• Journal of Pharmaceutical Investigation
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• v.34 no.1
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• pp.29-34
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• 2004

The solubility and stability of quercetin in various vehicles were determined. The solubility of quercetin at $28^{\circ}C$ increased in the rank order of isopropyl myristate < oleyl alcohol < propylene glycol monolaurate < oleoyl macrogol­6 glycerides < linoleoyl macrogol-6 glycerides < propylene glycol laurate (PGL) < propylene glycol monocaprylate (PGMC) < polyethylene glycol-8 glyceryl linoleate < caprylocaproyl macrogol-6 glycerides < diethylene glycol mono ethyl ether (DGME). The addition of DGME to non-aqueous vehicles such as PGL ad PGMC markedly increased the solubility of quercetin. From the stability studies, it was found that quercetin was unstable due to rapid oxidation by dissoved oxygen. The addition of a combination of ascorbic acid and edetic acid (EDTA) at 0.1 % markedly decreased the degradation rates of quercetin in 40% polyethylene glycol 400 in saline. Quercetin was relatively unstable in non-aqueous vehicles such as PGL and PGMC alone, and PGL-PGMC co-solvent The degradation of quercetin in such non-aqueous vehicles was fast, depending on temperature. The addition of butylated, hydroxytoluene, butylated hydroxyanisole, citric acid and/or EDTA at 0.1 % was effective in retarding the degradation of quercetin.

• Journal of Pharmaceutical Investigation
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• v.33 no.1
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• pp.45-49
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• 2003

The solubility and stability of ondansetron hydrochloride (OS) in various vehicles were determined. The effect of cyclodextrins (CD) on the solubility of OS in water was determined by equilibrium solubility method. The solubility of OS at $32^{\circ}C$ increased in the rank order of isopropyl myristate (IPM) < propylene glycol laurate (PGL) ${\ll}$ propylene glycol monolaurate < propylene glycol monocaprylate (PGMC) < poly(ethylene glycol) 400 < diethylene glycol mono ethyl ether (DGME) < ethanol < poly(ethylene glycol) 300 < water (36.1 mg/ml) ${\ll}$ propylene glycol (PG) (283 mg/ml). The addition of PG or DGME to non-aqueous vehicles such as IPM, PGL and PGMC markedly increased the solubility of OS. The addition of CDs in water increased the solubility. Apparent stability constant for the CD complexation with OS was calculated to be $25.5\;M^{-1}$ for $2-hydroxypropyl-{\beta}-CD\;(2HP{\beta}CD)$. Twenty mM ${\beta}-CD$, 69.4 mM sulfobutyl ether ${\beta}-CD$ and 115.4 mM $2HP{\beta}CD$ increased the aqueous solubilty of OS 1.27, 2.18 and 1.85 times, respectively. OS was stable in buffered aqueous solution (pH 5.0). However, OS was relatively unstable in non-aqueous vehicles in the order of PG

• Journal of Pharmaceutical Investigation
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• v.28 no.2
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• pp.121-126
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• 1998

The solubility and physicochemical stability of caroverine hydrochloride (CRV), an antispasmodic, in buffered aqueous solutions were studied using a reverse phase high performance liquid chromatography. The solubilty of the drug at pH 2.76-5.40 was similar at the range 31.9-36.2 mg/ml $(34^{circ}C)$, but, at the pH higher than 6.0, markedly decreased. The use of polyethylene glycol 400 as a cosolvent did not increase the solubility at any compositions examined. Moreover. increasing molar concentration of aqueous phosphate buffer from 0 to 0.5 M remarkably decreased the solubility. The degradation of CRY followed the apparent first-order kinetics. The degradation was accelerated with decreasing pH and increasing storage temperature. The half-lives for the degradation of CRY (1.0 mg/ml) at pH 1.28. 4.01 and 5.93 $(45^{\circ}C)$ were 2.8, 31.4 and 124 hr. respectively. The pHs of incubated solutions were to some extent lowered perhaps due to the formation of acidic degradation products. The addition of disodium edetate (0.01%) to the CRY solution (pH 4.95) retarded 2.5 times the degradation rate at $45^{\circ}C$, but the use of sodium bisulfite (0.1%) accelerated 2.9 times the rate. The activation energy for the CRY solution (20 mg/ml. pH 5.4) containing 0.01% EDTA was calculated to be 5.98 kcal/mole. When the solution was stored under nitrogen displacement in ampoule, there was no significant degradation even after 3 months at $40^{\circ}C$, indicating that protection from oxidation by air (oxygen) is essential for the complete stabilization of CRY solution.