用于帕金森病治疗的含有pramipexole口膜的配方和特征
Krisztián Pamlényi1, Géza Regdon1, Orsolya Jójárt-Laczkovich1
1Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6., H-6720 Szeged, Hungary.
概括
这项研究开发了用于帕金森病 (PD) 治疗的新型口腔聚合物薄膜,为吞药物提供了替代品. 最好的配方显示出良好的机械性能和生物相容性,用于有效的pramipexole二化输送.
科学领域:
- 制药科学 制药科学
- 生物材料科学 生物材料科学
- 神经退行性疾病研究研究
背景情况:
- 帕金森病 (PD) 给患者带来了显著的吞困难,使口服药物管理复杂化.
- 由于管理方面的挑战,现有的治疗方法往往难以满足患者的要求.
- 口腔药物输送通过绕过胃肠道提供了一个有希望的替代方案.
研究的目的:
- 开发和描述含有普拉米二化物 (PR) 的新型口腔聚合物薄膜,用于帕金森病治疗.
- 评估开发的薄膜的机械性能,粘粘性和生物相容性.
- 为了评估人体口腔细胞系中PR的体外透.
主要方法:
- 配制各种不同成分的口腔聚合物薄膜,包括塑化剂.
- 评估机械性能 (厚度,破裂硬度) 和粘粘性.
- 使用TR146口腔细胞系进行体外生物相容性测试.
- 在TR146细胞系中进行了pramipexole二化的体外透研究.
主要成果:
- 增塑剂提高了薄膜厚度和破裂硬度,但没有显著地损害粘粘性.
- 所有测试的薄膜配方在TR146细胞系上都表现出高细胞活力 (超过87%).
- 一种特定的配方 (3% SA+1% GLY-PR-Sample1) 被确定为口腔分娩的最佳配方.
结论:
- 口腔聚合物薄膜是帕金森病的可行的药物输送系统,可以克服吞困难.
- 开发的薄膜显示出良好的机械,粘膜和生物相容性.
- 优化的配方显示了通过口腔粘膜进行有效的普拉米醇二化输送的潜力,用于PD管理.
相关概念视频
01:24Parkinson's Disease: Treatment
303
Neurodegenerative disorders, such as Parkinson's Disease (PD), involve the gradual and irreversible destruction of neurons in particular brain areas. These disorders exhibit standard features like proteinopathies, selective vulnerability of some neurons, and an interaction of intrinsic properties, genetics, and environmental influences in neural injury.
Parkinson's Disease is primarily a result of the loss of dopaminergic neurons in the substantia nigra pars compacta. The cornerstone of...
Parkinson's Disease is primarily a result of the loss of dopaminergic neurons in the substantia nigra pars compacta. The cornerstone of...
303
01:15Parkinson's Disease: Overview
611
Neurodegenerative disorders are progressive diseases that cause irreversible damage and loss to neurons in specific brain areas. Examples of these disorders include Parkinson's disease, Alzheimer's disease, Multiple Sclerosis (MS), and Amyotrophic Lateral Sclerosis (ALS). These disorders share characteristics such as proteinopathies, selective neuronal vulnerability, and a complex interplay between genetic and environmental factors. The primary therapeutic goal for these conditions is...
611
01:24Cholinergic Antagonists: Pharmacokinetics
522
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...
522
01:18Drug Delivery: Enteral Route
526
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.
526
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
157
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...
157
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
346
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...
346