Solubilization of flavopiridol by pH control combined with cosolvents, surfactants, or complexants

Li, Ping; Tabibi, S. Esmail; Yalkowsky, Samuel H.

doi:10.1021/js990097r

Cited by 59 publications

(25 citation statements)

References 4 publications

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“…It is accepted that basic molecule ionize at low pH and cause increased interaction between the drug and solvent molecules and hence increase in the solubility. 29) Mirabegron was found to have a higher solubility at lower pH (12933 µg/mL at pH 1), while reversed trend was observed at higher pH (116 µg/ mL at pH 6). On the other hand, the LS salt/complex significantly reduced solubility and showed pH-independent solubility, which comprised 87, 87, and 95 µg/mL at pH 1, 3, and 6, respectively.…”

Section: Solubility Of Salts/complexesmentioning

confidence: 89%

Oral Sustained Release of a Hydrophilic Drug Using the Lauryl Sulfate Salt/Complex

Kasashima

Yoshihara

Yasuji

et al. 2016

CHEMICAL & PHARMACEUTICAL BULLETIN

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The objective of this study was to establish the key factor of the lauryl sulfate (LS) salt/complex for sustained release of a hydrophilic drug at various physiological pH levels. Mirabegron is a hydrophilic drug that exhibits pH-dependent solubility. Sodium lauryl sulfate (SLS) bound to mirabegron in a stoichiometric manner. The formation of the LS salt/complex significantly reduced mirabegron solubility and helped achieve sustained release of mirabegron over a wide range of pH levels. In addition to SLS, other additives containing a sulfate group formed salts/complexes with mirabegron and reduced its solubility at different pH levels. Furthermore, octyl sulfate (OS), myristyl sulfate (MS), and cetyl sulfate (CS) salts/complexes, which contain alkyl chains of different lengths, showed a lower solubility than mirabegron and promoted sustained release of mirabegron. The rank order of solubility and dissolution rate were as follows: OS salt/complex>LS salt/ complex>MS salt/complex>CS salt/complex, which corresponded to the rank of alkyl chain lengths. We conclude that the presence of a sulfate group and the length of the alkyl chain are key factors of the LS salt/ complex for sustained release of a hydrophilic drug at various physiological pH levels.

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Section: Solubility Of Salts/complexesmentioning

confidence: 89%

Oral Sustained Release of a Hydrophilic Drug Using the Lauryl Sulfate Salt/Complex

Kasashima

Yoshihara

Yasuji

et al. 2016

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…The combination of hydrotropes and cosolvent solubilization was also explored to improve the solubility of celecoxib [8][9][10][11] . The role of solvent in hydrotropic solubilization was observed by studying the effect of different hydrotropes like piperazine (3.0 M), urea (4.8 M) in combination with cosolvents PEG 600, PEG 400, PEG 200 and Eth as shown in Table 4 14-18 .…”

Section:  Solubilization Studies Using Combination Of Cosolvents Andmentioning

confidence: 99%

“…This suggested that the ability of a solvent to be hydrogen donor must be a key factor in solutropic solubilization phenomenon and there is no correlation between solvent polarity and hydrotropic solubilization (8)(9)(10)(11).…”

Section: Figure 11: Phase Solubility Diagram Of Celecoxib In Differenmentioning

confidence: 99%

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2012

IJPSR

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Celecoxib, a diaryl substituted pyrazole, is practically insoluble in water which precludes its use in parenteral and liquid dosage forms. This study explores the solubility enhancement of celecoxib using hydrotropy and cosolvency solubilization approaches. The equilibrium solubility studies were performed using hydrotropes piperazine, sodium citrate, and urea and cosolvents PEG 200, PEG 400, PEG 600, DMA, Ethanol and Propylene glycol at various temperatures. Parenteral formulations using hydrotrope and cosolvents were developed and studied for accelerated stability study. The solubility of celecoxib was found to increase upto 45 times in 3M piperazine solution and upto 10232 times in PEG 600 at 25±2 0 C. The results of solubilization study showed that the increase in solubility of celecoxib is smaller in piperazine and urea when used alone as compared to the increase in solubility which was found when these hydrotropes were used in combination with cosolvents PEG 600, PEG 400, DMA and Eth. Stability studies indicated that all the formulations stored were found to be stable for drug content, pH and change in physical appearance i.e. color, precipitation.

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“…At equilibrium, there is a dynamic, balanced process of dissolution of the solid into solution and recrystallization of the drug from solution. The molar aqueous solubility (S W ) can be empirically correlated to activity and crystal lattice energy via the general solubility equation (GSE) proposed by Yalkowsky (4,5): There are multiple computational tools for prediction of aqueous solubility including ACD Labs, COSMO-RS, QikPro, and others (6).…”

Section: Introductionmentioning

confidence: 99%

Determination of Thermodynamic Solubility of Active Pharmaceutical Ingredients for Veterinary Species: A New USP General Chapter

Apley¹,

Crist²,

Fellner³

et al. 2017

Dissolution Technol.

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Solubilization of flavopiridol by pH control combined with cosolvents, surfactants, or complexants

Cited by 59 publications

References 4 publications

Oral Sustained Release of a Hydrophilic Drug Using the Lauryl Sulfate Salt/Complex

Oral Sustained Release of a Hydrophilic Drug Using the Lauryl Sulfate Salt/Complex

Untitled

Determination of Thermodynamic Solubility of Active Pharmaceutical Ingredients for Veterinary Species: A New USP General Chapter

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