Abstract

PATENT STUDY FOR THE PROCESS OF SYNTHESIS OF GLICLAZIDE AND COMPOSITIONS WITH MODIFIED RELEASE CONTAINING THE SAME ACTIVE SUBSTANCE

Nadezhda I. Marchokova, Valentina B. Petkova* and Milen V. Dimitrov

ABSTRACT

Background: Sulfonylurea drugs are widely used for treatment of diabetes mellitus type 2 and from this group Gliclazide is mainly prescribed. The study aimed to summarize the available in ESPACENET database information for applications and granted patents which concerned process of synthesis/preparation of the active substance as well as for compositions with modified-release containing it. Methods: Patent status study was conducted for the period from 2000 to January 2018. The EPO database and especially the ESPACENET database was used. Documents found were divided into two main groups, namely for process of synthesis of active substance and for compositions with modified-release which contain gliclazide. Each group was subdivided into granted patents and applications of patent by using the International Patent Documentation (INPADOC) information. Results: Seven documents were found for process of synthesis of active substance - 3 granted patents and 4 applications for patent. For compositions with modified-release containing gliclazide were found 30 documents in the database – 14 granted patents and 16 patent applications. Seven of the applications found were at phase of substantive examination and four-PCT applications have not entered in European phase. Mainly the protection claimed in above mentioned documents was for composition (30) and technological approach (25). There were also claims for application of drug product, dissolution profile, particle size of the active substance, related substances, and equipment. Patent families were found for 4 granted patents and 6 applications for patent. Conclusion: In conclusion the period was characterized with relatively low activity of issuing of patents and submission of applications for patents for the process of gliclazide synthesis and compositions with modified-release of the active substance.

Keywords: Gliclazide, process of synthesis, active substance, modified-release composition, patent application, granted patent.