Taghi Hassanien Sagban, Abdulbaqi Mustafa R, Samein Laith Hamza, Rahmani Maha H Philip
Department of Pharmaceutics, College of Pharmacy, Al-Bayan University, Baghdad, Iraq.
College of Pharmacy, University of Mashreq, Baghdad, Iraq.
Int J Pharm Compd. 2023 Jul-Aug;27(4):340-346.
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.
微海绵是多孔交联聚合物，能够负载多种药物活性成分。除口服给药途径外，它们还用于局部长期治疗应用。其特点是活性成分分布高效，活性成分负载量低，通过改变释放特性在较长时间内释放药物。本研究的目的是开发一种包含雷米普利微海绵的新型药物递送系统。雷米普利是一种用于治疗高血压的抗高血压药物。它的口服生物利用度约为28%，通过肾脏排泄。当以速释剂型给药时，这种药物会产生多种副作用，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海绵，它们含有不同比例的雷米普利和尤特奇L 100，采用准乳液溶剂扩散技术制备，以避免副作用。研究了这些制剂的粒径和物理特性。通过傅里叶变换红外光谱、差示扫描量热法、载药效率、表面形态和粒径研究了聚合物/药物比例对微海绵物理特性和相容性的影响。此外，还进行了体外药物释放曲线研究。物理表征表明，微海绵制剂F1的载药效率和产率均有所提高。对所有制剂进行了体外溶出研究，并对结果进行了动力学分析，结果表明所有制剂中雷米普利的释放速率均发生了改变。本研究提供了一种基于微海绵技术的新型药物递送方法。
