title: Dissolution rate enhancement of gliclazide by ordered mixing.
abstract: The poorly water soluble antidiabetic drug gliclazide was selected to study the effect of excipients on dissolution rate enhancement. Ordered mixtures of micronized gliclazide with lactose, mannitol, sorbitol, maltitol and sodium chloride were prepared by manual shaking of glass vials containing the drug and excipient(s). Different water soluble excipients, addition of surfactant and superdisintegrant, drug concentration and carrier particle size influenced the dissolution rate of the drug. Dissolution rate studies of the prepared ordered mixtures revealed an increase in drug dissolution with all water soluble excipients. The order of dissolution rate improvement for gliclazide was mannitol > lactose > maltitol > sorbitol > sodium chloride. Composite granules of the particle size range 355-710 μm were superior in increasing the drug dissolution rate from ordered mixtures. Reducing the carrier particle size decreased the dissolution rate of the drug as well as the increase in drug concentration. Kinetic modeling of drug release data fitted best the Hixson-Crowell model, which indicates that all the ordered mixture formulations followed the cube root law fairly well.
authors.affiliation: Institute of Pharmaceutical Sciences and Drug Research, Seth G.L. Bihani S.D. College of Technical Education, Sri Ganganagar, Rajasthan, India. vikas.pharmaceutics@gmail.com
authors.forename: Vikas A
authors.initials: VA
authors.lastname: Saharan
authors.forename: Pratim K
authors.initials: PK
authors.lastname: Choudhury
mesh_terms: D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D005907:Gliclazide / Q000737:chemistry* / Q000627:therapeutic use; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000627:therapeutic use; D007785:Lactose / Q000737:chemistry; D008320:Maltose / Q000031:analogs & derivatives / Q000737:chemistry; D008962:Models, Theoretical; D010316:Particle Size; D010599:Pharmacokinetics; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry; D012995:Solubility; D013213:Starch / Q000031:analogs & derivatives / Q000737:chemistry; D013402:Sugar Alcohols / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry; D013535:Suspensions / Q000737:chemistry; D014867:Water
chemical_list: D004337:Drug Carriers; D005079:Excipients; D007004:Hypoglycemic Agents; D013402:Sugar Alcohols; D013501:Surface-Active Agents; D013535:Suspensions; D014867:Water; D012967:Sodium Dodecyl Sulfate; D008320:Maltose; D013213:Starch; C048390:sodium starch glycolate; C010745:maltitol; D005907:Gliclazide; D007785:Lactose