用洛皮纳维尔和里托纳维尔进行电无形固体分散,以提高溶解度和溶解速率
Ewelina Łyszczarz1, Oskar Sosna1, Justyna Srebro1,2
1Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Cracow, Poland.
Nanomaterials (Basel, Switzerland)
|October 15, 2024
概括
电成功地产生了洛皮纳维尔 (LPV) 和里托纳维尔 (RTV) 的无形固体分散 (ASD). 这种技术提高了这些难以溶解的抗逆转录病毒药物的可溶性和溶解率.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 洛皮纳维尔 (LPV) 和利托纳维尔 (RTV) 是具有较差溶解性的关键抗逆转录病毒药物,限制了它们的生物可用性.
- 无形固体分散 (ASD) 是提高难溶活性药物成分 (API) 溶解率和溶解率的关键策略.
研究的目的:
- 使用电旋技术开发洛皮纳维尔 (LPV) 和里托纳维尔 (RTV) 的新型无形固体分散 (ASD).
- 研究不同聚合物载体 (PVP,KVA,Eudragit E100) 和药物含量对LPV和RTVASDs的无形化和特性的影响.
主要方法:
- 电被用来制造含有LPV和RTV的含药纤维,使用各种聚合物载体.
- 描述包括显微镜,差分扫描热量计 (DSC),X射线衍射 (XRD),湿度评估和溶解研究.
主要成果:
- 电实现了LPV和RTV的完全无形化,无论聚合物矩阵或药物负载如何.
- 特定的聚合物组合,LPV的Eudragit E100和RTV的KVA,改善了平衡溶解度和溶解率,即使具有珠在弦形态.
- 电过程在为不溶性API制造ASD方面表现出有效性.
结论:
- 电是一种可行的技术,用于制造溶解不良的抗逆转录病毒药物如洛皮纳维尔和里托纳维尔的无形固体分散 (ASD).
- 聚合物载体的选择显著影响由此产生的ASDs的溶解性和溶解性能.
- 这项研究提出了一种新的方法来增强基本抗逆转录病毒药物的输送.
相关概念视频
Factors Affecting Dissolution: Particle Size and Effective Surface Area
750
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...
750
Factors Influencing Drug Absorption: Drug Dissolution
424
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...
424
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
289
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...
289
Factors Influencing Drug Absorption: Pharmaceutical Parameters
121
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...
121
Factors Influencing Drug Absorption: Physicochemical Parameters
237
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...
237
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.1K
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...
1.1K


