<abstract xmlns="http://www.w3.org/1999/xhtml"><p>Active ingredients in pharmaceuticals differ by their physico-chemical properties and their bioavailability therefore varies. The most frequently used and most convenient way of administration of medicines is oral, however many drugs are little soluble in water. Thus they are not sufficiently effective and suitable for such administration. For this reason a system of lipid based formulations (LBF) was developed. Series of formulations were prepared and tested in water and biorelevant media. On the basis of selection criteria, there were selected formulations with the best emulsification potential, good dispersion in the environment and physical stability. Samples of structurally different drugs included in the Class II of the Biopharmaceutics classification system (BCS) were obtained, namely Griseofulvin, Glibenclamide, Carbamazepine, Haloperidol, Itraconazol, Triclosan, Praziquantel and Rifaximin, for testing of maximal saturation in formulations prepared from commercially available excipients. Methods were developed for preparation of formulations, observation of emulsification and its description, determination of maximum solubility of drug samples in the respective formulation and subsequent analysis. Saturation of formulations with drugs showed that formulations 80 % XA and 20 % Xh, 35 % XF and 65 % Xh were best able to dissolve the drugs which supports the hypothesis that it is desirable to identify limited series of formulations which could be generally applied for this purpose.</p></abstract>

Active ingredients in pharmaceuticals differ by their physico-chemical properties and their bioavailability therefore varies. The most frequently used and most convenient way of administration of medicines is oral, however many drugs are little soluble in water. Thus they are not sufficiently effective and suitable for such administration. For this reason a system of lipid based formulations (LBF) was developed. Series of formulations were prepared and tested in water and biorelevant media. On the basis of selection criteria, there were selected formulations with the best emulsification potential, good dispersion in the environment and physical stability. Samples of structurally different drugs included in the Class II of the Biopharmaceutics classification system (BCS) were obtained, namely Griseofulvin, Glibenclamide, Carbamazepine, Haloperidol, Itraconazol, Triclosan, Praziquantel and Rifaximin, for testing of maximal saturation in formulations prepared from commercially available excipients. Methods were developed for preparation of formulations, observation of emulsification and its description, determination of maximum solubility of drug samples in the respective formulation and subsequent analysis. Saturation of formulations with drugs showed that formulations 80 % XA and 20 % Xh, 35 % XF and 65 % Xh were best able to dissolve the drugs which supports the hypothesis that it is desirable to identify limited series of formulations which could be generally applied for this purpose.

Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation

Astellas Pharma Europe BV, CTM Manufacturing Department, The

Folia Veterinaria

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Active ingredients in pharmaceuticals differ by their physico-chemical properties and their bioavailability therefore varies. The most frequently used and most...

Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation

Publié en ligne: 28 déc. 2016

Pages: 63 - 69

DOI: https://doi.org/10.1515/fv-2016-0040

Mots clés
biopharmaceutics classification system – class II drugs, lipid formulations, maximum saturation, spontaneous emulsification

© 2016 Šoltýsová, I. et al., published by De Gruyter Open

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation

Publié en ligne: 28 déc. 2016

Pages: 63 - 69

DOI: https://doi.org/10.1515/fv-2016-0040

Mots clésbiopharmaceutics classification system – class II drugs, lipid formulations, maximum saturation, spontaneous emulsification

© 2016 Šoltýsová, I. et al., published by De Gruyter Open

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Mots clés
biopharmaceutics classification system – class II drugs, lipid formulations, maximum saturation, spontaneous emulsification