The effects of formulation variables on apparent solubility and release characteristics of ibuprofen
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Aqueous solubility is an important pmualraatmieotne dr ievne flooprment studies of oral dosage forms as it is a determinant of oyr. Ialb bupiroaovfaeinl (abIiBl)i, wt hich is a chiral non-steroidal anti-inflammatory drug (NSAID), exisitosm eirni tc fwoo remnsa. Thnt e racemic form (racIB) is widely used clinically, although S (IB)+ i)-si tbuhper pofoetne (ntS isomer primarily responsible for the anti-inflammatory activitys. Ptudrieefso wrmeurlea ctiaornr ied out to identify the effect of solid and liquid additives on tavhieo sr oolfu tbihlei trya bceemhate and the isomer. The study also investigated the effect of feosr smuulcaht aiosn vrealreiaasbel controlling polymers on racemic ibuprofen tablet matrices. Eqe suoilluibbirliiutmy p shtausdies that were carried out on racIB and SIB in the presence of commcoanl p shoalrvmeanctesu itindicated that nonpolar solvents like PEG 300 and propylene igallylcyo li encxrpeoanseendt the aqueous solubility of both the compounds. Derivatized cycilnocdreexatsreidn ts ahelisro s olubility by molecular inclusion complexation. Comparison oofl eubqiuliiltiibersi sumh sowed that the S-form was solubilized to a greater extent trhma. n the racemic foFurther, binary solid dispersion sfyosrtmeumlsa ttehda tt wo serteu dy the effect of PEG 8000 on the dissolution rate of SIB showed p ions sitoilvueb cilhiatnyg. Thes e addition of nonionic ®surfactant (Pluronic (PL-F68)) to the dispersion system increased the release of SIB by about 70% at the end of 2 hrs, while the addition of anionic surfactant ((sodium lauryl sulfate (SLS)) resulted in more than 50% of the drug being released within 10 min, especially at low drug loadings. In general, the ternary systems fared much better than the binary systems for solubility enhancement. Physicochemical characterization by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD) indicated interstitial solid formation at low drug loadings. Finally, the effect of polymer blends on the dissolution rate and release kinetics of racemic ibuprofen from tablet matrices was studied. Carrageenans and cellulose ethers in combination prolonged ibuprofen release for up to 12-16 hrs and released the drug by non-Fickian (anomalous) mechanisms.