| Autor: | Noritsugu Morokoshi, Keiichi Nakashima, Shinichi Fukuyama, Tsutomu Yasuda, Noriaki Kihara, Shigetaka Koda |
|---|---|
| Rok vydání: | 1994 |
| Předmět: |
Pharmacology
Indole test PEG 400 Chemistry Formic acid medicine.drug_class Organic Chemistry Pharmaceutical Science Carboxamide Polyethylene glycol Medicinal chemistry Dosage form chemistry.chemical_compound mental disorders Glycerol medicine Molecular Medicine Organic chemistry Pharmacology (medical) Isomerization Biotechnology |
| Zdroj: | Pharmaceutical Research. 11:1704-1706 |
| ISSN: | 0724-8741 |
| DOI: | 10.1023/a:1018998813296 |
| Popis: | FK480 is a new synthetic non-peptide antagonist of cholecystokinin (CCK)-A receptors. The dosage form of FK480 is a soft capsule containing a solution of FK480 in a mixture of polyethylene glycol 400 (PEG 400) and glycerol to improve its bioavailability. Studies on the stability of this FK480 dosage form revealed that the main degradation occurred by optical isomerization at the asymmetric C-3 position of the pyrrolobenzodiazepine ring. The degradation reaction was accelerated by formic acid formed in a mixture of PEG 400 and glycerol. Addition of amino acids to the capsule solution retarded the isomerization by reacting with formic acid. Therefore, formic acid appears to accelerate optical isomerization of FK480. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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