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Comparative Bioequivalence Studies of Two Metformin Extended- Release Formulations in Healthy Thai Volunteers 两种二甲双胍缓释制剂在泰国健康志愿者体内的生物等效性比较研究
Pub Date : 2021-01-01 DOI: 10.23880/beba-16000151
K. V
Metformin is a first-line treatment for type 2 diabetic mellitus commonly used as a monotherapy or in a combination with other antidiabetic drugs. To control blood glucose levels, patients should be able to access to the treatment continuously. Thus, the Government Pharmaceutical Organization (GPO) had developed a generic metformin extended-release formulation as a low-cost alternative for patients and physicians. Two bioequivalence studies were conducted under fasting and fed conditions to compare the rate and extent of absorption between the test (Metformin XR 1000 mg) and reference (Glucophage XR 1000 mg) formulations. The study design for both studies was comparative randomized, open-label, single-dose, two-way crossover. Twenty-four subjects and fourteen eligible subjects were enrolled in the single-dose fasting and fed studies, respectively. Plasma concentrations of metformin were determined using a validated liquid chromatography tandem mass spectrometry method. The primary pharmacokinetics parameters including AUC 0-tlast , AUC 0−∞ and C max were statistically compared. The 90% confidence intervals of the geometric least squares mean ratio of log-transformed AUC 0-tlast , AUC 0−∞ and C max between the formulations were within 80.00-125.00% of bioequivalence criteria for both fasting and fed studies. The pharmacokinetic parameters following oral administration under fasting and fed conditions were comparable suggesting insignificant food effect on the absorption. The safety of metformin extended-release formulations was evaluated in healthy Thai subject. The test and reference products were well tolerated by the study subjects and no serious adverse events were reported in both studies. Based on the statistical indices, it was concluded that two metformin extended-release formulations were bioequivalent.
二甲双胍是2型糖尿病的一线治疗药物,通常作为单一疗法或与其他降糖药联合使用。为了控制血糖水平,患者应该能够持续接受治疗。因此,政府制药组织(GPO)开发了一种非专利二甲双胍缓释制剂,作为患者和医生的低成本替代品。在禁食和饲养条件下进行了两项生物等效性研究,以比较试验制剂(二甲双胍XR 1000 mg)和参比制剂(Glucophage XR 1000 mg)的吸收速率和程度。两项研究的设计均为比较随机、开放标签、单剂量、双向交叉。24名受试者和14名符合条件的受试者分别参加了单剂量禁食和喂养研究。采用有效的液相色谱串联质谱法测定血浆二甲双胍浓度。对主要药代动力学参数AUC 0-tlast、AUC 0−∞和cmax进行统计学比较。各配方间对数变换AUC 0-tlast、AUC 0−∞和cmax的几何最小二乘平均比值的90%置信区间均在80.00-125.00%的生物等效性标准范围内。在空腹和进食条件下口服给药后的药代动力学参数具有可比性,表明食物对吸收的影响不显著。在泰国健康受试者身上评价了二甲双胍缓释制剂的安全性。研究对象对试验产品和参考产品耐受良好,两项研究均未报告严重不良事件。通过统计指标,得出两种二甲双胍缓释制剂具有生物等效性的结论。
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引用次数: 0
Brief Review on Some Neurological Diseases Which Have Association with Trinucleotide Repeat Sequences 与三核苷酸重复序列有关的几种神经系统疾病综述
Pub Date : 2021-01-01 DOI: 10.23880/beba-16000152
Saberi B
Trinucleotide repeat sequences can be seen in some neurological diseases. This study will briefly review some of these neurological diseases and the associated trinucleotide repeat sequences.
三核苷酸重复序列在某些神经系统疾病中可见。本研究将简要回顾这些神经系统疾病及其相关的三核苷酸重复序列。
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引用次数: 0
Anti-Inflammation Effects of Rosmarinus Officinalis Extract Against Covid19 Virus ( In Silico Study) 迷迭香提取物抗新冠病毒抗炎作用的实验研究
Pub Date : 2021-01-01 DOI: 10.23880/beba-16000154
Nazari Vm
The critical condition of acute respiratory covid19 syndrome appeared to be the current health concern worldwide. It appeared at the beginning in Wuhan, China by end of 2019, soon after it spread to almost most of the global countries because of its high contagious properties. Precautionary procedures were the only helpful method to control the transmissions of person to person until any proper method of treatment or vaccine is established. Rosmarinus officinalis (RM) has strong anti-inflammation, anticancer and antibacterial effect. It is one of the probable choices of study against the outbreak of covid19 disease. In present article, we study in silico (molecular docking) characteristics of active compounds available in RM that is usually consumed as food additives and compare its biological effect with remdesivir and favipiravir as positive compounds based on docking properties. The actual active compounds in RM were selected based on their major roles in RM with desirable pharmacologic effects. The obtained results showed that both selected compounds were much stronger in inhibition of the studied proteins compared with remdesivir and favipiravir. Based on the combined scores in binding affinity, the drug-likeness properties of the ligands, showed to be better possible covid19 inhibitor compared with selected positive controls. The analysis of active site also showed that RM active compounds probably have the therapeutic efficacy against covid19 virus.
covid - 19急性呼吸道综合征的危重状况似乎是当前全球卫生关注的问题。由于其高传染性,它在全球几乎大多数国家传播后不久,于2019年底在中国武汉出现。在确定任何适当的治疗方法或疫苗之前,预防程序是控制人际传播的唯一有效方法。迷迭香(RM)具有较强的抗炎、抗癌和抗菌作用。这是应对2019冠状病毒病暴发的可能研究选择之一。本文研究了作为食品添加剂的紫苏中活性化合物的硅(分子对接)特性,并基于对接特性比较了其与瑞德西韦和法维吡拉韦作为正性化合物的生物学效应。根据其在中药中的主要作用和理想的药理作用,选择中药中的实际活性成分。结果表明,与瑞德西韦和法匹拉韦相比,所选化合物对所研究蛋白的抑制作用要强得多。根据结合亲和力的综合评分,与选定的阳性对照相比,配体的药物相似特性显示出更好的可能的covid - 19抑制剂。活性位点分析也表明,RM活性化合物可能具有抗新冠病毒的疗效。
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引用次数: 1
Effect of Dietary Inclusion of Ginger ( Zingiber officinale ) and Garlic ( Allium sativum ) Oil Mixture on the Growth Performance and Caecal Microbial Population of Broiler Chickens 饲粮中添加姜蒜油混合物对肉仔鸡生长性能和盲肠微生物群的影响
Pub Date : 2021-01-01 DOI: 10.23880/beba-16000153
Alagbe Jo
The objective of the present study was to determine effect of dietary inclusion of ( Zingiber officinale ) and garlic ( Allium sativum ) oil mixture (GIGM) on the growth performance and caecal microbial population of broiler chickens. One hundred and fifty one-day-old broiler chicks (Ross 308) were randomly allocated into 5 treatments with three replicates consisting of 10 birds each in a completely randomized design. Birds in treatment 1 (T1) was fed basal diet with 0 % inclusion of GIGM while T2, T3, T4 and T5 were given 0.1 %, 0.2 %, 0.3 % and 0.4 % respectively. Clean feed and water were offered ad libitum and all other management practices were strictly observed throughout the experiment which lasted for 56 days. Results obtained were used to determine weight gain (WG), average daily weight gain (ADWG), total feed intake (TFI), average daily feed intake (ADFI), feed conversion ratio (FCR) and microbial population of E.coli , Salmonella spp and Lactobacillus spp. ADWG, ADFI and FCR were significantly (P ˂ 0.05) influenced by the dietary inclusion of GIGM. ADWG were highest in T5 (47.80 g), T4 (45.75 g) and T3 (45.09 g), intermediate in T2 (39.59 g) and lowest in T1 (30.72 g). Lactobacillus spp increased as the level of dietary inclusion of GIGM increases (P ˂ 0.05). E.coli and Salmonella spp counts were significantly (P ˂ 0.05) different among the treatments. It was concluded that GIGM could be included in the diet of broilers up to 0.4 % without causing any deleterious effect on the performance and health of birds.
本试验旨在研究饲粮中添加生姜和大蒜油混合物对肉鸡生长性能和盲肠微生物群的影响。试验采用完全随机设计,将150只1日龄肉鸡(罗斯308)随机分为5个处理,每个处理3个重复,每个重复10只鸡。处理1 (T1)饲粮中添加0 %的GIGM, T2、T3、T4和T5饲粮中分别添加0.1%、0.2%、0.3%和0.4%的GIGM。试验期56 d,饲料和水不定期供应,其他各项管理均严格执行。结果表明,饲粮中添加GIGM对肉鸡增重(WG)、平均日增重(ADWG)、总采食量(TFI)、平均日采食量(ADFI)、饲料系数(FCR)以及大肠杆菌、沙门氏菌和乳酸菌的微生物数量有显著影响(P小于0.05)。ADWG在T5 (47.80 g)、T4 (45.75 g)和T3 (45.09 g)阶段最高,在T2阶段居中(39.59 g),在T1阶段最低(30.72 g)。乳酸菌数量随着饲粮中GIGM添加水平的增加而增加(P小于0.05)。大肠杆菌和沙门氏菌计数在不同处理间差异有统计学意义(P小于0.05)。由此得出,在肉鸡日粮中添加0.4%的GIGM对肉鸡生产性能和健康无不良影响。
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引用次数: 2
Overview of 3D Printing Technology 3D打印技术概述
Pub Date : 2021-01-01 DOI: 10.23880/beba-16000149
Hussain S
The pharmaceutical industry is advancing at an incredible rate. Novel drug formulations for targeted therapy have been developed all thanks to advances in modern sciences. Even so, the manufacturing sector of novel dosage forms is minimal, and the industry continues to rely on traditional drug delivery systems, particularly modified tablets. The use of 3D printing technologies in pharma companies has opened up new possibilities for printed products and device research and production. 3D Printing has slowly progressed from its original use as pre-surgical imaging templates and tooling molds to produce one-of-a-kind instruments, implants, tissue engineering scaffolds, testing platforms, and drug delivery systems. The most significant advantages of 3D printing technologies include the ability to produce small batches of drugs with custom dosages, forms, weights, and drug release profiles. The production of medicines in this manner could eventually contribute to the realization of the principle of personalized medicine. The biomedical industry and academia have also embraced 3D printing in recent years. It offers commercially available medical devices as well as a forum for cutting-edge studies in fields such as tissue and organ printing. This mini-review provides an overview of 3D printed technology in medicines.
制药行业正以惊人的速度发展。由于现代科学的进步,用于靶向治疗的新型药物配方已经开发出来。即便如此,新剂型的制造部门仍然很少,该行业继续依赖于传统的给药系统,特别是改性片剂。在制药公司中使用3D打印技术为打印产品和设备的研究和生产开辟了新的可能性。3D打印已经从最初的手术前成像模板和模具用途慢慢发展到生产独一无二的仪器、植入物、组织工程支架、测试平台和药物输送系统。3D打印技术最显著的优势包括能够生产具有定制剂量、形式、重量和药物释放概况的小批量药物。以这种方式生产药品最终可能有助于实现个性化医疗原则。近年来,生物医学行业和学术界也开始接受3D打印技术。它提供商用医疗设备,以及组织和器官打印等领域的前沿研究论坛。这篇迷你评论提供了药物3D打印技术的概述。
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引用次数: 6
Improvement of Vitamin D 3 Metabolites Level after Oral Administration of the Biofield Energy Treated Proprietary Test Formulation in Vitamin D 3 Deficiency Diet (VDD) Induced Rat Model 口服生物场能量处理专利试验制剂对维生素d3缺乏症大鼠模型维生素d3代谢产物水平的改善
Pub Date : 2020-01-01 DOI: 10.23880/beba-16000138
Jana S
The present experiment was evaluated to study of the effect of Consciousness Energy Healing Treatment (the Trivedi Effect ® ) on novel proprietary test formulation in male Sprague Dawley (SD) rats, fed with vitamin D3 deficiency diet (VDD) for the estimation of vitamin D3 metabolites in kidney tissue. A novel proprietary test formulation was formulated with a few minerals (magnesium, zinc, copper, calcium, selenium, and iron), vitamins (ascorbic acid, pyridoxine HCl, alpha tocopherol, cyanocobalamin, and cholecalciferol), Panax ginseng extract, β-carotene, and cannabidiol isolate. The novel test formulation was divided into two parts; one part was defined as the untreated test formulation, while the other part of the test formulation and the animals received Biofield Energy Healing Treatment by a renowned Biofield Energy Healer, Mr. Mahendra Kumar Trivedi. 25-OH vitamin D 3 level was significantly increased in the Biofield Energy Treated test formulation group (G5), Biofield Energy Treatment per se (G6), and 15-days pre-treatment of the Biofield Energy Treated test formulation (G7) groups by 21%, 22.9%, and 11.5%, respectively as compared with the disease control group (G2). Additionally, the level of 1,25-(OH) 2 D 3 was increased by 55% in the G6 group as compared with the G2. Further, the expression of CYP24A in kidney was increased by 13.9% in the G6 group, while CYP27B expression in kidney was significantly increased by 17.6%, 18.6%, 10.1%, and 15.6% in the G5, G6, G7 (Biofield Energy Treated test formulation from day -15), and G8 (Biofield Energy Treatment per se plus Biofield Energy Treated test formulation from day -15) groups, respectively as compared with the G4 group. Vitamin D receptor (VDR) expression was significantly increased by 69.5% and 31% in the G6 and G7 groups, respectively as compared with the G2 group. Overall, the results showed significant improvement of the availability of vitamin D 3 metabolites, that could be helpful for the vitamin D 3 deficiency persons to maintain good bone health and immunity. Therefore, the results suggest that there was significant slowdown in the disease progression and disease related all other complications/symptoms in the Biofield Energy Treatment group per se and/or Biofield Energy Treated Test formulation groups ( viz . G6, G7, G8, and G9) comparatively with the disease group.
本实验评估了意识能量治疗(Trivedi效应®)对新型专利试验配方的影响,雄性Sprague Dawley (SD)大鼠喂养维生素D3缺乏症饮食(VDD),以估计肾组织中维生素D3代谢物。一种新的专有测试配方由几种矿物质(镁、锌、铜、钙、硒和铁)、维生素(抗坏血酸、吡哆醇HCl、α生育酚、氰钴胺素和胆钙化醇)、人参提取物、β-胡萝卜素和分离大麻二酚组成。新试验配方分为两部分;一部分被定义为未经处理的测试配方,而另一部分测试配方和动物接受了著名生物场能量治疗师Mahendra Kumar Trivedi先生的生物场能量治疗。生物场能量处理测试配方组(G5)、生物场能量处理本身(G6)和生物场能量处理测试配方(G7)组预处理15天的25-OH维生素d3水平显著提高了21%、22.9%和11.5%。分别与疾病对照组(G2)比较。此外,与G2相比,G6组的125 -(OH) 2 d3水平升高了55%。此外,与G4组相比,G6组肾脏中CYP24A的表达增加了13.9%,而G5、G6、G7(第15天生物场能量处理试验配方)和G8(第15天生物场能量处理本身加生物场能量处理试验配方)组肾脏中CYP27B的表达分别显著增加了17.6%、18.6%、10.1%和15.6%。与G2组相比,G6组和G7组维生素D受体(VDR)表达量分别显著增加69.5%和31%。总的来说,结果显示维生素d3代谢产物的可用性显著改善,这可能有助于维生素d3缺乏症患者保持良好的骨骼健康和免疫力。因此,结果表明,生物场能量治疗组本身和/或生物场能量治疗试验配方组的疾病进展和与疾病相关的所有其他并发症/症状显著减缓。G6、G7、G8、G9)与疾病组比较。
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引用次数: 0
Bioavailability of Trans and Saturated Fatty Acids in Stuffed Cookies and Wafers Produced in Brazil 巴西生产的填充饼干和威化饼中反式脂肪酸和饱和脂肪酸的生物利用度
Pub Date : 2020-01-01 DOI: 10.23880/beba-16000143
Montilla Tcl
Several scientific studies highlight that trans fatty acids are harmful to health. The World Health Organization (WHO) considering the presence of trans fat in food recommends its total elimination by the year 2023. The Brazilian Health Surveillance Agency’s (ANVISA) Collegiate Board Resolution (RDC) No. 54, from November 2012, establishes that only foods with trans fat levels lower ≤ 0.1 g per portion can claim zero trans on the label. Stuffed cookies and wafers are important representatives of ultra-processed foods containing high levels of sugars and fats, being widely consumed for their low cost and accessibility. The objective of this study was to evaluate the levels of trans and saturated fat by gas chromatography (AOAC Official Method 996.06) in stuffed cookies and wafers, 31 stuffed cookies and 33 wafers were analyzed in the city of São Paulo, evaluating the amount of trans fats, between 0.01 to 1.56 g/serving and 0.01 and 2.56 g / serving in the filled wafers and cookies respectively. Therefore, it was found that some brands of stuffed wafers and wafers still present large amounts of trans fat in their composition causing risks to the consumer’s health
一些科学研究强调,反式脂肪酸对健康有害。考虑到食品中反式脂肪的存在,世界卫生组织(世卫组织)建议到2023年完全消除反式脂肪。2012年11月起,巴西卫生监督机构(ANVISA)大学理事会决议(RDC)第54号规定,只有反式脂肪含量低于每份≤0.1克的食品才能在标签上声明零反式脂肪。填充饼干和威化饼是含有高糖和高脂肪的超加工食品的重要代表,因其低成本和可获得性而被广泛消费。本研究的目的是用气相色谱法(AOAC官方方法996.06)评估填充饼干和华夫饼干中的反式脂肪和饱和脂肪含量,分析了圣保罗市31种填充饼干和33种华夫饼干,分别评估了填充饼干和饼干中反式脂肪的含量,分别在0.01 ~ 1.56 g/份和0.01 ~ 2.56 g/份之间。因此,我们发现一些品牌的夹心威化饼和威化饼的成分中仍然含有大量的反式脂肪,对消费者的健康构成了威胁
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引用次数: 0
Toxic Effect of Methylation and Chlorpyrifos on Liver of Male Rabbits 甲基化和毒死蜱对家兔肝脏的毒性作用
Pub Date : 2020-01-01 DOI: 10.23880/beba-16000140
Mohammed Saa
The irrational use of organ phosphorus insecticides in Yemen play a crucial role in the occurrence of many diseases affecting plants, animals, and man. Methidathion (MD) and Chlorpyrifos (CF) are two of widely used organ phosphorus insecticides in agriculture. The purpose of the present study was to investigate the in vivo effect of (MD) and (CF) on lipid peroxidation (LPO), antioxidant defense system in the liver cells and liver function in male rabbits after orally administration a single dose of 1/8 of LD50 of (MD) and (CF) period of 20 days. Thirty healthy male rabbits weighting 1400-1600g., were divided into 3 groups with 10 animals in each, first group served as control animals, they received 3ml.of corn oil, while animals in second and third groups received 1/8 of LD50 of (MD) and (CF) respectively. The level of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), lactate dehydrogenase (LDH), and gamma glutamyl transferase (γ-GT) in serum were analyzed, the level of (LPO), and methylglyoxal (MG), in liver homogenate were also studied. Results showed a significant (P<0.01) increase in all studied parameters in animals treated with (MD) and (CF) as compared to control animals. Our results indicated to the high toxicity of (MD) and (CF).
在也门,有机磷杀虫剂的不合理使用对影响植物、动物和人的许多疾病的发生起着至关重要的作用。灭磷磷(MD)和毒死蜱(CF)是农业上广泛使用的两种有机磷杀虫剂。本研究旨在探讨(MD)和(CF)在雄性家兔体内按1/8 LD50剂量单次口服(MD)和(CF) 20 d后,对肝细胞脂质过氧化(LPO)、抗氧化防御系统及肝功能的影响。健康公兔30只,体重1400-1600克。,分为3组,每组10只,第一组为对照动物,注射3ml;第二组和第三组分别给予(MD)和(CF) LD50的1/8。分析血清丙氨酸转氨酶(ALT)、天冬氨酸转氨酶(AST)、碱性磷酸酶(ALP)、乳酸脱氢酶(LDH)和γ-谷氨酰转移酶(γ-GT)水平,并研究肝脏匀浆中LPO和甲基乙二醛(MG)水平。结果显示,与对照组相比,(MD)和(CF)处理的动物各项指标均显著(P<0.01)升高。我们的结果表明(MD)和(CF)的高毒性。
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引用次数: 0
Formulation and Evaluation of Polymeric Bilayer Matrix Tablet Containing Glipizide and Metformin Hydrochloride 格列吡嗪-盐酸二甲双胍聚合物双层基质片的研制及评价
Pub Date : 2020-01-01 DOI: 10.23880/beba-16000139
Lakshmana Prabu S
The objective of the present study was to develop Bilayer tablets of Glipizide and metformin hydrochloride from polymeric matrices of HPMC K4M and Eudragit L-100. Drugs Glipizide and metformin hydrochloride are frontline anti-diabetic drugs prescribed in combination. Tablets were prepared by wet granulation method using different ratios of HPMC K4M and Eudragit L-100 and evaluated for its physicochemical properties, in vitro release profile and stability studies. The prepared granules physiochemical property results were within the limits and the formulated tablets hardness, friability and content uniformity was found to be between 5.1±0.1 and 5.9±0.3; 0.21 ±0.02 and 0.49±0.02%; 98.99 ±1.06 and 100.45±0.52 %w/w respectively. The invitro release was found to be observed for 12 hours in phosphate buffer pH 6.8 and compared with market formulation. The dissolution release of formulation was comparable with market formulation and the difference factor and similarity factor f1 and f2 were found to be 3.75 and 79.46 for metformin hydrochloride; 8.74 and 65.78 for glipizide respectively. Stability studies were carried out as per ICH guidelines and tested for its physicochemical properties and in vitro release studies. The stability study result reveals that the prepared formulation was stable.
以HPMC K4M和Eudragit L-100为聚合物基质制备格列吡嗪和盐酸二甲双胍双层片。格列吡嗪和盐酸二甲双胍是一线抗糖尿病药物。采用湿造粒法,以不同比例的HPMC K4M与乌龙茶L-100配制成片剂,考察其理化性质、体外释放特性及稳定性。制备的颗粒理化性能在限定范围内,其硬度、脆度、含量均匀度均在5.1±0.1 ~ 5.9±0.3之间;0.21±0.02和0.49±0.02%;w/w分别为98.99±1.06和100.45±0.52 %。在pH为6.8的磷酸盐缓冲液中,体外释放时间为12小时,并与市场配方进行了比较。盐酸二甲双胍的溶出度与市售制剂相当,差异因子f1和相似因子f2分别为3.75和79.46;格列吡嗪分别为8.74和65.78。根据ICH指南进行了稳定性研究,并对其物理化学性质和体外释放研究进行了测试。稳定性研究结果表明,所制制剂是稳定的。
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引用次数: 0
Bioavailability of Phenolic Compounds in Food and their Properties in Cellular Protection 食品中酚类化合物的生物利用度及其细胞保护特性
Pub Date : 2020-01-01 DOI: 10.23880/beba-16000145
M. J.
{"title":"Bioavailability of Phenolic Compounds in Food and their Properties in Cellular Protection","authors":"M. J.","doi":"10.23880/beba-16000145","DOIUrl":"https://doi.org/10.23880/beba-16000145","url":null,"abstract":"","PeriodicalId":8995,"journal":{"name":"Bioequivalence &amp; Bioavailability International Journal","volume":"116 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81277800","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
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Bioequivalence &amp; Bioavailability International Journal
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