Thermal-Dependent Dehydration Process and Intramolecular Cyclization of Lisinopril Dihydrate in the Solid State

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概要

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• The pathway of dehydration and intramolecular cyclization of lisinopril dihydrate in the solid state was investigated using differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and a combination of thermal analyzer with Fourier transform infrared microspectroscopy (thermal FT-IR microscopic system). The results indicate that the dehydration from the solid-state lisinopril dihydrate had a two-step process from dihydrate to monohydrate at 76℃ and then from monohydrate to anhydrate at 99-101℃, which could be clearly observed from the above three methods. Only the thermal FT-IR microscopic system could give vital information on diketopiperazine (DKP) formation via intramolecular cyclization in anhydrous lisinopril. A new peak at 1670 cm^<-1> assigned to the carbonyl band of DKP formation was clearly evidenced. The water of reaction by-product was liberated at a temperature >157℃ and appeared on the IR spectra near 3200-3400 cm^<-1>. Moreover, the peak at 1574 cm^<-1> assigned to carboxylate shifted to 1552 cm^<-1> due to the DKP formation. The peak at 1670 cm^<-1> related to the DKP formation changed slightly in intensity from 147℃ and significantly near 157℃. DSC and TGA methods were poor for use in supplying information on DKP formation in lisinopril. The thermal FT-IR microscopic system is useful from the view point that it can quickly and directly show the solid-state stability of drug.

• 公益社団法人日本薬学会の論文
• 2000-12-01

著者

• Lin S‐y

  Veterans General Hospital‐taipei Taipei Twn

• Chen Ting-fang

  Biopharmaceutics Laboratory Department Of Medical Research And Education Veterans General Hospital-t

• WANG Shun-Li

  Biopharmaceutics Laboratory, Department of Medical Research & Education, Veterans General Hospital-T

• LIN Shan-Yang

  Biopharmaceutics Laboratory, Department of medical Research & Education, Veterans General Hospital-T

• Wang Shun-li

  Biopharmaceutics Laboratory Department Of Medical Research & Education Veterans General Hospital

• Lin Shan-yang

  Biopharmaceutical Laboratory Department Of Medical Reseach And Education Veterans General Hospital-t

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• Reaction Kinetics of Solid-state Cyclization of Enalapril Maleate Investigated by Isothermal FT-IR Microscopic System
• Thermal-Dependent Dehydration Process and Intramolecular Cyclization of Lisinopril Dihydrate in the Solid State
• pH-Dependent Coordination of Metal-Lisinopril Complex Investigated by Attenuated Total Reflection/Fourier Transform Infrared Spectroscopy
• Use of Microscopic FT-IR/DSC Combined System for the Study of Glass Transition Temperatures of Polymers
• Compression Behavior of the Different Grades of Ethyl Cellulose

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