通过准乳液溶剂扩散 (QESD) 结晶增强拉米武丁的流动性:对表面活性剂的影响,QbD概念的粒子形态学和平板电脑压缩挑战的全面研究
Nagaraja Sreeharsha1, Lakshmi Radhika Gajula2, Srikruthi K S3
1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Hofuf, Al-Ahsa 31982, Kingdom of Saudi Arabia; Department of Pharmaceutics, Vidya Siri College of Pharmacy, Off Sarjapura Road, Bangalore 560035, India.
概括
这项研究优化了使用准乳液溶剂扩散 (QESD) 结晶的拉米武丁 (LMD) 球形聚合物,改善了HIV-1和乙肝治疗的流动性和减少存储问题. 这种新方法增强了药物配方特性.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 化学工程是化学工程的重要组成部分.
背景情况:
- 拉米武丁 (LMD) 对于HIV-1和乙型肝炎的治疗至关重要,但其流动性和储存聚合性不佳.
- 由于这些物理限制,LMD的直接平板电脑压缩是无效的,需要颗粒化.
研究的目的:
- 使用响应表面方法和准乳液溶剂扩散 (QESD) 结晶,优化拉米武丁 (LMD) 球形聚合物.
- 调查表面活性剂对LMD聚合物特性的影响,并评估它们适用于直接压缩的适用性.
主要方法:
- 响应表面方法与中央复合材料设计,以优化诸如Tween,Span和乙度等因素.
- 准乳液溶剂扩散 (QESD) 结晶技术使用单溶剂,抗溶剂和表面活性剂 (HPMC,聚酸盐80,酸单酸盐).
- 差异分析 (ANOVA) 用于优化和评估颗粒大小,产量,形态,流动性和储存聚合物.
主要成果:
- QESD结晶成功地产生了空心的球形LMD聚合物,显著改善了流动性和减少了储存聚合物.
- 优化的聚合物能够直接压缩成片,与传统方法相比,在分解和体外药物释放方面显示出积极的结果.
- 由于有多孔结构而导致的平板印刷速度的挑战,通过调整生产参数来解决.
结论:
- QESD结晶技术对于生产具有增强制药性质的拉米武丁 (LMD) 聚合物是有效的.
- 这种方法提供了一个可行的替代传统颗粒,改善药物配方和交付.
- 进一步优化加工参数对于大规模的平板电脑制造有利.
相关概念视频
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
129
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...
129
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
800
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...
800
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
295
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...
295
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
196
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...
196
01:27Factors Influencing Drug Absorption: Drug Dissolution
464
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...
464
01:15Theories of Dissolution: Diffusion Layer Model
732
Dissolution, the process by which drug particles dissolve in a solvent, is explained by the diffusion layer model, a theoretical framework that simulates the absorption of oral drugs and allows us to analyze experimental data.
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
732