Abstract
Purpose: Triple solid dispersion adsorbates (TSDads) and spherical agglomerates (SA) present new techniques that extensively enhance dissolution of poorly soluble drugs. The aim of the present study is to hasten the onset of hypoglycemic effect of glimepiride through enhancing its rate of release from tablet formulation prepared from either technique.Methods: Drug release from TSDads or SA tablets with different added excipients was explored. Scanning electron microscopy (SEM) and effect of compression on dissolution were illustrated. Pharmacodynamic evaluation was performed on optimized tablets.Results: TSDads & SA tablets with Cross Povidone showed least disintegration times of 1.48 and 0.5 min. respectively. Kinetics of drug release recorded least half-lives (54.13 and 59.83min for both techniques respectively). Cross section in tablets displayed an organized interconnected matrix under SEM, accounting for the rapid access of dissolution media to the tablet core. Components of tablets filled into capsules showed a similar release profile to that of tablets after compression as indicated by similarity factor. The onset time of maximum reduction in blood glucose in male albino rabbits was hastened to 2h instead of 3h for commercial tablets.Conclusion: After optimization of tablet excipients that interacted differently with respect to their effect on drug release, we could conclude that both amorphisation and spheronization were equally successful in promoting in vitro dissolution enhancement as well as providing a more rapid onset time for drug action in vivo.
Highlights
A variety of technical problems are usually encountered in the pharmaceutical industry when dealing with the formulation of insoluble drugs,[1] often leading to a suboptimal drug product
The present study aims to test and compare the applicability of new amorphisation and spheronization techniques viz: Triple solid dispersion adsorbate (TSDads) or spherical agglomerates (SA) in attaining best results in dissolution enhancement of glimepiride, as well as studying the effect of compression on dissolution parameters
Drug content evaluation in ternary solid dispersion (TSD), Triple solid dispersion adsorbates (TSDads) & SA All assayed samples of TSD & TSDads resulted in 98100% glimepiride content, indicating uniformity of drug distribution within different matrices
Summary
A variety of technical problems are usually encountered in the pharmaceutical industry when dealing with the formulation of insoluble drugs,[1] often leading to a suboptimal drug product. Poor aqueous solubility of drugs affects both their in vitro dissolution rate,[2] as well as their pharmacological activity.[3] continuous efforts have been dedicated for the treatment of such problem through a different design of particle technology[4] and particle engineering processes, such as spray freezing into liquids,[5] sonocrystallization,[6,7] and others.[8] In general, most preliminary pretreatment of particles relies upon making a change in the drug crystallinity, the so-called amorphisation techniques.[9] Amorphous forms of drugs are characterized by a disordered arrangement of molecules in the solid state This is accompanied by a higher state of free energy, enabling faster extent and rate of drug dissolution.[10,11] Another well-known strategy for decreasing drug crystallinity is particle spheronization which was achieved in literature via different techniques and mechanisms;[12] enabling dissolution enhancement of poorly soluble drugs.[13] Direct tabletting of pharmaceutical materials involves dry blending and compaction of the active pharmaceutical ingredient with the necessary excipients and lubricants.
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