| Nateglinide controlled release tablet containing compressionable enteric coated granules. | |
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MedLine Citation:
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PMID: 20823590 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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We designed a single unit type controlled release tablet containing nateglinide to decrease both postprandial blood glucose level (PBG) and fasting blood glucose level (FBG) in normal beagle dogs. The tablet contains 60 mg of nateglinide in an immediate release portion, and 90 mg of nateglinide in a controlled release portion. Compressionable enteric coated granules were selected as the controlled release portion to primarily decrease FBG, and they were prepared by an aqueous coating with Eudragit. Three types of nateglinide controlled release tablets were obtained, and their weights were 418.1-425.1 mg/tablet containing the above compressionable enteric coated granules. Even after tableting, the dissolution behavior of enteric coated granules was maintained approximately. In vivo single oral administration studies using normal male beagle dogs demonstrated that these tablets were able to decrease both PBG and FBG. The relative bioavailability values of the obtained tablets containing enteric coated granules having a dissolution pH of 6.0 and 6.8 were estimated at about 57.2 and 60.8% respectively against nateglinide immediate release tablets. In an in vivo repeated administration study with the tablets containing enteric coated granules having a dissolution pH of 6.8 (an interval: 8 h), decreases in both PBG and FBG were observed continuously twice. On the basis of the above results, it is expected to enable control of both PBG and FBG for moderate and severe diabetes patients with a controlled release formulation containing a short-acting type oral blood glucose regulator, not only nateglinide but also meglitinides (repaglinide, mitiglinide, etc.). |
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Authors:
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Chisato Makino; Hidetoshi Sakai; Akira Yabuki |
Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Chemical & pharmaceutical bulletin Volume: 58 ISSN: 1347-5223 ISO Abbreviation: Chem. Pharm. Bull. Publication Date: 2010 Sep |
Date Detail:
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Created Date: 2010-09-08 Completed Date: 2011-01-13 Revised Date: 2011-03-08 |
Medline Journal Info:
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Nlm Unique ID: 0377775 Medline TA: Chem Pharm Bull (Tokyo) Country: Japan |
Other Details:
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Languages: eng Pagination: 1136-41 Citation Subset: IM |
Affiliation:
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Pharmaceutical Research Laboratories, Ajinomoto Co Inc, awasaki, Kanagawa 210-8681, Japan. chisato_makino @ajinomoto.com |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Animals Blood Glucose / drug effects* Cyclohexanes / administration & dosage*, blood, pharmacology Delayed-Action Preparations / chemistry* Dogs Hypoglycemic Agents / administration & dosage*, blood, pharmacology Male Phenylalanine / administration & dosage, analogs & derivatives*, blood, pharmacology Solubility Tablets, Enteric-Coated |
| Chemical | |
Reg. No./Substance:
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0/Blood Glucose; 0/Cyclohexanes; 0/Delayed-Action Preparations; 0/Hypoglycemic Agents; 0/Tablets, Enteric-Coated; 105816-04-4/nateglinide; 63-91-2/Phenylalanine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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