NDLI: Study of the polymorphic behaviour of some local anesthetic drugs

Content Provider	Springer Nature Link
Author	Giron, D. Draghi, M. Goldbronn, C. Pfeffer, S. Piechon, P.
Copyright Year	1997
Abstract	The local anesthetic drug tetracaine hydrochloride is described in the Europ. Pharmacopea with a melting point of 148°C or with a range of 134 to 147°C due to the melting points of two other forms. The polymorphic behaviour of tetracaine hydrochloride has been studied by using thermal treatments, storage at 92% r.h., crystallizations and equilibrations with saturated solutions. Samples were characterized by X-ray diffraction, IR, thermal analysis and elemental analysis. Since some findings were difficult to interpret, temperature resolved X-ray diffraction was used additionally for the understanding of the thermal behaviour of tetracaine hydrochloride. In this study the polymorphic behaviour of some other local anesthetic drugs is compared.Ten different forms of tetracaine hydrochloride: six anhydrous crystalline forms, an amorphous form, a hemihydrate, a monohydrate and a tetrahydrate were identified. The relationships between all forms are given.The heating curve of the commercial form 1 is very dependent on the heating rate. This anhydrous form 1 is the thermodynamic stable modification at ambient temperature. The form 2 is reversibly enantiotrope to form 1. The four other modifications called 3, 4, 5 and 6 are monotropes of form 1.Only forms 1 and 5 are stable at ambient temperature. Form 1 is hygroscopic only at high humidity level of 92% r.h., form 5 is hygroscopic at 61% r.h. Both transform into the monohy-drate.No polymorphic forms of tetracaine base, dibucaine hydrochloride, procaine hydrochloride or prilocaine hydrochloride were found.The commercial form of bupivacaine hydrochloride is a monohydrate. Thermal treatment at 200°C gives one anhydrous form. As demonstrated by temperature resolved X-ray diffraction two other forms are detected by heating and cooling processes between 100 and 170°C. Equilibrations and crystallization experiments show that solvates are easily obtained in different solvents.Temperature resolved X-ray diffraction is a very efficient tool as a support to DSC for the identification of the transition processes and interpretation of thermal events and thermodynamic relationships. Equilibration experiments are very adequate to find out the thermodynamically stable form at ambient temperature (solvent mediated transitions).
Starting Page	913
Ending Page	927
Page Count	15
File Format	PDF
ISSN	00225215
Journal	Journal of thermal analysis
Volume Number	49
Issue Number	2
e-ISSN	15728943
Language	English
Publisher	Kluwer Academic Publishers
Publisher Date	1997-01-01
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	anesthetic drugs bupivacaine hydrochloride dibucaine hydrochloride DSC polymorphism prilocaine hydrochloride procaine hydrochloride solvent mediated transitions temperature resolved X-ray diffraction tetracaine base tetracaine hydrochloride thermodynamic relationships Physical Chemistry Analytical Chemistry Polymer Sciences Inorganic Chemistry Measurement Science and Instrumentation
Content Type	Text
Resource Type	Article

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