title: A novel application of α-glucosyl hesperidin for nanoparticle formation of active pharmaceutical ingredients by dry grinding.
abstract: The effectiveness of α-glucosyl hesperidin (Hsp-G) as a novel grinding aid for the preparation of drug nanoparticles by dry grinding was investigated. Poorly water-soluble drugs and Hsp-G were mixed at a weight ratio of 1/5 and ground for 60 min by a vibrational ball mill. It was evident that all poorly water-soluble drugs used in this study formed nanoparticles after the ground mixtures were dispersed into distilled water. The dissolution profile of glibenclamide from the ground mixtures of glibenclamide/Hsp-G showed dramatic improvement from that of untreated drug crystals. Administration of the ground mixture of glibenclamide/Hsp-G to rats resulted in a significantly higher rate of decrease in blood glucose levels than that of untreated glibenclamide. The area above the time-curve of plasma-glucose concentrations using the ground mixture of glibenclamide/Hsp-G was 6-fold higher than that using untreated glibenclamide. The improved dissolution rate due to nanoparticle formation of glibenclamide, induced by co-grinding with Hsp-G, was responsible for this improvement.
authors.affiliation: Laboratory of Pharmaceutical Engineering, Gifu Pharmaceutical University, Gifu, Japan.
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Tozuka
authors.forename: Masaaki
authors.initials: M
authors.lastname: Imono
authors.forename: Hiromasa
authors.initials: H
authors.lastname: Uchiyama
authors.forename: Hirofumi
authors.initials: H
authors.lastname: Takeuchi
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000032:analysis; D004339:Drug Compounding / Q000295:instrumentation / Q000379:methods*; D005079:Excipients / Q000737:chemistry*; D005960:Glucosides / Q000737:chemistry*; D005905:Glyburide / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D006569:Hesperidin / Q000031:analogs & derivatives* / Q000737:chemistry; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000008:administration & dosage / Q000737:chemistry*; D033362:Powder Diffraction; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013499:Surface Properties; D014961:X-Ray Diffraction
chemical_list: D001786:Blood Glucose; D005079:Excipients; D005960:Glucosides; D007004:Hypoglycemic Agents; D004364:Pharmaceutical Preparations; C487382:glucosyl hesperidin; D006569:Hesperidin; D005905:Glyburide