关于开发含有desloratadine的口腔可分散膜的初步研究
Özden Çakmakyapan1, Fatma Nur Tuğcu Demiröz1, Zeynep Şafak Teksin1
1Gazi University Faculty of Pharmacy, Department of Pharmaceutical Technology, Ankara, Türkiye.
Turkish journal of pharmaceutical sciences
|March 7, 2025
概括
研究人员开发了稳定的口腔可分散膜 (ODF) 用于低溶性药物德斯洛拉塔丁 (DL). 这些膜提供了改善的药物加载和患者遵守,显示出出色的机械性能和快速解体.
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
- 材料科学 材料科学 材料科学
背景情况:
- 口腔可分散膜 (ODF) 为各种人口群体提供了增强的患者遵守.
- 德拉他丁 (DL) 是一种水溶性较差且对氧化敏感的药物,需要先进的输送系统.
研究的目的:
- 开发和描述含有德斯洛拉塔丁 (DL) 的口腔可分散膜 (ODF).
- 为稳定和有效的DL装载ODF优化配方和工艺参数.
主要方法:
- 用于制备20种薄膜配方的溶剂造方法.
- 特性包括外观,机械性能,厚度,分解时间和内容均性.
- 不同扫描热量计 (DSC) 用于形态和兼容性研究;抗氧化剂查稳定性.
主要成果:
- 开发出具有良好的机械性能 (抗拉强度6.21-10.34 MPa) 和分解率<60s的均ODF.
- 使用精选的辅助剂,增加DL溶解度和药物载荷能力到3%.
- 获得了无颗粒薄膜 (F20),具有出色的厚度和内容均性 (RSD=4.6%,AV=5).
结论:
- 成功开发了稳定的desloratadine口腔可分散膜,具有增强的药物负载.
- 优化的ODF配方 (F20) 呈现出用于制药应用的理想特征.
- 这些ODF代表了一种有前途的剂型,可以改善德斯洛拉塔丁的使用和患者的服药.
相关概念视频
Factors Affecting Dissolution: Particle Size and Effective Surface Area
660
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...
660
Drug Delivery: Enteral Route
361
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.
361
Factors Influencing Drug Absorption: Pharmaceutical Parameters
112
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...
112
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
164
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...
164
Factors Influencing Drug Absorption: Drug Dissolution
395
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...
395
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
276
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...
276


