cell line.In this experiment, two points are more evident: first, poly lactic-co-glycolic acid has a major impact on 5-FU release due to higher degradation and rate of diffusion in nanoparticle solution; and second, nanoparticles with a larger surface area and smaller particle size have a lower half-maximal inhibitory concentration (IC50) value. The IC50 of all nanoparticles was significantly higher (p=0.0145) than that of the free 5-FU controlled group (8.34Nm). The cytotoxicity would be greater if the IC50 value was lower. Nanoparticles with an 18-minute sonication time was found to  be more cytotoxic than those with PLGA nanoparticles containing 12% polyvinyl alcohol. In this experiment 10% w/w 5-FU loaded poly lactic-co-glycolic acid nanoparticles was prepared for laboratory research to translational research for the treatment of lung cancer.
迄今为止,非小细胞肺癌(NSCLC)约占所有肺癌类型的84%。每年,不分性别,NSCLC的目标是全世界的许多社区。5-氟尿嘧啶(5-FU)是一种类似于尿嘧啶的抗癌化合物。这种药能消灭多个肿瘤细胞。但5-FU最大的障碍是它很容易在血液中代谢,最终导致抗癌活性降低。因此,需要一个完善的给药系统来克服所有相关的挑战。本实验尝试采用溶剂蒸发法制备负载5-FU的聚乳酸-共乙醇酸纳米颗粒,并观察了负载5-FU的聚乳酸-共乙醇酸分子量、负载量、超声时间对10% w/w负载5-FU的PLGA纳米颗粒对人A549等基因细胞株的细胞毒作用的影响。在本实验中,有两点更为明显:第一,聚乳酸-羟基乙酸在纳米颗粒溶液中具有较高的降解和扩散速率,对5-FU的释放有重要影响;其次,表面积越大、粒径越小的纳米颗粒,其半最大抑制浓度(IC50)值越低。各纳米颗粒的IC50均显著高于游离5-FU对照组(8.34Nm) (p=0.0145)。IC50值越低,细胞毒性越大。超声时间为18分钟的纳米颗粒比含有12%聚乙烯醇的PLGA纳米颗粒具有更大的细胞毒性。本实验制备了10% w/w 5-FU负载的聚乳酸-羟基乙酸纳米颗粒,用于实验室研究到肺癌治疗的转化研究。
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引用次数: 3
Estimation the Safety of Parenteral Resveratrol in Mice 小鼠静脉注射白藜芦醇的安全性评价
Rehab AM. Jawad, H. Sahib
   Resveratrol is polyphenolic compound has many biochemical and biological effects on several organs. Therefore, resveratrol can be used to treat many diseases. The aim was to evaluate resveratrol safety when used in a parenteral single bolus dose. This study was conducted on 60 mice (30 males and 30 females). Each male and female mice divided into 6 groups (five mice per group). All mice groups given 1% DMSO and five different doses of resveratrol (5, 2.5, 1.25, 0.625, 0.312) gm/kg intraperitonially given to five groups respectively. The mice were continuously monitored during 14 days. The number of deaths, changes in general behavior, changes in physiological activity, and signs of toxicity were reported. On day 15 blood was collected using a jugular vein puncture to obtain blood samples for hematological and biochemical analysis. All mice were euthanized under anesthesia. The heart, lung, liver, kidney, and gonads were dissected and sent for histopathological study. The result showed that at dose 0.312gm/kg neither signs of toxicity nor death were detected. The LD50 dose was 1.18 g/kg for female and 1.07 g/kg for male mice. The body weight change, biochemical and hematological assay, revealed that at doses 1.25 g/kg,0.625,0.312 g/kg for both sexes no significant changes had reported in comparison with a control group (p?0.05). Histopathological examination revealed that at doses 1.25 g/kg for both sexes no significant tissue changes had reported in comparison with a control group (p?0.05). In conclusion resveratrol has dose-dependent toxicity when used intraperitoneally in Swiss Albino mice and the non-observed adverse effect level at dose 0.312 g/kg.
白藜芦醇是一种多酚类化合物,对多种器官具有多种生物化学作用。因此,白藜芦醇可用于治疗多种疾病。目的是评估白藜芦醇在单次静脉注射时的安全性。本研究在60只小鼠(30只雄性和30只雌性)上进行。每只雌雄小鼠分为6组(每组5只)。各组小鼠分别给予1% DMSO和5种不同剂量(5、2.5、1.25、0.625、0.312)gm/kg白藜芦醇灌胃。在14天内对小鼠进行连续监测。报告了死亡人数、一般行为变化、生理活动变化和中毒迹象。第15天采用颈静脉穿刺采血,采集血样进行血液学和生化分析。所有小鼠均在麻醉下安乐死。解剖心、肺、肝、肾、性腺,送组织病理检查。结果表明,在0.312gm/kg剂量下,未发现毒性和死亡迹象。雌性小鼠LD50为1.18 g/kg,雄性小鼠LD50为1.07 g/kg。体重变化,生化和血液学分析显示,在1.25 g/kg,0.625,0.312 g/kg剂量下,与对照组相比,两性均无显著变化(p?0.05)。组织病理学检查显示,在1.25 g/kg剂量下,与对照组相比,两性均未报告明显的组织变化(p?0.05)。结论白藜芦醇对瑞士白化病小鼠腹腔注射具有剂量依赖性毒性,剂量为0.312 g/kg时未观察到不良反应水平。
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引用次数: 1
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Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
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