Effect of formulation variables on in vitro drug release and micromeritic properties of modified release ibuprofen microspheres

• Published in: Journal of microencapsulation Vol. 16; no. 4; pp. 475 - 487
• Main Authors: PERUMAL, D, DANGOR, C. M, ALCOCK, R. S, HURBANS, N, MOOPANAR, K. R
• Format: Journal Article
• Language: English
• Published: Colchester Informa UK Ltd 01.07.1999; Taylor & Francis; Informa
• Subjects: Biological and medical sciences; Bones, joints and connective tissue. Antiinflammatory agents; Delayed-Action Preparations; Drug Compounding - methods; Emulsions - chemistry; Excipients - pharmacology; General pharmacology; Ibuprofen - chemistry; Ibuprofen;Eudragit;Microspheres;Emulsifiers;Modified Release;Drug Delivery; Kinetics; Medical sciences; Microscopy, Electron, Scanning; Microspheres; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polymers - chemistry; Encapsulation; Microsphere; Pharmaceutical technology; Sucrose; Emulsification; Controlled release form; Control release polymer; Fatty ester; Drug carrier; Emulsifier; In vitro; Non steroidal antiinflammatory agent; Acrylic acid polymer; Ibuprofen; Dosage form; Arylpropionic acid derivatives; Active ingredient; Coating; Release
• ISSN: 0265-2048; 1464-5246
• DOI: 10.1080/026520499288924

Modified release microspheres of the non-steroidal anti-inflammatory drug, ibuprofen, were formulated and prepared using the emulsion solvent diffusion technique. The contribution of various dispersed phase and continuous phase formulation factors on in vitro drug release and micromeritic characteristics of microspheres was examined. The results demonstrated that the use of Eudragit RS 100 and Eudragit RL 100 as embedding polymers modified the drug release properties as a function of polymer type and concentration. Eudragit RS 100 retarded ibuprofen release from the microspheres to a greater extent than Eudragit RL 100. The drug/polymer concentration of the dispersed phase influenced the particle size and drug release properties of the formed microspheres. It was found that the presence of emulsifier was essential for microsphere formation. Increasing the concentration of emulsifier, sucrose fatty acid ester F-70, decreased the particle size which contributed to increased drug release properties. Scanning electron microscopy revealed profound distortion in both the shape and surface morphology of the microspheres with the use of magnesium stearate as added emulsifier. The application of an additional Eudragit RS 100 coat onto formed microspheres using fluid bed technology was successful and modulated the drug release properties of the coated microspheres.