Design of Nateglinide Controlled Release Tablet Containing Erosion Matrix Tablet and Multiple Administration Study in Normal Beagle Dogs

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概要

• 論文の詳細を見る

• We designed a single unit type tablet formulation containing nateglinide to decrease both postprandial blood glucose level (PBG) and fasting blood glucose level (FBG) in normal beagle dogs. The tablet was a dry coated tablet comprising both a core tablet (an erosion matrix tablet: a controlled release portion(nateglinide: 90 mg)) and an outer shell (an immediate release portion (nateglinide: 60 mg)). The weight, the diameter and the hardness of the obtained tablet were 416.1 mg, 10 mmφ, about 60 N, respectively. The dissolution study of the obtained tablet in pH 1.2 or 6.8 showed that the nateglinide in the immediate release portion dissolved in almost 30 min., and that 30 min after the dissolution test started, the nateglinide in the controlled release portion had dissolved slowly. An in vivo single oral administration study using normal beagle dogs showed the bioavailability value of the obtained nateglinide dry coated tablets against nateglinide immediate release tablets was 73.6%, although the value of nateglinide controlled release tablets containing enteric coated granules was 57.2—60.8%. An in vivo multiple oral administration study (b.i.d. (interval: 12 h), 8 d) using normal beagle dogs showed the reproducibility of nateglinide absorption. In addition, decreases in both PBG and FBG were observed. The ability to decrease the blood glucose level did not weaken during a multiple administration. On the basis of the above results, a controlled release formulation containing a short-acting type oral blood glucose regulator, not only nateglinide but meglitinides (repaglinide, mitiglinide, etc.) was suggested to enable control of both PBG and FBG for moderate and severe diabetes patients.

• 社団法人 日本薬学会の論文

著者

• Okano A

  National Institute Of Livestock And Grassland Science

• Okano A

  Pharmaceutical Research Laboratories Ajinomoto Co. Inc.

• Okano Akira

  Pharmaceutical Research Laboratories Ajinomoto Co. Inc

• Makino Chisato

  Pharmaceutical Research Laboratories, Ajinomoto Co., Inc.

• Sakai Hidetoshi

  Pharmaceutical Research Laboratories, Ajinomoto Co., Inc.

• Yabuki Akira

  Pharmaceutical Research Laboratories, Ajinomoto Co., Inc.

• Okano Akira

  Pharmaceutical Research Laboratories, Ajinomoto Co., Inc.

関連論文

• Design of Nateglinide Controlled Release Tablet Containing Erosion Matrix Tablet and Multiple Administration Study in Normal Beagle Dogs
• Effect of Decrease in Both Postprandial Blood Glucose (PBG) and Fasting Blood Glucose (FBG) Levels in Normal Beagle Dogs with Nateglinide Enteric Coated Granules and Immediate Release Tablets
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