Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation
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 effect...
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| Format: | Article |
| Language: | English |
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Sciendo
2016-12-01
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| Series: | Folia Veterinaria |
| Subjects: | |
| Online Access: | https://doi.org/10.1515/fv-2016-0040 |
| _version_ | 1818730389476212736 |
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| author | Šoltýsová I. Toropilová D. de Vringer T. |
| author_facet | Šoltýsová I. Toropilová D. de Vringer T. |
| author_sort | Šoltýsová I. |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-17T23:01:00Z |
| format | Article |
| id | doaj.art-21cb6954fa8246009b5c50a4bb8f2897 |
| institution | Directory Open Access Journal |
| issn | 2453-7837 |
| language | English |
| last_indexed | 2024-12-17T23:01:00Z |
| publishDate | 2016-12-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Folia Veterinaria |
| spelling | doaj.art-21cb6954fa8246009b5c50a4bb8f28972022-12-21T21:29:24ZengSciendoFolia Veterinaria2453-78372016-12-01604636910.1515/fv-2016-0040fv-2016-0040Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and SaturationŠoltýsová I.0Toropilová D.1de Vringer T.2University of Veterinary Medicine and Pharmacy, Institute of biology, zoology and radiobiology, Komenského 73, 041 81 Košice, The Slovakia RepublicUniversity of Veterinary Medicine and Pharmacy, Institute of biology, zoology and radiobiology, Komenského 73, 041 81 Košice, The Slovakia RepublicAstellas Pharma Europe BV, CTM Manufacturing Department, The NetherlandsActive 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.https://doi.org/10.1515/fv-2016-0040biopharmaceutics classification system – class ii drugslipid formulationsmaximum saturationspontaneous emulsification |
| spellingShingle | Šoltýsová I. Toropilová D. de Vringer T. Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation Folia Veterinaria biopharmaceutics classification system – class ii drugs lipid formulations maximum saturation spontaneous emulsification |
| title | Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation |
| title_full | Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation |
| title_fullStr | Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation |
| title_full_unstemmed | Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation |
| title_short | Lipid Based Formulations of Biopharmaceutics Classification System (BCS) Class II Drugs: Strategy, Formulations, Methods and Saturation |
| title_sort | lipid based formulations of biopharmaceutics classification system bcs class ii drugs strategy formulations methods and saturation |
| topic | biopharmaceutics classification system – class ii drugs lipid formulations maximum saturation spontaneous emulsification |
| url | https://doi.org/10.1515/fv-2016-0040 |
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