Lipid-based formulations (LBFs) have demonstrated a great potential in enhancing the oral absorption of poorly water-soluble drugs.体外切合LBFS相当困难,因为这些配方的人工处理复杂。论文中,我们先简单介绍胃肠消化 [.]
Der Beltrag Lipid-based formulations (LBFs) have demonstrated a great potential in enhancing the oral absorption of poorly water-soluble drugs.建模LBFs in vivo 相关联度(IVIVCs)相当困难,原因是这些配方处理复杂 invivo 本文先简要介绍脂液/LBF消化及其与增强口服吸药关系依据IVCs概念,审查tembetro/em模式当前状况,为LBFs建立IVCs,同时讨论该领域未来前景i/em测试便于理解和预测固态剂量表性能,常不模仿LBFs处理试管 消化模型更近似胃肠生理学比较有希望选择IVC建模中尽管取得了一些成功,但这些模型的精度和一致性仍有待验证,特别是人文数据A reliable IVIVC model can not only reduce the risk, time, and cost of formulation development but can also contribute to the formulation design and optimization, thus promoting the clinical translation of LBFs. Access the full article Yanping Huang, Qin Yu, Zhongjian Chen, Wei Wu, Quangang Zhu, Yi Lu, Conclusions
In vitro and in vivo correlation for lipid-based formulations: Current status and future perspectives,
Acta Pharmaceutica Sinica B, 2021, ISSN 2211-3835,https://doi.org/10.1016/j.apsb.2021.03.025.
(https://www.sciencedirect.com/science/article/pii/S2211383521000976)
The feasibility of LBF use in oral drug delivery has been fully recognized by both academia and industry.建设IVCs优先研究,为促进LBFs开发提供强效工具开发各种体外模型以理解并预测LBFs活性性能然而,当前模型都无法完全仿照活体LBFs总体过程,导致常失AIVCs努力通过密切模拟胃肠生理学提高体外模型预测力LBFs.s/ps/ps/derBeitrag
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.
Four formulations of nanostructured lipid carriers (NLC) loaded with curcuminoids where prepared, testing two types of solid lipids (Compritol® 888 ATO and Precirol® ATO 5) and two kinds of stabilizers (poloxamer 407 and polysorbate 80).111至214纳米和多差指数之间的粒度值 < 0.3号注册,低Z潜在值 [.]
Beitrag Four formulations of nanostructured lipid carriers (NLC) loaded with curcuminoids where prepared, testing two types of solid lipids (Compritol® 888 ATO and Precirol® ATO 5) and two kinds of stabilizers (poloxamer 407 and polysorbate 80).粒度值111至214纳米和多差指数 < 0.3注册,由于稳定器的非离散性,Z潜在值较低结果表明,表面活性体类型对体外释放率和卷积素前活皮肤渗透能力有影响。
DerBetrag
Labrafac
lipophile WL 1349 is our third choice oily vehicle as it is derived from short chain fatty acids and is more in favor of portal uptake.
Water dispersible surfactants
Due to their composition they enable instant emulsification of the formulation upon contact with water, which is advantageous for example if drops are take with a glass of water.
Both Labrafil® M 1944 CS and Labrafil® M 2125 CS contains long chain fatty acids in favor of lymphatic transport, the former being derived from apricot kernel oil and the second from corn oil.
More on cannabinoids delivery this by Gattefossé
Der Beitrag Tinctures or oily solutions for CBD erschien zuerst auf Pharma Excipients.
Supersaturable SMEDDS, a versatile dosage form, was investigated for improving the biopharmaceutical attributes and eradicating the food effect of poorly water soluble drug efavirenz.目标:当前研究开发efavirenz加载超饱和自微化药送系统提高生物药效方法:开展了预演研究以确定优化范围 [.]
Der Belterg Supersaturable SMEDDS, a versatile dosage form, was investigated for improving the biopharmaceutical attributes and eradicating the food effect of poorly water soluble drug efavirenz. Objective: The present research pursues development of efavirenz loaded supersaturable self-microemulsifying drug delivery system (SS SMEDDS) for improving biopharmaceutical performance. Methods: Preformulation studies were carried out to determine the optimized range of lipid excipients to develop stable supersaturated SMEDDS (ST SMEDDS).SSSDD配方编译时添加hyprymecellose作为聚合降水抑制器开发型SSSDDS通过体外超饱和研究评价超饱和行为并用硅对接模拟分子模拟分解用生物相关介质模拟胃肠区域填充/加固条件药理学方法确定吸附行为.
Present work investigates the possibility of a polyethyleneglycolylated (PEGylated) microemulsion (ME) to deliver drug to the posterior segment of eye.三安氏素axonide(TA)被选为示范药,该药在子宫内疾病中广泛使用。基于溶解度和模变能力,选择微模分量并获取最优配方.
BeitragPresent work investigates the possibility of a polyethyleneglycolylated (PEGylated) microemulsion (ME) to deliver drug to the posterior segment of eye.三安氏素axonide(TA)被选为示范药,该药在子宫内疾病中广泛使用。基于溶解和乳化能力选择微模组件并使用伪相图获取最优配方优化比 CapmulMCM C8(oil):aconMC8-2PEPE-PEG2000装有TA的PEGYLEDME体外评价开发PEGYed装填TA时均匀稳定不可对视并能够接触后视点传入部分。
向视网膜交付毒品受两种屏障阻塞:沉浸和流畅ME系统报告良好 克服薄膜屏障超流性屏障使用PEGYL化磷素ibjant可生物降解非毒并附加于ME界面,离开PEG链水分分阶段ME以提取流体中较长循环效果开发PEGYLEDME当前调查能力足以保持加载染料循环达6H和6H,与纯染料溶液和非PEGYETME相比,数量更高PEGylation was also proven true for its utility in topical ocular ME for retinal drug delivery. Download the full publication here: Triamcinolone Acetonide-Loaded PEGylated Microemulsion for the Posterior Segment of Eye
CONTINUE READING THE FULL ARTICLE HERE
Der Beitrag Triamcinolone Acetonide-Loaded PEGylated Microemulsion for the Posterior Segment of Eye erschien zuerst auf Pharma Excipients.
The central nervous system (CNS), namely the brain, still remains as the hardest area of the human body to achieve adequate concentration levels of most drugs, mainly due to the limiting behavior of its physical and biological defenses.lipid纳米胶囊作为多功能平台出现解决这些屏障,高效提供不同的药用有效载荷 [.]
Der Beitrag The central nervous system (CNS), namely the brain, still remains as the hardest area of the human body to achieve adequate concentration levels of most drugs, mainly due to the limiting behavior of its physical and biological defenses.lipid纳米胶片作为一个多功能平台出现解决这些屏障,并高效提供不同的药用有效载荷,因为它们有多种长处。 可以快速、免溶和可扩缩过程生产,它们的特性可微调以制作最优脑药送工具此外,油脂纳米囊表面修改可进一步提高中枢神经系统生物可用性结合这些特征与替代投送方法并发,以阻塞或完全绕过脑屏障,可能充分利用脂纳米胶片向当前处理选项提供的治疗先进技术。 Thus,本审查意在批判性解决油纳米胶片开发问题,并突出关键特征,这些特征可调整改善面向中神经系统投送的特性,主要通过静脉注射法,以及如何利用CNS的病理微环境并讨论促进向脑剖面投送药物的不同路线,以及通过将修改油脂纳米胶片与新/智能管理路线合并实现协同效果More on liquid nano capsules Der Beitrag Lipid nanocapsules to enhance drug bioavailability to the central nervous system erschien zuerst auf Pharma Excipients.
Benznidazole (BZ) tablets are a unique form of treatment available for treating Chagas disease.开发液态配方中易口服儿科病人治疗,特别是新生儿,迫切需要开发性能、安全性能和适配生物药剂与BZ片状物性能相同sEDDS自模配送系统:Cagas疾病处理新替代毒理表 erzienzust auf Benznidazole (BZ) tablets are a unique form of treatment available for treating Chagas disease.开发液态配方中易口服儿科病人治疗,特别是新生儿,迫切需要开发性能、安全性能和适配生物药剂与BZ片状物性能相同自模药送系统可提高BZ等药物生物可用性,BZ水溶性差和渗透性低。
Pepermore在使用BZ-SEDDS处理的动物中未观察到生物毒性增加BZ-SEDDS体外和体外数据加在一起显示,BZ输入SEDDS并不会改变其能力、效果和安全性。BZ-SEDDS可是一种比较实用和个性化口服液量表,而压片BZ槽则悬浮处理新生儿和幼童,即用不同水性液模化SEDDS并使用服药弹性的优势More on SEEDS of Benznidazole
Der Beitrag Benznidazole Self-Emulsifying Delivery System: A Novel Alternative Dosage Form For Chagas Disease Treatment erschien zuerst auf Pharma Excipients.
Self-emulsifying drug delivery systems (SEDDS) are one of the proven methods to increase solubility and bioavailability of poorly soluble drugs.SEDDS为异向混合体,由油类、表面活性物组成,有时还分解设计化配方用于改善口吸高脂性复合物多脂基药物提供系统在文献和 [.]
Der Betrag
Self-emulsifying drug delivery systems (SEDDS) are one of the proven methods to increase solubility and bioavailability of poorly soluble drugs.
SEDDS are isotropic mixtures, consisting of oils, surfactants, and sometimes cosolvents.设计化配方用于改善口吸高脂性复合物多脂制药物提供系统在文献中广泛报告,其中包括简单油解法、粗化、多变干比和复杂自化、微化或纳米化药提供系统。
自化过程取决于多种因素,如油质性质、表面作用学、共振学、油/浮比和极化考虑到大规模生产的易易性以及SEDDS的稳健性,几种配方可用商业方式使用这一技术文章试图概述SEDDS应用、编译文献数据、商业产品及其描述Download the full article on SEDDS here: self-emulsifying-drug-delivery-systems-and-their-marketed-products-a-review.pdfDer Beitrag Self-emulsifying Drug Delivery Systems and their Marketed Products: A Review erschien zuerst auf Pharma Excipients.
In this study, we develop and apply a high-throughput screening pro- tocol to investigate the activity of non-ionic surfactants, with a broad range of hydrophilic–lipophilic balance values, against ABCB1-mediated efflux transport and ABCC2-mediated efflux transport.Caco-2机盘生长7天,然后用测试材料浸泡 [.]
Beitrag In this study, we develop and apply a high-throughput screening pro- tocol to investigate the activity of non-ionic surfactants, with a broad range of hydrophilic–lipophilic balance values, against ABCB1-mediated efflux transport and ABCC2-mediated efflux transport. Methods Caco-2 cells were grown for 7 days in 96-well plates, then washed and incubated with the test materials for 2 h in the presence of 2.5 lM of either rho- damine 123 (R-123) or 5(6)-Carboxy-20,70 dichlorofluorescein diacetate as probes of ABCB1 and ABCC2, respectively. Key findings Of the surfactants tested, no activity against ABCC2 was detected and all surfactants showing efficacy against ABCB1 had a HLB value of 22 or below.ABCB1作用排序为polxamer335>polxamer40>CrovolA-70>MyrjS-40>polxamer184>polxamer182>Etocas40>Tween20>Etocas29>Tween80>AccononC-44>span20关于抑制作用,流益区域分布比HLB值更重要 。
Der Beitrag High-throughput screening of excipients with a biological effect erschien zuerst auf Pharma Excipients.
To improve the dissolution and oral bioavailability of valsartan (VST), we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMED) composed of Capmul® MCM (oil), Tween® 80 (surfactant), Transcutol® P (cosurfactant), and Poloxamer 407 (precipitation inhibitor) but encountered a stability problem (Transcutol® P-induced weight loss in storage) after solidification.[.]
DerBeitrag To improve the dissolution and oral bioavailability of valsartan (VST), we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMED) composed of Capmul® MCM (oil), Tween® 80 (surfactant), Transcutol® P (cosurfactant), and Poloxamer 407 (precipitation inhibitor) but encountered a stability problem (Transcutol® P-induced weight loss in storage) after solidification. In the present study, replacing Transcutol® P with Gelucire® 44/14 resulted in a novel SuSMED formulation, wherein the total amount of surfactant/cosurfactant was less than that of the previous formulation.固化S-SUSMED粒子编译方法将含有VST的SUSMED与选择性固态载体L-HPC和FloritePS-10相混合,VST均以不定状态存在ssmed平板板直接压缩附加前接收者后6个月存储量和杂质变化完全稳定(40+2摄氏度和75+5%相对湿度)。
下载整篇文章pdf:s/www.mdpi.com/1999-4923/112/58See also more information on lipid excipients.
Der Beitrag Improved Dissolution and Oral Bioavailability of Valsartan Using a Solidified Supersaturable Self-Microemulsifying Drug Delivery System Containing Gelucire® 44/14 erschien zuerst auf Pharma Excipients.
An innovative delivery system for melatonin, based on the incorporation of solid lipid microparticles in orodispersible films (ODFs) made of maltodextrin, was designed and developed.喷雾凝聚技术生成双模微粒(10%和20% w/w)并标注 [.]
/derBetrag An innovative delivery system for melatonin, based on the incorporation of solid lipid microparticles in orodispersible films (ODFs) made of maltodextrin, was designed and developed.液晶粒子介于两种不同的melatonin浓度(10%和20% w/w)上,喷凝技术使用两种不同的脂质载荷(tisearin和氢化投影机油)生成,并用体积、固态、药加载和释放药模式定性。
Der Beitrag A new melatonin oral delivery platform based on orodispersible films erschien zuerst auf Pharma Excipients.
Implication of Quantitative Selection of Each Excipient in Product Development Excipients' role in designing different dosage forms does not require any introduction.以上这些添加物与药理活性物质并发增加这些特性的主要目的是增加大数配方并传递所期望的[.]
Beitrag Excipients' role in designing different dosage forms does not require any introduction.以上这些添加物与药理活性物质并发增加这些特性的主要目的是增加大片配方并传递期望属性始发者像药物一样,需要验证和标准化下一章简单介绍不同用量表使用前接收者,包括固态用量表、液态用量表和半固态用量表计药先进配方领域的持续开发,我们还覆盖纳米化前接收者。 Implication of Quantitative Selection of Each Excipient in Product Development
Der Beitrag Current Developments in Excipient Science – Implication of Quantitative Selection of Each Excipient in Product Development erschien zuerst auf Pharma Excipients.