RESEARCH ON ENHANCING THE SOLUBILITY OF 8mg CANDESARTAN TABLETS

Keywords: solubility, candesartan cilexetil, candesartan 8 mg, tablet

Candesartan cilexetil is a prodrug of angiotensin II receptor blocker

(ARB). It is an eﬀective antihypertensive but it has poor water solubility,

resulting in low oral bioavailability. Research objective: enhancing the

solubility of candesartan cilexetil to improve the bioavailability of the

drug. Research method: to use a solid dispersion system to increase the

solubility of candesartan cilexetil, thereby improving the bioavailability

of the drug. Research results: The solid dispersion was successfully pre-

pared by using polyethylene glycol 4000 (PEG 4000) as a hydrophilic car-

rier with a drug-to-polymer ratio of 1:3. The formulation (F8) consisted

of candesartan cilexetil (8 mg), PEG 4000 (24 mg), sodium starch glyco-

late (8 mg), FlowLac 100 (116.8 mg), and a lubricant blend of magnesium

stearate and talc (1.6 mg of each). Comparative in vitro dissolution test-

ing showed that the F8 exhibited significantly increased active substance

release compared to several generic products and it was comparable to

ATACAND®. The research confirms that the solid dispersion method

is a potential method for improving the biopharmaceutical performance

of poorly water-soluble drugs.