RPTLC determination of log<i>P</i>of structurally diverse neutral compounds

Völgyi, Gergely; Deák, Katalin; Vámos, J; Valkó, Klára; Takács‐Novák, Krisztina

doi:10.1556/jpc.21.2008.2.12

Cited by 15 publications

(12 citation statements)

References 24 publications

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“…The tendency of ketoconazole and miconazole to remain solubilized after dilution. Solvent systems comprising 0.1% polysorbate 80, 20% ethanol, and ammonium acetate (pH 3.1) and 100, 75 and 50 mg/mL ketoconazole and 30, 20, and 10 mg/mL miconazole were diluted tenfold with 0.9% sodium chloride infusion to reach final concentrations of 10 mg/mL, 7.5 mg/mL, and 5 mg/mL for ketoconazole and 3 mg/mL, 2 mg/mL and 1 mg/ mL for miconazole where log D (pH) is the apparent partition coefficient at a given pH, log P is the partitioning coefficient, the log D (pH) value of the azoles can be determined (34). Using Eqs.…”

Section: Optimizing the Concentration Of Excipientsmentioning

confidence: 99%

Composition Optimization and Stability Testing of a Parenteral Antifungal Solution based on a Ternary Solvent System

et al. 2010

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Abstract. An intravenous solution is a dosage forms intended for administration into the bloodstream. This route is the most rapid and the most bioavailable method of getting drugs into systemic circulation, and therefore it is also the most liable to cause adverse effects. In order to reduce the possibility of side effects and to ensure adequate clinical dosage of the formulation, the primarily formulated composition should be optimized. It is also important that the composition should retain its therapeutic effectiveness and safety throughout the shelf-life of the product. This paper focuses on the optimization and stability testing of a parenteral solution containing miconazole and ketoconazole solubilized with a ternary solvent system as model drugs. Optimization of the solvent system was performed based on assessing the risk/ benefit ratio of the composition and its properties upon dilution. Stability tests were conducted based on the EMEA (European Medicines Agency) "guideline on stability testing: stability testing of existing active substances and related finished products". Experiments show that both the amount of co-solvent and surface active agent of the solvent system could substantially be reduced, while still maintaining adequate solubilizing power. It is also shown that the choice of various containers affects the stability of the compositions. It was concluded that by assessing the risk/benefit ratio of solubilizing power versus toxicity, the concentration of excipients could be considerably decreased while still showing a powerful solubilizing effect. It was also shown that a pharmaceutically acceptable shelf-life could be assigned to the composition, indicating good long-term stability.

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Section: Optimizing the Concentration Of Excipientsmentioning

confidence: 99%

Composition Optimization and Stability Testing of a Parenteral Antifungal Solution based on a Ternary Solvent System

et al. 2010

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“…While the problem is very comprehensively discussed in the case of HPLC [24], comparative studies by TLC were almost undone. The papers published so far in this field describe a relationship between slope and intercept [25], an effect of a modifier on some steroids set [26], a comparison of several modifiers [27] and a trial to standardize the conditions [28], where acetone (while not water-like modifier) was proposed as the best choice.…”

Section: Introductionmentioning

confidence: 99%

Revisiting thin-layer chromatography as a lipophilicity determination tool—A comparative study on several techniques with a model solute set

Komsta

Skibiński

Berecka

et al. 2010

Journal of Pharmaceutical and Biomedical Analysis

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“…[107][108][109]. Recently, a validated RP-TLC method was proposed for parallel estimation of the lipophilicity of chemically diverse neutral compounds or weak acids and bases [110]. To cover a wide range of lipophilicity, two optimized RP-TLC systems were used: one for moderate lipophilic compounds (log P = 0 -3) and another for highly lipophilic molecules (log P = 3 -6).…”

Section: Potentiometric Methodsmentioning

confidence: 99%