Analysis of the state of water in semisolid formulations using MRIand its contribution to the formulation stability

使用 MRI 分析半固体制剂中的水状态及其对制剂稳定性的贡献

• 批准号: 23790057
• 负责人: ONUKI Yoshinori
• 金额: $ 1.5万
• 依托单位: Hoshi University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Young Scientists (B)
• 财政年份: 2011
• 资助国家: 日本
• 起止时间: 2011 至 2013
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-23790057/
• 关键词: MRI; 製剤安定性; エマルション製剤; クリーム剤; ADC マップ; 相分離; 非破壊的モニタリング; ADCマップ; 非侵襲的モニタリング; 油水分散系; 相分離挙動

A nondestructive method for monitoring creaming of emulsion-based formulations is in great demand because it allows us to understand fully their instability mechanisms. This study was aimed at demonstrating the usefulness of magnetic resonance (MR) techniques, including magnetic resonance imaging (MRI) and MR spectroscopy, for evaluating the physicochemical stability of emulsion-based formulations. Emulsions that are applicable as the base of practical skin creams were used as test samples. The creaming oil droplet layer and aqueous phase were clearly distinguished by quantitative MRI by measuring T1 and the apparent diffusion coefficient. Components in a selected volume in the emulsions could be analyzed using MR spectroscopy. Then, model emulsions having different hydrophilic-lipophilic balance (HLB) values were tested, and the optimal HLB value for a stable dispersion was determined. In addition, the MRI examination enables the detection of creaming occurring in a polyethylene tube, which is commonly used for commercial products, without losing any image quality. These findings strongly indicate that MR techniques are powerful tools to evaluate the physicochemical stability of emulsion-based formulations. This study will make a great contribution to the development and quality control of emulsion-based formulations.

人们非常需要一种用于监测乳液配方乳化的非破坏性方法，因为它使我们能够充分了解其不稳定机制。本研究旨在证明磁共振 (MR) 技术（包括磁共振成像 (MRI) 和 MR 光谱）在评估乳剂配方的物理化学稳定性方面的有用性。可用作实用护肤霜基础的乳液被用作测试样品。通过测量 T1 和表观扩散系数，通过定量 MRI 清楚地区分乳化油滴层和水相。可以使用磁共振波谱分析乳液中选定体积的成分。然后，测试具有不同亲水亲油平衡（HLB）值的模型乳液，并确定稳定分散体的最佳HLB值。此外，MRI 检查可以检测商业产品中常用的聚乙烯管中发生的乳化现象，而不会损失任何图像质量。这些发现有力地表明，MR 技术是评估乳液配方物理化学稳定性的有力工具。这项研究将对乳液制剂的开发和质量控制做出巨大贡献。

项目成果

Nondestructive monitoring of creaming of oil-in-water emulsion-based formulations using magnetic resonance imaging

使用磁共振成像对水包油乳液配方的乳化进行无损监测

• 发表时间: 2013
• 作者: Onuki; Y.; Horita; A.; Kuribayashi; H.; Okuno; Y.; Obata; Y.; Takayama; K.
• 通讯作者: K.

Relationship between diffusivity of water molecules inside hydrating tablets and their drug release behavior elucidated by magnetic resonance imaging

磁共振成像阐明补水片内水分子扩散性与其药物释放行为之间的关系

• 发表时间: 2012
• 作者: Kikuchi; S.; Onuki; Y.; Kuribayashi; H.; Takayama; K.
• 通讯作者: K.

イブプロフェン固体分散体製剤の調製と評価

布洛芬固体分散体制剂的制备及评价

• 发表时间: 2013
• 作者: 乙黒沙織;林祥弘;大貫義則;小幡誉子;高山幸三
• 通讯作者: 高山幸三

Latent structure analysis of the process variables and pharmaceutical responses of an orally disintegrating tablet

口腔崩解片的工艺变量和药物反应的潜在结构分析

• 发表时间: 2012
• 作者: Hayashi; Y.; Oshima; E.; Maeda; J.; Onuki; Y.; Obata; Y.; Takayama; K.
• 通讯作者: K.

MRIによる水分子可視化技術を利用した外用剤基剤用ヒドロゲルの物性評価

利用MRI水分子可视化技术评价外用水凝胶的物理性质

• 发表时间: 2013
• 作者: 白井郁佳;大貫義則;西川昌人;小幡誉子;髙山幸三
• 通讯作者: 髙山幸三