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In Vitro and In Silico Screening Analysis of Artabotrys sumatranus Leaf and Twig Extracts for α-Glucosidase Inhibition Activity and Its Relationship with Antioxidant Activity 漆树叶片和枝条提取物对α-葡萄糖苷酶抑制活性的体外和体内筛选分析及其与抗氧化活性的关系
IF 2.5 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-12-22 DOI: 10.3390/scipharm91010002
D. Rosa, B. Elya, M. Hanafi, A. Khatib, M. I. Surya
Artabotrys sumatranus is one of the Artabotrys species, which lives in Sumatera, Java, and Borneo in Indonesia. No research has been found related to its activity. The objective of this study was to explore the potential of A. sumatranus leaf and twig extracts as the source of an anti-diabetic agent through the α-glucosidase inhibition mechanism, as well as the relationship between the antioxidant and the α-glucosidase inhibition activities in these extracts. Ethanol extracts from leaf and twig A. sumatranus were subjected to several assays: total phenolic content, total flavonoid content, antioxidant activity using DPPH (2,2-diphenyl-1-picrylhydrazyl), radical scavenging activity, and FRAP (ferric reducing antioxidant power) analysis, as well as α-glucosidase inhibition. Later, GC-MS (gas chromatography-mass spectrometer) and LC-MS/MS (liquid chromatography-mass spectrometer/mass spectrometer) analysis were conducted to identify the compounds inside the extracts. The identified compounds were tested for potential α-glucosidase inhibition activity using a molecular docking simulation. As a result, the A. sumatranus leaf extract showed more potential than the twig extract as α-glucosidase inhibitor and antioxidant agent. In addition, from the comparison between the measured quantities, it can be deduced that most of the α-glucosidase active compounds in the A. sumatranus are also antioxidant agents. Several active compounds with a high affinity to α-glucosidase inhibition were identified using the molecular docking simulation. It was concluded that A. sumatranus twig and leaf extracts seem to be potential sources of α-glucosidase inhibitors.
苏门答腊虎(Artabotrys sumatranus)是生活在印度尼西亚苏门答腊、爪哇和婆罗洲的一种虎。没有发现与它的活动有关的研究。本研究旨在通过对α-葡萄糖苷酶的抑制机制,探讨苏门答腊叶、枝提取物作为抗糖尿病药物的潜力,并探讨其抗氧化活性与α-葡萄糖苷酶抑制活性之间的关系。研究了苏门答腊叶和枝条乙醇提取物的总酚含量、总黄酮含量、DPPH(2,2-二苯基-1-苦酰肼)抗氧化活性、自由基清除活性、FRAP(铁还原抗氧化能力)分析以及α-葡萄糖苷酶抑制作用。通过GC-MS(气相色谱-质谱)和LC-MS/MS(液相色谱-质谱/质谱)分析,鉴定提取物中的化合物。通过分子对接模拟测试鉴定的化合物对α-葡萄糖苷酶的潜在抑制活性。结果表明,苏门答腊叶提取物比枝提取物更有潜力作为α-葡萄糖苷酶抑制剂和抗氧化剂。此外,从测定量的比较可以推断,苏门答腊中大部分α-葡萄糖苷酶活性化合物也是抗氧化剂。通过分子对接模拟,鉴定出几个对α-葡萄糖苷酶抑制具有高亲和力的活性化合物。结果表明,苏门答腊树枝和叶子提取物可能是α-葡萄糖苷酶抑制剂的潜在来源。
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引用次数: 2
Oral Bioavailability Enhancement of Vancomycin Hydrochloride with Cationic Nanocarrier (Leciplex): Optimization, In Vitro, Ex Vivo, and In Vivo Studies 阳离子纳米载体提高盐酸万古霉素的口服生物利用度:优化,体外,离体和体内研究
IF 2.5 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-12-21 DOI: 10.3390/scipharm91010001
Menna M. Abdellatif, S. M. Ahmed, M. EL-NABARAWI, M. Teaima
To explore the performance of the cationic nanocarrier leciplex (LPX) in escalating the oral bioavailability of vancomycin hydrochloride (VAN) by promoting its intestinal permeability. With the aid of a D-optimal design, the effect of numerous factors, including lipid molar ratio, cationic surfactant molar ratio, cationic surfactant type, and lipid type, on LPX characteristics, including entrapment efficacy (EE%), particle size (P.S.), polydispersity index (P.I.), zeta potential value (Z.P.), and steady-state flux (Jss) were assessed. The optimized formula was further evaluated in terms of morphology, ex vivo permeation, stability, cytotoxicity, and in vivo pharmacokinetic study. The optimized formula was spherical-shaped with an E.E. of 85.2 ± 0.95%, a P.S. of 52.74 ± 0.91 nm, a P.I. of 0.21 ± 0.02, a Z.P. of + 60.8 ± 1.75 mV, and a Jss of 175.03 ± 1.68 µg/cm2/hr. Furthermore, the formula increased the intestinal permeability of VAN by 2.3-fold compared to the drug solution. Additionally, the formula was stable, revealed good mucoadhesive properties, and was well tolerated for oral administration. The in vivo pharmacokinetic study demonstrated that the VAN Cmax increased by 2.99-folds and AUC0-12 by 3.41-folds compared to the drug solution. These outcomes proved the potentiality of LPX in increasing the oral bioavailability of poorly absorbed drugs.
探讨阳离子纳米载体复合剂(LPX)通过促进盐酸万古霉素(VAN)的肠通透性来提高其口服生物利用度的作用。通过d -优化设计,评估了脂质摩尔比、阳离子表面活性剂摩尔比、阳离子表面活性剂类型和脂质类型等因素对LPX吸附效率(EE%)、粒径(P.S.)、多分散性指数(P.I.)、zeta电位值(Z.P.)和稳态通量(Jss)等特性的影响。进一步从形态、体外渗透、稳定性、细胞毒性和体内药代动力学研究等方面对优化后的配方进行评价。优化后的配方呈球形,E.E.为85.2±0.95%,P.S.为52.74±0.91 nm, P.I.为0.21±0.02,zp为+ 60.8±1.75 mV, Jss为175.03±1.68µg/cm2/hr。此外,与药物溶液相比,该配方使VAN的肠通透性提高了2.3倍。此外,该配方稳定,具有良好的粘接性能,口服耐受性好。体内药代动力学研究表明,与药物溶液相比,VAN Cmax增加了2.99倍,AUC0-12增加了3.41倍。这些结果证明了LPX在提高吸收不良药物的口服生物利用度方面的潜力。
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引用次数: 1
Effect of Aqueous Extracts of Quercus resinosa on the Mechanical Behavior of Bigels 松香栎水提物对Bigels力学行为的影响
IF 2.5 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-11-28 DOI: 10.3390/scipharm90040073
J. Gallegos‐Infante, María del Pilar Galindo-Galindo, M. Moreno‐Jiménez, N. Rocha‐Guzmán, R. González-Laredo
Quercus resinosa leaves are rich in polyphenol compounds, however, they are unstable to several chemical and physical factors that limit their activity. Several methods have been developed to solve such problems, among which bigels can be mentioned and obtained using hydrogels and oleogels. The mechanical characterization of this type of materials is by using rheological methods. Although the use of these methods is well documented, the Carreau-Yasuda model has been little used to evaluate the effect of polyphenols on the mechanical behavior of bigels. Therefore, bigels were obtained from hydrogels (guar gum/xanthan gum, 0.5/0.5% w/v) and oleogels (sesame oil/sorbitan monostearate 10% w/w). Micrographs, linear viscoelasticity range, frequency sweep, and single shear tests were performed. The data were analyzed using ANOVA and Tukey test (p < 0.05); micrographs showed linear relationship between polyphenols concentration and droplet size. Liquid fraction of bigels showed a pseudoplastic behavior, while the parameters of Carreau-Yasuda model showed that the highest value of the complex viscosity at zero shear was at the lowest concentration of extract; the relaxation time presented the lowest value at higher concentrations of extracts. These results indicate that the presence of polyphenols modifyes the mechanical behavior of bigels.
松皮栎叶含有丰富的多酚类化合物,但由于受到多种化学和物理因素的限制,其活性不稳定。为了解决这类问题,已经开发了几种方法,其中可以使用水凝胶和油凝胶来制备凝胶。这类材料的力学特性是通过流变学方法进行的。虽然这些方法的使用有很好的文献记载,但carau - yasuda模型很少用于评估多酚对bigels力学行为的影响。因此,从水凝胶(瓜尔胶/黄原胶,0.5/0.5% w/v)和油凝胶(芝麻油/山梨糖单硬脂酸10% w/w)中获得凝胶。显微照片,线性粘弹性范围,频率扫描和单剪切测试进行。数据分析采用方差分析和Tukey检验(p < 0.05);显微图显示多酚浓度与液滴大小呈线性关系。液体组分表现出假塑性行为,而carau - yasuda模型参数表明,零剪切时复合黏度的最大值出现在最低萃取物浓度时;提取物浓度越高,松弛时间越短。这些结果表明,多酚的存在改变了bigels的力学行为。
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引用次数: 3
Uptake of Cationic PAMAM-PLGA Nanoparticles by the Nasal Mucosa 阳离子PAMAM-PLGA纳米粒子在鼻黏膜中的吸收
IF 2.5 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-11-25 DOI: 10.3390/scipharm90040072
Mohammed A. Albarki, M. Donovan
Nanoparticles provide promising advantages in advanced delivery systems for enhanced drug delivery and targeting. The use of a biodegradable polymer such as PLGA (poly lactic-co-glycolic acid) promotes improved nanoparticle safety and, to some extent, provides the ability to modify nanoparticle surface properties. This study compared the effect of altering the surface charge on the translocation of PLGA nanoparticles across excised nasal mucosal tissues. Nanoparticles (average diameter of 60–100 nm) loaded with Nile Red (lipophilic fluorescent dye) were fabricated using a nanoprecipitation method. The effects of nanoparticle surface charge were investigated by comparing the transfer of untreated nanoparticles (negatively charged) and positively charged PLGA nanoparticles, which were modified using PAMAM dendrimer (polyamidoamine, 5th generation). All nanoparticles were able to be transferred in measurable quantities into both nasal respiratory and olfactory mucosae within 30 min. The total nanoparticle uptake was less than 5% of the nanoparticle mass exposed to the tissue surface. The cationic nanoparticles showed a significantly lower transfer into the mucosal tissues where the amount of nanoparticles transferred was 1.8–4-fold lower compared to the untreated negatively charged nanoparticles. The modification of the nanoparticle surface charge can alter the nanoparticle interaction with the nasal epithelial surface, which can result in decreasing the nanoparticle transfer into the nasal mucosa.
纳米颗粒在用于增强药物递送和靶向的先进递送系统中提供了有希望的优势。可生物降解聚合物如PLGA(聚乳酸-乙醇酸)的使用促进了纳米颗粒安全性的提高,并且在某种程度上提供了改性纳米颗粒表面性质的能力。本研究比较了改变表面电荷对PLGA纳米颗粒在切除的鼻粘膜组织中移位的影响。使用纳米沉淀法制备了负载尼罗红(亲脂性荧光染料)的纳米颗粒(平均直径为60–100 nm)。通过比较未处理的纳米颗粒(带负电荷)和带正电荷的PLGA纳米颗粒的转移,研究了纳米颗粒表面电荷的影响,这些纳米颗粒是使用PAMAM树状大分子(聚酰胺胺,第5代)修饰的。所有纳米颗粒都能够在30分钟内以可测量的量转移到鼻呼吸和嗅觉粘膜中。纳米颗粒的总摄取量小于暴露于组织表面的纳米颗粒质量的5%。阳离子纳米颗粒向粘膜组织的转移明显较低,与未处理的带负电荷纳米颗粒相比,转移的纳米颗粒量低1.8-4倍。纳米粒子表面电荷的修饰可以改变纳米粒子与鼻上皮表面的相互作用,从而减少纳米粒子向鼻粘膜的转移。
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引用次数: 1
Enhancement of the Solubility and Dissolution Rate of Telmisartan by Surface Solid Dispersions Employing Superdisintegrants, Hydrophilic Polymers and Combined Carriers 超崩解剂、亲水性聚合物和复合载体对替米沙坦溶解度和溶出率的影响
IF 2.5 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-11-04 DOI: 10.3390/scipharm90040071
Reem A. Aldeeb, M. El-Miligi, M. EL-NABARAWI, Randa Tag, Hany M. S. Amin, A. A. Taha
Telmisartan (Tel) is a potent antihypertensive drug with a very poor aqueous solubility, especially in pH ranging from 3 to 9 (i.e., biological fluids) that results in poor bioavailability. Our aim was to improve Tel solubility and dissolution rates without the need for expensive multistep procedures, and without inclusion of alkalinizers. This study adopted the use of surface solid dispersions (SSDs) employing superdisintegrants, hydrophilic polymers and combined carriers including a superdisintegrant with a hydrophilic polymer. Tel-SSDs were formulated using thesolvent evaporation method. Compatibility between Tel and different carriers was examined via FT-IR. Tel-SSDs were evaluated optically and thermally to reveal a complete loss of the crystalline nature of the drug. Both drug content and percentage yield were calculated to judge the efficiency of the preparation technique used. Saturation, aqueous solubility, and dissolutions rates were determined. Dissolution profiles were studied using model dependent and independent approaches and were subjected to the pair-wise procedure using the DDsolver software program. Effect of aging was studied by comparing the drug content and dissolution profiles of freshly prepared SSDs with aged samples. All Tel-SSDs showed acceptable physical properties. Tel-SSDs showed pertinent enhancement related to the carrier used. Combined surface solid dispersions employing superdisintegrant croscarmellose sodium with either hydrophilic polymer PEG 4000 or Poloxamer 407 gave remarkable enhancement in solubility and dissolution rates of Tel where more than 90% of the drug was released within 20 min. The effect of aging results proved a non-significant difference in the drug content and dissolution profiles between fresh and aged samples. Formulation of Tel SSDs using combined carriers proved to be effective in enhancing the aqueous solubility and dissolution rates of Tel, as well as showing good stability upon aging.
替米沙坦(Tel)是一种有效的降压药,水溶性非常差,特别是在pH值为3至9的生物液体中(即生物液体),导致生物利用度差。我们的目的是提高Tel的溶解度和溶解速率,而不需要昂贵的多步骤程序,也不包括碱化剂。本研究采用表面固体分散体(ssd),采用超崩解剂、亲水聚合物和包括超崩解剂和亲水聚合物的组合载体。采用溶剂蒸发法制备tel - ssd。利用傅里叶变换红外光谱(FT-IR)研究了Tel与不同载体的相容性。对tel - ssd进行了光学和热评估,揭示了药物晶体性质的完全丧失。通过计算药物含量和产率来判断所采用的制备工艺的效率。测定了饱和度、水溶性和溶解率。使用模型依赖和独立的方法研究溶解剖面,并使用DDsolver软件程序进行配对程序。通过比较新鲜制备的固态硬盘与老化样品的药物含量和溶出度,研究老化对固态硬盘的影响。所有tel - ssd的物理性能均可接受。tel - ssd显示出与所使用的载体相关的相关增强。采用超崩解剂交联棉糖钠的表面固体分散体与亲水性聚合物PEG 4000或Poloxamer 407联合使用,可显著提高Tel的溶解度和溶出率,其中90%以上的药物在20分钟内释放。陈化结果表明,新鲜样品和陈化样品的药物含量和溶出谱无显著差异。采用复合载体制备的Tel固态硬盘可有效提高Tel的水溶性和溶解速率,并具有良好的老化稳定性。
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引用次数: 2
Anti-Sporotrichotic Activity, Lambert-W Inhibition Kinetics and 3D Structural Characterization of Sporothrix schenckii Catalase as Target of Glucosinolates from Moringa oleifera 辣木葡糖酸盐靶向申克氏孢子丝过氧化氢酶的抗孢子丝菌活性、Lambert-W抑制动力学及三维结构表征
IF 2.5 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-11-04 DOI: 10.3390/scipharm90040070
E. Sierra-Campos, M. Valdez-Solana, E. Ruiz-Baca, Erica K. Ventura-García, Claudia Avitia-Domínguez, M. Aguilera-Ortíz, A. Téllez-Valencia
Most human fungal infections exhibit significant defensive oxidative stress responses, which contribute to their pathogenicity. An important component of these reactions is the activation of catalase for detoxification. To discover new antifungal chemicals, the antifungal activity of methanol extracts of Moringa oleifera from two commercial products (Akuanandi and Mas Lait) was investigated. The methanolic extracts’ activity against Sporothrix schenckii was determined using an assay for minimum inhibitory concentration (MIC) and minimum lethal concentration (MLC). The MIC concentrations varied between 0.5 μg/mL and 8 μg/mL. Akuanandi extract had the lowest MIC (0.5 μg/mL) and MLC (1 μg/mL) values. M. oleifera methanolic extracts were tested for catalase inhibition. The Ki values of the M. oleifera extract against S. schenckii catalase (SsCAT) was found to be 0.7 μg/mL for MOE-AK and 0.08 μg/mL for MOE-ML. Catalase’s 3D structure in SsCAT is unknown. The homology of SsCAT was modeled with an in silico study using a 3D structure from SWISS MODEL and validation the predicted 3D structure was carried out using PROCHECK and MolProbity. Docking simulations were used to analyze protein interactions using Pymol, PoseView, and PLIP. The results revealed that M. oleifera glucosinolates interacts with SsCAT. A molecular interaction analysis revealed two inhibitor compounds (glucosinalbin and glucomoringin) with high binding affinity to key allosteric-site residues. The binding energies revealed that glucosinalbin and glucomoringin bind with high affinity to SsCAT (docking energy values: −9.8 and −9.0 kcal/mol, respectively). The findings of this study suggest that glucosinolates derived from M. oleifera could be used instead of synthetic fungicides to control S. schenckii infections. We hope that the findings of this work will be valuable for developing and testing novel natural anti-sporothrix therapeutic agents in the future.
大多数人类真菌感染表现出显著的防御性氧化应激反应,这有助于其致病性。这些反应的一个重要组成部分是活化过氧化氢酶解毒。为了发现新的抗真菌化学物质,对两种商品辣木(Akuanandi和Mas Lait)甲醇提取物的抗真菌活性进行了研究。采用最小抑制浓度(MIC)和最小致死浓度(MLC)测定甲醇提取物对申克孢子菌的活性。MIC浓度在0.5 ~ 8 μg/mL之间变化。黄芪提取物的MIC (0.5 μg/mL)和MLC (1 μg/mL)最低。研究了油桐甲醇提取物对过氧化氢酶的抑制作用。结果表明,油菜花提取物对申氏葡萄球菌过氧化氢酶(SsCAT)的Ki值分别为0.7 μg/mL和0.08 μg/mL。过氧化氢酶在SsCAT中的三维结构尚不清楚。利用SWISS MODEL的三维结构对SsCAT的同源性进行了计算机模拟研究,并利用PROCHECK和MolProbity对预测的三维结构进行了验证。对接模拟使用Pymol、PoseView和PLIP分析蛋白质相互作用。结果表明,油橄榄硫代葡萄糖苷与SsCAT相互作用。分子相互作用分析显示,两种抑制剂(glucosinalbin和gluccomoringin)与关键变构位点残基具有高结合亲和力。结合能表明,硫代葡萄糖苷和糖化蛋白与SsCAT的结合具有较高的亲和力(对接能分别为- 9.8和- 9.0 kcal/mol)。本研究结果提示,从油橄榄中提取的硫代葡萄糖苷可代替合成杀菌剂用于控制申克氏葡萄球菌感染。我们希望这项工作的发现将对未来开发和测试新的天然抗孢子菌治疗药物有价值。
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引用次数: 0
Ethanolic Extract of Ocimum sanctum Linn. Inhibits Cell Migration of Human Lung Adenocarcinoma Cells (A549) by Downregulation of Integrin αvβ3, α5β1, and VEGF 香蒲乙醇提取物。整合素αvβ3、α5β1和VEGF下调对人肺腺癌细胞(A549)迁移的抑制作用
IF 2.5 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-10-31 DOI: 10.3390/scipharm90040069
Ulayatul Kustiati, S. Ergün, S. Karnati, D. Nugrahaningsih, D. L. Kusindarta, H. Wihadmadyatami
Adenocarcinoma lung cancer is a type of non-small cell lung carcinoma (NSCLC), which accounts for 85% of lung cancer incidence globally. The therapies that are being applied, both conventional therapies and antibody-based treatments, are still found to have side effects. Several previous studies have demonstrated the ability of the ethanolic extract of Ocimum sanctum Linn. (EEOS) as an ethnomedicine with anti-tumor properties. The aim of this study was to determine the effect of Ocimum sanctum Linn. ethanolic extract in inhibiting the proliferation, angiogenesis, and migration of A549 cells (NSCLC). The adhesion as well as the migration assay was performed. Furthermore, enzyme-linked immunosorbent assay (ELISA) was used to measure the expression of αvβ3 integrins, α5β1 integrins, and VEGF. The cells were divided into the following treatment groups: control (non-treated/NT), positive control (AP3/inhibitor β3 80 µg/mL), cisplatin (9 µg/mL), and EEOS at concentrations of 50, 70, 100, and 200 µg/mL. The results showed that EEOS inhibits the adhesion ability and migration of A549 cells, with an optimal concentration of 200 µg/mL. ELISA testing showed that the group of A549 cells given EEOS 200 µg/mL presented a decrease in the optimal expression of integrin α5β1, integrin αvβ3, and VEGF.
腺癌肺癌症是一种非小细胞肺癌(NSCLC),占全球癌症发病率的85%。正在应用的疗法,包括传统疗法和基于抗体的疗法,仍然被发现有副作用。先前的几项研究已经证明了香蒲乙醇提取物的能力。(EEOS)作为一种具有抗肿瘤特性的民族医学。本研究的目的是为了确定香蒲的作用。乙醇提取物抑制A549细胞(NSCLC)的增殖、血管生成和迁移。进行粘附和迁移测定。此外,酶联免疫吸附试验(ELISA)用于测量αvβ3整合素、α5β1整合素和VEGF的表达。将细胞分为以下治疗组:对照组(未治疗/NT)、阳性对照组(AP3/抑制剂β3 80µg/mL)、顺铂(9µg/mL)和浓度分别为50、70、100和200µg/mL的EEOS。结果表明,EEOS抑制A549细胞的粘附能力和迁移,最佳浓度为200µg/mL。ELISA测试显示,给予200µg/mL EEOS的A549细胞组整合素α5β1、整合素αvβ3和VEGF的最佳表达降低。
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引用次数: 1
Fabrication of Hydroxypropyl Methylcellulose Orodispersible Film Loaded Mirtazapine Using a Syringe Extrusion 3D Printer 注射挤出3D打印机制备羟丙基甲基纤维素口服分散膜
IF 2.5 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-10-26 DOI: 10.3390/scipharm90040068
Tanpong Chaiwarit, Niphattha Aodsab, Pimonnart Promyos, P. Panraksa, S. Udomsom, Pensak Jantrawut
Depression is a mental illness causing a continuous negative feeling and loss of interest and affects physical and mental health. Mirtazapine (MTZ) is an effective medicine for treating depression, but patients lack compliance. However, transforming a pharmaceutical dosage form to an orodispersible film (ODF) could resolve this issue. This study aims to fabricate ODF-loading mirtazapine, using a syringe extrusion 3D printer, and compare its properties with the solvent-casting method. The ODFs were prepared by dissolving the mirtazapine in a hydroxypropyl methylcellulose E15 solution, and then fabricated by a 3D printer or casting. The 3D printing was accurate and precise in fabricating the ODFs. The SEM micrographs showed that the mirtazapine-printed ODF (3D-MTZ) was porous, with crystals of mirtazapine on the film’s surface. The 3D-MTZ exhibited better mechanical properties than the mirtazapine-casted ODF (C-MTZ), due to the 3D-printing process. The disintegration time of the 3D-MTZ in a simulated salivary fluid, pH 6.8 at 37 °C, was 24.38 s, which is faster than the C-MTZ (46.75 s). The in vitro dissolution study, in 0.1 N HCl at 37 °C, found the 3D-MTZ quickly released the drug by more than 80% in 5 min. This study manifested that 3D-printing technology can potentially be applied for the fabrication of ODF-containing mirtazapine.
抑郁症是一种精神疾病,会导致持续的负面情绪和兴趣丧失,并影响身心健康。米氮平(MTZ)是治疗抑郁症的有效药物,但患者缺乏依从性。然而,将药物剂型转化为口服分散膜(ODF)可以解决这个问题。本研究旨在使用注射器挤出3D打印机制备ODF负载米氮平,并将其性能与溶剂浇铸法进行比较。ODF是通过将米氮平溶解在羟丙基甲基纤维素E15溶液中制备的,然后通过3D打印机或铸件制造。3D打印在ODF的制造中是准确和精确的。SEM显微照片显示,米氮平印刷的ODF(3D-MTZ)是多孔的,膜表面有米氮平晶体。由于3D打印工艺,3D-MTZ表现出比米氮平浇铸的ODF(C-MTZ)更好的机械性能。3D-MTZ在模拟唾液液(pH 6.8,37°C)中的崩解时间为24.38 s,比C-MTZ(46.75 s)快。在37°C的0.1N HCl中进行的体外溶出度研究发现,3D-MTZ在5分钟内快速释放药物80%以上。该研究表明,3D打印技术有可能应用于制造含有米氮平的ODF。
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引用次数: 4
Modification of Taxifolin Properties by Spray Drying 喷雾干燥法改性紫杉醇的性能
IF 2.5 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-10-24 DOI: 10.3390/scipharm90040067
A. Taldaev, R. Terekhov, I. Selivanova, Denis I. Pankov, M. Anurova, I. Markovina, Zhaoqing Cong, Siqi Ma, Zhengqi Dong, Feifei Yang, Y. Liao
Taxifolin is known as an active pharmaceutical ingredient (API) and food supplement due to its high antioxidant activity, multiple pharmacological effects, and good safety profile. Previously, taxifolin spheres (TS) were obtained from industrially produced API taxifolin in Russia (RT). In our work, we perform a pharmaceutical analysis of this new taxifolin material versus RT. TS is an amorphous material; however, it is stable without the polymer carrier, as confirmed by Fourier transform infrared spectroscopy. Both RT and TS demonstrate high safety profiles and are assigned to Class 1 of the Biopharmaceutical Classification System based on the results of experiments with MDCK cells. The water solubility of the new taxifolin form was 2.225 times higher compared with RT. Hausner ratios for RT and TS were 1.421 and 1.219, respectively, while Carr indices were 29.63% and 19.00%, respectively. Additionally, TS demonstrated sustained release from tablets compared with RT: the half-life values of tablets were 14.56 min and 20.63 min for RT and TS, respectively. Thus, TS may be a promising object for developing oral antiseptics in the form of orally dispersed tablets with sustained release patterns because of its anti-inflammatory, -protozoal, and -viral activities.
紫杉醇因其高抗氧化活性、多种药理作用和良好的安全性而被称为活性药物成分(API)和食品补充剂。以前,taxifolin球体(TS)是从俄罗斯(RT)工业生产的原料药taxifolin中获得的。在我们的工作中,我们对这种新的taxifolin材料与rt进行了药物分析。TS是一种非晶材料;傅里叶变换红外光谱证实,在没有聚合物载体的情况下,它是稳定的。基于MDCK细胞的实验结果,RT和TS均显示出较高的安全性,并被列为生物制药分类系统的第1类。RT和TS的Hausner比值分别为1.421和1.219,Carr指数分别为29.63%和19.00%。此外,与RT相比,TS表现出片剂的缓释:RT和TS片剂的半衰期分别为14.56 min和20.63 min。因此,由于其抗炎、原虫和病毒活性,TS可能是开发具有缓释模式的口服分散片剂的有希望的对象。
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引用次数: 2
Concepts for a New Rapid and Simple HPLC Method for Simultaneous Determination of Metoprolol and Meldonium in Pharmaceutical Dosage Forms 同时测定药品剂型中美托洛尔和美度铵的快速简便高效液相色谱新方法的构想
IF 2.5 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2022-10-17 DOI: 10.3390/scipharm90040065
M. Piponski, M. Horyn, Kristina Grncaroska, O. Oleshchuk, E. Petrovska, Stefan Angelevski, T. Uglyar, T. Kucher, L. Logoyda
Simultaneous determination of the tandem of drugs, like meldonium and metoprolol, with enormous polarity differences between them, requires thorough research and careful selection of chromatographic conditions. The three different CN-cyano groups with link-based particle columns, LiChrospher CN, Waters Spherisorb CNRP, Zorbax CN SB stationary phases, were tested, in an isocratic elution system, with a running mobile phase containing various concepts of composition contents. They were first with buffering salts which included acetonitrile and ammonium phosphate in one group, and then without buffering salts but with diluted acids, composed of acetonitrile and diluted acids as the second group. We can conclude that the most optimal concepts, in terms of expressiveness and environmental friendliness, were concepts using of column Zorbax CN SB (4.6 mm i.d.× 250 mm, 5 μm) and mobile phase ACN—0.15% NH4H2PO4 (50:50 and 60:40, v/v). There are very poor available data about ideas and usable information about the development of methods for simultaneous determination of these two active substances with polarity differences between them. We suggest that our work offered detailed and successful solutions for the mentioned aim using less sophisticated equipment for quality control and a lab for routine manufacturing control.
同时测定麦地那和美托洛尔等药物的串联,它们之间存在巨大的极性差异,需要彻底研究和仔细选择色谱条件。在等度洗脱系统中,用含有各种组成含量概念的流动相测试了具有连接基颗粒柱的三种不同的CN氰基,即LiChrospher CN、Waters Spherisorb CNRP、Zorbax CN SB固定相。它们首先使用缓冲盐,其中包括乙腈和磷酸铵作为一组,然后没有缓冲盐,但使用由乙腈和稀释酸组成的稀释酸作为第二组。我们可以得出结论,就表现力和环境友好性而言,最理想的概念是使用Zorbax CN SB柱(4.6mm i.d.×250mm,5μm)和流动相ACN-0.15%NH4H2PO4(50:50和60:40,v/v)的概念。关于同时测定这两种具有极性差异的活性物质的方法的开发,现有的想法和可用信息非常少。我们建议,我们的工作为上述目标提供了详细而成功的解决方案,使用不太复杂的设备进行质量控制,并使用实验室进行常规制造控制。
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引用次数: 0
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Scientia Pharmaceutica
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