Study of equilibrium solubility measurement by saturation shake-flask method using hydrochlorothiazide as model compound

Baka, Edit; Comer, John; Takács‐Novák, Krisztina

doi:10.1016/j.jpba.2007.10.030

Cited by 381 publications

(248 citation statements)

References 22 publications

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“…The reviewed publications showed that different grades of water were used as media to determine the solubility of drug substance: double-distilled water (6)(7)(8); double deionized water (9), Milli-Q® purified water (10), 18.2 MΩ.cm/ 0.22 μm (11); Milli-Q®ultrapure water, conductivity less than 0.1 μS cm (12,13); ultrapure water Elix® Millipore (14); distilled water (5,15-21) deionized water (22)(23)(24)(25)(26); distilled, deionized, and filtered water (27); purified water (28)(29)(30)(31)(32)(33)(34)(35)(36); demineralized water (37). The type of water was not specified in 19 of 51 studies (37%) (38)(39)(40)(41)(42)(43)(44)(45)(46)(47)(48)(49)(50)(51)(52)(53)(54)(55)(56).…”

Section: Watermentioning

confidence: 99%

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Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

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Abstract.The introduction of the biopharmaceutics drug classification system (Biopharmaceutics Classification System (BCS)), in 1995, provided a simple way to describe the biopharmaceutics behavior of a drug. Solubility and permeability are among the major parameters, which determine the fraction dose absorbed of a drug substance and consequently its chances to be bioavailable. The purpose of this review is to summarize the evolution of the media used for determining solubility and dissolution and how this can be used in modern drug development. Over the years, physiologically adapted media and buffers were introduced with the intention to better predict the in vivo solubility and dissolution of drug substances. Water, buffer solutions, compendial media, micellar solubilization media, and biorelevant media are reviewed. At this time point, there is no universal medium available which can be used to predict every drug substance's solubility or a drug product's in vivo dissolution behavior. However, there have been many improvements and additions made to media to optimize their in vivo predictability; for example, the current phosphate concentrations in buffers seem to be too high to correlate with the carbonate buffer concentrations in vivo. Biorelevant media were updated to correlate them better with the composition of human intestinal fluids. The BCS was introduced into regulatory sciences as a scientific risk management tool to waive bioequivalence studies under certain conditions. Today's different guidance documents define the dose-solubility ratio differently. As shown for amoxicillin, this can cause more confusion than certainty for globally operating companies. Harmonization of BCS guidelines is highly desirable.

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Section: Watermentioning

confidence: 99%

“…Maleate (32), Britton-Robinson universal (19,25,39), and glycine buffers (31) were selected, respectively, in the rate of 2.2% (1 out of 46 studies), 6.5% (3 out of 46 studies), and 2.2% (1 out of 46 studies), for the shake-flask method.…”

Section: Buffer Solutionsmentioning

confidence: 99%

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

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“…With its poor aqueous solubility in the physiological pH-range and its high intestinal permeability Celecoxib has been established as a proper candidate for BA enhancement via lipid-based formulations. Solubility screening of Celecoxib in different oils was performed with a slightly modified saturation shake-flask method [27][28][29] : in a 2 mL sample vial an excess of Celecoxib was added to 1 mL oil. The resulting suspensions were subjected to moderate agitation (150 rpm) in a mechanical shaker (IKA KS 3000 I Control, Staufen, Germany) for 48 h at 50 C and then allowed to equilibrate at 50 C for another 15 min.…”

Section: Solubility Studiesmentioning

confidence: 99%

Enzymatically Modified Shea Butter and Palm Kernel Oil as Potential Lipid Drug Delivery Matrices

Obitte

Zorn

Oroz‐Guinea

et al. 2018

Euro J Lipid Sci & Tech

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Drug formulations based on lipids can enable a significantly better delivery of a pharmaceutically active substance and thus enhance their bioavailability. However, natural fats and oils usually have properties, which do not allow their direct use for drug delivery. Therefore, we have modified palm kernel oil (PKO) and shea butter (SB) via lipase-catalyzed transesterification using either glycerol -to create a diglyceride-enriched lipid -or using hexanoic acid via acidolysis -to alter their fatty

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“…The equilibrium CN solubility in diverse formulations was determined according to previously reported studies (Baka, Comer, Takács-Novák, 2008) with some modifications. After at least a three-day equilibration period, samples were withdrawn, centrifuged, and assayed using ultra-performance liquid chromatography (UPLC) (Abdel-Hamid et al, 2012;Shahba, Mohsin, Alanazi, 2012a).…”

Section: Equilibrium Solubility Studiesmentioning

confidence: 99%

Optimization of self-nanoemulsifying formulations for weakly basic lipophilic drugs: role of acidification and experimental design

Shahba

Kazi

Alanazi

et al. 2016

Braz. J. Pharm. Sci.

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Formulators face great challenges in adopting systematic approaches for designing self-nanoemulsifying formulations (SNEFs) for different drug categories. In this study, we aimed to build-up an advanced SNEF development framework for weakly basic lipophilic drugs, such as cinnarizine (CN). First, the influence of formulation acidification on CN solubility was investigated. Second, formulation self-emulsification in media with different pH was assessed. Experimentally designed phase diagrams were also utilized for advanced optimization of CN-SNEF. Finally, the optimized formulation was examined using cross polarizing light microscopy for the presence of liquid crystals. CN solubility was significantly enhanced upon external and internal acidification. Among the various fatty acids, oleic acid-based formulations showed superior self-emulsification in all the tested media. Surprisingly, formulation turbidity and droplet size significantly decreased upon equilibration with CN. The design was validated using oleic acid/ Imwitor308/Cremophor El (25/25/50), which showed excellent self-nanoemulsification, 43-nm droplet size (for CN-equilibrated formulations), and 88 mg/g CN solubility. In contrast to CN-free formulations, CN-loaded SNEF presented lamellar liquid crystals upon 50% aqueous dilution. These findings confirmed that CN-SNEF efficiency was greatly enhanced upon drug incorporation. The adopted strategy offers fast and accurate development of SNEFs and could be extrapolated for other weakly basic lipophilic drugs. Uniterms: Self-nanoemulsifying formulations/solubility. Cinnarizine/lipophilic drugs. Acidification/ experimental design. Solubility enhancement.

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Study of equilibrium solubility measurement by saturation shake-flask method using hydrochlorothiazide as model compound

Cited by 381 publications

References 22 publications

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Enzymatically Modified Shea Butter and Palm Kernel Oil as Potential Lipid Drug Delivery Matrices

Optimization of self-nanoemulsifying formulations for weakly basic lipophilic drugs: role of acidification and experimental design

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