开发和评估基于固体分散的尼索尔迪平因子语言膜
Yahya Alhamhoom1, Abhay Sharma2, Shivakumar Hagalavadi Nanjappa2
1Department of Pharmaceutics, College of Pharmacy, King Khalid University, Al Faraa, Abha 62223, Saudi Arabia.
Pharmaceuticals (Basel, Switzerland)
|November 25, 2023
概括
这项研究开发了Nisoldipine (NIS) 语言下膜,使用固体分散来克服生物可用性差. 这些新片显著改善了NIS的溶解,并为口服提供了有前途的替代品.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
背景情况:
- 尼索尔迪平 (NIS) 是一种通道阻塞剂,由于水溶性差和广泛的系统前代谢,其生物利用率低 (约为5%).
- 目前的口服配方在有效地将NIS输送到系统循环中面临着挑战.
研究的目的:
- 开发基于尼索尔迪平固体分散 (NISSD) 的子语言膜,以增强NIS溶解和生物可用性.
- 为了研究潜力下语言交付绕过肠道新陈代谢和改善治疗结果.
主要方法:
- 阶段溶解性研究发现Soluplus®是NIS的最佳载体.
- 使用溶剂蒸发制备了NIS固体分散剂 (NISSDs).
- 生物粘合性舌下膜是通过使用HPMC E5,HPMC E15和HEC EF聚合物与PEG 400作为可塑剂的溶剂造制成的.
主要成果:
- 福利埃变换红外光谱学证实了NIS在NISSDs中的化学完整性.
- 优化的舌下膜 (NISSD含有2%的HPMC E5) 显示出最小的厚度,高折叠耐久性和强大的生物粘合性.
- 这种膜表现出快速分解 (28.66±3.05秒),并在30分钟内实现了几乎完全的药物释放 (94.24±1.22%).
结论:
- 通过将NISSDs制成快速溶解的生物粘合性舌下膜,可以显著增强NIS溶解.
- 语言下输送提供了一种可行的策略,以规避系统前代谢并改善尼索尔迪平的口服生物利用性.
相关概念视频
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
855
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...
855
01:18Drug Delivery: Enteral Route
463
The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
463
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
134
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...
134
01:27Factors Influencing Drug Absorption: Drug Dissolution
521
The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
521
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
208
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...
208
01:15Theories of Dissolution: Diffusion Layer Model
773
Dissolution, the process by which drug particles dissolve in a solvent, is explained by the diffusion layer model, a theoretical framework that simulates the absorption of oral drugs and allows us to analyze experimental data.
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
773