开发和优化基托-酸基粘膜膜,用于口腔输送卡普托普里尔
Krisztián Pamlényi1, Hala Rayya1, Alharith A A Hassan1
1Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6., H-6720 Szeged, Hungary.
Pharmaceutics
|April 26, 2025
概括
酸盐-酸盐口膜为高血压危机提供了更好的卡普托普利 (CAP) 输送. 这些优化的膜确保了高药含量和立即释放,绕过口服限制.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 生物材料是一种生物材料.
背景情况:
- 作为一种ACE抑制剂的卡普托普利 (CAP) 面临生物可用性挑战,原因是口服时肝脏的第一通代谢.
- 粘膜口膜为增强CAP输送提供了可行的替代方案,绕过肝脏代谢.
- 高血压管理可以从替代药物输送系统中受益,提供更好的患者服药性和有效性.
研究的目的:
- 为了配制和优化色素酸盐粘膜膜,用于口服卡普托普里尔 (10毫克和20毫克).
- 应用设计质量 (QbD) 和实验设计 (DoE) 原则,以实现高效的配方开发.
- 评估这些电影在管理高血压危机方面的潜力.
主要方法:
- 素 (CHI) 和酸 (AA) 用于通过溶剂造来制造粘膜.
- 设计质量 (QbD) 和实验设计 (DoE) 用于配方优化.
- 在实验室内进行了粘结,破裂硬度,药物含量,药物分布和溶解的研究.
主要成果:
- 优化的CAP装载薄膜在体外表现出极好的粘结力 (> 15N) 和破裂硬度 (> 14N).
- 影片显示药物含量高 (>95%) 均分布,符合药物库标准.
- FT-IR和RAMAN光谱证实了成功的药物结合和辅助剂相互作用 (键).
- 溶解试验表明,从两个薄膜度中,托普利尔立即释放.
结论:
- 开发的酸盐-酸盐口腔膜满足了卡普托普里尔输送的所有关键质量属性要求.
- 优化的配方 (CHI 1.4%,AA 2.5%,糖醇 0.3%) 是口服卡普托普里尔的有希望的系统.
- 这种方法提供了一种有效的策略,通过改善药物的生物可用性和绕过口服限制来管理高血压危机.
相关概念视频
01:18Drug Delivery: Enteral Route
331
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.
331
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
101
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...
101
01:24Cholinergic Antagonists: Pharmacokinetics
373
Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations, while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and...
373
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
601
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...
601
01:22Factors Influencing Drug Absorption: Physicochemical Parameters
179
The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
179
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
148
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...
148