Views

CrossRef citations to date

Altmetric

Research Article

Multicomponent crystals of gliclazide and tromethamine: preparation, physico-chemical, and pharmaceutical characterization^*

Giovanna BruniC.S.G.I. – Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia, Italy; Correspondence[email protected]

Vittorio BerbenniC.S.G.I. – Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia, Italy;

Lauretta MaggiDepartment of Drug Sciences, University of Pavia, Pavia, Italy

Piercarlo MustarelliC.S.G.I. – Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia, Italy;

Valeria FriuliDepartment of Drug Sciences, University of Pavia, Pavia, Italy

Chiara FerraraC.S.G.I. – Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia, Italy;

Francesca PardiC.S.G.I. – Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia, Italy;

Federica CastagnaC.S.G.I. – Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia, Italy;

Alessandro GirellaC.S.G.I. – Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia, Italy;

Chiara MilaneseC.S.G.I. – Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia, Italy;

Amedeo MariniC.S.G.I. – Department of Chemistry, Physical-Chemistry Section, University of Pavia, Pavia, Italy;

show all

Abstract

Objective: To improve the pharmaceutical behavior of the oral antidiabetic agent gliclazide through the synthesis of multicomponent crystals with tromethamine.

Methods: Multicomponent crystals were prepared by solvent evaporation method, kneading, and combining mechanical and thermal activation. DSC, FT-IR spectroscopy, X-ray diffraction, SEM-EDS, and SSNMR were used to investigate their formation. Measurements of solubility and dissolution rate were carried out for the pharmaceutical characterization.

Results: The formation of multicomponent crystals of gliclazide and tromethamine was confirmed by all the techniques. In particular, FT-IR and NMR measurements revealed that the interaction between drug and coformer leads to significant changes of the hydrogen bond scheme, and that almost all the functional groups of the two molecules are involved. The dissolution profile of the new phase is significantly better than that of both pure gliclazide and of the reference commercial product Diabrezide^®.

Conclusions: The new system shows an improved pharmaceutical behavior and could be formulated in a dosage form to obtain a rapid and complete release of the drug available for absorption.

Keywords:

Disclosure statement

No potential conflict of interest was reported by the authors.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Order Reprints Request Corporate Permissions

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

Request Academic Permissions

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.

Multicomponent crystals of gliclazide and tromethamine: preparation, physico-chemical, and pharmaceutical characterization^*

Information for

Open access

Opportunities

Help and information

Multicomponent crystals of gliclazide and tromethamine: preparation, physico-chemical, and pharmaceutical characterization*

Abstract

Disclosure statement

Reprints and Corporate Permissions

Academic Permissions

Related research

To cite this article:

Download citation

Information for

Open access

Opportunities

Help and information

Keep up to date

Your download is now in progress and you may close this window

Login or register to access this feature

Multicomponent crystals of gliclazide and tromethamine: preparation, physico-chemical, and pharmaceutical characterization^*