直接压缩片:洞察透增强剂可加工性和稳定性的重要性
A Fagan1, L M Bateman2, M O'Mahony3
1SSPC, Taighde Éireann - Research Ireland Centre for Pharmaceuticals, School of Pharmacy, University College Cork, Cork T12 YT20, Ireland.
International journal of pharmaceutics
|October 11, 2025
概括
通过透增强剂甲酸盐 (C10) 和盐酸盐 (SNAC) 直接压缩胰岛素是可行的. 含有辅助剂的配方在压缩和储存过程中提高了可制造性和增强了胰岛素稳定性.
科学领域:
- 制药技术 制药技术 制药技术
- 药物输送系统 药物输送系统
- 生物制药生物制药公司
背景情况:
- 口服交付面临挑战,通常由化学透增强剂如甲酸盐 (C10) 和盐酸盐 (SNAC) 解决.
- 与增强剂共同配制酸具有需要进一步研究的加工和配制障碍.
研究的目的:
- 研究使用C10和SNAC作为模型透增强剂的直接压缩胰岛素紧剂的合理开发.
- 评估C10和SNAC的物理和机械性能,以确定它们是否适合直接压缩.
- 为了评估在这些配方中压缩和储存期间的胰岛素稳定性.
主要方法:
- 评估了C10和SNAC的物理和机械性能.
- 加入微晶纤维素 (MCC) 和聚烯 (PVP) K30以改善紧缩.
- 在不同压力 (100和200MPa) 上制定和生产直接压缩胰岛素紧剂.
- 在加速条件下评估药物释放,物理稳定性 (展开,聚合) 和化学稳定性 (除氧化,聚合).
主要成果:
- C10表现得很差,而SNAC的流量很差,但压缩性优越.
- 添加辅助剂 (MCC,PVP) 改善了两种增强剂的紧缩特性.
- 胰岛素紧剂在30分钟内完全释放,不受压缩压力的影响.
- 胰岛素在机械应力下表现出极好的物理稳定性,并在配方和储存时减少了除化/聚合.
结论:
- 用C10或SNAC直接压缩胰岛素可以通过适当的辅助剂实现.
- 配方显著提高了胰岛素在加工和储存期间的可制造性和稳定性.
- 这项研究为优化口服直接压缩配方提供了洞察力.
相关概念视频
Factors Influencing Drug Absorption: Pharmaceutical Parameters
402
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
402
Bioavailability Enhancement: Drug Permeability Enhancement
186
Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
186
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
196
Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
196
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
500
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
500
Formulation and Manufacturing Process: Physical Attributes of Generic Tablets and Capsules
306
Bioequivalence in generic drugs, such as tablets and capsules, refers to their pharmaceutical equivalence to the brand-name counterparts. However, for therapeutic equivalence, manufacturers must also consider physical attributes like size, shape, and weight (FDA Guidance for Industry, December 2003). Discrepancies in these aspects could impact patient compliance and cause medication errors. For instance, swallowing difficulties, often experienced with larger tablets or capsules, can lead to...
306
Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
149
Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
149


