Low density multiparticulate system for pulsatile release of meloxicam.

Abstract

A blend of floating and pulsatile principles of drug delivery system would have the advantage that a drug can be released in the upper GI tract after a definite time period of no drug release. A multiparticulate floating-pulsatile drug delivery system was developed using porous calcium silicate (Florite RE) and sodium alginate, for time and site specific drug release of meloxicam. Meloxicam was adsorbed on the Florite RE (FLR) by fast evaporation of solvent from drug solution containing dispersed FLR. Drug adsorbed FLR powder was used to prepare calcium alginate beads by ionotropic gelation method, using 3(2) factorial design. Developed formulations were evaluated for yield, entrapment efficiency, image analysis, surface topography, mechanical strength, apparent density, buoyancy studies and dissolution studies. Entrapment efficiency of different formulations varied from 70% to 94%. Formulations show a lag period ranging from 1.9 to 7.8 h in acidic medium followed by rapid release of meloxicam in simulated intestinal fluid USP, without enzymes (SIF). Complete drug release in SIF occurred in less than 1h from the formulations. The size of beads varied from 2.0 to 2.7 mm for different batches. Prepared beads were spherical with crushing strength ranging from 182 to 1,073 g. Floating time was controlled by density of beads and hydrophobic character of drug. A pulsatile release of meloxicam was demonstrated by a simple drug delivery system which could be useful in chronopharmacotherapy of rheumatoid arthritis.

• Authors: Sameer Sharma, Atmaram Pawar
• Journal: International journal of pharmaceutics (Int J Pharm) Vol. 313 Issue 1-2 Pg. 150-8 (Apr 26 2006) ISSN: 0378-5173 [Print] Netherlands
• PMID: 16540268 (Publication Type: Journal Article)

Chemical References

• Alginates
• Anti-Inflammatory Agents, Non-Steroidal
• Calcium Compounds
• Delayed-Action Preparations
• Drug Carriers
• Hexuronic Acids
• Silicates
• Thiazines
• Thiazoles
• Glucuronic Acid
• calcium silicate
• Meloxicam

Topics

• Alginates (chemistry)
• Anti-Inflammatory Agents, Non-Steroidal (chemistry)
• Calcium Compounds (chemistry)
• Chemistry, Pharmaceutical
• Compressive Strength
• Delayed-Action Preparations
• Drug Carriers (chemistry)
• Glucuronic Acid (chemistry)
• Hexuronic Acids (chemistry)
• Hydrogen-Ion Concentration
• Kinetics
• Meloxicam
• Particle Size
• Porosity
• Silicates (chemistry)
• Solubility
• Surface Properties
• Thiazines (chemistry)
• Thiazoles (chemistry)