Hot-melt extrusion has found extensive application as a feasible pharmaceutical technological option over recent years.HME应用包括溶性增强、口味掩码和持续释放毒品生物可用性增强是当今科学热题,HME的主要应用之一是非静态固态分布t-mel-Expression/
Hot-melt extrusion has found extensive application as a feasible pharmaceutical technological option over recent years.HME应用包括溶性增强、口味掩码和持续释放毒品生物可用性增强是当今科学热题,HME主要应用之一是非态固态散射量。
本审查描述HME技术最重要的方面及其用于准备固态散射量,作为提高易溶性药物溶性的一种药方配制策略springer.com/article/10108/s12249-021-7#citeas目标='blank'rel=nopener'Simosss热-MeltExpressive:产品开发路径图aspsPharmScitech 22, 184(2021年)。https://doi.org/10.1208/s12249-021-02017-7
See the new webinar about HME and ASD here:
Der Beitrag Hot-Melt Extrusion: a Roadmap for Product Development erschien zuerst auf Pharma Excipients.
Hypothesis Colloidal aggregation phenomena have been found responsible for the supersaturation of poorly water-soluble drugs, potentially leading to bioavailability enhancements.与粗沉淀物不同,相位分离卷状物预期会提高药超饱和性能因此,高比例类联应该与超饱和度和动能相关ts/www.pharmaexsubjects.com/news/
Hypothesis
Colloidal aggregation phenomena have been found responsible for the supersaturation of poorly water-soluble drugs, potentially leading to bioavailability enhancements.与粗沉淀物不同,相位分离卷状物预期会提高药超饱和性能因此,高比例类联应该与超饱和度和动能相关当前研究的首要目标是提供模型albendazole超饱和性与12个聚合物结合的机智理解。
The oral bioavailability of curcumin is limited, attributed to its low solubility or dissolution and poor absorption.Gelucise48/16和TPGS混合小鼠配方提高分解率Curcumin散落于这些熔脂表面作用物中,这些表面作用物随后被载体吸附并编译成粒子 [.]
Beitrag
The oral bioavailability of curcumin is limited, attributed to its low solubility or dissolution and poor absorption.s/www.pharmaexsubjects.com/product/gelcire-48-16/曲曲宁散落于这些熔脂表面活性剂中,然后吸附到载波上,通过分解分解成粒子临界小鼠富集度/mcrocrystaleulose表单湿质并阻抗从粒子释放crubin可溶水稀释剂增加释放优化配方释放超过90%的药 并保持超饱和水平混合小鼠系统对曲南有效交付系统,而粒子配方则由半固脂组成趣味配方策略springer.com/article/10.1208/s12249-021-02032-8和Amin,P.DGelucire /sup>48/16和TPG混合Mielles及其用Excrien化技术编译解析率crubinhttps://doi.org/1208/s12249-0232-8/plllexY4宽度='bs-divider全小'/ptlipse='text-ali
A deep eutectic solvent (DES) is a eutectic system consisting of hydrogen bond donor and acceptor has been suggested as a promising formulation strategy for poorly soluble drugs.aDES由1:2摩尔比值中的coline氯化酸和leulica酸组成,用于拟出模型药原生液解s/www.pharmaexsubjects.com/news/formations-aprient-deep-eutctics/
A deep eutectic solvent (DES) is a eutectic system consisting of hydrogen bond donor and acceptor has been suggested as a promising formulation strategy for poorly soluble drugs.由1:2摩尔比值中氯化物和悬浮酸组成的DES设计模型药液解法。
该配方测试 invitro (药释放和渗透性)和sem>invivo (鼠标模型),并比对不定浸泡物性能和商业缓冲纳米晶体配方研究中首次直接将DES配方与其他既定赋能配方作比较invitro 药物发布研究表明DES配方和无变表都能够诱导显性超饱和继而下药降水为了减少降水风险,HPCC预先解析解析介质,成功减降水量与发布研究结果一致, 体外 渗透研究显示,与纳米晶体配方相比,DES配方和无变式表单对药有较高渗透性。
However无法直接转换为鼠性能提高 vivo 与Namcrystal配方DES配方(34+++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++++Eriksen、Annette Bauer-Brandl、Jukka Rantanen、Korbinian Löbmann赋能配方:体外和体外对比纳米晶素、无态深度电解素基础配方,国际药理学杂志X卷32021https://doi.org/10.1016/j.jpx.2021100083.
Der Betrag
Amorphous solid dispersions (ASDs) are popular for enhancing the solubility and bioavailability of poorly water-soluble drugs.使用各种方法制作asds并出现新手法本审查更新概述制作asds技术物理稳定性是ASD关键质量属性,配方效果 [.]
DerBeitrag Amorphous solid dispersions (ASDs) are popular for enhancing the solubility and bioavailability of poorly water-soluble drugs.使用各种方法制作asds并出现新手法本审查更新概述制作asds技术物理稳定性是ASD关键质量属性,已讨论了配方、设备及流程变量的影响,并讨论了下游处理对ASD物理稳定性的影响。选择策略建议确定合适的制造方法,这些方法可能有助于开发满足物理稳定性a/p/struct/dowload全文本 : Commonly used polymers for ASD preparation
Polymer Tg(°C) Solubility in solvents Hydroxypropyl methylcellulose 175‒185 Water, ethanol:dichloromethane (1:1, 2:1), methyl acetate:methanol (1:1) Hydroxypropyl methylcellulose acetate succinate 100‒110 Caustic water, acetone, methanol, dichloromethane, chloroform Hydroxypropyl methylcellulose phthalate 133‒137 Water, acetone, ethyl acetate, methyl ethyl ketone, ethanol:dichloromethane (1:1) methanol, dichloromethane, tetrahydrofuran Polyvinylpyrrolidone 175‒180 Water, acetone, ethanol, methanol, ethyl acetate, methyl ethyl ketone, dichloromethane, tetrahydrofuran Polyvinylpyrrolidone/vinyl acetate 70‒110 Water, acetone, ethanol, methanol, ethyl acetate, methyl ethyl ketone, dichloromethane, tetrahydrofuran Polymethacrylates derivatives (Eudragit®-L100, S100) >150 Water (only L100), acetone, ethanol, methanol, ethanol:dichloromethane (1:1) Cellulose acetate phthalate 160‒170 Acetone, ethyl acetate, methyl ethyl ketone Soluplus® 72 water, acetone, ethanol, methanol, dichloromethane
Source: Pharmaceutical amorphous solid dispersion: A review of manufacturing strategies
Conclusions
A successful development of amorphous solid dispersion formulations depends on three primary factors: active pharmaceutical ingredient properties, stabilizing polymer, and processing technology.聚合物为稳定药态化提供基础和基本基础,过程提供将系统变换成非态式所需的能量进程有效性对生成、捕捉和保存无变形式至关紧要成功这些过程取决于处理时间和超饱和条件形成固化散射时产生。
尽管在1960年代初发现固化散射,但用固化散射概念解决溶解挑战数十年来一直有限,部分原因是缺乏商业上可行的处理技术。然而,过去20年在开发药用ASD产品方面取得了显著进展,因为我们对ASD系统及其制造技术的理解有了相当大的发展,除开发数项产品外,还产生数项商业产品。喷雾干燥和HME成为制药行业ASD准备的主体,而更新方法则不断添加到工具箱中,保证提高产品质量、生产率和/或提高性能。
DerBeitrag
Chrysin (CHR), a flavone found in multiple vegetables, fruits and mushrooms has been explored so far as a neurotropic, anti-inflammatory and anti-cancer biomolecule.低溶性生物用量限制其治疗益为了避免这些缺陷,本调查报告Chrysin唇片开发CLPs开发 [.]
DerBeitrag Chrysin (CHR), a flavone found in multiple vegetables, fruits and mushrooms has been explored so far as a neurotropic, anti-inflammatory and anti-cancer biomolecule.低溶性生物用量限制其治疗益为了避免这些缺陷,本调查报告Chrysin脂质开发。
Der Beitrag Electrostatic deposition assisted preparation, characterization and evaluation of chrysin liposomes for breast cancer treatment erschien zuerst auf Pharma Excipients.
Atorvastatin (ATV) is a poorly water-soluble drug that exhibits poor oral bioavailability.因此,当前研究设计开发ATV固态分布系统,提高溶性、药物释放和口服生物可用性ATV各种自定义用传统和微波驱动熔化法编译s/news/gruci-solids-discriptions-atorvasta-calcium/
Atorvastatin (ATV) is a poorly water-soluble drug that exhibits poor oral bioavailability.因此,当前研究设计开发ATV固态分布系统,提高溶性、药物释放和口服生物可用性ahref=s/www.pharmaex接受者.com/product/gelucire-48-16/配制自定义特征描述不同物理化学特征描述、释放药和口服生物可用性研究不同物理化学特征分析结果显示ATV在各种SD中的分子分布。
溶性(1.95-9.32折叠)明显增强,ATV编译自定义比纯ATV药内容检测范围为96.19%+2.14%至98.34%+1.32%药发布结果显示ATV编译自自定义比纯药和市场牌子大增配方F8显示高分解性能(%DEsub>30 值80.65++3.05)ACU < sub>0-t < 559.95+623.3ng/hmlAUC 0-t 573.94+398.9ng/hml4837.4 ± 174.7 ng/h ml).springer.com/article/10.1208/s1221-02019-5https://doi.org/1208/s12249-0215
Der BeitragDerBeitrag
Crystallinity in an amorphous solid dispersion (ASD) may negatively impact dissolution performance by causing lost solubility advantage and/or seeding crystal growth leading to desupersaturation.研究的目标是评价Biculamide/Polyvinil-crystality内残留晶体化生成ASDss
Crystallinity in an amorphous solid dispersion (ASD) may negatively impact dissolution performance by causing lost solubility advantage and/or seeding crystal growth leading to desupersaturation.研究的目的是评价Bicalutamide/Polyvinyrli内射光谱学、极分光显微镜学和扫描电子显微镜学用来描述晶体动能和机制特征完全不动asd(0%晶度)不完全分解并结晶化为元可变多态(2形)非沉入条件下实现更高程度超饱和度,因为核分离前初始解密畅通性 。
ACSD内含剩余晶性显著降低超饱和度固介晶化(矩阵结晶化)耗尽非态固态,生长稳定多态水槽条件下完全不动asd和晶体混合比含剩余晶性assds快速释放后一系统矩阵结晶化导出高聚化晶体并具有高相对面积求解介晶化不是集中损耗的重要驱动力,因为当PVA出现求解时晶化增速慢BCL/PVAACDs残留晶化高风险来源于(1)晶子快速矩阵晶化传播和(2)稳定晶形生长这项研究对含残留晶性ASD性能分解有影响springer.com/article/10.1208/s12248-021-00598-6i>APSJ 23 23> 69>2021https://doi.org/10.1208/s12248-021-00598-6
Der Beitrag Amorphous Solid Dispersions Containing Residual Crystallinity: Competition Between Dissolution and Matrix Crystallization erschien zuerst auf Pharma Excipients.
Kollicoat® Smartseal (Methyl methacrylate and diethylaminoethyl methacrylate copolymer dispersion) which is used for taste masking and moisture protection, has shown the ability for forming solid dispersion.本研究旨在比照高熔点模型Itraconahrefs/www.pharmaexccepties.com/news/carrier-biopity-itraconazole/
Kollicoat® Smartseal (Methyl methacrylate and diethylaminoethyl methacrylate copolymer dispersion) which is used for taste masking and moisture protection, has shown the ability for forming solid dispersion.本研究旨在比照高熔点像Itraconazole模型研究in-vihrefs/www.pharmaex接收者.com/hot-melt-extrusi因此,拥有承运人可解决所有这些问题,将使业界为开发配方多选承运人。因此,作者试图解决这一问题并证明小承运人开发HME技术的能力Itraconadole固态散射编译、标注并测试大鼠的in-vivo 性能结果表明载波温度范围为120°C-220°C,行为良好Itraconazole对载波产生整形效果invitro 结果显示20倍溶性高于平面itraconazole.
hrefs/s/www.pharmaexsubjects.com/product/kolicoat-smartsal-30-d/science/abs/pi探索新载体提高Itraconazole生物可用性:热熔扩展固化分布https://doi.org/10.1016/j.jddst.2021.102541.
Der Beitrag Exploring novel carrier for improving bioavailability of Itraconazole: Solid dispersion through hot-melt extrusion erschien zuerst auf Pharma Excipients.
The endogenous molecule, S-adenosyl-L-methionine (SAMe) is a key factor due to its role in the methylation cycle and modulation of monoaminergic neurotransmission.多位精神失常与单亚胺基系统相关联,因此SAMe血液和脑膜流体水平对大萧条治疗很重要固脂纳米粒子 [...]
>Der BeitragThe endogenous molecule, S-adenosyl-L-methionine (SAMe) is a key factor due to its role in the methylation cycle and modulation of monoaminergic neurotransmission.多位精神失常与单亚胺基系统相关联,因此SAMe血液和脑膜流体水平对大萧条治疗很重要在这次研究中,为增加SAMe有限口服生物可用性准备了固态脂质粒子,SLN基纳米复合粒子(SAME-SLN-NC)利用进化聚合物对肠膜系统作被动选择得到进一步发展In this manner, it was also aimed to protect SAMe loaded SLN from harsh gastric environment as well as hepatic first-pass metabolism.
Highlights
To increase the oral bioavailability of SAMe, a naturally occurring molecule which has crucial role in many biochemical pathways, for depression treatment.
To obtain SLN nanocomposite particles using enteric polymers to protect SAMe loaded SLN from the gastric environment.
To improve intestinal SAMe permeability via passively targeted lipid-based drug carrier systems.
Dynamic light scattering (DLS) analysis of SLN was performed, drug content was measured, SAMe release patterns were examined and the permeation ability of SAMe was investigated by the Parallel Artificial Membrane Permeability Assay (PAMPA) to characterize SAMe loaded SLN formulation.PAMPA结果显示SAME-SLN平均粒度242纳米显示SAME渗透性比纯药强SLN纳米复合粒子获取延迟释放毒品表示保护酸气介质中装药SLNSAME溶液或粒子悬浮用0.45(w/v)hyprosyme药代参数显示,口服SLN配方后SAMe相对生物可用性提高归结于通过淋巴路径完全吸收脂质矩阵sup>d/sup>和2sup>d/sup>和4sup>s/sup提高S-Adenosyl-L-Methionine口服生物可用性研究:SLN和SLNNNhttps://doi.org/10.1016/j.chemphyslip.20211086.
Der Beitrag
Apremilast (APST) is an effective inhibitor of phosphodieasterase 4 (PDE4) which is the first oral drug for the treatment of adult patients with active psoriatic arthritis.Aprimilist低溶性限制它分解和生物可用性arefs/www.pharmaexsubjects.com/Pharma
Apremilast (APST) is an effective inhibitor of phosphodieasterase 4 (PDE4) which is the first oral drug for the treatment of adult patients with active psoriatic arthritis.Aprimilast 低溶性限制分解和生物使用研究开发APST固散d-a-tocoX-RPD、差分扫描卡路里和Fleier变红外线分光测量用法描述固差特征,结果显示APST固差变异性 。 Invitro 分解研究表明磷酸缓冲saline固差分解率显著提高,在10分钟内释放90%
Moreover, ivo C max 和AUC Last 分别比APST表B高近22倍和12.9倍APST固散TPGS和PVA是一个替代药提供系统,提高APST溶性和口服生物可用性。 ahref='https://link.springer.com/article/10.1208/s12249-021-x'目标shttps://doi.org/10.1208/s12249-021-02005-xMore about Vitamin E TPGS:
Der Beitrag Development of Apremilast Solid Dispersion Using TPGS and PVPVA with Enhanced Solubility and Bioavailability erschien zuerst auf Pharma Excipients.
Kollicoat® Smartseal (Methyl methacrylate and diethylaminoethyl methacrylate copolymer dispersion) which is used for taste masking and moisture protection, has shown the ability for forming solid dispersion.本研究旨在比照高熔点模型ItraconatoHME热熔化极强 [.]
Der Betrag
Kollicoat® Smartseal (Methyl methacrylate and diethylaminoethyl methacrylate copolymer dispersion) which is used for taste masking and moisture protection, has shown the ability for forming solid dispersion.本研究旨在比照高熔点像Itraconatole模型研究in-vi热熔放大法(HME)是商业上非常接受的提高溶性技术。
然而,有有限聚合物可用,原因是处理窗口狭窄、温和行为低或稳定成形固散因此,拥有承运人可解决所有这些问题,将使业界在开发配方时对承运人作更多选择。因此,作者试图解决这一问题并证明小承运人开发HME技术的能力Itraconadole固态散射编译、标注并测试大鼠的in-vivo 性能结果表明载波温度介于120至220摄氏度之间显示良好的热塑行为Itraconazole对载波产生整形效果in-vitro 结果显示近似溶性提高20折叠平面Itraconazole.
热分析结果KollicatSmartseal显示高载波高可溶性增强Itraconascience/abs/pi探索新载波提高Itraconazole生物可用性固态分布热熔化,药送科技杂志,2021年https://doi.org/10.1016/j.jddst.2021.102541.Der Beitrag Exploring novel carrier for improving bioavailability of Itraconazole!s/schienzufta
The objective of this study was to fabricate a novel drug delivery system using Soluplus® (polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer) and glycyrrhizic acid to improve solubility, bioavailability, and anti-hyperuricemic activity of aloe emodin (AE).AE加载混合小鼠(AE-M)用薄膜水分法编译最优AE-M粒子小尺寸数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数度数分数
The objective of this study was to fabricate a novel drug delivery system using Soluplus® (polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer) and glycyrrhizic acid to improve solubility, bioavailability, and anti-hyperuricemic activity of aloe emodin (AE).AE加载混合小鼠(AE-M)用薄膜水分法编译最优AE-M含有小尺寸粒子(30.13+1.34Nm)高封装效率(m/m,%)90.3+1.08%.
磷酸缓冲解法pH7.4磷酸缓冲解法pH6.8盐酸水解法pH 1.2与免费AE相比,AE-M药效研究显示,相对口服生物利用率提高3.09倍,表明混合小鼠可促进胃肠吸收更重要的是,AE-M通过抑制模型鼠XOD活性有效减少urec酸水平。 脚踝肿化程度,Interleukin-1和IL-6相关炎因子水平均下降AE-M合起来展示了提高AE生物可用性、抗膜活度和反点火的潜力:slink.sprinanger.com/article/10.1007/sl3346-021-00969-8translRes. (2021).https://doi.org/10.1007/s1336-021-0096-8 Der Betrag
The current study deals with formulation and evaluation of nateglinide solid dispersion (SD) incorporate into tablet formulation for controlled release of the drug.方法:NateglinideSD使用crospovidone编译并评价药含量和药分解优化自定义配方用HPCCK100和Cederela口香糖嵌入平板理表板配方都
DerBeitrag
The current study deals with formulation and evaluation of nateglinide solid dispersion (SD) incorporate into tablet formulation for controlled release of the drug.
Methods: The nateglinide SD prepared using crospovidone and evaluated for drug content and drug dissolution.优化自定义配方用HPCCK100和Cederela口香糖嵌入平板所有片状配方评为压缩前、压缩后、药分解和前受体兼容性研究。
Conclusion: The combination of SD and application of hydrophilic and hydrophobic polymers in matrix formation facilitated superior dissolution and absorption profile with greater patient compliance.
Sunitha, et al.: Development, characterization of nateglinide SD, and incorporation into tablet formulation for controlled release of drug – Asian Journal of Pharmaceutics • Jan-Mar 2021 • 15 (1) | 122 – Download full article here: Design, Development, and Evaluation of Controlled Release Tablets of Nateglinide Solid Dispersions
MATERIALS AND METHODS
The drug nateglinide, HPMC K 4M, HPMC K 15M, HPMC K 100M, and crospovidone were gifted from Hetero drugs Ltd, Hyderabad.The excipients Soluplus, Kolliphor ELP, and Kolliphor RH40 were purchased from Gattefosse, Mumbai.Lactose,talcsylpriodone (/div>