干燥方法对Canagliflozin纳米晶体的再分散性和溶解的影响:一种比较方法
Yagmur Pirincci Tok1,2,3, Burcu Demiralp2, Sevgi Güngör2
1Department of Pharmaceutical Technology, Faculty of Pharmacy, İstanbul Health and Technology University, İstanbul 34275, Türkiye.
Pharmaceuticals (Basel, Switzerland)
|February 27, 2026
概括
开发固体卡纳格利弗洛辛纳米晶体 (CFZ-NCs) 改善了口服药物输送. 喷雾干燥增强了CFZ-NC的再分散性和药片溶解,为这种SGLT-2抑制剂提供了一种有前途的方法.
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
- 纳米技术纳米技术
背景情况:
- 卡纳格里弗洛辛 (CFZ) 是一种糖共运输体2 (SGLT-2) 抑制剂,具有较差的水溶性和透性,限制了口服生物可用性.
- 将CFZ纳米悬浮转化为固体纳米晶体 (CFZ-NCs) 的目的是提高物理稳定性,并使平板电脑配方成为可能.
- 解决低口服生物可用性对于有效的SGLT-2抑制剂治疗至关重要.
研究的目的:
- 从纳米悬浮中开发CFZ纳米晶体 (CFZ-NCs) 的稳定固体形式.
- 为了将CFZ-NCs配制成一个带有改进的再分散性和溶解性的片剂形式.
- 评估开发的纳米晶片片的稳定性和体外性能.
主要方法:
- 使用流体床颗粒和喷雾干燥技术,以实现干燥的CFZ-NCs的适当再分散性.
- 研究了喷雾干燥的关键过程参数,以优化CFZ-NC的重新分散性.
- 喷雾干燥纳米晶片 (NCs-SD-TAB) 的稳定性在各种存储条件下 (25°C/60%RH和40°C/75%RH) 进行了三个月的评估.
主要成果:
- 喷雾干燥为CFZ-NCs提供了最高的再分散性指数 (94%).
- 与对照片和市场上销售的产品相比,NCs-SD-TAB在体外溶解率显著更高.
- 在模拟的胃肠道pH条件下,观察到NCs-SD-TAB的药物释放在15分钟后增加了三倍.
结论:
- 纳米晶体技术是提高卡纳格利弗洛辛可溶性和口服输送的有希望的策略.
- 喷雾干燥是一种有效的方法,用于生产适合用于片剂配方的可重新分散的CFZ纳米晶体.
- 开发的NCs-SD-TAB提供了更好的溶解性能,可能会提高治疗效率.
相关概念视频
Factors Affecting Dissolution: Particle Size and Effective Surface Area
1.8K
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
1.8K
Factors Influencing Drug Absorption: Pharmaceutical Parameters
664
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...
664
In Vitro Drug Dissolution: Alternative Methods
291
Alternative drug dissolution methods include the rotating bottle, intrinsic dissolution test, peristalsis, and the Franz diffusion cell method. The rotating bottle method involves meticulously rotating tightly capped controlled-release beads in a temperature-controlled bath. Periodic decanting of samples allows for residue assay, followed by refilling with fresh medium and testing at various pH levels to emulate the gastrointestinal tract conditions.In contrast, the intrinsic dissolution test...
291
Drug Dissolution: Requirements and Profile Comparison
340
The acceptance criteria for dissolution profile data are anchored in Q values, representing the percentage of drug dissolved within a specified period. This assessment unfolds in three stages:First Stage: The test passes if all six drug dosage units are equal to or greater than Q plus 5%; otherwise, the sample proceeds to the second stage.Second Stage: The average of twelve units must be equal to or greater than Q, with no unit falling below Q - 15% to pass; if not, it progresses to the final...
340
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
791
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
791
Bioavailability Enhancement: Drug Solubility Enhancement
345
Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
345


