Abstract
The lists of essential medicines of the World Health Organization (WHO) and Brazil include gliclazide as an alternative to the oral antidiabetic drug of first choice, metformin, in the treatment of type 2 diabetes mellitus because of its pharmacokinetic profile and few side effects. Thus, it is also considered by WHO and the International Pharmaceutical Federation (FIP) as a drug candidate to biowaiver, which is the evaluation of how favorable the biopharmaceutics characteristics are in order to obtain waiver from the relative bioavailability/bioequivalence (RB/BE) studies to register new medicines. This paper presents a review about the solubility, permeability and dissolution of gliclazide. A critical analysis of the information allowed to identify gliclazide as a Biopharmaceutics Classification System (BCS) Class II drug. Therefore, new drugs in immediate release dosage forms will not be eligible for biowaiver. Regarding the extended release dosage forms, besides the limited solubility, no information on the comparative dissolution profile was found, which would be necessary to analyze a possible biowaiver for a smaller dosage. It can be concluded that the registration of new medicines containing gliclazide must undergo RB/BE studies, since there is not enough evidence to recommend the replacement and waiver of such studies for immediate and extended release formulations.
Highlights
Gliclazide is an oral antidiabetic drug (OAD) used to treat the most common type of diabetes mellitus, the type 2 (DM2), one of the most prevalent chronic non-transmissible diseases in the world, with estimated 463 million cases (20–79 years old) in 2019, accountable for high death rates and health costs worldwide [1]
The values found in the literature for the partition coefficient octanol-water (Log P) of gliclazide, obtained by in silico models, suggest high permeability of the drug, once the Log P values were higher than the reference value of metropolol (Log P = 1.72), a standard drug of high permeability
The development of biopharmaceutical studies to replace relative bioavailability/bioequivalence (RB/BE) studies should be encouraged, aiming at reducing the time and costs involved in the drug registration and development process
Summary
Gliclazide is an oral antidiabetic drug (OAD) used to treat the most common type of diabetes mellitus, the type 2 (DM2), one of the most prevalent chronic non-transmissible diseases in the world, with estimated 463 million cases (20–79 years old) in 2019, accountable for high death rates and health costs worldwide [1]. Gliclazide is considered an effective OAD, because it promotes good glycemic control and reduces the markers of endothelial inflammation and the risks of serious macrovascular and microvascular events combined [2]. The use of this drug is associated with a reduction in platelet hyperreactivity [6], low risk of hypoglycemia and excellent results in relation to long-term cardiovascular safety [7] It is an appropriate therapy for diabetic patients who do not obtain glycemic control only with an adequate diet [5] and it can be a therapy considered for patients with signs of partial failure of insulin production, with mild to moderate hyperglycemia, thin and oligosymptomatic [8,9]
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