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Der Pharmacia Sinica
ISSN: 0976-8688
Eurosc i con Conference on
Medicinal Chemistry
and Biosimilars
M a r c h 2 5 - 2 6 , 2 0 1 9
B u d a p e s t , H u n g a r y
Medicinal Chemistry & Biosimilars 2019
S
tudies of drug-excipient compatibility represent an important phase in the preformulation stage of the development of
all dosage forms. In summary, knowledge of drug-excipient interactions is a necessary prerequisite to the development
of dosage forms that are stable and of good quality. Drug-excipient compatibility studies have been used as an approach for
accepting/rejecting excipients for use in pharmaceutical formulations, thus allowing the rapid optimization of a dosage form
with respect to patentability, processing, drug release, elegance, and physicochemical stability. To assess the drug-excipients
compatibility, the analytical techniques like differential scanning calorimetry (DSC) and Fourier Transform infrared spectroscopy
(FT-IR) and high performance liquid chromatography (HPLC) were adopted. Dapagliflozin is indicated for the management of
diabetes mellitus type 2, and functions to improve glycemic control in adults when combined with diet and exercise. Dapagliflozin
is a sodium-glucose cotransporter 2 inhibitor, which prevents glucose reabsorption in the kidney. Using dapagliflozin leads to
heavy glycosuria (glucose excretion in the urine), which can lead to weight loss and tiredness. Dapagliflozin was approved by
the FDA on Jan 08, 2014. Dapagliflozin is not recommended for patients with type 1 diabetes mellitus or for the treatment of
diabetic ketoacidosis. In the present study, the possible interactions between Dapagliflozin and some excipients (Microcrystalline
cellulose, lactose, anhydrous, crospovidone, silicon dioxide, magnesium stearate and film coating materials) were evaluated by
examining the pure drug or drug-excipient powder mixtures which were stored under different conditions (40 ± 2ºC, RH 75 ± 5%)
and different period (30, 90 and 180 days) using DSC, FT-IR and HPLC. No concrete evidence of interaction was observed between
drug and the
excipients.Onthe basis of the results obtained from DSC, FT-IR and HPLC studies, all the excipients used were found
to be compatible with the drug and can be used for the development of formulation.
kian.navaee@chemist.comEvaluation of drug-excipients interaction in
the formulation of dapagliflozin, a novel oral
antidiabetic drug, film-coated tablets
Kian Navaee and Fatemeh Soltani
Shahre Daru Pharmaceutical Co, Iran
Der Pharmacia Sinica 2019, Volume:10
DOI: 10.21767/0976-8688-C1-003