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ƒtƒBƒ‹ƒ€ƒR[ƒeƒBƒ“ƒO‚π•Ή—p‚΅‚½“—n«–ς•¨‚Μ•ϊo§Œδ
[…@Œ[˜NAΞˆδ@’B–νAˆΙ”φ@Šx
ŒΓΞ@—_”VA—ι–؁@–LŽjA”Ί–μ@˜a•v
Summary
Glibenclamide (GCM), which was poorly water soluble anti-diabetic agent, was treated with highly branched cyclic dextrin (HBCD) by using MechanofusionπΡ system to improve its dissolution behavior. When a physical mixture (PM) of HBCD and GCM was coground for 30 min at room temperature, composite particles of HBCD covered with crystalline GCM was observed as well as micronized GCM particles. The ground mixture (GM) was dispersed into methacrylic acid copolymer suspension and spray-coated on surfaces of sucrose core particles. Surfaces of the particles obtained at 98.8% yield were covered with a polymeric film ca. 8ƒΚm thick containing the micronized GCM. According to the JP15 dissolution test, drug release profile from each sample was evaluated. As a result, GCM concentrations released from PM, GM and the coated particles were 0.5, 8.5 and 5.2ƒΚg/mL, respectively, in artificial intestinal fluid after 2 hours. Since drug release from coating particles was not detected in the artificial gastric fluid (less than 0.1ƒΚg/mL), multifunctional, which was solubility enhancing and enteric, particles were prepared.
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