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Enhancement of solubility and dissolution of ibuprofen microparticle prepared by ultrasonic spray drying 超声喷雾干燥法提高布洛芬微粒的溶解度和溶出度
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.30
Revika Rachmaniar, C. Panatarani, I. Joni, Marline Abdasah, T. Rusdiana
Ibuprofen (IBU) is one of the most commonly used nonsteroidal anti-inflammatory drugs with high permeability and low solubility. The aims of this research is to improve the solubility and dissolution of the IBU by reducing particle size using ultrasonic spray drying method and utilizing watersoluble polymer (polyvinyl alcohol (PVA)) and surfactant (sodium lauryl sulphate (SLS)) for particles formulation. The results showed that increasing amount of PVA, smaller particle size of as-prepared IBU-PVA-SLS was obtained, 6.3-fold smaller than untreated IBU. The in vitro drug release study for simulated gastric fluid without enzymes (0.1 N HCl or Buffer pH 1.2) shows the dissolution of prepared IBU-PVA-SLS significantly increase 2.4-fold higher than untreated IBU for dissolution time of 30 minutes. While the solubility of the IBU-PVA-SLS was increased 4.7-fold compare to untreated IBU. In general, IBU possessing relatively high dissolution in intestinal fluid. In contrast, the finding of recent investigation on dissolution of IBU-PVA-SLS is significantly increase in gastric fluid, either due to smaller particles size or PVA-SLS. Thus, despite the PVA and SLS determine the particles formation during polymerization yielding smaller particle size, they also responsible for effective drug delivery system. It was concluded that PVA and SLS in ultrasonic spray drying technique for IBU preparation successfully reduces the particle size and effectively enhances the solubility and dissolution rate of poorly water-soluble IBU in 0.1 N HCl.
布洛芬(Ibuprofen, IBU)是最常用的高通透性、低溶解度的非甾体类抗炎药之一。本研究的目的是通过超声波喷雾干燥法减小颗粒尺寸,利用水溶性聚合物(聚乙烯醇(PVA))和表面活性剂(十二烷基硫酸钠(SLS))进行颗粒配方,提高IBU的溶解度和溶解度。结果表明,随着PVA添加量的增加,制备的IBU-PVA- sls的粒径变小,比未处理的IBU小6.3倍。无酶模拟胃液(0.1 N HCl或缓冲液pH 1.2)体外药物释放研究表明,在溶出时间为30分钟时,制备的IBU- pva - sls的溶出度比未处理的IBU显著提高2.4倍。与未治疗的IBU相比,IBU- pva - sls的溶解度提高了4.7倍。一般来说,IBU在肠液中具有较高的溶出度。相比之下,最近对IBU-PVA-SLS溶出的研究发现,胃液中IBU-PVA-SLS的溶出明显增加,这可能是由于颗粒尺寸较小或PVA-SLS所致。因此,尽管PVA和SLS在聚合过程中决定了颗粒的形成,产生更小的颗粒尺寸,但它们也负责有效的药物输送系统。综上所述,PVA和SLS在制备IBU的超声波喷雾干燥技术中成功地减小了IBU的粒径,有效地提高了难水溶性IBU在0.1 N HCl中的溶解度和溶解速率。
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引用次数: 3
Chemical composition, antioxidant, anticholinesterase and anti-urease activities of Sideritis pisidica Boiss. & Heldr. endemic to Turkey 甜菜黄螺旋体的化学成分、抗氧化活性、抗胆碱酯酶和抗脲酶活性。& Heldr。土耳其特有的
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.13
Ebru Deveci, Gülsen Tel‐Çayan, H. Yıldırım, M. Duru
The objective of this study was to investigate the chemical composition, antioxidant, anticholinesterase and anti-urease activities of essential oil, hexane, acetone and methanol extracts of Sideritis pisidica Boiss. & Heldr. The essential oil and fatty acid composition were analyzed by GC and GC/MS. δ-Cadinene (19.5 %), T-cadinol (16.7 %) and β-cubebene (10.4 %) were identified as the main compounds of the essential oil whereas the most abundant compounds of fatty acids were found as linolenic (42.7 %), palmitic (31.3 %) and linoleic (13.4%) acids. The methanol extract demonstrated the highest antioxidant activity in all tests, except for metal chelating assay. The hexane extract was found to be significantly active in metal chelating (IC50: 22.97±1.36 μg/mL), acetylcholinesterase (62.54±0.88 %) and urease inhibitory (78.93±0.17 %) assays. These results show that the Sideritis pisidica could be used as the potential source of natural products in the food and pharmaceutical areas.
摘要本研究主要研究了猪Sideritis pisidica Boiss挥发油、己烷、丙酮和甲醇提取物的化学成分、抗氧化活性、抗胆碱酯酶和抗脲酶活性。& Heldr。采用气相色谱(GC)和质谱(GC/MS)分析了精油和脂肪酸组成。δ-Cadinene(19.5%)、T-cadinol(16.7%)和β-cubebene(10.4%)是挥发油的主要成分,而亚麻酸(42.7%)、棕榈酸(31.3%)和亚油酸(13.4%)是挥发油中含量最多的脂肪酸。除金属螯合试验外,甲醇提取物在所有试验中均表现出最高的抗氧化活性。正己烷提取物对金属螯合(IC50: 22.97±1.36 μg/mL)、乙酰胆碱酯酶(62.54±0.88%)和脲酶抑制(78.93±0.17%)均有显著活性。结果表明,该菌可作为食品和医药领域天然产物的潜在来源。
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引用次数: 11
Plants Used as Painkiller in Folk Medicine in Turkey-I STOMACHACHE 土耳其民间医药中用作止痛药的植物——胃痛
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.0
Meryem Seyda Erbay, S. Anıl, G. Melikoğlu
There are many plants used by the public in the treatment of various diseases in Turkey.The folk remedies prepared with these plants from which treatment and how they used have been reached to day-to-day by transferring the generations. Ethnobotanic researches and traditional treatment methods are recorded and it is aimed to contribute to drug development studies.In this study, which was prepared by screening of ethnobotanical researches, 221 taxa which used in traditional treatment against stomachache in Turkey are reached and the scientific , local names, families, used parts of these taxa and the forms used in stomachache were compiled. According to the research done, families that are commonly used for stomachache are Lamiaceae (59 taxa), Asteraceae (28 taxa), Rosaceae (14 taxa), Apiaceae (12 taxa), Hypericaceae (8 taxa) and Fabaceae (7 taxa). The main reason why these family plants are used against stomach ache is that they contain essential oils with stomach related effect. The most commonly used parts of the plants for treatment are herba, leaf, flower, fruit, root and seed. The parts used may be prepared as decoction or infusion in the form of tea, eaten fresh or after being cooked, or by mixing with honey; the herba of some plants is made into mush then put on the stomach is used externally in the treatment of stomachache.
在土耳其,公众使用许多植物来治疗各种疾病。用这些植物准备的民间偏方,从哪里治疗和如何使用,已经通过代代相传达到了日常。记录民族植物研究和传统治疗方法,旨在为药物开发研究做出贡献。本研究通过对民族植物学研究资料的筛选,获得了土耳其传统治疗胃痛的221个分类群,并对这些分类群的学名、地名、科、使用部位和胃痛治疗形式进行了整理。研究表明,常用于胃痛的科有Lamiaceae(59个分类群)、Asteraceae(28个分类群)、rosacaceae(14个分类群)、Apiaceae(12个分类群)、Hypericaceae(8个分类群)和Fabaceae(7个分类群)。这些科植物被用来治疗胃痛的主要原因是它们含有与胃有关的精油。植物中最常用的部分是草药、叶子、花、果实、根和种子。所使用的部分可以以茶的形式制成汤剂或冲剂,新鲜食用或煮熟后食用,或与蜂蜜混合食用;将某些植物的草药制成糊状,涂在胃上,外用治疗胃痛。
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引用次数: 6
Characterization of Sideritis trojana Bornm. essential oil and its antimicrobial activity 先天性特洛伊黄疸的特征。精油及其抑菌活性
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.14
H. Kırmızıbekmez, N. Karaca, B. Demirci, Fatih Demirci
The components of the essential oil obtained from the dried aerial parts of Sideritis trojana Bornm. by hydrodistillation was analyzed both by GC-FID and GC-MS, simultaneously. Overall 57 compounds were identified representing 83.8% of the oil. The major components of the oil were identified as valeranone (11.3%), α-bisabolol (10.9%) and β-caryophyllene (8.8%), respectively. The composition of the oil showed quantitative chemical variation from previously studied material in terms of its major components. Moreover, the essential oil was evaluated for its in vitro antibacterial and anticandidal activities using a broth microdilution method. A selected panel of standard strains of Gram (+) and Gram (-) human pathogens as well as Candida albicans were used in the assay. As a preliminary result, it was observed that the oil displayed relatively moderate antibacterial activity against Helicobacter pylori with MIC value of 250 μg/mL when compared to standard antimicrobials. As a conclusion, it is worthwhile to evaluate the plant material against a broader spectrum of activities.
从牛蒡草干燥的空气部分提取的精油成分。气相色谱- fid和气相色谱-质谱联用分析。总共鉴定出57种化合物,占油的83.8%。主要成分分别为缬草酮(11.3%)、α-双abolol(10.9%)和β-石竹烯(8.8%)。在主要成分方面,油的组成与先前研究的材料显示出定量的化学变化。此外,采用肉汤微量稀释法评价了精油的体外抗菌和抗念珠菌活性。选择一组革兰氏(+)和革兰氏(-)人类病原体的标准菌株以及白色念珠菌用于测定。初步结果表明,与标准抗菌剂相比,该油对幽门螺杆菌的抑菌活性相对中等,MIC值为250 μg/mL。综上所述,对植物材料进行更广泛的活性评价是值得的。
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引用次数: 10
Development of a validated high-performance liquid chromatographic method for the determination of Lurasidone in pharmaceuticals 建立高效液相色谱法测定药物中鲁拉西酮的方法
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.32
Sakine Atila Karaca, Duygu Yeniceli Uğur
A new, rapid and simple HPLC method for determination of Lurasidone in its tablets has been developed and validated. Lurasidone and internal standard (Chlorpromazine) was separated on a Zorbax XDB C8 column (4.6 x 50 mm, 3.5 μm particle size) set at 40°C and quantified by ultraviolet detection at 230 nm. The mobile phase was phosphate buffer (pH:3, 20 mM): acetonitrile: methanol (55:10:35, v/v/v) with a flow rate of 1.2 mL/min. Retention times of Chlorpromazine and Lurasidone was 4.73 and 6.89 minutes, respectively. The method was found linear over the concentration range of 0.5-50 μg/mL Lurasidone. Limit of detection and quantification values for Lurasidone was 0.1295 and 0.4317 μg/mL, respectively. The intra- and inter day precisions were less than 2% and the mean recoveries were 100.32%, which indicated that the method was precise and accurate. All other validation parameters were found within acceptable limits. The validated method has been successfully applied for determination of Lurasidone in its tablets. Keywords:
建立了一种快速简便的高效液相色谱法测定鲁拉西酮片剂中鲁拉西酮的含量。鲁拉西酮和内标氯丙嗪在Zorbax XDB C8色谱柱(4.6 × 50 mm, 3.5 μm粒度)上分离,柱温为40°C,紫外检测波长为230 nm。流动相为磷酸缓冲液(pH: 3,20 mM):乙腈:甲醇(55:10:35,v/v/v),流速为1.2 mL/min。氯丙嗪和鲁拉西酮的保留时间分别为4.73和6.89 min。在0.5 ~ 50 μg/mL鲁拉西酮浓度范围内,该方法线性良好。鲁拉西酮的检出限和定量值分别为0.1295和0.4317 μg/mL。日内、日间精密度小于2%,平均加样回收率为100.32%,表明该方法精密度高、准确度高。所有其他验证参数均在可接受范围内。该方法可用于鲁拉西酮片剂的含量测定。关键词:
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引用次数: 3
Biosynthesis of copper nanoparticles using aqueous extract of Capparis spinosa fruit and investigation of its antibacterial activity 红椒果实水提物生物合成纳米铜及其抑菌活性研究
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.31
Katrin Ebrahimi, Sima Shiravand, H. Mahmoudvand
The present study was aimed to use the aqueous extract of Capparis spinosa to synthesize the copper nanoparticles and also evaluated their antibacterial activities again some pathogenic bacterial strains. UV-vis spectroscopy analyses, fourier transform of infrared (FTIR), scanning electron microscopy (SEM), and energy dispersive X-ray (EDX) were used to identify the synthesized nanoparticles. The antimicrobial activity of the synthesized copper nanoparticles was investigated using disk diffusion method and broth microdilution against some Gram-positive and Gram-negative bacteria. After adding the extract to the copper sulfate solution, the color of the solution changed from light blue to yellowish green. Existence of a maximum peak at the wavelength of 414 nm confirmed the formation of the copper nanoparticles. FTIR spectrum analysis showed that the factor groups created a coating extract on the surface of the nanoparticles. Scanning electron microscopy demonstrated the particle size between 17 and 41 nm. These findings showed that Staphylococcus aureus and Bacillus cereus as Gram-positive bacteria were most susceptible to synthesized copper nanoparticles in comparison with the Gram-negative bacteria (Klebsiella pneumoniae, and Escherichia coli). The obtained findings demonstrated that the aqueous extract of C. spinosa acts as a reviver and stabilizer factor. The synthesized copper nanoparticles demonstrated activity against both Grampositive and Gram-negative bacteria.
本研究旨在利用刺毛椒水提物合成铜纳米颗粒,并对其对病原菌的抑菌活性进行评价。利用紫外可见光谱(UV-vis)、红外傅立叶变换(FTIR)、扫描电镜(SEM)和能量色散x射线(EDX)对合成的纳米颗粒进行了表征。采用圆盘扩散法和微量肉汤稀释法研究了合成的铜纳米颗粒对革兰氏阳性和革兰氏阴性细菌的抑菌活性。将提取物加入硫酸铜溶液后,溶液的颜色由淡蓝色变为黄绿色。在414 nm处存在最大峰,证实了铜纳米颗粒的形成。FTIR光谱分析表明,这些因子基团在纳米颗粒表面形成了涂层提取物。扫描电镜显示颗粒尺寸在17 ~ 41 nm之间。这些结果表明,与革兰氏阴性菌(肺炎克雷伯菌和大肠杆菌)相比,作为革兰氏阳性菌的金黄色葡萄球菌和蜡样芽孢杆菌对合成铜纳米颗粒最敏感。实验结果表明,棘豆水提物具有恢复剂和稳定剂的作用。合成的铜纳米颗粒对革兰氏阳性和革兰氏阴性细菌均有活性。
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引用次数: 42
The action of monoterpenoids with promising antiparkinsonian activity on fertility of Drosophila melanogaster 具有抗帕金森活性的单萜类化合物对果蝇生育能力的影响
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.29
M. Trushin, R. Khamidullina, O. Ardashov, K. Volcho, N. Salakhutdinov
Adequate treatment of Parkinson’s disease is an important medical issue. Patients are suffered from numerous side effects of the widely used drugs. It has been found recently that monoterpenoid (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl) cyclohex-3-ene-1,2-diol and its diacetate demonstrate high antiparkinsonian activity in some animal models. At the same time, their genetic safety was not studied yet. The aim of this research was to investigate the effect of these compounds with antiparkinsonian activities on reproduction of D. melanogaster. Over 4000 of fruitflies cultivated under the action of these compounds were analyzed. It was found that the chemicals did not provoke genetic mutations or alter reproduction of D. melanogaster. The possible explanations for the detected phenomena are provided. It was found that the compounds do not affect fertility in Drosophila..
帕金森病的适当治疗是一个重要的医学问题。这些被广泛使用的药物有许多副作用,病人饱受其苦。最近在一些动物模型中发现单萜(1R,2R,6S)-3-甲基-6-(丙-1-烯-2-基)环己基-3-烯-1,2-二醇及其二乙酸酯具有较高的抗帕金森活性。同时,它们的遗传安全性尚未得到研究。本研究的目的是探讨这些具有抗帕金森活性的化合物对黑胃鼠生殖的影响。对这些化合物作用下栽培的4000多只果蝇进行了分析。结果发现,这些化学物质不会引起基因突变,也不会改变黑腹天鼠的繁殖。对探测到的现象给出了可能的解释。结果表明,这些化合物不影响果蝇的生育能力。
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引用次数: 0
Prescribing pattern of antidiabetic drugs in type 2 diabetic patients of Noakhali city in Bangladesh 孟加拉国Noakhali市2型糖尿病患者抗糖尿病药物的处方模式
Pub Date : 2017-10-03 DOI: 10.12991/MPJ.2017.24
A. Chowdhury, Niloy Sen, Sujan Banik
The aim of the study was to describe the recent trends in the prescription pattern of antidiabetic drugs and sociodemographic characteristics of type 2 diabetic patients in Noakhali city of Bangladesh. This hospital based prospective, cross-sectional study was carried out in three diabetic hospitals of Noakhali during the period of December, 2016 to February, 2017. A total of 200 outpatients were included in this study by following simple random procedure. Among 200 participants, 73.5% were treated with monotherapy and 26.5% were treated with polytherapy with the highest percentage (37.5%) of commonly prescribed group drugs of sulfonylureas, but lonely metformin (biguanide) was the most commonest (28%) drug among oral hypoglycemic agents. The most accounted fixed dose combination was sulfonylurea with biguanide, and biguanide with glucodiase inhibitors. The highly prescribed insulin preparations was insulin mixtures (11%) among the patients. Drugs were prescribed by traditional brand names (100%) of different local or foreign companies and 15% of prescription were contained at least one multivitamin supplement. It was focused from this study that oral hypoglycemic agents (OHA) yet dominate the prescribing pattern, but there was a shifting trend towards insulin preparation in the management of Type 2 diabetes mellitus.
本研究的目的是描述孟加拉国Noakhali市2型糖尿病患者抗糖尿病药物处方模式的最新趋势和社会人口学特征。本研究于2016年12月至2017年2月在Noakhali的三家糖尿病医院进行前瞻性横断面研究。本研究采用简单随机方法,共纳入200例门诊患者。在200名受试者中,73.5%的人接受单一治疗,26.5%的人接受多种治疗,其中磺胺脲类常用药物的比例最高(37.5%),但单用二甲双胍(双胍)是口服降糖药中最常见的(28%)药物。最常见的固定剂量组合是磺脲与双胍类药物,以及双胍类药物与糖苷酶抑制剂。高处方胰岛素制剂为胰岛素混合物(11%)。这些药物均使用不同本地或外国公司的传统品牌(100%),15%的处方中至少含有一种复合维生素补充剂。本研究的重点是口服降糖药(OHA)仍占主导地位,但在2型糖尿病的治疗中,有向胰岛素制剂转变的趋势。
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引用次数: 10
In vitro gene silencing effect of chitosan/shRNA PDGF-D nanoparticles in breast cancer 壳聚糖/shRNA PDGF-D纳米颗粒在乳腺癌中的体外基因沉默作用
Pub Date : 2017-10-03 DOI: 10.12991/MPJ.2017.21
Ceyda Ekentok, S. Turan, J. Akbuğa
Breast cancer is the most common cancer worldwide in women and it is highly malignant and fatal. PDGF-D plays role in regulation of many cellular processes such as angiogenesis. PDGF-D is overexpressed in many types of cancers and promote tumor growth and metastasis. Silencing of PDGF-D gene by using shRNA with an appropriate carrier system may decrease tumor growth and metastasis. In our study, we prepared chitosan nanoparticles loaded with five different shRNA plasmids targeting different exons of PDGF-D gene. Then, nanoparticles were characterized in vitro and transfection efficiency of these nanoparticles were investigated in breast cancer cell lines (MCF- 7, MDA-MB-231 and MDA-MB-435). The effects of single and multiple shRNA sequences, molecular weight of chitosan (150 kDa and 400 kDa) and the amount of shRNA (100 and 500 μg) on the characterization and transfection efficiencies of nanoparticles have been studied. Size of nanoparticles changed between 200-400 nm and approximately 95-100% encapsulation efficiency were obtained. Release of shRNA changed with the molecular weight of chitosan. It was obtained that formulation containing shRNA plasmid targeting PDGF-D exon 6 (NP1) has the highest silencing efficiency in MDA-MB-231 cell line. It was also evaluated that chitosan can be a suitable gene delivery system for shRNA targeting PDGF-D.
乳腺癌是世界上最常见的女性癌症,它是高度恶性和致命的。PDGF-D在许多细胞过程中起调节作用,如血管生成。PDGF-D在许多类型的癌症中过度表达,促进肿瘤生长和转移。利用shRNA和合适的载体系统沉默PDGF-D基因可能会抑制肿瘤的生长和转移。在我们的研究中,我们制备了负载五种不同shRNA质粒的壳聚糖纳米颗粒,靶向PDGF-D基因的不同外显子。然后,在体外对纳米颗粒进行了表征,并研究了这些纳米颗粒在乳腺癌细胞系(MCF- 7、MDA-MB-231和MDA-MB-435)中的转染效率。研究了单、多shRNA序列、壳聚糖分子量(150 kDa和400 kDa)、shRNA用量(100和500 μg)对纳米颗粒表征和转染效率的影响。纳米颗粒的尺寸在200 ~ 400 nm之间变化,封装效率约为95 ~ 100%。壳聚糖的分子量改变了shRNA的释放量。结果表明,含有靶向PDGF-D外显子6 (NP1) shRNA质粒的制剂在MDA-MB-231细胞株中具有最高的沉默效率。壳聚糖可作为靶向PDGF-D的shRNA基因传递系统。
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引用次数: 3
Analytical and Sales Data Comparison of Reference Product of Insulin Aspart and its Biosimilar in Turkey 阿斯帕特胰岛素及其生物仿制药参比产品在土耳其的分析与销售数据比较
Pub Date : 2017-06-24 DOI: 10.12991/marupj.323591
Onur Hakkı Dal, A. Sezer
Son yillarda ilac sanayinin ve ilac biyoteknolojisinin en populer konularindan biri biyobenzerlerdir. Uretimleri daha karmasik surecler iceren biyoteknolojik urunler, patentlerinin de bitmeye yaklasmasi veya bitmesi ile ilgi odagi olmaktadir. Jenerik urunler ile karsilastirildiginda karmasik surecler sadece uretim ile sinirli degildir. Gelistirme, klinik surecleri ve pazara erisim surecleri de zorlu ve maliyetlidir. Bu zorluklara ragmen biyobenzer gelistiren ve gelistirme calismalari devam eden bircok sirket bulunmaktadir. Jenerikler ile iliskili olarak gectigimiz uzun yillara ait net veriler olmasina ragmen biyobenzerler icin bircok baslik jeneriklere kiyasla yeni tartisilmaya baslanmistir. Bu basliklar arasinda biyobenzerlerin ekonomik katkisi, kamu maliyetine etkileri, hasta erisimi, klinik calismalar ve referans urun ile karsilastirma calismalarini sayabiliriz. Bu arastirma kapsaminda 1982 yilinda ilk onay alip, rekombinant DNA teknolojisi ile uretilmis biyolojik urun olan insulin iceren urunlerin kuresel ve Turkiye’deki satislari ele alinmistir. Arastirmada ayrica referans insulin aspart urunu ile insulin aspart biyobenzerinin analitik olarak karsilastirilmasi ele alinmistir, gelistirme ve ruhsat sureclerinde kullanilabilecek olasi basliklar irdelenmistir.
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引用次数: 0
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Marmara Pharmaceutical Journal
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