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In Vitro Drug Release Testing: Overview, Development and Validation01:10

In Vitro Drug Release Testing: Overview, Development and Validation

In vitro dissolution and drug release tests assess how quickly and how much of a drug is released from its dosage form into an aqueous medium under standardized laboratory conditions. These tests are essential tools in pharmaceutical development and quality assurance, offering insight into the drug's performance before clinical use.During formulation development, dissolution testing identifies incomplete or inconsistent drug release issues. It also supports decisions on selecting the optimal...
In Vitro Drug Dissolution: Compendial Testing Models I01:13

In Vitro Drug Dissolution: Compendial Testing Models I

Compendial dissolution methods are standardized procedures defined by pharmacopeias to evaluate the rate at which a drug dissolves in a specific medium. These methods ensure batch-to-batch consistency, enable quality control, and support the prediction of drug bioavailability. They are critical for both immediate and modified-release drug products.The apparatuses used for dissolution testing differ in their design and mechanical function, but all aim to simulate the physiological environment of...
Modified-Release Drug Delivery Systems: Rate-Programmed II01:19

Modified-Release Drug Delivery Systems: Rate-Programmed II

Rate-programmed drug delivery systems release drugs in a controlled manner to maintain therapeutic levels. Three main designs include reservoir, matrix, and hybrid systems.Reservoir systems consist of a drug core enclosed within a membrane that controls drug release. In non-swelling reservoir systems, polymers like ethyl cellulose or polymethacrylates are used. These do not hydrate in aqueous media and control release through membrane thickness, porosity, or insolubility. This type includes...
Modified-Release Drug Delivery Systems: Drug Release Characteristics01:22

Modified-Release Drug Delivery Systems: Drug Release Characteristics

Drug release from modified-release dosage forms is designed to achieve specific therapeutic effects by controlling the rate and extent of drug release. The classification of these drug release systems is based on key pharmacokinetic assumptions: drug disposition follows first-order kinetics, drug release is the rate-limiting step in absorption, and the released drug is rapidly and completely absorbed.There are four major models of drug release patterns. The first model is the slow zero-order...
Modified-Release Drug Delivery Systems: Rate-Programmed I01:22

Modified-Release Drug Delivery Systems: Rate-Programmed I

Rate-programmed drug delivery systems (DDS) are designed to release drugs at specific, controlled rates to maintain consistent therapeutic levels. These systems are categorized based on their release mechanisms, including dissolution-controlled DDS, diffusion-controlled DDS, and combined dissolution-diffusion-controlled DDS.In dissolution-controlled DDS, the release rate depends on the slow dissolution of the drug itself or the surrounding matrix. Drugs with inherently slow dissolution rates,...
Modified-Release Drug Delivery Systems: Stimuli-Activated01:30

Modified-Release Drug Delivery Systems: Stimuli-Activated

Stimuli-activated drug delivery systems are designed to release drugs in response to specific physical, chemical, or biological stimuli. These systems often utilize hydrogels—three-dimensional, hydrophilic polymer networks capable of swelling in aqueous environments and retaining significant fluid volumes. Upon exposure to particular stimuli, these hydrogels undergo structural transitions that allow the embedded drug to be released. Due to this adaptive behavior, such systems are also called...

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Updated: Jun 11, 2026

PLGA Nanoparticles Formed by Single- or Double-emulsion with Vitamin E-TPGS
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从基于PLGA的可生物降解植入物释放药物的机制模型用于体外释放测试:开发和验证.

Naresh Mittapelly1, Alexandre Djehizian1, Krishna Chaitanya Telaprolu1

  • 1Certara Predictive Technologies (CPT), Simcyp Division, Level 2-Acero, 1 Concourse Way, Sheffield S1 2BJ, U.K.

ACS applied bio materials
|October 18, 2024
PubMed
概括

一个新的机械模型通过分析关键质量属性和释放过程来预测聚甲基化物 (PLGA) 植入物中的药物释放. 该模型有助于优化PLGA配方设计,以有效地提供药物.

关键词:
基于PLGA的固体植入物.可生物降解的植入物.在体外释放测试试验 (in vitro release testing) 进行.长效注射剂 长效注射剂机械模型模型机械模型

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科学领域:

  • 聚合物科学和药物输送系统.
  • 生物材料和制药工程.

背景情况:

  • 药物从聚酸糖化物 (PLGA) 配方中的释放受众多因素的影响.
  • 了解这些因素是优化特定应用程序的药物释放配置文件的关键.

研究的目的:

  • 开发一种机械模型,用于预测基于PLGA的固体植入物中的*in vitro*药物释放.
  • 将关键质量属性 (CQA) 和关键释放机制纳入模型.

主要方法:

  • 开发了一种用于PLGA植入物*in vitro*药物释放的机制模型.
  • 该模型整合了聚合物水解,药物溶解,扩散和介质流入.
  • 使用四种不同药物的*体外*释放数据验证了该模型.

主要成果:

  • 该模型准确地解释了关键质量属性和释放率过程.
  • 经验证的模型成功预测了布塞雷林,阿法梅拉诺提德,布里莫尼丁和纳法雷林植入物的释放概况.
  • 证明了该模型在优化PLGA配方设计方面的潜力.

结论:

  • 开发的机械模型为PLGA植入物中药物释放动力学提供了宝贵的见解.
  • 将这种模型与PBPK建模相结合,可以预测*in vivo*性能,并支持生物等价性研究.