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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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Physicians’ Perception and Practice of Prescribing Vitamin B Combination versus Antiepileptic Drugs for Diabetic Neuropathy: Content Validity, Reliability and Pilot Study 医生对联合使用维生素B与抗癫痫药物治疗糖尿病神经病变的认知和实践:内容效度、信度和初步研究
Narmin Essa, M. Aladul
Background: Diabetic neuropathy (DN) is the most common complication of diabetes mellitus causing increased morbidity and mortality. Although international guidelines did not include vitamins and dietary supplements in any line of management, these agents were prescribed by a significant number of physicians either as preventive or treatment of DN. This study aimed to develop a validated questionnaire that examines the physicians’ perception and practice towards prescribing vitamins or dietary supplements for DN treatment. Method: The questionnaire was developed upon literature review via PubMed, Medline, Web of Science, Scopus, and Google Scholar. The questionnaire was revised upon experts’ views and opinions. The constructed questionnaire was validated by the means of content validity and internal consistency. Finally, the developed questionnaire was piloted in a small representative sample of the original future aimed research target population, to test its applicability and feasibility. Results: A total of 19 items questionnaire were developed in two domains (perception and practice). Content validity analysis results met a satisfactory level, in which the S-CVI/UA value was 0.84 and 0.89 for clarity and relevance respectively. The questionnaire also showed good reliability, in which the Cronbach’s alphas was 0.824. Conclusion: This study showed the ability to construct a questionnaire with good levels of content validity and reliability that can cover different aspects of the current state of perception and practice among physicians regarding the management of DN.
背景:糖尿病性神经病变(DN)是糖尿病最常见的并发症,发病率和死亡率增高。尽管国际指南没有将维生素和膳食补充剂纳入任何管理范畴,但相当多的医生将这些药物作为DN的预防或治疗处方。本研究旨在制定一份有效的问卷调查,以检查医生对处方维生素或膳食补充剂治疗DN的看法和做法。方法:通过PubMed、Medline、Web of Science、Scopus、谷歌Scholar等网站的文献综述,编制问卷。根据专家的意见和意见对问卷进行了修订。通过内容效度和内部一致性对构建的问卷进行验证。最后,开发的问卷在原来的未来研究目标人群的一个小代表性样本中进行试点,以测试其适用性和可行性。结果:共编制了认知和实践两个领域的19项问卷。内容效度分析结果令人满意,清晰度和相关性的S-CVI/UA值分别为0.84和0.89。问卷的信度也很好,Cronbach 's alpha为0.824。结论:本研究能够构建具有良好内容效度和信度的问卷,涵盖医生对DN管理的认知和实践现状的不同方面。
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引用次数: 0
Chitosan- (Prunus avium) Gum Nanocapsules Loaded with Orange Peel Extract 壳聚糖-柑桔皮提取物纳米胶囊
Tahani Alidee, H. Habbal, F. Karabet
The orange peel extract (OE) is an additive material that has been used widely as a natural antioxidant source and bioactive compounds in Pharmaceutical and food sector. The poor stability and degradation of this extract were considered problems in the industry. New technologies have been introduced recently to prevent this degradation as encapsulation. In this work, chitosan (CS) and Prunus avium gum (PG) were proposed as promising based materials for encapsulation OE via ionic gelation method.  The effect of different ratios of CS: PG and CS: OE on encapsulation efficiency (EE %) and the capsules size were investigated. The EE% of CS-PG was ranged from 60.63 to 87.06 % with a size range of 40 to 95nm according to Atomic Force Microscope (AFM) images. The formulation with the highest EE% was chosen to be characterized by FTIR, scanning electron microscope (SEM), and in vitro release study. The FTIR spectra confirm the cross-linking between the NH3+ group in CS and the negative functional group (-COO-) in PG. According to SEM micrographs, the capsules showed a spongy porous structure. The in vitro release study indicated that the release of OE from CS-PG matrix in the acidic and neutral medium was 55.15 and 52.67% respectively after incubation for 240 minutes. This study found that CS-PG can be used as an effective wall matrix for encapsulating OE and delivering it into the gastrointestinal system.
橙皮提取物作为一种天然抗氧化源和生物活性化合物,在医药和食品领域得到了广泛的应用。该提取物稳定性差,易降解,是业界普遍存在的问题。最近引入了新技术来防止这种退化,如封装。本文提出了壳聚糖(CS)和李树胶(PG)作为离子凝胶法制备OE的基础材料。考察了不同配比CS: PG和CS: OE对其包封率(EE %)和胶囊大小的影响。原子力显微镜(AFM)显示,CS-PG的EE%范围为60.63 ~ 87.06%,粒径范围为40 ~ 95nm。采用红外光谱(FTIR)、扫描电镜(SEM)和体外释放研究等方法对EE%最高的制剂进行表征。FTIR光谱证实了CS中的NH3+基团与PG中的负官能团(- coo -)之间存在交联。SEM显微图显示,胶囊呈海绵状多孔结构。体外释放研究表明,CS-PG基质在酸性和中性培养基中培养240 min后,OE的释放量分别为55.15%和52.67%。本研究发现CS-PG可作为OE包封并输送至胃肠道系统的有效壁基质。
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引用次数: 0
Pharmacological aspects of Borago officinalis (Borage): A review article 琉璃苣(Borago officinalis)的药理研究综述
Ruaa Mohammed Ibrahim, Dhuha Abdul Saheb Alshammaa
Abstract: Borago officinalis is highly interesting amongst nutritional and medical source relate to its high composition of some useful phytochemical compound. It is great plants with bright blue star-shaped flowers present in most world regions and usually known as borage. The Borago phytochemical analysis showed the presence of alkaloids, tannins, flavonoids, phenolic acids, essential oil, vitamins and others. Borage is cultivated all over the world and used in traditional medicine as a demulcent, diuretic, emollient, tonic, expectorant, for the treatment of coughs, inflammation and swelling, and other diseases. In herbal medicine, Borage seed oil (BSO) has been utilized for many progres­sive illnesses as a treatment agent. The BSO compounds include p-simen-8-L, ?-caryophyllene, sesquiterpenes, monoterpenes, alpha-linoleic, gammalinoleic and linoleic acid. BSO is famed to be the richest vegetable origin of gamma (?)-linoleic acid (GLA). Borage officinalis possess different pharmacological properties including antinociceptive, antioxidant, radioprotective, memory improving, hepatoprotective, antinflammatory, and analgesic effects.
摘要:蒲公英富含多种有益的植物化学成分,是一种备受关注的营养和药用来源。它是一种伟大的植物,有着明亮的蓝色星形花朵,在世界上大多数地区都有,通常被称为琉璃苣。Borago植物化学分析显示,其中含有生物碱、单宁、类黄酮、酚酸、精油、维生素等。琉璃苣在世界各地都有种植,在传统医学中用作镇痛剂、利尿剂、润肤剂、滋补剂、祛痰剂,用于治疗咳嗽、炎症和肿胀等疾病。在草药中,琉璃苣籽油(BSO)已被用作许多进行性疾病的治疗剂。BSO化合物包括对西门-8- l、-石竹烯、倍半萜、单萜、α -亚油酸、γ -亚麻油酸和亚油酸。BSO以富含γ(?)-亚油酸(GLA)的蔬菜而闻名。琉璃苣具有抗伤、抗氧化、抗辐射、改善记忆、保护肝脏、抗炎、镇痛等药理作用。
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引用次数: 1
The Protective Effects of N-acetylcysteine against 5-Fluorouracil Induced Intestinal Toxicity in Albino Rats n -乙酰半胱氨酸对5-氟尿嘧啶致白化大鼠肠道毒性的保护作用
M. Al-Hamdany, A. Al-Hubaity
5-fluorouracil (5-FU) is a is Pyrimidine analogue widely used in the treatment of various malignancies It belongs to  the antimetabolites family that acts during the S-phase of the cell cycle thus it prevents DNA synthesis.N-acetylcysteine is nutritional complement acts as antioxidant.The purpose  of the current study is to investigate whether there is a protective  role  of N-acetylcystein against intestinal toxicity induced by 5-fluorouracil in albino rats.18 healthy adult rats were distributed into 3 groups of 6 rats for each. Group A as a control group.Group B injected with 5-FU (20 mgs dissolved in 2ml normal saline per kilogram body weight intraperitoneally for 7 successive days while Group C received N-acetylcysteine 200 mg per kilogram body weight 24 hour prior to FU injections for 7 consecutive days. The animals were sacrificed specimens of intestine (colon) tissue of the three groups were removed and prepared for light microscopic examination.The sections were stained with Harris Hematoxylin and Eosin (H&E) stain and Masson's trichrome stain. Results showed increase in the depth of the colonic crypts in group B rats as compared to the control group, mucinous degeneration of the intestinal mucosal cells along with necrosis, and inflammatory cells infiltration in the lamia propria. The appearance of the crypts is nearly normal in group C with reduction in the depth and normal columnar epithelium lining the crypts the study concluded that 5-FU seriously affects the structure of the intestinal tissue and pretreatment with NAC protects the intestinal tissue against the toxic effects provoked by 5FU via antioxidant effect.
5-氟尿嘧啶(5-FU)是一种广泛用于治疗各种恶性肿瘤的嘧啶类似物,它属于抗代谢物家族,在细胞周期的s期起作用,从而阻止DNA合成。n -乙酰半胱氨酸是一种营养补体,具有抗氧化剂的作用。本研究旨在探讨n -乙酰半胱氨酸对5-氟尿嘧啶致白化病大鼠肠道毒性是否具有保护作用。健康成年大鼠18只,随机分为3组,每组6只。A组作为对照组。B组连续7天腹腔注射5-FU (20 mg溶解于每公斤体重2ml生理盐水中),C组在FU注射前24小时注射n -乙酰半胱氨酸200 mg /公斤体重,连续7天。处死动物,取各组肠(结肠)组织标本,进行光镜检查。切片采用Harris苏木精和伊红(H&E)染色和Masson三色染色。结果显示,B组大鼠结肠隐窝深度较对照组增加,肠黏膜细胞黏液变性伴坏死,固有层有炎性细胞浸润。C组隐窝外观基本正常,隐窝深度减少,隐窝内壁柱状上皮正常,提示5-FU严重影响肠组织结构,NAC预处理可通过抗氧化作用保护肠组织免受5FU引起的毒性作用。
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引用次数: 1
Lipid -Lowering Effect of Polysaccharide (Pectin) of Viscum album L. Plant in Rats 甘露多糖(果胶)对大鼠的降脂作用
D. Pozdnyakov, S. Adzhiakhmetova, N. Chervonnaya, S. Oganesyan
Disturbances of lipid metabolism is a predisposing factor of cardiovascular diseases, which are accompanied by high mortality rates of the population - ischemic heart disease and ischemic stroke. Plant polysaccharides can be promising remedies for correction of lipid imbalance. In this regard, the aim of the study was to assess the hypolipidemic activity of polysaccharides isolated from the leaves of mistletoe. The test-object was the leaves of the white mistletoe (Viscum album L.) growing on the apple (Malus domestica Borkh.), and the pear (Pyrus communis L.). Polysaccharides (water-soluble polysaccharides and pectin substances) were quantitatively determined by the gravimetric method followed by reprecipitation from ethanol. The qualitative composition was evaluated by thin layer chromatography. Functional groups in polysaccharides were determined by titrimetric method. The hypolipidemic activity of the obtained polysaccharides was determined under oral administration at a dose of 100 mg / kg in Wistar rats by the change of the concentration of total cholesterol, triglycerides, LDL and HDL cholesterol. The change of the content of cholesteryl ester transfer protein and Niemann-Pick C1-Like1 protein was also determined. As a result, it was found that among the polysaccharides in the leaves of mistletoe, pectin substances are predominate, which belong to the group of low-esterified pectins. A significant content of free carboxyl groups in pectins from the leaves of mistletoe was also found. The study of hypolipidemic activity showed that, among the polysaccharides of mistletoe leaves, pectin substances exert a more pronounced effect on lipid metabolism, the use of which reduced the content of triglycerides, total cholesterol and LDL cholesterol with an increase in LDL cholesterol in rats, probably due to a decrease in the activity of cholesteryl ester transfer protein and Niemann-Pick C1-Like1 protein. At the same time, at the level of the trend, mistletoe pectins showed a higher level of activity than analogous compounds obtained from the leaves of host-plants. It should be noted that the severity of the pharmacological effect of mistletoe pectins did not depend on the host-plants. Thus, based on the obtained results, it can be assumed that pectins obtained from the mistletoe leaves can be a potentially effective and safety hypolipidemic agent.
脂质代谢紊乱是心血管疾病的易感因素,心血管疾病伴随着高死亡率的人群-缺血性心脏病和缺血性中风。植物多糖是一种很有前途的治疗脂质失衡的药物。在这方面,本研究的目的是评估从槲寄生叶中分离的多糖的降血脂活性。试验对象是生长在苹果(Malus domestica Borkh.)和梨(Pyrus communis L.)上的白槲寄生(Viscum album L.)的叶子。用重量法定量测定多糖(水溶性多糖和果胶物质),然后用乙醇再沉淀。采用薄层色谱法对其定性组成进行评价。用滴定法测定多糖中的官能团。以100mg / kg剂量口服Wistar大鼠,通过改变总胆固醇、甘油三酯、低密度脂蛋白和高密度脂蛋白胆固醇的浓度来测定所得多糖的降血脂活性。测定了胆固醇酯转移蛋白和Niemann-Pick C1-Like1蛋白含量的变化。结果表明,槲寄生叶多糖中以果胶物质为主,属低酯化果胶类。槲寄生叶的果胶中游离羧基含量也很高。降血脂活性研究表明,槲寄生叶多糖中果胶物质对脂质代谢的影响更为明显,果胶物质的使用降低了大鼠体内甘油三酯、总胆固醇和LDL胆固醇的含量,使LDL胆固醇升高,可能是由于降低了胆固醇酯转移蛋白和Niemann-Pick C1-Like1蛋白的活性。同时,在趋势水平上,槲寄生果胶表现出比从寄主植物叶片中获得的类似化合物更高的活性水平。应该指出的是,槲寄生果胶的药理作用的严重程度并不取决于寄主植物。因此,根据所获得的结果,可以假设从槲寄生叶子中获得的果胶可能是一种潜在有效和安全的降血脂剂。
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引用次数: 0
Role of Fasting Mimicking Diet in Farnesoid x Receptor for Suppressing Epithelial-to-Mesenchymal Transition, Cell Cycle Progression, and Viability of Prostate Cancer Cells 禁食模拟饮食在Farnesoid x受体抑制前列腺癌细胞上皮向间质转化、细胞周期进展和活力中的作用
W. Al-khfajy, I. Arif, Basma T. Al-sudani
The systemic and resistant nature of metastatic castration-resistant prostate cancers (mCRPC) renders it largely incurable even after intensive multimodal therapy. Proliferation, survival, and epithelial-mesenchymal transition (EMT) are three fundamental events that are deeply linked to carcinogenesis.  Hence, it is necessary to find a new combination of several therapies, targeting those vital mechanisms without causing side effects. Significant research works have shown differential low expression of the metabolic Farnesoid X receptor (FXR) in primary and metastatic prostate cancer suggesting their importance in prostate pathogenesis. Obticholic acid (INT 747), a potent FXR agonist is widely used in primary biliary cholangitis, and Fasting mimicking Diet (FMD) both were drastically showed effects on different cancer progression. We hypothesized that FXR and FMD may inhibit proliferation and the metastatic phenotype in PC-3 prostate cancer cells. Analyses of the cell viability, cell cycle, migration, and matrigel invasion assays were performed to elucidate how INT 747 and /or FMD functions in prostate cancer. In this study, INT 747 treatment caused apoptotic morphological changes and significantly reduced the survival of PC-3 cells incubated in normal mediums.  Furthermore, we showed that the combination of the INT 747 and FMD was much more harmful to cancer cells than the treatment with INT 747 or FMD alone. Moreover, our study showed that INT 747 either alone or combined with FMD robustly induced cell cycle arrest at the S phase. Interestingly, the combination treatment on PC-3 cells not only showed several lines of evidence of apoptotic cells death but also inhibited carcinogenic potential as evaluated by impairment of spheroid formation capacity and delayed wound healing and matrigel invasion. At the cellular level, FXR activation resulted in down-regulation of procaspase -3, vimentin, and MMP9, which triggers apoptotic cell death, cell cycle arrest, and switch from mesenchymal to an epithelial phenotype. Collectively, FXR activation alone markedly decreases, and when combined with FMD abrogates the survival and carcinogenic potential of metastatic prostate cancer cells.  
转移性去势抵抗性前列腺癌(mCRPC)的系统性和耐药性使其即使经过强化的多模式治疗也基本上无法治愈。增殖、存活和上皮-间质转化(epithelial-mesenchymal transition, EMT)是与癌变密切相关的三个基本事件。因此,有必要找到几种治疗方法的新组合,针对这些重要机制而不产生副作用。重要的研究工作表明,代谢性法内酯X受体(FXR)在原发性和转移性前列腺癌中的低表达差异表明其在前列腺发病机制中的重要性。Obticholic acid (int747)是一种有效的FXR激动剂,广泛用于原发性胆道胆管炎,而空腹模拟饮食(FMD)对不同的癌症进展都有显著的影响。我们假设FXR和FMD可能抑制PC-3前列腺癌细胞的增殖和转移表型。通过分析细胞活力、细胞周期、迁移和基质侵袭试验来阐明INT 747和/或FMD在前列腺癌中的作用。在本研究中,INT 747处理引起了PC-3细胞在正常培养基中的凋亡形态学改变,并显著降低了PC-3细胞的存活率。此外,我们还发现,与单独使用INT 747或FMD相比,INT 747和FMD联合使用对癌细胞的危害要大得多。此外,我们的研究表明,无论是单独使用INT 747还是与FMD联合使用,都能强烈地诱导细胞周期阻滞在S期。有趣的是,对PC-3细胞的联合治疗不仅显示出凋亡细胞死亡的多项证据,而且通过球体形成能力的损害、伤口愈合和基质侵袭的延迟来评估,还抑制了致癌潜力。在细胞水平上,FXR的激活导致procaspase -3、vimentin和MMP9的下调,从而引发凋亡细胞死亡、细胞周期阻滞,并从间充质表型向上皮表型转换。总的来说,FXR单独激活显著降低,当与FMD联合使用时,消除了转移性前列腺癌细胞的存活和致癌潜力。
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引用次数: 2
The Ameliorating Effect of Oral Paquinimod Administration against Imiquimod Induced Psoriasis-like Inflammation in Mice 口服帕喹莫德对咪喹莫德诱导的小鼠银屑病样炎症的改善作用
R. Khaleel, M. Zalzala
                 Psoriasis is a chronic, inflammatory condition that primarily affects the skin, hair, and joints and is associated with significant humanistic and economic consequences. Psoriasis was induced in mice in this work using an imiquimod 5% cream, an immune response modifier that can cause psoriasis-like skin inflammation when given orally. Paquinimod is prepared as a suspension and has been orally given to mice before imiquimod application. The current study found that paquinimod suspension reduced psoriasis area and severity index, spleen index, skin thickness ,TNF-α,IL-23,IL17 level and gene expression of TNF-α,Nf-KB,IL-1B,IL-17in the (Paquinimod suspension+imiquimod) group substantially more than the (vehicle suspension+imiquimod) groups.
牛皮癣是一种慢性炎症性疾病,主要影响皮肤、头发和关节,并与重大的人文和经济后果有关。在这项工作中,使用5%咪喹莫特乳膏在小鼠中诱导牛皮癣,这是一种免疫反应调节剂,口服后可引起牛皮癣样皮肤炎症。帕喹莫德制备为悬浮液,在咪喹莫德应用前给小鼠口服。目前的研究发现,帕喹莫德混悬液组的银屑病面积和严重程度指数、脾脏指数、皮肤厚度、TNF-α、IL-23、il -17水平以及TNF-α、Nf-KB、IL-1B、il -17的基因表达明显大于(整车混悬液+米喹莫德)组。
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引用次数: 0
Optimization of Bis-anthraquinones Production from Endophytic Fungi Diaporthe sp. GNBP-10 内生真菌Diaporthe sp. GNBP-10产双蒽醌的优化
L. Oktavia, Evana Evana, Reza Fahardita, A. Agusta
Bis-anthraquinones with a unique molecular backbone, (+)-2,2’-epicytoskyrin A (epi) and (+)-1,1′-bislunatin (bis), was produced by endophytic fungi Diaporthe sp GNBP-10 associated with Gambir plant (Uncaria gambier). Epi and bis possess robust antimicrobial activity toward various pathogens. This study focus on knowing the optimum condition of epi and bis production from Diaporthe sp GNBP-10. A series of culture media with various nutrient compositions was investigated in epi and bis production. The content of epi and bis was determined by measuring the area under the curve from TLC-densitometric (scanner) experiment. The linear regression analysis was then applied to obtain the results. The optimized epi and bis production was observed in liquid media 3 containing potato starch and dextrose with the amount of epi produced is 0.484mg while bis content is 0.163mg. The presence of carbohydrates, whether simple sugar or carbohydrate complex, plays an essential role in the bis-anthraquinones production from Diaphorthe sp culture. The presence of minerals and excessive protein sources did not significantly affect bis-anthraquinones production.  Keywords: bis-anthraquinone, Diaporthe sp, culture media, regression, TLC scanner
甘比亚(Uncaria gambier)特有的内生真菌Diaporthe sp GNBP-10可产生具有独特分子骨架((+)-2,2′-epicytoskyrin a (epi)和(+)-1,1′-bislunatin (bis))的双蒽醌类化合物。Epi和his对多种病原菌具有较强的抑菌活性。本文主要研究了以Diaporthe sp GNBP-10为原料生产epi的最佳工艺条件。研究了一系列不同营养成分的培养基在epi及其生产中的应用。采用薄层扫描密度法测定epi和his的含量。然后应用线性回归分析得到结果。在含有马铃薯淀粉和葡萄糖的液体培养基3中,epi的产量为0.484mg, his的含量为0.163mg。碳水化合物的存在,无论是单糖还是碳水化合物复合物,在双蒽醌的产生中起着至关重要的作用。矿物质的存在和过量的蛋白质来源对双蒽醌的产生没有显著影响。关键词:双蒽醌,Diaporthe sp,培养基,回归,TLC扫描
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引用次数: 0
Preparation and in Vitro Evaluation for Different Types of Ondansetron Hydrochloride Transdermal Patches 不同剂型盐酸昂丹司琼透皮贴剂的制备及体外评价
Karima Abd allatif, Jameela Ali Hasian
This research aims to develop transdermal patches of Ondansetron hydrochloride (OSH) with different types of polymers, ethyl cellulose and, polyvinyl pyrrolidone k30 in a ratio (3:0.5,3:1,3:2,2:1,1:1) with propylene glycol 20%w/w as a plasticizer. Prepared transdermal patches were evaluated for physical properties. The compatibility between the drug and excipients was studied by Differential scanning calorimetry (DSC), where there is no interaction between the drug and polymers. From the statistical study, there is a statistical difference between all the prepared formulations p<0.05. In-vitro Release study of transdermal patches was performed by using a paddle over the disc. The release profile of OSH followed Korsmeyer - Peppas Model in P2, P4 formulations and, Higuchi Model in P1, P3, P5 formulations. The best formulation P6 carrying EC:PVP in ratio1:1 released 96.47% of ondansetron hydrochloride during 12 h. The release profile of P6 followed the Higuchi model and correlation coefficient  (r2 = 0.9815)
本研究旨在以丙二醇20%w/w为增塑剂,以不同类型的聚合物乙基纤维素和聚乙烯吡罗烷酮k30按3:0.5,3:1,3:2,2:1,1:1的比例制备盐酸昂丹西琼透皮贴剂(OSH)。对制备的透皮贴片进行物理性能评价。用差示扫描量热法(DSC)研究了药物与赋形剂之间的相容性,其中药物与聚合物之间没有相互作用。从统计学研究来看,各制剂间差异有统计学意义p<0.05。透皮贴剂的体外释放研究是通过在椎间盘上使用桨来进行的。P2、P4剂型的OSH释放曲线符合Korsmeyer - Peppas模型,P1、P3、P5剂型的Higuchi模型。最佳处方P6在12 h内对盐酸昂丹司琼的释放量为96.47%,释放曲线符合Higuchi模型,相关系数(r2 = 0.9815)。
{"title":"Preparation and in Vitro Evaluation for Different Types of Ondansetron Hydrochloride Transdermal Patches","authors":"Karima Abd allatif, Jameela Ali Hasian","doi":"10.31351/vol32iss1pp147-155","DOIUrl":"https://doi.org/10.31351/vol32iss1pp147-155","url":null,"abstract":"This research aims to develop transdermal patches of Ondansetron hydrochloride (OSH) with different types of polymers, ethyl cellulose and, polyvinyl pyrrolidone k30 in a ratio (3:0.5,3:1,3:2,2:1,1:1) with propylene glycol 20%w/w as a plasticizer. Prepared transdermal patches were evaluated for physical properties. The compatibility between the drug and excipients was studied by Differential scanning calorimetry (DSC), where there is no interaction between the drug and polymers. From the statistical study, there is a statistical difference between all the prepared formulations p<0.05. In-vitro Release study of transdermal patches was performed by using a paddle over the disc. The release profile of OSH followed Korsmeyer - Peppas Model in P2, P4 formulations and, Higuchi Model in P1, P3, P5 formulations. The best formulation P6 carrying EC:PVP in ratio1:1 released 96.47% of ondansetron hydrochloride during 12 h. The release profile of P6 followed the Higuchi model and correlation coefficient  (r2 = 0.9815)","PeriodicalId":14509,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-06-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87294491","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: 0
Autophagy or Apoptosis: Anticancer Molecular Mechanism of Epigallocatechin Gallate with Natural Polyphenol Effect on HepG2 Cells Viability 自噬或凋亡:表没食子儿茶素没食子酸酯与天然多酚作用对HepG2细胞活力的抗癌分子机制
R. Hafidh, Z. Ali, A. Abdulamir
Background: The anticancer impact of Epigallocatechin gallate (EGCG) the highly active polyphenol of green tea was abundantly studied.  Though, the exact mechanism of its cytotoxicity is still under investigation. Objectives: Hence, the current study designed to investigate the molecular target of EGCG in HepG2 cells on thirteen autophagy- and/or apoptosis- related genes. Methods: The apoptosis detection analyses such as flow cytometry and dual apoptosis assay were used. The genes expression profile was explored by the real-time quantitative-PCR. Results: EGCG increases G0/G1 cell cycle arrest and the real-time apoptosis markers proteins leading to stimulate apoptosis in 70% of the treated HepG2 cells. The up-regulation was recorded in two of autophagy inhibitory genes (FOS-1, FOS-2) and apoptosis inducer gene (DDIT3). While the other ten genes expressed down-regulation after treatment. The down regulation was manifested in the genes of mitochondrial autophagy marker proteins (BNIP3, BNIP3L, and NBR1), the autophagy regulator genes (BIRC5, MAPK9), and the gene that implicated in protein biosynthesis and protein modification (ITGB1). The genes that have pro-apoptotic function in cells (CAPNS1, CFLAR, EIF4G, and RB1) were also showed down-regulation after treatment. Conclusion: Thus, the results demonstrated a potential effect of EGCG to induce apoptosis rather than autophagy in the treated HepG2 cells that could play a good target for therapy. 
背景:对绿茶中高活性多酚表没食子儿茶素没食子酸酯(EGCG)的抗癌作用进行了大量研究。尽管如此,其细胞毒性的确切机制仍在研究中。因此,本研究旨在探讨EGCG在HepG2细胞中对13个自噬和/或凋亡相关基因的分子靶点。方法:采用流式细胞术、双细胞凋亡法进行细胞凋亡检测。实时荧光定量pcr检测基因表达谱。结果:EGCG增加70% HepG2细胞的G0/G1细胞周期阻滞和实时凋亡标记蛋白导致细胞凋亡。自噬抑制基因FOS-1、FOS-2和凋亡诱导基因DDIT3表达上调。其余10个基因在处理后表达下调。线粒体自噬标志蛋白(BNIP3、BNIP3L和NBR1)、自噬调节基因(BIRC5、MAPK9)和与蛋白质生物合成和蛋白质修饰相关的基因(ITGB1)均出现下调。细胞中具有促凋亡功能的基因(CAPNS1、CFLAR、EIF4G、RB1)在治疗后也出现下调。结论:EGCG具有诱导HepG2细胞凋亡而非自噬的潜在作用,可作为治疗HepG2细胞的良好靶点。
{"title":"Autophagy or Apoptosis: Anticancer Molecular Mechanism of Epigallocatechin Gallate with Natural Polyphenol Effect on HepG2 Cells Viability","authors":"R. Hafidh, Z. Ali, A. Abdulamir","doi":"10.31351/vol32iss1pp167-176","DOIUrl":"https://doi.org/10.31351/vol32iss1pp167-176","url":null,"abstract":"Background: The anticancer impact of Epigallocatechin gallate (EGCG) the highly active polyphenol of green tea was abundantly studied.  Though, the exact mechanism of its cytotoxicity is still under investigation. Objectives: Hence, the current study designed to investigate the molecular target of EGCG in HepG2 cells on thirteen autophagy- and/or apoptosis- related genes. Methods: The apoptosis detection analyses such as flow cytometry and dual apoptosis assay were used. The genes expression profile was explored by the real-time quantitative-PCR. Results: EGCG increases G0/G1 cell cycle arrest and the real-time apoptosis markers proteins leading to stimulate apoptosis in 70% of the treated HepG2 cells. The up-regulation was recorded in two of autophagy inhibitory genes (FOS-1, FOS-2) and apoptosis inducer gene (DDIT3). While the other ten genes expressed down-regulation after treatment. The down regulation was manifested in the genes of mitochondrial autophagy marker proteins (BNIP3, BNIP3L, and NBR1), the autophagy regulator genes (BIRC5, MAPK9), and the gene that implicated in protein biosynthesis and protein modification (ITGB1). The genes that have pro-apoptotic function in cells (CAPNS1, CFLAR, EIF4G, and RB1) were also showed down-regulation after treatment. Conclusion: Thus, the results demonstrated a potential effect of EGCG to induce apoptosis rather than autophagy in the treated HepG2 cells that could play a good target for therapy. ","PeriodicalId":14509,"journal":{"name":"Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-06-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88140569","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}
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Iraqi Journal of Pharmaceutical Sciences ( P-ISSN: 1683 - 3597 , E-ISSN : 2521 - 3512)
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