Formulation and Evaluation of Microspheres of Ramipril

Abstract

Background: Ramipril an antihypertensive medicine has a 28 percent oral bioavailability and is promptly eliminated from the body through the kidneys. When Ramipril is administered as an immediate dosage form, it has also been linked to a wide range of side effects, including hypotension, an increase in potassium level, and angioedema. The present study was therefore conducted in an effort to reduce the drug's negative effects and boost its bioavailability.
 Objectives: In the current work, ramipril microspheres are created and evaluated utilizing the solvent evaporation method and natural or synthetic polymers. Use natural polymers like ramipril, sodium hydroxide, potassium dihydrogen orthophosphate, dichloromethane (DCM), and synthetic polymers like ethyl cellulose, eudragit RL100, etc.
 Methods: A solvent evaporation technique was used to create the microsphere, and polymers like EudragitRL100 and ethyl cellulose were used. Particle size analysis, percent entrapment efficiency, Differential scanning calorimetry (DSC), Drug encapsulation efficiency (DEE), FTIR spectroscopy, in vitro release research, and stability study were all performed on the produced formulations.
 Results: The results were observed to be within the normative ranges. The FT-IR analysis of the formulations indicated there was no interaction between Ramipril and other excipients. The range of entrapment efficiency was found to be between 68.7 and 94.08%. The drug release investigation was conducted in gastrointestinal fluid (SGF) for 12 hours and demonstrated the largest quantity of drug release in a regulated and sustained manner over a prolonged length of time. The size of the microsphere was in the range of 25.7 to 49.2 m. According to the DSC study, molecules of drugs are uniformly dispersed in an amorphous state.
 Conclusion: The designed formulation was discovered to be stable and it provides a potential system for the controlled and sustained distribution of ramipril.
 Keywords: Ramipril, EudragitRL100, Ethylcellulose, Potassium dihydrogen orthophosphate, Solvent evaporation method.