کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2083348 1545333 2015 16 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Characterisation of selected active agents regarding pKa values, solubility concentrations and pH profiles by SiriusT3
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی بیوتکنولوژی یا زیست‌فناوری
پیش نمایش صفحه اول مقاله
Characterisation of selected active agents regarding pKa values, solubility concentrations and pH profiles by SiriusT3
چکیده انگلیسی


• pKa values and solubility properties of 34 APIs were determined using SiriusT3.
• Experimentally obtained, calculated and published pKa values showed good agreement.
• Measured and calculated intrinsic solubility values indicated several deviations.
• Solubility-pH profiles showed the expected shape and appearance.

The aim of this work was to determine pKa values and solubility properties of 34 active agents using the SiriusT3 apparatus. The selected drug substances belong to the groups of ACE-inhibitors, β-blockers, antidiabetics and lipid lowering substances. Experimentally obtained pKa and intrinsic solubility values were compared to calculated values (program ACD/ChemSketch) and pKa values to published data as well. Solubility-pH profiles were generated to visualise the substance solubility over the gastrointestinal pH range. The relationship between the solubility characteristic of a substance, its bioavailability and categorisation according to the Biopharmaceutics Classification System (BCS) was examined as well. The results showed a good agreement between experimentally obtained, calculated and published pKa values. The measured and calculated intrinsic solubility values indicated several major deviations. All solubility-pH profiles showed the expected shape and appearance for acids, bases or zwitterionic substances. The obtained results for the pKa and solubility measurements of the examined active agents may help to predict their physicochemical behaviour in vivo, and to understand the bioavailability of the substances according to their BCS categorisation. The easy and reproducible determination of pKa and solubility values makes the SiriusT3 apparatus a useful tool in early stages of drug and formulation development.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutics and Biopharmaceutics - Volume 92, May 2015, Pages 155–170
نویسندگان
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