在OrPhylloTM中评估不同配方的兼容性,OrPhylloTM是个性化口膜的即用基础
Bruna Marianni1, Hudson Polonini1, Savvas Koulouridas1
1Fagron BV, Rotterdam, The Netherlands.
International journal of pharmaceutical compounding
|March 31, 2025
概括
这项研究证实OrPhylloTM是一个合适的基础,用于合成口腔可分散膜 (ODF). 该研究确定了ODF配方中的12种活性药物成分 (API) 的过时使用日期 (BUD),以确保药物的稳定性和患者的遵守.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 复合药房 复合药房 复合药房
背景情况:
- 口腔可分散膜 (ODF) 为患有吞困难的患者提供了有效的解决方案.
- 通过快速的口服分解,ODF增强了药物输送,提高了合规性和生物可用性.
- 对于复合ODFs的稳定性和超出使用日期 (BUDs) 的确定仍然存在挑战.
研究的目的:
- 评估12种活性药物成分 (API) 的兼容性和确定BUDs,这些活性药物成分 (API) 用OrPhylloTM.合成ODF.
- 在定义的储存条件下评估ODF配方的物理化学完整性.
- 为了验证OrPhylloTM作为ODF生产的可靠基础.
主要方法:
- 通过OrPhylloTM基础,12个API被编制成ODF.
- 使用经过验证的超高性能液态染色学 (UHPLC) 方法评估了兼容性和稳定性.
- 配方在室温 (15-30°C) 下进行了加快和长期稳定性测试,长达180天,包装在囊中.
主要成果:
- 已建立的各种API的BUD:巴克洛芬 (180天), cetirizine (60天),辅酶Q10 (180天),德克斯特罗梅索芬 (180天),基托 (180天为12.5mg,60天为25mg),洛拉塔丁 (180天),梅洛西卡姆 (180天),米诺克西尔 (180天),丹塞龙 (90天为2mg,30天为8mg),西尔代纳菲尔 (180天),塔达拉菲尔 (180天) 和特拉马多尔 (150天).
- 在整个研究期间,ODF配方的物理化学完整性得到证明.
- 确认由于剂型的非水性性质,无需进行抗微生物有效性测试 (AET).
结论:
- OrPhylloTM是一个适合和坚固的工具,用于将广泛的API合成ODF.
- 建立的BUD为药剂师和患者提供了关于ODF稳定性和保质期的关键数据.
- 这项研究支持复合ODF的临床应用,特别是针对弱势患者群体.
相关概念视频
Factors Influencing Drug Absorption: Pharmaceutical Parameters
104
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...
104
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
159
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...
159
Factors Affecting Dissolution: Particle Size and Effective Surface Area
647
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...
647
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
832
Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
832
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
263
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...
263
Factors Influencing Drug Absorption: Drug Dissolution
378
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...
378


