Hassanien Sagban Taghi, Mustafa R Abdulbaqi, Laith Hamza Samein, Maha H Philip Rahmani
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When administered in an instant dosage form, this medicine produces several side effects, including postural hypotension, hyperkalemia, and angioedema. Included in this study were six distinct formulas of microsponges containing ramipril and Eudragit L 100 at varied ratios that were prepared by using the Quasi-emulsion solvent diffusion technique to avoid side effects. The particle size and physical characteristics of these formulations were investigated. The effects of the polymer/drug ratio on the physical features of a microsponge's physical and compatibility study was performed by using the Fourier transform infrared spectroscopy, differential scanning calorimetry, loading efficiency, surface morphology, and particle sizes. In addition, an in vitro drug-release profile was conducted. The physical characterization showed that the loading efficiency and production yield were both improved for microsponge formulation F1. 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引用次数: 0
摘要
微球是一种多孔交联聚合物,能够装载多种药物活性成分。除了口服给药途径外,它们还用于长期治疗应用。它们的特征是活性成分的有效分布,活性成分以较低的量加载,通过改变释放特性在较长的时间内释放药物。本研究的目的是开发一种新型的药物递送系统,包括雷米普利微泵。雷米普利是一种用于治疗高血压的抗高血压药物。它具有约28%的口服生物利用度,并通过肾脏被消除。当以即时剂量给药时,这种药物会产生几种副作用,包括体位性低血压、高钾血症和血管性水肿。本研究包括六种不同配方的微乳液,它们含有不同比例的雷米普利和Eudragit L 100,通过使用准乳液溶剂扩散技术制备,以避免副作用。研究了这些配方的粒度和物理特性。通过使用傅立叶变换红外光谱、差示扫描量热法、负载效率、表面形态和粒径,研究了聚合物/药物比例对微乳液物理特征和相容性的影响。此外,还进行了体外药物释放谱。物理表征表明,微乳液配方F1的负载效率和生产产率都得到了提高。对所有制剂进行了体外溶出度研究,并对结果进行了动力学分析,结果表明雷米普利的释放速率在所有制剂中都发生了变化。本研究提供了一种基于微泵技术的新型药物递送方法。
Formulation and In Vitro Evaluation of a Ramipril Entrapped in a Microsponge-based Drug-delivery System.
Microsponges are porous cross-linked polymers, which have the ability to load a wide range of pharmaceutical active ingredients. They are used topically for long-term treatment applications in addition to the oral route of administration. They are characterized by the efficient distribution of active ingredients, which are loaded at a low quantity to release the drug over longer periods of time by altering the release characteristics. The objective of this study was to develop a novel drug-delivery system that included ramipril microsponges. Ramipril is an antihypertensive drug used in the treatment of elevated blood pressure. It has about 28% oral bioavailability and is eliminated through the kidneys. When administered in an instant dosage form, this medicine produces several side effects, including postural hypotension, hyperkalemia, and angioedema. Included in this study were six distinct formulas of microsponges containing ramipril and Eudragit L 100 at varied ratios that were prepared by using the Quasi-emulsion solvent diffusion technique to avoid side effects. The particle size and physical characteristics of these formulations were investigated. The effects of the polymer/drug ratio on the physical features of a microsponge's physical and compatibility study was performed by using the Fourier transform infrared spectroscopy, differential scanning calorimetry, loading efficiency, surface morphology, and particle sizes. In addition, an in vitro drug-release profile was conducted. The physical characterization showed that the loading efficiency and production yield were both improved for microsponge formulation F1. In vitro dissolution studies were performed on all formulations, and the findings were analyzed kinetically, revealing that the ramipril release rate was altered in all formulations. This study offers a new medication delivery method based on microsponge technology.
期刊介绍:
The International Journal of Pharmaceutical Compounding (IJPC) is a bi-monthly, scientific and professional journal emphasizing quality pharmaceutical compounding. IJPC is the only publication that covers pharmaceutical compounding topics relevant and necessary to empower pharmacists to meet the needs of today"s patients. No other publication features hands-on, how-to compounding techniques or the information that contemporary pharmacists need to provide individualized care.