Formulation and evaluation of glimepiride solid dispersion tablets

Abstract

The poor dissolution rate of water-insoluble drugs is still a major problem conforming the pharmaceutical industry. The most common method for improving the solubility is by increasing the surface area of the drug through micronization. But, in practice the effect of micronization is often disappointing, especially when the drugs are encapsulated or tablet. It is generally recognized that low solubility or dissolution rate often becomes a rate-limiting step in absorption of poorly water soluble drugs. Therefore, the enhancement of the dissolution rate of poorly water-soluble drugs after oral administration is one of the most challenging aspects of modern pharmaceutics. Olanzepine (2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno [2, b] [1, 5]benzodiazepine possess antipsychotic activity and exhibits very slight solubility in water and as a consequence it exhibit low bioavailability after oral administration Therefore, the improvement of olanzepine dissolution from its oral solid dosage forms is an important issue for enhancing its bioavailability and therapeutic efficacy. The purpose of present work is to improve the solubility of Olanzepine by preparing its dispersion with polymer PEG (Poly Ethylene Glycol) using solvent evaporation technique.

A basic insight into the stability and manufacturing aspects of solid dispersions

“…The commercial viability of solid dispersion technology is still not cent percent, but it is a promising technology [43] Valasartan Gelucire-50/13 Hot melt granulation [44] Nimodipine Plasdone-S630, Eudragit-E100 Hot melt granulation [45] Paracetamol PVP Kneading technique [46] Fluvastatin PVP, Eudragit-E100, Chitosan Melt mixing, solvent evaporation [47] Aceclofenac Lactose, mannitol, urea Solvent evaporation [48] Acyclovir PVP K30, PEG 6000 Solvent evaporation [49] Furosemide Crospovidone Kneading technique [50] Itraconazole Eudragit-E100 Melt/cool [51] Irbesartan HPMC E5LV Spray drying [52] Magnesium salts Lecithin,Betaine Solvent evaporation [53] Hydrochlorothiazide Captopril Kneading [54] Ketoprofen and nifedipine Ethyl cellulose Hot melt extrusion [55] Verapamil hydrochloride HPMCK4M, eudragit RSPO Solvent evaporation [56] Gliclazide PEG 8000 Fusion solvent [57] Gliclazide PEG 6000 Fusion [58] Etoricoxib PVP K30, PEG 4000 Solvent evaporation [59] Fenofibrate PEG 6000, poloxamer 407 Fusion solvent [60] Indomethacin Gelucire-50/13, PEG 4000 Hot melt extrusion [61] Pizotifen malate Povidone Dissolution , solvent evaporation [62] Piroxicam MCC, potato starch Co evaporation [63] Indomethacin PEG 6000, myrj 52, lactose, sorbitol, dextrin, eudragit® E100 Solvent evaporation, coevaporation [64] Acyclovir PEG Hot melt, solvent evaporation [65] Glimepiride PEG4000, HPC or lactose Solvent evaporation [66] Ketoconazole β-cyclodextrin Solvent evaporation [67] Nimodipine Ethyl vinyl acetate, Eudragit RL 100, Ethyl acetate Solvent [68] Terbinafine hydrochloride PEG 6000, PVP K30 Melting and solvent [69] Chlordiazepoxide PVP, Eudragit E100, Mannitol and Sorbitol Solvent [70] Glimepiride Poloxamer 188 (PXM 18) - [71] Aceclofenac HPMC, Carbopol 940 Solvent [72] Gliclazide Polyethylene glycol 6000 Fusion [73] Bicalutamide PVPK30 - …”

Formulation and evaluation of binary and ternary solid dispersions of domperidone by solvent evaporation method

“…PMs were prepared by simple trituration of the drug and carriers with their respective weight ratios in a porcelain mortar for 5 min. PMs were sieved and stored as mentioned earlier until use (Gill et al, 2010).…”

Effect of Hydrophilic Carriers for Solubility and Dissolution Enhancement of Sulfamerazine by Solid Dispersions Technique

“…The solid dispersion techniques help in reducing the harmful effects. Thus, the present research aims to investigate the effect of hydrophilic carriers on enhancing the solubility and dissolution rate of SMZ by using the solid dispersion technique [12][13][14].…”