通过半固体挤出实现个性化药物输送:探索聚乙烯醇-联合乙烯酸乙酸) kopo 聚合物用于含基化物载入的薄膜
Karin Korelc1, Bjarke Strøm Larsen1, Anna-Lena Heintze2
1Department of Pharmacy, University of Oslo, P.O. Box 1068 Blindern, Oslo 0316, Norway.
概括
定制聚乙烯醇-联合乙乙酸) (PVA/PVAc) 共聚合物比率可以实现个性化的药物输送膜. 调整单体比率可以有效调整甲酸 (HCT) 的释放和透性,而更高的乙烯基酒精含量可以增强药物释放.
科学领域:
- 聚合物科学和材料科学
- 制药科学 制药科学
- 药物输送系统是药物输送系统.
背景情况:
- 个性化药物递送需要具有可调节性质的系统.
- 聚乙烯醇-联合乙乙酸) (PVA/PVAc) 共聚合物通过单体比率的修改提供可调性特性.
- 甲 (HCT) 由于溶解性差,点高和透性低,因此存在配方挑战.
研究的目的:
- 研究PVA/PVAc共聚合物的不同乙烯醇 (VA) 和乙烯酸乙烯 (VAc) 单体比对酸 (HCT) 薄膜的特性的影响.
- 评估半固体挤出用于制备HCT-PVA/PVAc薄膜的适用性.
- 评估开发的HCT膜的药物分布,释放动力学,透性和细胞毒性.
主要方法:
- 制备五种具有不同的VA/VAc比率的PVA/PVAc共聚合物.
- 对共聚合物的特性进行表征.
- 使用半固体挤出制造HCT-PVA/PVAc薄膜.
- 药物分销的同质性评估.
- 在体外药物释放研究.
- 使用HT29-MTX细胞单层的透性研究.
- 细胞毒性测定.细胞毒性测定.
主要成果:
- 所有测试的PVA/PVAc共聚合物都适合半固体挤出,具有更高的VA比例,产生更好的机械性能.
- 甲在微米级的膜内均分布.
- VA/VAc单体比率显著影响了HCT释放率,较高的VA含量导致释放增加.
- 在不同配方中观察到不同的HCT透性.
- 在任何测试的HCT-PVA/PVAc配方中都没有检测到细胞毒性.
结论:
- 聚乙烯/PVAc共聚合物的单体比是决定薄膜特性,药物释放和透性的关键因素.
- 半固体挤出是一种生产HCT-PVA/PVAc薄膜的可行方法,解决了与HCT相关的挑战.
- 由于PVA/PVAc共聚合物的可调性,可以方便个性化药物输送,允许灵活的剂量和有吸引力的剂型设计,特别适用于儿科应用.
相关概念视频
Factors 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
Drug Distribution: Volume of Distribution
5.1K
The volume of distribution refers to the theoretical volume necessary to contain the entire amount of an administered drug at the same concentration observed in the blood plasma. The body's intracellular fluid compartment, which makes up two-thirds of the total body water, is contrasted with the extracellular fluid compartment—comprising plasma and interstitial fluid—that accounts for one-third. The volume of distribution can vary depending on the characteristics of the drug.
5.1K
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
312
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...
312
Antihypertensive Drugs: Thiazide-Class Diuretics
688
Thiazide diuretics are sulfonamide derivatives featuring a benzothiadiazine ring system in their molecular structure. Based on this structure, thiazide diuretics can be categorized into two groups: thiazide-type and thiazide-like diuretics. Thiazide-type diuretics, including hydrochlorothiazide and chlorothiazide, consist of a benzothiadiazine backbone with an attached sulfonamide group. Thiazide-like diuretics, such as chlorthalidone and indapamide, lack the thiazide ring but demonstrate...
688
Factors Influencing Drug Absorption: Physicochemical Parameters
301
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...
301


