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使用PBPK建模和仿真对眼科药膏进行临床眼科暴露外推

Maxime Le Merdy¹, Ming-Liang Tan², Viera Lukacova³

¹Simulations Plus, Inc., PO Box 12317, Research Triangle Park, North Carolina, 27709, USA. maxime.lemerdy@simulations-plus.com.

The AAPS journal

|October 1, 2025

概括

基于眼部生理学上的药理动力学 (PBPK) 模型可以预测人眼中药物暴露. 这项研究验证了眼部PBPK模型的奥洛辛药膏,显示了眼科药物开发的准确的临床前到临床外推.

科学领域:

药理动力学和药物新陈代谢
眼部药物输送眼部药物输送
计算建模计算建模

背景情况:

通用眼科药物开发需要有效的生物等价性 (BE) 评估.
基于眼部生理学上的药理动力学 (PBPK) 模型提供了对眼睛组织内药物分布的非侵入性见解.
之前的工作验证了眼部PBPK模型,用于将子对溶液和悬浮剂的暴露转化为人类暴露.

研究的目的:

证明眼部PBPK模型对预测人类暴露于眼科药膏的有用性.
作为眼部PBPK建模的案例研究,提出ofloxacin (OFL) 膏.
评估眼部部位吸收和传输 (OCATTM) 模型对眼科膏的预测能力.

主要方法:

在GastroPlus®中使用OCATTM模型开发了用于OFL溶液和膏的眼部PBPK模型.
整合了OFL释放动力学,药膏应用时间,以及子眼睛的眼睛吸收/分布参数.
调整生理参数以模拟人类眼睛生理学和预测人类暴露.

主要成果:

OCATTM模型准确地描述了在子中观察到的水性幽默度,无论是OFL溶液还是药膏.
膏配方参数 (希古奇释放率,应用时间) 被调整为与子数据相匹配.
预测OFL溶液和膏的人类水性度处于观察值范围之内.

结论:

经过验证的眼部PBPK模型证明了ofloxacin药膏的临床前提取成功.
这种方法支持使用眼部PBPK模型来预测人类接触眼科膏的情况.
需要进一步的案例研究来确认这些发现对其他眼科膏产品的概括性.

关键词:

PBPKK PBPK 的意思是什么意思一个通用的通用.眼睛中的PBPKK.眼科膏眼科膏

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