Most of the promising drugs in development channels are poorly water-soluble drugs which limit formulation approaches, clinical application because of their low dissolution and bioavailability.药厂当前的主要挑战 是提高药物水溶性的建议策略固态散射被认为是[.]
/p>Der Betrag Most of the promising drugs in development channels are poorly water-soluble drugs which limit formulation approaches, clinical application because of their low dissolution and bioavailability.制药业当前的主要挑战有提高药物水溶性的建议策略。 单片分布被认为是用几种成功营销产品克服这些问题的主要进化固分解概述为高效药提供系统,但需要设计具体药用表提高水溶性低药的溶性与生物可用性。 单分解可用溶剂蒸发、熔化和超临界流体技术等数种方法制作本审查旨在提供过去几年固散编程技巧和聚合物使用最新趋势概述Along with the various pharmaceutical strategies and future visions for the solubilization of poorly water-soluble drugs Download the full article as a PDF here Article information: Talla S, Wadher K, Umekar M, Lohiya R.近期相关方法推介固态分布JDDT[互联网]15Aug.2021[引用20Aug.2021]11(4-S):247-5Available from: http://jddtonline.info/index.php/jddt/article/view/4963 Der Beitrag Recent and Relevant Methodology in the Advancement of Solid Dispersion erschien zuerst auf Pharma Excipients.Table 1: Summary related to overall techniques used recently with continually used polymer
SD Techniques Drugs Polymers Ref. Solvent evaporation Dutasteride (DUT) Microcrystalline cellulose [16] Oleanolic acid (OA) Leucine [17] Efonidipine hydrochloride HPMC-AS [18] Sirolimus Polyvinylpyrrolidone (PVP), Poloxamer 188 and Cremophore RH40 [19] Febuxostat (FB) Polyvinylpyrrolidone (PVP K30) and poloxamer [20] Ticagrelor TPGS and Neusilin® US2 [21] Candesartan cilexetil (CC) Tromethamine (Tris) [22] Progesterone (PG) Hydroxypropyl methylcellulose (HPMC), Hydroxypropyl methylcellulose acetate succinate (HPMCAS), Microcrystalline cellulose (MCC), Polyvinylpyrrolidone (PVP) and silica (SiO2) [23] Andrographolide (ADG) Silica (SiO2) [24] Hot melt extrusion Fenofibrate (FNB) PVP VA64 [28] Baicalein Kollidon VA64 and Eudragit EPO [29] Indomethacin (IND), Itraconazole (ITZ), and Griseofulvin (GSF) Eudragit EPO, Eudragit L-100-55, Eudragit L-100, HPMCAS-LF, HPMCAS-MF, Pharmacoat 603, and Kollidon VA-64 [30] Indomethacin (IND) Magnesium aluminium and lithium magnesium sodium silicates [31] Carbamazepine (CBZ) Eudragit EPO [33] Osthole (OS) Plasdone S-630, HPMC-E5, Eudragit EPO, and Soluplus [34] Lacidipine Soluplus and PVP VA64 [35] Triamterene D-mannitol [36] Melt agglomeration Diazepam Polyethylene glycol (PEG) 3000 or Gelucire 50/13 [39] Lu-X Rylo MG12, Gelucire 50/13, PEG 3000, or poloxamer 188 [41] Lumefantrine Polyethylene glycol (PEG) 6000 or Poloxamer 188 [42] Spray drying method Indomethacin (IMC) Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol [44] Ibuprofen Curcumin [45] Candesartan cilexetil (CC) PVPK30 [46] Pioglitazone PVP K17, PVP K30, and HPMC E3 [47] Darunavir Hydroxypropyl methylcellulose (HPMC), hydroxypropyl methylcellulose acetate succinate (HPMC AS) and polyvinylpyrrolidone K-30 (PVP) [48] Tadalafil (TDL) Glycyrrhizin [49] Nisoldipine Polyethylene glycol 4000 (PEG4000) [50] Ketoprofen vinyl-pyrrolidone based polymers [51] Efavirenz Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®) [52] Lyophilization Efavirenz Polyvinylpyrrolidone (PVP) K-30 [55] Famotidine Soluplus® (SP) [56] Prednisolone Bovine serum albumin (BSA) [57] Diclofenac sodium (DS) Ethylcellulose (ECand chitosan (CS)) [58] Mebendazole (MBZ) low-substituted hydroxypropylcellulose (L-HPC) [59] Exemestane Phospholipid/sodium deoxycholate [60] Valsartan (VAL) Polyethylene glycol 6000 (PEG6000) and hydroxypropylmethylcellulose [61] Telmisartan Polyvinylpyrrolidone (PVP) K30 [62] Tadalafil (Td) HPMC, MC, PVP, PVP-VA, Kollicoat IR and Soluplus [63] Fusion method Torcetrapib, itraconazole, and lopinavir HPMCAS (L, M, and H), copovidone, Soluplus, PEG1500, Vitamin-E TPGS, Kolliphor EL, and Eudragit [64] Spironolactone (SPL) Polyethylene glycol 4000 (PEG 4000) [65] Itraconazole Eudragit E100 [66] Efavirenz Polyethylene glycol8000, polyvinylpyrrolidone K30 [67] Thiocolchicoside (TCS) Poloxamer-188 [69] Piroxicam Solutol and Gelucire [70] Atorvastatin calcium, cefuroxime axetil, clotrimazole, ketoconazole and metronidazole benzoate Citric acid and sodium bicarbonate [71] Atorvastatin Polyvinyl pyrrolidone K30 (PVP), polyethylene glycol 6000 (PEG), Soluplus®, and chitosan [73] Carvedilol (CARV) Polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), Soluplus® and Eudragit® [74] Cefuroxime axetil (CA) Silica [77] Glyburide Silica [78] Bifendate Poly (ethylene oxide) (PEO) [79] Budesonide Polyethylene glycol 4000 and 6000 and [80] Cefixime trihydrate Soluplus [81] Furosemide Crospovidone [82] Co- precipitation method Quercetin (Que) HPMCAS-HF, HPMCAS-MF and HPMCAS-LF [83] Lumefantrine HydroxypropylmethylcellulosePhthalate (HPMCP), hydroxypropylmethylcellulose acetate succinate (HPMCAS), poly (methacrylic acid-ethyl acrylate) (EL100) and cellulose acetate phthalate (CAP) [86] Silymarin HPMC E 15LV [87] GDC-0810 Hydroxypropyl methylcellulose acetate succinate [88] Electrospinning Ibuprofen (IBU) HPMCAS and HPMCP-HP55 [92] Itraconazole (ITRA) PVPVA64 [93] Spironolactone Poly (vinylpyrrolidone-co-vinyl acetate) [94] Itraconazole [ITR] Polyvinylpyrrolidone-vinyl acetate [95] Meloxicam Eudragit E [98]
Interested in Advances In Amorphous Solid Dispersion Technologies: Spray drying?See the on-demand webinar!
Amorphous solid dispersions (ASDs) are regarded as one of the most promising techniques for poorly-soluble active pharmaceutical ingredients (API).超饱和状态下Assds热动不稳定很容易在水介质中解压Ritonavir(RTV)被选为评价溶性增强和内吸抑制的示范药 [.]
Der Beitrag
Amorphous solid dispersions (ASDs) are regarded as one of the most promising techniques for poorly-soluble active pharmaceutical ingredients (API).超饱和状态下ASD热动不稳定性很容易在水介质中反吸附 。
HPMCAS-HF/SLS组合过滤,通过溶剂蒸发法编程转盘固态散射RTV SD exhibited enhanced dissolution manner, while the oral bioavailability of RTV SD was equivalent with the Reference Standard Norvir® but increased significantly compared to the ternary physical mixture.
Thus, the ternary SD system might be promisingly employed as efficient drug delivery system for RTV, while the HPMCAS-HF/SLS combination could be recommended as effective excipient for fabricating steady solid dispersions loading poorly soluble API.
Article information: Qingran Guan, Qisan Ma, Yanna Zhao, Xinxin Jiang, Huaizhen Zhang, Min Liu, Zhengping Wang, Jun Han, Cellulose derivatives as effective recrystallization inhibitor for ternary ritonavir solid dispersions: in vitro-in vivo evaluation, Carbohydrate Polymers, 2021.https://doi.org/10.1016/j.carbpol.2021.118562.
Interested in amorphous solid dispersions?Don't miss our new webinar:
Der Beitrag Cellulose derivatives as effective recrystallization inhibitor for ternary ritonavir solid dispersions: in vitro-in vivo evaluation erschien zuerst auf Pharma Excipients.
Amorphous solid dispersion (ASD) dosage forms can improve the oral bioavailability of poorly water-soluble drugs, enabling the commercialization of new chemical entities and improving the efficacy and patient compliance of existing drugs.开发强效ASD剂量表可能具有挑战性,往往需要多重配法迭代、长时段和高成本.com/news/development-acalabrutib-sad-bablets/
Amorphous solid dispersion (ASD) dosage forms can improve the oral bioavailability of poorly water-soluble drugs, enabling the commercialization of new chemical entities and improving the efficacy and patient compliance of existing drugs.强效ASD剂量表开发可能具有挑战性,往往需要多重配法迭代、长时和高成本。
本研究描述精化体外和硅法开发ASD平板板HPMCAS-H和-M级聚合物在初始筛选研究中提供最长abrutinib超饱和度,HPMCAS-H级ACDs提供高气道分解测试曲线下最高体积面积 < 2简单化方法将关键药效、聚合物和肠子特性与试管并用硅工具消除acrutib-Adroisib-Solid-Diserion-Tables.pdf目标表示承诺减少开发ASD产品的时间和成本。
/ahrefsss/www.pharmaexbens.com/wp-cont/uploads/2021/08/In-Vitro-In-Silco-tools-f-Streed-development-Acalabrutib-Ad-Diser-Tables.pdfStewart 清晨罗莎莱斯 J.A亚当MS摩根MMvodak D.TVitro-InSilico工具简化Acalabrutib单片板开发, 药学 2021 , 13 1257https://doi.org/10.3390/pharmaceutics13081257Der Beitrag In Vitro-In Silico Tools for Streamlined Development of Acalabrutinib Amorphous Solid Dispersion Tablets erschien zuerst auf Pharma Excipients.
In this series of webinars we will discuss the latest developments in the fields of amorphous solid dispersion (ASD) focusing on Excipient Key Attributes linked to the most popular technologies: Hot Melt Extrusion (HME), Spray Drying and their Downstream Processing.9月22日,3pmCEST,9amESTREGTER这里喷雾广泛应用技术 [.]
derBeitrag In this series of webinars we will discuss the latest developments in the fields of amorphous solid dispersion (ASD) focusing on Excipient Key Attributes linked to the most popular technologies: Hot Melt Extrusion (HME), Spray Drying and their Downstream Processing. Spray drying is widely applied technology used in Amorphous Solid Dispersions (ASD).It is a single step process converting ASD solutions, based on the active ingredient, polymer and solvent, into powder for further processing in a dry form. Looking into the recent FDA approvals of ASDs, more than 60% of the drug products are formulated with HPMCAS (Developed by Shin-Etsu under the brand name Shin-Etsu AQOAT®) via spray drying technology. However, there is still a need of understanding the impact of the formulation and process parameters on the final ASD powder characteristics. Shin-Etsu, ProCepT and Xedev will present recent advances in spray drying. The objective of this web-seminar is to address: First presentation: Spray drying of amorphous solid dispersions (ASD): small scale screening of batches containing less than 50 mg API Speaker: Presentation abstract: As the number of new compounds with poorly water-soluble properties is continuously increasing, the use of amorphous solid dispersions (ASD) has become a common strategy to increase the bioavailability of the active pharmaceutical ingredient (API) during early drug development.然而,在早期药开发期间,有限量API(例如< 1g)可用ProCepT4M8-TriX喷雾干燥机为小批量(即小批量)进行ACD筛选提供了机会最小60-100mg固态因此,用有限量API,可评估选择聚合物与API组合成稳定不定矩阵的能力Current study illustrates the minimal required batch size on the ProCepT 4M8-TriX spray dryer in order to obtain sufficient material for solid state characterization and an indicative yield for a larger scale process. Speaker biography: Elien de Coninck, PhD: Elien obtained her doctoral degree in Pharmaceutical Sciences at Ghent University in 2020.在制药技术实验室中,她侧重于API/atty酸悬浮法:多片段使用表的创新药生产技术ProCepT/Xedev曾以博士生身份协作提升普法进程,Based on multiple customer projects executed since Xedev was founded in 2012, the Xedev Team became an expert in formulation and process development for ASDs via spray drying. Filip Van der Gucht: Filip Van der Gucht has a Master in Chemical Engineering BioTechnology and is CEO from ProCepT and Xedev.flip积累了25年手操作技巧 干燥、聚积化、混合和 Second presentation: Spray Drying Formulations with HPMCAS (Hypromellose Acetate Succinate) Speaker: Presentation abstract: HPMCAS (Shin-Etsu AQOAT®) is the most widely used excipient for spray drying solid dispersion formulation due to its unique properties of improving solubility, maintaining supersaturation, and good stability of the drug product.在这次演示中,我们调查中型喷雾干燥器中流程参数(喷雾气、固态富集和干温度)对基于HPMCAS的非态固散粉性效果speaker自传: shogoWarashina Der Beitrag Web-Seminar series: Advances In Amorphous Solid Dispersion Technologies: Spray drying erschien zuerst auf Pharma Excipients.Wednesday 22 September, 3pm CEST, 9am EST
Elien de Coninck, PhD, Project Manager @ Xedev & Filip Van der Gucht, CEO @ ProCepT/Xedev
Shogo Warashina, Technical Sales Manager @ Shin-Etsu
See the first webinar of the webinar series here: Hot Melt Extrusion
DerBeitrag
最大值DL研究的目的是调查药用化学结构与PVAa基础ACDsLOC关系受调查复合体共享常用脚架替换不同功能组,仅能生成氢联结,仅生成卤素联结,氢联结和卤素联结,或仅与聚合物非特异性交互X射线光电光谱学和红外光谱学研究并证实分子间交互作用。
药与聚合物间含氢联结的ASD LoCs较低值,而仅能形成卤素联结或与聚合物非特异性交互作用的复合物则高得多LOCs各种药-聚合物交互作用对ASD分解性能的影响突出,深入了解药-聚合物化学结构对LOS和ASD总体性能的作用。
/ahref='https://pubs.acs.org/doi/full/101021/acs.molpharmaceut.1c00419'津门诺夫清清奇安慕拉因杜尔卡、易高和GeoffZ级张和林恩泰勒Molecular Pharmaceutics. Article ASAP.DOI:10.1021/acs.molpharmaceut.1c00419Der Beitrag Impact of Drug–Polymer Intermolecular Interactions on Dissolution Performance of Copovidone-Based Amorphous Solid Dispersions erschien zuerst auf Pharma Excipients.
Among many methods to mitigate the solubility limitations of drug compounds, amorphous solid dispersion (ASD) is considered to be one of the most promising strategies to enhance the dissolution and bioavailability of poorly water-soluble drugs.口服吸药增强ASD主要归结为高可见药物溶解度 [.]
Der Beitrag Among many methods to mitigate the solubility limitations of drug compounds, amorphous solid dispersion (ASD) is considered to be one of the most promising strategies to enhance the dissolution and bioavailability of poorly water-soluble drugs.口服吸药增强ASD主要归结为高可见药物溶解性。 上个十年中,随着新知识和先进分析技术的应用,富药瞬态元化阶段常在ASD解析超饱和阶段中突出显示扩展药吸附和生物用量提高可归结于这种富药阶段的可变性论文中,我们检视(i)元富集药级形成和稳定背后的可能理论,重点是非经典核化fs/www.pharmaexsubjects.com/wp-content/uploads/2021/08/Drug-Rich-Slipse-Stella LJones D.S.安德鲁斯GP杜H天田Y药理学 药理学 2021 , 13 ,889https://doi.org/10.3390/pharmatutics1306089
The bioavailability of insoluble crystalline active pharmaceutical ingredients (APIs) can be enhanced by formulation as amorphous solid dispersions (ASDs).关键稳定因素之一是生成分子级的药-聚合物交互数组核磁共振实验
The bioavailability of insoluble crystalline active pharmaceutical ingredients (APIs) can be enhanced by formulation as amorphous solid dispersions (ASDs).关键稳定因素之一是生成分子级的药-聚合物交互多核多核磁共振实验用多种药加载时识别这些交互作用。
d低药加载 <20wt>,我们显示 1 HQsup>13 C跨空异核关联实验识别acsup>14 Nsup>1 Hexo核多量一致性实验hpserphen/HPMC-ASACDSD///www.pharmaexccepties.com/wp-content/uploads/2021/08/Drug-Pemer-In-In-Actimophen-Hydropylos-Acss.org/docente-Actuous-Solid-Diserations-Reveed-MHawarden和Frédéric BlancMolecular Pharmaceutics Article ASAP.DOI:10.1021/acs.molpharmaceut.1c00427
Der Beitrag Drug–Polymer Interactions in Acetaminophen/Hydroxypropylmethylcellulose Acetyl Succinate Amorphous Solid Dispersions Revealed by Multidimensional Multinuclear Solid-State NMR Spectroscopy erschien zuerst auf Pharma Excipients.
Solid dispersions (SDs) are one of the successfully applied methods to improve the solubility and dissolution rates of poorly water-soluble drugs.sds通常是API聚合系统,API分子分布于聚合矩阵中研究的目的是用不同技术准备自定义并用不同的聚合矩阵比较 [.]
DerBeitrag Solid dispersions (SDs) are one of the successfully applied methods to improve the solubility and dissolution rates of poorly water-soluble drugs.sds通常是API聚合系统,API分子分布于聚合矩阵中The objective of this study was to prepare SDs by different techniques and with different polymeric matrices and compare them with the physical mixtures in terms of dissolution properties. Preparation of solid dispersion with different polymers and by different techniques. Solid state characterization of prepared solid dispersions. Characterization of dissolution properties of solid dispersion – Wood's and flow-through cell dissolution. Prediction of flow-through cell dissolution behaviour according to the specific release rate based on Wood's dissolution. Tadalafil was used as a model poorly water-soluble drug, which was combined with hydrophilic polymers Kollidon® 12 PF, Kollidon® VA 64 and Soluplus®.结果显示,聚合物分子量增加后,水益聚合物在分解期间增聚更多次,反之,药物释放下降表示Kollidons的存在对加速tadalafil发布有正面效果,另一方面Solupluscience/abs/pii/S17732495084目标='blank'renoopener'https://doi.org/10.1016/j.jddst.2020.101518. Der Beitrag Preparation of solid dispersions with respect to the dissolution rate of active substance erschien zuerst auf Pharma Excipients.
Highlights
Find out more about parenteral excipients here:
This research demonstrates the influence of laser speed and the drug particle size on the manufacturing of amorphous solid dispersions (ASD) and dosage forms thereof using selective laser sintering 3-dimensional (3D) printing.单步制造ASD可能使用选择性激光交换三维打印过程,但ASD编译机制是 [.]
derBeitrag
This research demonstrates the influence of laser speed and the drug particle size on the manufacturing of amorphous solid dispersions (ASD) and dosage forms thereof using selective laser sintering 3-dimensional (3D) printing.单步制造asd使用选择激光三维打印过程是可能的,然而,通过此过程构建asd机制不完全理解,需要深入调查ASD生成机制是聚合载体中药物在选择激光交换过程扩散和分解,而药粒大小在生成ACDs中起着关键作用,因为交错过程没有混合作用。
Therein,Indomethacin使用为模型药并注入原料中(https//www.pharmaexemiders.com/product/kollidon-va-64/使用SLS3D打印过程处理这些原料时速度为50、75和100mm/s扫描特征测试和性能测试显示药原变换MANOVA和ANOVA分析显示激光速度和药粒大小严重影响药物表面溶解度和释放量。粒子大小对固态和性能3D打印assdsssssssssssssss.com/wp-content/uploadss2021/08/Impact-ofLaser-Speed-Drop-Sizive-Stering3DssssJaraM.O.斯温尼亚州皮拉伊AR马努兹扎曼激光速度和药粒子大小对选择激光定时3D打印非态固态分片。 药理学 2021 , 13 1149https://doi.org/10.3390/pharmaceutics13081149
Find out more about 3D printing in our 3D printing special here!
Der Beitrag Impact of Laser Speed and Drug Particle Size on Selective Laser Sintering 3D Printing of Amorphous Solid Dispersions erschien zuerst auf Pharma Excipients.
Amorphous solid dispersions can improve the solubility and dissolution rate of poorly soluble drugs.剩余晶体性可不利地影响配方设计不变状态的分解研究的目的是开发近红外光谱学/irs-redual-crystative-carbapie/
Amorphous solid dispersions can improve the solubility and dissolution rate of poorly soluble drugs.剩余晶体性可不利地影响配方设计不变状态的分解研究的目的是开发近红外光谱学(NIRS),作为一种潜在的实时线性方法检测残留晶度和carbamazepine多态数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组数组CBZ表二和表三分别出现在30%和50%CBZ溶解分解中,表一和表三混合检测出50%CBZ热熔压样本固态式CBZ均经X射线分片确认实验结果显示NIR能够检测剩余晶体CBZ并用光谱二分解CBZ表三Hoag应用近红外光谱检测卡马齐平剩余晶度-Solupluhttps://doi.org/10.1016/jdst.20211213.
Bead coating or fluid-bed coating serves as an auspicious solvent-based amorphous solid dispersion (ASD) manufacturing technique in respect of minimization of potential physical stability issues.溶剂选择对珠子涂层过程及其生成粒子配方的影响 据我们所知 从未调查本研究的目的为 [.]
DerBeitrag Bead coating or fluid-bed coating serves as an auspicious solvent-based amorphous solid dispersion (ASD) manufacturing technique in respect of minimization of potential physical stability issues.溶剂选择对珠子涂层过程及其生成粒子配方的影响据我们所知从未调查过。 本项研究因此旨在调查溶剂对珠子涂层过程本身的影响(即可制造性)和固态特征聚合物系统feldipses.com/product/kollidon-va-64/带珠子涂层的药检方法显示相似能力制造不同有机溶剂的高药载ASDs.
Find out more about povidones:
Der Beitrag Solvent influence on manufacturability, phase behaviour and morphology of amorphous solid dispersions prepared via bead coating erschien zuerst auf Pharma Excipients.
This work aimed to use hot-melt extrusion (HME) and dual fused deposition modeling (FDM) 3D printing technology to develop a novel intragastric floating and sustained-release drug delivery system.气态悬浮持久释放片片板使用HPMC 15LV为单片壳使用药用核心和多效酸 [.]
This work aimed to use hot-melt extrusion (HME) and dual fused deposition modeling (FDM) 3D printing technology to develop a novel intragastric floating and sustained-release drug delivery system.气相浮动持续释放片片板使用HPMCHME15LV/a3DMAX软件用于设计核心和补充外壳,内含顶部空格和底部释放药窗(半半半半数半数半数半数半数半数半数半数半数半数半数半解药窗医学特征分析 固分散评价 和药物释放行为研究模型药在所有配方中保持稳定,部分药在稀释丝片和3D印制片片变换引入空格将平板密度降低到0.9g/cm
Find out more about 3D printing in our 3D printing special here!
Der Beitrag 3D Printed Intragastric Floating and Sustained-release Tablets with Air Chambers erschien zuerst auf Pharma Excipients.
Fused deposition modelling-based 3D printing of pharmaceutical products is facing challenges like brittleness and printability of the drug-loaded hot-melt extruded filament feedstock and stabilization of the solid-state form of the drug in the final product.研究的目的是调查药载对可打印性和物理稳定性的影响ts/www.pharmaexsubjects.com/news/drug-load3d打印性/
Fused deposition modelling-based 3D printing of pharmaceutical products is facing challenges like brittleness and printability of the drug-loaded hot-melt extruded filament feedstock and stabilization of the solid-state form of the drug in the final product.研究的目的是调查药载对可打印性和物理稳定性的影响穷玻璃前环礁喷出量为10-30%
Find out more about 3D printing in our 3D printing special here!
Der Beitrag Influence of Drug Load on the Printability and Solid-State Properties of 3D-Printed Naproxen-Based Amorphous Solid Dispersion erschien zuerst auf Pharma Excipients.
In this work, we employed broad-band dielectric spectroscopy to determine the solubility limits of nimesulide in the Kollidon VA64 matrix at ambient and elevated pressure conditions.聚合物矩阵中药物的溶解性随压力增加而下降,分子动态控制反吸附过程s
BeitragIn this work, we employed broad-band dielectric spectroscopy to determine the solubility limits of nimesulide in the Kollidon VA64 matrix at ambient and elevated pressure conditions.聚合物矩阵中的药物溶解性随压力增加而下降,分子动态控制超饱和药-聚合物溶液超值内吸附过程Finally, based on the presented results, one can conclude that by transposing vertically the results obtained at elevated pressures, one can obtain the solubility limit values corresponding to low temperatures.
This approach was validated by the comparison of the experimentally determined points with the theoretically obtained values based on the Flory–Huggins theory.
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Article information: Krzysztof Chmiel, Justyna Knapik-Kowalczuk, Ewa Kamińska, Lidia Tajber, and Marian Paluch.Molecular Pharmaceutics, Article ASAP./strong>DOI:10.1021/acs.molpharmaceut1.0264
The purpose of this study was to use hydroxypropyl-β-cyclodextrin (HP-β-CD) as a novel carrier in solid SNEDDS and solid dispersions to enhance the solubility and oral bioavailability of poorly water-soluble dexibuprofen.新奇脱丁加固SNEDDS由脱丁加油、玉米油、聚索贝特80、CremophorityEL和HP-ET-CD组成,权比为45/35/50/15/100高亮hypropyyl-e-cyclodexrin uns
derBetragThe purpose of this study was to use hydroxypropyl-β-cyclodextrin (HP-β-CD) as a novel carrier in solid SNEDDS and solid dispersions to enhance the solubility and oral bioavailability of poorly water-soluble dexibuprofen.The novel dexibuprofen-loaded solid SNEDDS was composed of dexibuprofen, corn oil, polysorbate 80, Cremophor® EL, and HP-β-CD at a weight ratio of 45/35/50/15/100.
Highlights
Hydroxypropyl-β-cyclodextrin (HP-β-CD) was used as a novel carrier in solid SNEDDS and solid dispersions.
Solid SNEDDS was fabricated with corn oil, polysorbate 80, Cremophor® EL, and HP-β-CD.
Solid dispersion was prepared with HP-β-CD and polysorbate 80.
Solid SNEDDS considerably improved the bioavailability of dexibuprofen.
This solid SNEDDS spontaneously formed a nano-emulsion with a size of approximately 120 nm.不同于传统固态SNEDDS编译collid silica载运器,这种反exiboprofen加载固态SNEDDS展示球形结构类似用HP-D-CD制备的反exiprofen固体散射物,在固态SNEDS中观察到晶状药变异无分子交互作用。
与固态散射和反exiprofen粉末比较,固态SNEDS显著增强药溶解性AUCHP-ET-CD是SNEDS提高dexuprofen口服生物可用性的新潜在载体。Der Beitrag New potential application of hydroxypropyl-β-cyclodextrin in solid self-nanoemulsifying drug delivery system and solid dispersion erschien zuerst auf Pharma Excipients.