Silymarin, a flavonolignan, derived from Silybum marianum, family Asteraceae has long been used as a hepatoprotective remedy.Silymarin有细胞保护活动 因为它有抗氧化特性 和自由提取活动药效学研究过去三十年显示Silymarin吸收不良和快速新陈代谢,特别是第二阶段代谢和最终口服差 [.]
DerBeitragSilymarin, a flavonolignan, derived from Silybum marianum, family Asteraceae has long been used as a hepatoprotective remedy.Silymarin有细胞保护活动 因为它有抗氧化特性 和自由提取活动药代学研究过去三十年显示Silymarin吸收力差,快速新陈代谢化学,特别是第二阶段新陈代谢和最终口服生物利用率差Quercetin是食用蔬菜和水果中的裂变物,它是一种强效抗氧化物并显示各种生物功能Querestin提高血液水平和药效量,因为它是P-Glycoprotein抑制器并抑制药物代谢酶。
bthSilymarin先进型配方如聚合纳米粒子可成功使用提高生物用量和Silymarin控件对肝细胞silymarinquestin自发仿真溶解法编译PNPs使用可生物分解聚合物PLGAApigenin (Apig) is used as a model drug due to its many beneficial bio-activities and therapeutic potentials.水溶性差和存储稳定性低限制了药区应用的可行性为解决此问题,本研究开发纳米聚合物/NEPS使用抗氧化聚合物/D-ffelly聚乙酸
Apigenin (Apig) is used as a model drug due to its many beneficial bio-activities and therapeutic potentials.水溶性差和存储稳定性低限制了药区应用的可行性研究用反毒聚合物、Apig化学稳定性显著提高,并因与BSFL油和AV油Nes合并而提高抗氧化能力,特别是单TPGSNes单端TPGSNES还展示最佳Apig皮肤沉积未来应用局部Apig投送NES-GelTheir rheological characteristics were dominated by the surfactant ratios of HL to TPGS.
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Article information: Chou, T.-H.!Nugroho D.S.长JY郑义秀梁城邓小J内温封装和特征化基于反氧化聚合二元交付。 ObjectiveApgenins 2021 , 13 1016https://doi.org/10.3390/polym1301016
Despite its proven efficacy in diverse metabolic disorders, quercetin (QU) for clinical use is still limited because of its low bioavailability.D-A-Tocopherol聚乙烯1000sucnate(TPGS)经批准为安全药辅助物,并配有标记抗氧化物和防炎活动在当前研究中,对数个自载自译自算系统进行了调查,以改进 [.]
Despite its proven efficacy in diverse metabolic disorders, quercetin (QU) for clinical use is still limited because of its low bioavailability.D-A-List/pmc-isochem/在当前研究中,对数个QU自译自语系统(SNEDDS )进行了调查,提高QU生物可用性。XterraCsub>18 列(4.6x100mm5m)和UV检测280nm解析法分离法梯度系统乙醇和磷酸缓冲pH3开发RP-HPLC方法显示低检测限值7.65和22.09纳克/ml和LOQs23.19和66.96纳克/mlSNEDDS选公式中含有50%span类=html-itic's/spans类=shtml-itic's/spansle=tTPGS, 30%聚乙醇200(PEG200)和20%sspan类='html-itic'/span>/span类=sitic'slic's/span药代物学研究显示SNEDDS生物利用率比悬浮提高149.8%。开发HPLC方法证明简单敏感QU和TPGs口服新SNEDS公式后对老鼠等离子并发判定值 。 下载整页pdf:
Supersaturated lipid-based drug delivery systems are increasingly being explored as a bio-enabling formulation approach, particularly in preclinical evaluation of poorly-water soluble drugs.以热导超饱和方式增加药载量,结果增强某些药体的活性接触量,而对于其他药体,例如cinnarizine,超饱和脂基系统被认为无益增加s
serBeitragSupersaturated lipid-based drug delivery systems are increasingly being explored as a bio-enabling formulation approach, particularly in preclinical evaluation of poorly-water soluble drugs.热诱发超饱和增加药量导致某些药的体外接触增加,而对于其他药,例如cinnarizine,超饱和脂基系统被认为不利于提高Vivo生物可用性假设集降水抑制器减少毒品降水可能解决这一限制因此,对有降水抑制器或无降水抑制器的素超饱和基于脂的药送系统药代剖面图进行了比较。5个降水抑制器选择调查基础是对21个前接收者进行高排量筛选Vivo结果显示,长链单片或中链单片配方加5%降水抑制器显示松鼠生物利用率总体增加趋势,尽管Poloxamer 407+LCM系统仅统计性大幅增加(e.ACU0-24h比LCM增加2.7倍,无降水抑制器)。降水抑制器似乎减轻了二维降水从二维二维齐纳和总体生物可用性,可与先前报告的非超饱和脂系统下药后cinnarizine相仿简言之,对于超饱和脂基药送系统(如cinnarizine)中易降水的药物,加入降水抑制器可减轻这一风险,并提供机会使接触最大化,这在早期效果和毒理学评价中是最合宜的。Continue to read how to improve in vivo absorption of cinnarizine from supersaturated lipid-based drug delivery systems
Keywords: Supersaturated lipid-based drug delivery systems, Precipitation inhibitors, High throughput screening, Bio-enabling formulations, Pharmacokinetic profiles, Soluplus, Vitamin E-TPGS
Der Beitrag Exploring precipitation inhibitors to improve in vivo absorption of cinnarizine from supersaturated lipid-based drug delivery systems erschien zuerst auf Pharma Excipients.
Press release – Contact: Patti Griggs 856-533-1870 PMC Isochem announces today that it is accelerating the strategic development and manufacture of polyamino acids (PAA) as functional excipients used in complex formulations and drug delivery solutions.以自身内部资源为基础并拥有完全综合技术并处于以下领先位置.
Der Beitrag Press release – Contact: Patti Griggs 856-533-1870 PMC Isochem announces today that it is accelerating the strategic development and manufacture of polyamino acids (PAA) as functional excipients used in complex formulations and drug delivery solutions.PMCIsochem成为PAA和持久伙伴的可靠提供方。 PMC Isochem ISODEL® offer at a glance: About PMC Isochem PMC Isochem provides product/process development, regulatory approvals, pilot scale and full plant-scale production of drug intermediates, active pharma ingredients (APIs) and functional excipients for major pharmaceutical companies worldwide to serve the medical needs of Oncology, Cardiovascular, Infectious, Gastro-Intestinal, Neurology and rare diseases.PMCIsochem设施组合法国三个站点-Genenvilierss、Pithiviers和Vert-Le-Petit-设施全由GMPUSFDA审核生产药厂PMCIsochem有230+雇员作为全资法国集团子公司运行。
The combination of polymeric surfactants with different features into mixed micelles give access to properties that may be superior to the single-component micelles.在这次工作中,我们调查D-A-Topheryl聚乙酸酯混合物中的协同效应,PORXMines(又称TETronic)、pH响应和热凝聚聚ENO-PEO-polypre[.]
Der Beitrag
The combination of polymeric surfactants with different features into mixed micelles give access to properties that may be superior to the single-component micelles.In this work, we investigated synergistic effects in mixtures of D-α-Tocopheryl polyethylene glycol succinate (TPGS) with poloxamines (also known as Tetronic), pH-responsive and thermogelling polyethylene oxide (PEO)-polypropylene oxide (PPO) 4-arm block copolymers.
We examined the morphology of the self-assembled micelles of TPGS with Tetronic 1107 (T1107) and 908 (T908) in the presence of naproxen (NA), used as a model drug, and assessed the capacity of the single and mixed micelles to trap the guest, using a combination of small-angle neutron scattering (SANS) and NMR spectroscopy (1D, 2D-NOESY and diffusion NMR), over a range of compositions and temperatures, in the dilute regime and gel state.NA没有以单片形式与T1107或T908发生交互作用,但它被嵌入小鼠超出临界小鼠温度(CMT)的疏水芯相形之下,TPGS 鼠标结构不因有NA而改变,但核心体积扩展除外,这是NA优先积聚的结果。
单片小鼠的溶性随温度而显著提高,混合小鼠生成TPGS和pooxamine之间的溶性中间增强值,Poloxamine随TPGS/Poloxame比率提高而增加单片混合小鼠打包生成的Micellar水凝胶,BCC宏拉特氏体结构没有因药的存在而改变(至少0.2千兆字节/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒/秒science/abs/pii/S016732203725目标ss/blankrel=noopener noreferr>Blanco-Prieto、Carlos Aydillo、Aurel RadulescuDreiss, Gustavo González-Gaitano,Poloxamine/D-A-Topheryl聚乙酸https://doi.org/10.1016/j.molliq.2020.114930.
See the video about Vitamin E TPGS here:
Der Beitrag Poloxamine/D-α-Tocopheryl polyethylene glycol succinate (TPGS) mixed micelles and gels: Morphology, loading capacity and skin drug permeability erschien zuerst auf Pharma Excipients.
Plant-derived phenolic compounds have multiple positive health effects for humans attributed to their antioxidative, anti-inflammatory, and antitumor properties, etc.这些效果在很大程度上取决于生物机体中的生物可用性生物存取性,并因此生物存取性在很大程度上取决于生物体结构与形式,例如通过复合s/
Plant-derived phenolic compounds have multiple positive health effects for humans attributed to their antioxidative, anti-inflammatory, and antitumor properties, etc.这些效果在很大程度上取决于生物机体中的生物可用性生物存取性并因此生物可用性在很大程度上取决于生物体所输入的结构和形式,例如通过复合食物矩阵或净化分离倍数复合体与食物中或消化期间的其他大型分子(蛋白类、脂肪类、饮食纤维类、多功能类)发生交互作用,极大地影响生物接触生物机体,但由于倍数复合体机制复杂,尚未充分检测此区模拟胃消化法是常用体外测试之一,用于评估苯丙化合物生物存取性封装法可积极影响生物可获取性与生物可用性,因为它能确保
Check the encapsulation materials and methods in the following tables as of this publication
Encapsulation of phenolic acids and stilbenes
| Core Material | Wall Material | Encapsulation Method |
|---|---|---|
| ferulic acid | chitosan-tripolyphosphate pentasodium | ionic gelation |
| ferulic acid | poly-D,L-lactide-co-glycolide (PLGA) | double emulsion |
| caffeic acid | poly-D,L-lactide-co-glycolide (PLGA) | emulsion |
| syringic acid | D-Alpha tocopheryl polyethylene glycol 1000 succinate (TPGS) | thin-film dispersion |
| trans-resveratrol | zein | electrospraying |
| trans-resveratrol | poly-D,L-lactide-co-glycolide (PLGA) | precipitation |
Encapsulation of flavonoids
| Flavonoid Category | Core Material | Wall Material | Encapsulation Method |
|---|---|---|---|
| flavanols | quercetin | chitosan | ionic gelation |
| flavanols | quercetin | poly(lactic-co-glycolic acid) (PLGA) | emulsion diffusion evaporation |
| flavanols | quercetin | soluplus micelles | film dispersion |
| flavanols | quercetin | linseed oil, GMS, P6, Tween 80, 1,1-propylene glycol | high pressure homogenization |
| flavanols | quercetin | poly-D,L-lactide (PLA) | solvent evaporation |
| flavanols | quercetin | glycerol monostearate (GMS), medium chaintriglycerides (MCT), soy lecithin | emulsifying and solidifying |
| flavanols | quercetin | zein, 2-hydroxypropyl-β-cyclodextrin | spray-drying |
| flavanols | quercetin | casein, 2-hydroxypropyl-β-cyclodextrin | coacervation |
| flavanols | quercetin | poly(lactic-co-glycolic acid) (PLGA) | solvent displacement |
| flavanols | quercetin | ethylcellulose | precipitation |
| flavanols | quercetin | soy lecithin, glyceryl tridecanoate, glyceryl tripalmitate, vitamin E acetate, Kolliphor HS15 | phase inversion |
| flavanols | quercetin | (β-CD)-dodecylcarbonate | freeze-drying |
| flavanols | kaempferol | chitosan, sodium tripolyphosphate | ionic gelation |
| flavanols | kaempferol | lecithin–chitosan | electrostatic self-assembly |
| flavanols | fisetin | DOPC, cholesterol, DODA-PEG2000 | liposomes |
| flavanols | fisetin | PLGA (poly-lactide-co-glycolic acid), HPβCD (hydroxyl propyl beta cyclodextrin) | emulsion, freeze drying |
| flavones | tangeretin | zein | emulsion |
| flavones | apigenin | soybean oil, Tween 80 | in vitro digestion, in vivo pharmacokinetics |
| flavones | rutin | chitosan | ionic gelation |
| flavanones | naringenin | phospholipid, cholesterol, sodium cholate, and isopropyl myristate | liposomes by thin-film dispersion |
| flavan-3-ols | epigallocatechin gallate (EGCG) | gum arabic, maltodextrin | spray drying |
| flavan-3-ols | epigallocatechin gallate (EGCG) | chitosan-tripolyphosphate | freeze-drying |
| flavan-3-ols | catechin hydrate | phosphatidylcholine (PC) | liposomes |
| flavan-3-ols | catechin hydrate | horse chestnut, water chestnut and lotus stem starch | freeze drying |
| flavan-3-ols | green tea catechins | soy protein | emulsion |
| flavan-3-ols | green tea catechins | vitamin C and xylitol, γ-cyclodextrin and hydroxypropylmethyl cellulose phthalate | film-forming |
| flavan-3-ols | green tea catechins | hydroxypropyl methyl cellulose phthalate | coating |
| flavan-3-ols | tea catechins | corn oil and polysorbate 80 | emulsion |
| isoflavones | daidzein | phospholipid | film-homogenization |
| isoflavones | genistein | Soluplus® and Vitamin E d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) | organic solvent evaporation |
Encapsulation of anthocyanins
| Core Material* | Wall Material | Encapsulation Method |
|---|---|---|
| blackberry purees | β-cyclodextrin | molecular inclusion |
| saffron anthocyanins | β-glucan and β-cyclodextrin | spray drying |
| Vaccinium ashei extracts | whey protein isolate | spray drying |
| Bryophyllum pinnatumextract | β-cyclodextrin | emulsion |
| bran extract | maltodextrin, gum arabic, whey protein isolate | spray drying |
| bran extract | alginate-whey protein isolate | ionic gelation |
| sour cherries skins extract | whey proteins isolate | freeze-drying |
| bilberry extract | whey protein, citrus pectin | emulsification and thermal gelation |
| anthocyanins standards mixture | cyclodextrins | freeze-drying |
| anthocyanins standards mixture | chitosan hydrochloride, carboxymethyl chitosan, β-Lactoglobulin | ionic gelation |
| bilberry extract | pectin amide | extrusion |
| bilberry extract | pectin amide with an additional shellac coating | emulsification/heat gelation |
| bilberry extract | whey proteins | spray drying |
| black carrot extract | polycaprolactone | double emulsion |
| black carrot extract | cholesterol and non-ionic surfactant (Tween 20) | niosome method |
| mulberry-extracted anthocyanin | alginate/chitosan | spray drying and external gelation |
| red pepper waste | whey protein | spray drying and freeze-drying |
| bilberry extract | whey protein isolate | gelation |
* Source of anthocyanins
Keywords: bioaccessibility!模拟胃肠消化目标交付控制释放封装技巧coating materials
Der Beitrag Role of the Encapsulation in Bioavailability of Phenolic Compounds erschien zuerst auf Pharma Excipients.
The nature of the interaction of bile salt micelles with exogenous surfactants used in formulations and the consequent impact on drug solubilisation is not well understood.常假设添加表面活性将提高药物的溶解性,而这往往单在水中就属实。infs/www.pharmaexcceptips.com/surfactants/mixed-miles/
The nature of the interaction of bile salt micelles with exogenous surfactants used in formulations and the consequent impact on drug solubilisation is not well understood.常假设添加表面活性将提高药物的溶解性,而这往往单在水中就属实。研究中,我们调查了一系列典型非离子配方表面活性物(KolliphorEL、VitaminETPGS和数组Pruronicss)与bil盐+ 除浮点F68外,疏水和浮点作用都膨胀了易盐混合小鼠,并得出结论说,虽然小鼠体积增加,但溶解环境比单易盐小鼠条件差。science/artist.com/science/article/pii/S037873307468目标Clulow, Bryce Barber, Malinda Salim, Tim Ryan, Ben J.spanspan类/textformss.com/surfactants/surfactants/a/a/
The aim of this study was to control the dissolution rate and permeability of cilostazol.为提高活性药素解析率,应用热熔放大技术准备固散为了控制肠道渗透性而不论食物摄取量,HME进程优化基础 [.]
DerBeitrag The aim of this study was to control the dissolution rate and permeability of cilostazol.为提高活性药素解析率,应用热熔放大技术准备固散为了控制胃肠道渗透性而不论食物摄取量,HME过程优化基于生理药代物学模拟exrude使用实验室规模双螺旋切片并用恒定摄取速率制作。 PBPK模拟参数敏感分析后进行 Next解析测试显示 裂变溶性提高 单比ciostazol基于PSA分析,表面作用感应利用热熔溢出技术制作出平分布脂质片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片状片ilostazol配方比市场化配方更快吸收优化热熔化配方。
https://doi.org/10.3390/pharmaceutics12080757
Used Excipients: KollidonVA64, Vitamin E TPGS, Microcrystalline Cellulose (MCC)
Der Beitrag Preparation of Hot-Melt Extruded Dosage Form for Enhancing Drugs Absorption Based on Computational Simulation erschien zuerst auf Pharma Excipients.
d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) has been widely used in a variety of oral applications to enhance dissolution, solubility, and/or bioavailability of poorly-water soluble drugs.此外,TPGS的使用有可能最大限度地减少质子泵抑制器或H2受体阻塞器共同管理的病人中常见的氯水效应TPGS unclements/www.pharmaexccepties.com/biopity-enchancement/tpgs-surfactant-disolute-effects/
d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) has been widely used in a variety of oral applications to enhance dissolution, solubility, and/or bioavailability of poorly-water soluble drugs.此外,TPGS的使用有可能最大限度地减少质子泵抑制器或H2受体阻塞器共同管理的病人中常见的氯水效应The incorporation of TPGS in tablets, however, can have undesirable effects on compaction, physical stability, and processing.
Highlights
• We demonstrated a systematic approach using HSWG to effectively incorporate TPGS into solid oral formulations to capitalize on the bioperformance enhancement of TPGS while maintaining tablet integrity.• TPGS-based HSWG formulations minimize achlorhydric effects and dissolution sensitivity against various attributes of a poorly water-soluble drug.
• TPGS-based HSWG formulations enable excellent downstream processing and improve flow properties of drug A (poor flow, cohesivity, and agglomeration) through a HSWG process.
• Formulation robustness was demonstrated through similar dissolution profiles despite containing different attributes of a poorly water-soluble drug.
Therefore, the goal of this study was to develop a systematic approach using high-shear wet granulation (HSWG) to effectively incorporate TPGS into solid oral formulations to enhance bioavailability under achlorhydric conditions without tablet defects.TPGS水平优化定义基于分解性能、生物性能、物理稳定性和平板特性TPGs含HSWG配方大为改善处理和流性并优于干粒化配方此外,HSWG配方强健性通过相似分解剖面貌得到证明,尽管含有差分水分解药的不同属性因此,HSWG配方加TPGS可不仅最小化氯水效应,而且最小化分解敏感度以对抗差分水分药可变属性More on the effect of TPGS surfactant on dissolution sensitivity
Keywords Wet granulation, TPGS, Dissolution, Surfactant, Poorly water-soluble drug, Bioavailability, Poloxamer 407 (Lutrol F 127), polyoxyl 35 castor oil (Cremophor EL), sodium lauryl sulfate (Texapon K 12 P PH),d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS), Polysorbate 80
Der Beitrag Effect of TPGS surfactant on dissolution sensitivity of a poorly water-soluble drug using high-shear wet granulation erschien zuerst auf Pharma Excipients.