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Acridone-based acetylcholinesterase inhibitors: synthesis, antioxidant activity and molecular modeling 吖啶酮基乙酰胆碱酯酶抑制剂:合成、抗氧化活性和分子模拟
Pub Date : 2018-12-26 DOI: 10.5138/09750215.2313
H. A. El-gizawy, F. A. Omar, Prof. Mohammed Abdalla Hussein
Acridone is a unique naturally occurring alkaloid known to associate with several biological activities. 2,3-dimethoxy-10-methyl-10,8a-dihydroacridin-9(8aH)-one (4) and its precursor 2-((3,4-dimethoxyphenyl)methylamino)benzoic acid (3) were synthesized and investigated for potential antioxidant and inhibitory activity against acetylcholinestrase. The synthetic pathway involves reaction of 2-(methylamino) benzoic acid (1) with 4-chloro-1,2-dimethoxybenzene (2) in presence of CuO and K2CO3 to give the precursor 3. Subsequent, cyclcondensation of 3 with Conc. H2SO4 afforded the anticipated acridone 4. Furthermore, the dimethoxyacridone derivative 4 showed potent antiacetylcholinesterase (ACHE) activity at (100 uM) with IC50 = 9.25 uM that is as potent as the reference drug rivastigmine. Assessment of total antioxidant activity of compounds 3 & 4 in comparison to known standard compounds revealed the following order: α-tocopherol > Acridone 4 > trolox > butylated hydroxyl anisole (BHA) > butylated hydroxyl toluene (BHT) > compound 3. Molecular docking characteristics of 3 & 4 within the active site of AChE (PDB: 1ACJ) co-crystallized with 9-amino-tetrahydroacridine (Tacrine) have been studied. Interestingly, the results revealed comparable binding poses to the co-crystallized ligand and demonstrates good correlation of the binding energy (DG) with the observed IC50-values. This finding suggests that compounds 3 & 4 exhibit good antioxidant effect and inhibition of acetylcholinesterase, which might provide profitable candidates in management of Alzheimer’s disease.
吖啶酮是一种独特的天然生物碱,已知与几种生物活性有关。合成了2,3-二甲氧基-10-甲基-10,8 -二氢吖啶酮-9(8aH)- 1(4)及其前体2-((3,4-二甲氧基苯基)甲胺)苯甲酸(3),并对其潜在的抗氧化和抑制乙酰胆碱酯酶活性进行了研究。合成途径是2-(甲氨基)苯甲酸(1)与4-氯-1,2-二甲氧基苯(2)在CuO和K2CO3存在下反应生成前体3。随后,3与Conc循环缩合。H2SO4提供了预期的吖啶酮4。此外,二甲氧基吖啶酮衍生物4在(100 μ m)下显示出较强的抗乙酰胆碱酯酶(ACHE)活性,IC50 = 9.25 μ m,与参比药物利瓦斯汀的活性相当。与已知标准化合物相比,化合物3和4的总抗氧化活性评价顺序为:α-生育酚>吖啶酮4 > trolox >丁基羟基茴香醚(BHA) >丁基羟基甲苯(BHT) >化合物3。研究了AChE (PDB: 1ACJ)与9-氨基-四氢吖啶共结晶(Tacrine)活性位点内3和4的分子对接特性。有趣的是,结果显示了与共结晶配体相似的结合姿态,并且表明结合能(DG)与观察到的ic50值具有良好的相关性。这一发现提示化合物3和4具有良好的抗氧化作用和抑制乙酰胆碱酯酶,可能为阿尔茨海默病的治疗提供有益的候选药物。
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引用次数: 3
Current Aspects and Therapies for Wound healing 伤口愈合的现状和治疗方法
Pub Date : 2018-08-25 DOI: 10.5138/09750215.2205
H. Popli, Reena Badhwar
Injury to the skin provides a new challenge, as wound healing is a complex and intricate process. Nonhealing wounds represent a significant cause of morbidity and mortality for a large portion of the population. Delayed wound healing is one of the major therapeutic and economic issues in medicine today. Wound healing requires a concerted effort of remodeling of various components of the connective tissue in the presence of appropriate cytokines and growth factors. Unfortunately we still do not understand the actual mechanism of wound healing. This review is an effort to provide information about current challenges of wound healing and their management, recent advances in wound care technology and current management guidelines for the treatment of wounds and ulcers. Various steps like microbial control, subsidence of inflammation, regeneration of connective tissue, angiogenesis and epithelialisation should take place in a time-bound sequence. The development of new and effective interventions in Wound care remains an area of intense research.
皮肤损伤提供了一个新的挑战,因为伤口愈合是一个复杂而复杂的过程。无法愈合的伤口是很大一部分人发病和死亡的重要原因。延迟伤口愈合是当今医学中主要的治疗和经济问题之一。伤口愈合需要在适当的细胞因子和生长因子的存在下,对结缔组织的各种成分进行协调一致的重塑。不幸的是,我们仍然不了解伤口愈合的实际机制。本综述旨在提供当前创面愈合及其管理的挑战,创面护理技术的最新进展以及目前创面和溃疡治疗的管理指南。微生物控制、炎症消退、结缔组织再生、血管生成和上皮化等步骤应按一定的时间顺序进行。在伤口护理中开发新的有效的干预措施仍然是一个深入研究的领域。
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引用次数: 1
Limonene and BEZ 235 induce apoptosis in COLO-320 and HCT-116 colon cancer cells 柠檬烯和BEZ 235诱导COLO-320和HCT-116结肠癌细胞凋亡
Pub Date : 2018-08-25 DOI: 10.5138/09750215.2240
Raja Ratna Reddy Yakkanti, Manisha Singh, V. Kabra, P. C. Sekhar, K. SreejaVamsi, B. Reddy, S. Ramamoorthy, C. Reddy
Deregulated apoptosis is the hall mark of many cancers, therefore every defect in apoptosis pathway could be a potential target for cancer treatment.The anticancer mechanism of limonene could be multifactorial. However, induction of apoptosis in cancer cells is proposed as the predominant mechanism in several of preclinical studies. Therefore, we determined to investigate the role of apoptosis in the anticancer activity of limonene and BEZ235 combination in COLO-320 and HCT-116 colon cancer cells. Cells after treatments were assessed for apoptosis by DAPI staining for fluorescent microscopic examination of apoptotic cells, estimation of caspases activities, Bcl-2 family proteins in addition to cell cycle analysis by flowcytometry. Results show that both drugs induced apoptosis as demonstrated by increased caspases activity, significant alterations in pro and anti-apoptotic proteins of Bcl-2 family in promoting apoptosis and cell cycle arrest at G1 phase. Over all, it is indicated that limonene and BEZ exerted anticancer activity is mediated through induction of apoptosis involving mitochondria mediated intrinsic death pathway in the selected CRC cells.
不受调控的细胞凋亡是许多癌症的标志,因此细胞凋亡途径的每一个缺陷都可能成为癌症治疗的潜在靶点。柠檬烯的抗癌机制可能是多因素的。然而,在一些临床前研究中,诱导癌细胞凋亡被认为是主要的机制。因此,我们决定在COLO-320和HCT-116结肠癌细胞中研究凋亡在柠檬烯和BEZ235联合抗肿瘤活性中的作用。通过DAPI染色检测凋亡细胞的荧光显微镜检查,估计caspase活性,Bcl-2家族蛋白以及流式细胞术分析细胞周期。结果表明,两种药物均诱导细胞凋亡,表现为caspases活性升高,Bcl-2家族促凋亡蛋白和抗凋亡蛋白显著改变,促进细胞凋亡和细胞周期阻滞于G1期。综上所述,柠檬烯和BEZ发挥抗癌活性是通过诱导凋亡介导的线粒体介导的CRC细胞内在死亡途径。
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引用次数: 0
Formulation, Optimization and Evaluation of Self Emulsifying Immediate Release Tablet of Nebivolol HCl using 32 Factorial Design 盐酸奈比洛尔自乳化速释片的优选及32因子设计评价
Pub Date : 2018-08-25 DOI: 10.5138/09750215.2235
Tanvi Mukund Siriah, P. Puranik
Nebivolol Hydrochloride (NEB) is a lipophilic molecule with low solubility in GI fluid, and high metabolism which leads to its low oral bioavailability 12%. The aim of the present investigation was to develop immediate release self emulsifying tablet (IR-SET) as solid SMEDDS to enhance the solubility and permeability of the drug. Solubility study, pseudo-ternary phase diagrams and 3 2 factorial design were used to select the components of the system and optimize the composition of liquid SMEDDS. Optimal L-SMEDDS contains Kollisolv GTA, Tween 80 and Propylene glycol as oil, surfactant and co-surfactant, respectively in the ratio of 20:26.66:53.34 % w/w, formulates L-SMEDDS with droplet size (55.98 nm), PDI (0.37), emulsification time (16±1.52 sec) and drug content (97.43±0.30 %).  The liquid SMEDDS were adsorbed onto Neusilin US2 by adsorbtion technique to form S-SMEDDS. DSC and SEM studies suggested that NEB in the S-SMEDDS may be present in the molecular dispersed state and was sufficiently adsorbed onto solid carrier, respectively. S-SMEDDS was compressed into IR-SET by direct compression method and composition of IR-SET was optimized using 3 2 factorial design. Optimal IR-SET showed disintegration time (92 + 0.57 sec), droplet size (68.57 nm), PDI (0.34) and drug content (96.33±0.15 %). In vitro dissolution studies and ex vivo diffusion studies in rat stomach suggested that SMEDDS played an important role in solubility and permeability enhancing effect. Accelerated stability studies indicated that formulation were stable. Our results illustrated the increase in solubility and permeability of drug from IR-SET.
盐酸奈比洛尔(NEB)是一种亲脂分子,在胃肠道液体中溶解度低,代谢高,口服生物利用度低12%。本研究的目的是开发立即释放自乳化剂(IR-SET)作为固体SMEDDS,以提高药物的溶解度和渗透性。通过溶解度研究、伪三元相图和32因子设计对体系的组分进行了选择,并对液体SMEDDS的组成进行了优化。优选的L-SMEDDS以Kollisolv GTA、Tween 80和丙二醇为油、表面活性剂和助表面活性剂,分别以20:26.66:53.34 % w/w的比例配制,得到液滴尺寸(55.98 nm)、PDI(0.37)、乳化时间(16±1.52秒)和药物含量(97.43±0.30%)的L-SMEDDS。通过吸附技术将液态SMEDDS吸附在Neusilin US2上,形成S-SMEDDS。DSC和SEM研究表明,S-SMEDDS中的NEB可能以分子分散状态存在,并被充分吸附在固体载体上。采用直接压缩法将S-SMEDDS压缩成IR-SET,并采用32因子设计优化IR-SET的组成。最佳IR-SET样品的崩解时间为92±0.57秒,液滴大小为68.57 nm, PDI为0.34,药物含量为96.33±0.15%。体外溶出和体外胃内扩散实验表明,SMEDDS具有增强溶解度和通透性的作用。加速稳定性研究表明该制剂是稳定的。我们的结果表明IR-SET增加了药物的溶解度和渗透性。
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引用次数: 0
Particle Size Characterization- Techniques, Factors and Quality-by-design Approach 粒度表征。技术、因素和质量设计方法
Pub Date : 2018-05-25 DOI: 10.5138/09750215.2204
R. K. Dhamoon, H. Popli, G. Aggarwal, Madhu Gupta
Particle size characterization is one of the key areas involved in quality assurance. The concept of particle size and size characterization acts as a foundation for all the processes involved in theproduction of a formulation; from manufacturing to quality control operations. Particle size characterization dictates many properties of the finished product. Particle size characterization of samples is important to make a better quality product, improve its appearance, taste, texture and shelf-life. There are many instruments for particle size characterization that are available commercially. Each instrument is based on a different technique and each technique is based on a different principle. Selecting the right particle size characterization technique for the given sample is a challenging decision. The choice of technique is made according to the sample. Sometimes even a combination of techniques is used to obtain accurate results. There are several factors upon which choice of technique depends like size range, sample quantity, cost effectiveness etc. To ensure appropriate quality standards in the field of particle sizing and particle size characterization, ICH and US-FDA have recently insisted on including Quality-by-design approach in thepharmaceutical industry. Application of QBD approach to particle size characterization techniques ensures a resilient method which gives reproducible results. It aids in reducing result and method variations and promotes productivity and quality. The main objectives of this review are first, to understand the principle, instrumentation, and working of commercially used techniques and to compare their pros and cons; secondly, to study the factors which govern the choice of technique and lastly, to understand the concept of Quality by design and its role in particle size characterization through some example. Keywords: Particle size characterization; techniques; factors;QBD
粒度表征是质量保证的关键领域之一。粒径和粒径表征的概念是配方生产中涉及的所有过程的基础;从制造到质量控制操作。粒度表征决定了成品的许多特性。样品的粒度表征对于制造质量更好的产品,改善其外观、味道、质地和保质期至关重要。市面上有许多用于粒度表征的仪器。每种乐器都基于不同的技术,每种技术都基于不同的原理。为给定的样品选择正确的粒度表征技术是一个具有挑战性的决定。根据样品来选择工艺。有时甚至结合使用多种技术来获得准确的结果。有几个因素取决于技术的选择,如尺寸范围,样品数量,成本效益等。为了确保颗粒尺寸和粒度表征领域的适当质量标准,ICH和US-FDA最近坚持将质量设计方法纳入制药行业。应用QBD方法的粒度表征技术,确保弹性的方法,提供可重复的结果。它有助于减少结果和方法的变化,并提高生产率和质量。本综述的主要目的是:首先,了解商业上使用的技术的原理、仪器和工作原理,并比较它们的优缺点;其次,研究控制技术选择的因素;最后,通过一些例子,了解设计质量的概念及其在粒度表征中的作用。关键词:粒度表征;技术;因素;QBD
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引用次数: 9
In vitro evaluation of Transdermal Patch of Palonosetron for Antiemetic Therapy 帕洛诺司琼透皮贴剂止吐的体外评价
Pub Date : 2018-01-23 DOI: 10.5138/09750215.2186
Atul Tripathi, P. Tyagi, A. Vyas, Beena Gidwani, Amol Chandekar, H. Sharma
Skin is one of the routes for systemic delivery of drugs through various drug delivery system. A transdermal Drug Delivery System (TDDS) is one of the most reliable and useful system to deliver drug systemically through skin. Generally medicated patch is placed on skin for delivery of medication through it into the blood stream. The aim of present study was to formulate and evaluate Palonosetron transdermal patch in vitro that could be used for antiemetic therapy. The incorporation ofPalonosetron a serotonin 5-HT 3 antagonist drug was envisaged. The TDDS was prepared by solvent evaporation technique and was evaluated for organoleptic characteristics and other physicochemical properties Thickness, Weight variation, Drug content uniformity, Tensile strength, % Elongation, Folding endurance & Moisture content. The in vitro permeation study of the patch was carried out through KesaryChein diffusion cell as barrier membrane. Phosphate buffer pH 7.4 was used as dissolution medium and the temperature was maintained at 37 ± 1 0 C. The in vitro permeation study of the prepared patch indicated a time dependent increase in drug release throughout the study. The percentage of cumulative drug release was found to be 76.25% in 24 hours.The study shows a new approach to work in with Palonosetron.
皮肤是通过各种给药系统给药的途径之一。透皮给药系统(TDDS)是一种最可靠、最实用的通过皮肤给药系统。一般来说,药物贴片是贴在皮肤上,通过它将药物输送到血液中。本研究的目的是研制并评价帕洛诺司琼体外透皮贴剂用于止吐的效果。帕洛诺司琼是一种5-羟色胺5-羟色胺3拮抗剂。采用溶剂蒸发法制备TDDS,并对TDDS的感官特性和其他理化性能进行了评价,包括厚度、重量变化、药物含量均匀性、拉伸强度、伸长率、折叠耐久性和水分含量。采用KesaryChein扩散细胞作为屏障膜,对该贴片进行体外透性研究。以pH 7.4的磷酸盐缓冲液作为溶出介质,温度保持在37±10℃。所制备贴片的体外渗透研究表明,在整个研究过程中,药物释放呈时间依赖性增加。24 h内累积释药率为76.25%。这项研究显示了一种与帕洛诺司琼一起工作的新方法。
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引用次数: 3
Preparation of cyclodextrin nanoparticles and evaluation of its effect on the capacitation of bovine spermatozoa used in the in vitro fertilization 纳米环糊精的制备及其对体外受精牛精子获能效果的评价
Pub Date : 2018-01-23 DOI: 10.5138/09750215.2196
H. Salem, M. Raslan, H. Suliman, T. Essam, S. Abd-Allah
This study was conducted to produce nanosized cyclodextrin (NCD) and assess its effect on bovine spermatozoa during In vitro fertilization (IVF) to optimize the capacitation media for successful IVF. Therefore, Four cyclodextrin formulations were prepared and characterized. Data analysis revealed the best formula (F2) showed a smallest particle size (15 nm), zeta potential (-37 mv), and higher yield percentages (95%) was selected for spem capacitation. Motile spermatozoa were separated from frozen-thawed semen by a swim-up procedure and capacitated in IVF-TALP medium with different formulae of NCD or CD or without treatments (control) and incubated for 3hours(hr) at 38°C and evaluated every one (hr) interval. Data analysis revealed that the formulation of cyclodextrin nanoparticles (F2 ) after (2hr) incubation in the media gave best effect on sperm capacitation and acrosme reaction (AR) and effect of sperm treated with NCD on fertilization rate was evaluated. The results showed that the proportion of Oocytes fertilized was increased significantly in F2 (60%) than in the control (35%), and cyclodextrin group (50%) groups ( p <0.05). It could be inferred from this investigation that cyclodextrin nanoparticles can be used for biomedical interventions in bovine spermatozoa. NCD improve sperm motility, viability, and (AR), also fertilization rate of sperm treated with NCD increase. So NCD gave positive effect on sperm functions during IVF.
本研究通过制备纳米环糊精(NCD)并评估其在体外受精(IVF)过程中对牛精子的影响,以优化体外受精成功的获能培养基。为此,制备了四种环糊精制剂并对其进行了表征。数据分析表明,最佳配方(F2)为最小粒径(15 nm)、zeta电位(-37 mv)和较高的获能率(95%)。通过游动程序将活动精子从冻融精液中分离出来,并在不同配方的NCD或CD或未处理(对照)的IVF-TALP培养基中充能,在38°C下孵育3小时(hr),每隔一小时(hr)进行评估。结果表明,体外培养2hr后的环糊精纳米颗粒(F2)对精子获能和顶体反应(AR)效果最佳,并评价了NCD处理后精子受精率的影响。结果表明:F2组受精卵比例(60%)显著高于对照组(35%)和环糊精组(50%)(p <0.05);由此可以推断,环糊精纳米颗粒可用于牛精子的生物医学干预。NCD可改善精子活力、生存力和AR,提高精子受精率。因此,非传染性疾病对体外受精过程中精子功能有积极影响。
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引用次数: 2
Quality control and standardization of FACA® syrup FACA®糖浆的质量控制和标准化
Pub Date : 2018-01-23 DOI: 10.5138/09750215.2166
S. Ouedraogo, S. Traoré, J. Ouédraogo, Moumouni Koala, L. Belemnaba, N. Ouedraogo, F. Kini, S. Ouédraogo, I. Guissou
Sickle cell disease is a major public health problem. It is the first genetic disease in the world. FACA syrup offers an alternative treatment. It is a dry powder preparation of two components, the roots barks of Zanthoxylum zanthoxyloides Lam. (Rutaceae) Zepernick, Timler and Calotropis procera . Ait. R.B.r. (Asclepiadaceae). The product was developed at Institute for Research in Health Sciences (IRSS) from a traditional recipe used in Burkina Faso for treatment of sickle cell crises. This study aimed to establish physical-chemical, pharmaco technical and microbiological control parameters essential for the standardization of the phytomedicine. This valuation concerned specifications of moisture content, pH, the fingerprint by thin layer chromatography, pesticide residues, heavy metal content, microbial quality, and total ash. These charcteristics were determined by the methods prescribed by the World Health Organization (1998) and the European Pharmacopoeia 6th edition. The results have shown that dry syrups and reconstituted syrups were sweet, slightly spicy with a bitter after taste, a white room color and a faint odor. The density at the preparation was 0.985 and the pH was 5.93. After 2 months of storage in the laboratory, the organoleptic parameters of the reconstituted syrups have not changed. They were mold free, the density remained around 1 and the pH between 5 and 4. These parameters have shown that the quality of plants powders and these medicine comply with the recommendations of the European pharmacopoeia. Faca syrup may contribute to the better management of sickle cell disease in children.
镰状细胞病是一个主要的公共卫生问题。这是世界上第一个遗传性疾病。FACA糖浆提供了另一种治疗方法。它是由花椒根皮两种成分组成的干粉制剂。(芸香科)Zepernick, Timler和Calotropis procera。河中的小岛。R.B.r。(萝摩科)。该产品是由卫生科学研究所(IRSS)根据布基纳法索用于治疗镰状细胞危象的传统配方开发的。本研究旨在建立植物药标准化所必需的理化、药理学和微生物控制参数。该评价涉及水分含量、pH值、薄层色谱指纹图谱、农药残留、重金属含量、微生物质量和总灰分的规格。这些特征是根据世界卫生组织(1998年)和欧洲药典第6版规定的方法确定的。结果表明,干糖浆和重组糖浆是甜的,微辣,苦味,白色的房间颜色和微弱的气味。制备时的密度为0.985,pH为5.93。在实验室保存2个月后,重组糖浆的感官参数没有变化。它们没有霉菌,密度保持在1左右,pH值在5到4之间。这些参数表明植物粉末和这些药物的质量符合欧洲药典的建议。法卡糖浆可能有助于更好地管理儿童镰状细胞病。
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引用次数: 0
Formulations and evaluation of Cyclodextrin complexed Ceadroxil loaded nanosponges 环糊精配合塞地螺醇纳米海绵的制备及性能评价
Pub Date : 2017-10-31 DOI: 10.5138/09750215.2180
P. Dubey, H. Sharma, S. Shah, C. Tyagi, Amol Chandekar, R. Jadon
Cefadroxil (CFD) is a broad spectrum antibiotic that acts against an extensive variety of bacteria, including Gram-positive and Gram-negative bacteria. The major drawback of orally administered drug like cefadroxil is its shorter half life of 1.2 hrs. The goal of the study is to prolong the drug release, producing a desired blood serum level, reduction in drug toxicity and improving the patient compliance by prolonging the dosing intervals. Cyclodextrin-based nanosponges (NS) are a novel class of cross-linked derivatives of cyclodextrins. They have been used to increase the solubility of poorly soluble actives, to protect the labile groups and control the release. This study aimed at formulating complexes of CFDwith three types of β-cyclodextrin NS obtained with different cross-linking ratio (viz. 1:2, 1:4 and 1:8 on molar basis with the cross-linker) to protect the lactone ring from hydrolysis and to prolong the release kinetics of CFD. Crystalline (F 1:2 , F 1:4 and F 1:8 ) and paracrystalline NS formulations were prepared. XRPD, DSC and FTIR studies confirmed the interactions of CFDwith NS. XRPD showed that the crystallinity of CFD decreased after loading. CFD was loaded as much as 21%, 37% and 13% w/w in F 1:2 , F 1:4 and F 1:8 , respectively while the paracrystalline NS formulations gave a loading of about 10% w/w or lower. The particle sizes of the loaded NS formulations were between 450 and 600 nm with low polydispersity indices. The zeta potentials were sufficiently high (-20 to -25 mV) to obtain a stable colloidal nanosuspension. The in vitro studies indicated a slow and prolonged CFD release over a period of 24 h. The NS formulations protected the lactone ring of CFD after their incubation in physiological conditions at 37°C for 24 h with a 80% w/w of intact lactone ring when compared to only around 20% w/w of plain CFD.
头孢地诺辛(CFD)是一种广谱抗生素,对多种细菌起作用,包括革兰氏阳性和革兰氏阴性细菌。口服药物如头孢地洛辛的主要缺点是半衰期较短,只有1.2小时。本研究的目的是通过延长给药间隔,延长药物释放时间,产生理想的血清水平,降低药物毒性,提高患者的依从性。环糊精基纳米海绵(NS)是一类新型的环糊精交联衍生物。它们已被用于提高难溶性活性的溶解度,保护不稳定基团和控制释放。本研究旨在与三种不同交联比(即与交联剂摩尔比为1:2、1:4和1:8)的β-环糊精NS配制CFD配合物,以保护内酯环不被水解,并延长CFD的释放动力学。制备了结晶型(f1:2, f1:4和f1:8)和准晶型NS配方。XRPD、DSC和FTIR研究证实了cfd与NS的相互作用。XRPD显示,加载后CFD的结晶度下降。在f1:2、f1:4和f1:8配方中,CFD的载荷分别为21%、37%和13% w/w,而准晶NS配方的载荷约为10% w/w或更低。负载的NS配方粒径在450 ~ 600 nm之间,多分散性指数较低。zeta电位足够高(-20 ~ -25 mV),可以获得稳定的胶体纳米悬浮液。体外研究表明,CFD在24小时内释放缓慢且延长。NS配方在37℃生理条件下孵育24小时后,内酯环的完整性为80% w/w,而普通CFD仅为20% w/w左右。
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引用次数: 14
Sustained release formulation of metformin-solid dispersion based on gelucire 50/13- PEG4000: an in vitro study 基于凝胶50/13- PEG4000的二甲双胍固体分散体缓释制剂的体外研究
Pub Date : 2017-10-31 DOI: 10.5138/09750215.2162
M. A. Momoh, C. Ugwu, T. C. Jackson, Ngumezi C Udodiri
Metformin is a hydrophilic hypoglycemic agent with permeability and short half-life problems which leads to its low bioavailability. Solid dispersion is one of the unique approaches, to improve bioavailability profiles of drugs. The aim of this study was to prepare and evaluate solid dispersions (SDs) of metformin with polyethylene glycol 4000 (PEG 4000) and Gelucire®50/13 in order to increase its permeability and bioavailability. Solid dispersions of Metformin containing various ratios of PEG 4000: Gelucire®50/13 (1:1, 1:2, 2:1, 1:4, 4:1 as Batch A, Batch B, Batch C, Batch D and Batch E) were prepared using solvent evaporation and fusion techniques. The physical mixtures which served as controls were also prepared. The SDs were evaluated using encapsulation efficiency, percentage yield. The formulations were also characterized with FTIR and DSC. The in vitro drug release studies were also evaluated. The results obtained showed that solid dispersion formulations at pH, 1.2 and 7.4 demonstrated higher release rates than the pure drug. The SDs showed high drug release rates and encapsulation efficiency (% EE) although Batch C containing PEG 4000 and Gelucire 50/13 in the ratio of 2:1 appeared as the batch with most % EE, drug release with broad melting peak. The release rate of metformin increased with increasing amount of PEG 4000. Batch C, SDs containing PEG 4000 and Gelucire 50/13 in the ratio of 2:1 were found to be the most optimized batch with enhanced encapsulation efficiency, most drug release and therefore, improved permeability and bioavailability of metformin.
二甲双胍是一种亲水性降糖剂,具有渗透性和半衰期短的问题,导致其生物利用度低。固体分散是提高药物生物利用度的独特方法之一。本研究的目的是用聚乙二醇4000 (PEG 4000)和Gelucire®50/13制备和评价二甲双胍固体分散体(SDs),以提高其渗透性和生物利用度。二甲双胍固体分散体含有不同比例的PEG 4000: Gelucire®50/13(1:1,1:2,2:1,1:4,4:1,批次A,批次B,批次C,批次D和批次E)使用溶剂蒸发和融合技术制备。还制备了作为对照的物理混合物。用包封率、产率对SDs进行评价。并用FTIR和DSC对配方进行了表征。体外释药研究也进行了评价。结果表明,在pH、1.2和7.4条件下,固体分散制剂的释放率高于纯药物。结果表明,PEG 4000与Gelucire 50/13的比例为2:1的C批具有较高的药物释放率和包封效率(% EE),释药峰宽。二甲双胍的释放率随PEG 4000用量的增加而增加。结果表明,以PEG 4000和Gelucire 50/13的比例为2:1的SDs包封效果最佳,包封效率高,释药量大,提高了二甲双胍的渗透性和生物利用度。
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引用次数: 1
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International Journal of Drug Delivery
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