Analytical tools for the determination of pharmacokinetic parameters in vitro: case study with matrix metalloproteinase inhibitors
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| 1. Verfasser: | |
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| Format: | Abschlussarbeit Buch |
| Sprache: | English |
| Veröffentlicht: |
Münster
2016
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| Schlagworte: | |
| Online-Zugang: | Inhaltsverzeichnis Inhaltsverzeichnis |
| Beschreibung: | 205 Seiten Illustrationen 21 cm |
Internformat
MARC
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| 100 | 1 | |a Galla, Fabian |d 1987- |e Verfasser |0 (DE-588)1084809206 |4 aut | |
| 245 | 1 | 0 | |a Analytical tools for the determination of pharmacokinetic parameters in vitro |b case study with matrix metalloproteinase inhibitors |c vorgelegt von Fabian Galla |
| 264 | 1 | |a Münster |c 2016 | |
| 300 | |a 205 Seiten |b Illustrationen |c 21 cm | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
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| 502 | |b Dissertation |c Westfälische Wilhelms-Universität Münster |d 2016 | ||
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Datensatz im Suchindex
| _version_ | 1804176352347160576 |
|---|---|
| adam_text | CONTENT
1
INTRODUCTION.........................................................................................................................5
1.1 PHARMACOKINETICS AND PHARMACODYNAMICS
...........................................................
5
1 YY2 MATRIX
METALLOPROTEINASES..........................................................................................6
1 YY3 MATRIX METALLOPROTEINASE
INHIBITORS..........................................................................8
1.4 POSITRON EMISSION
TOMOGRAPHS................................................................................9
1.5
LIPOPHILICITY................................................................................................................11
1.6 PLASMA PROTEIN
BINDING............................................................................................13
1.7
BIOTRANSFORMATION.....................................................................................................14
1.7.1
METABOLJSM.........................................................................................................14
1.7.2 MODEL SYSTEMS FOR METABOLISM STUDIES 16
1.73 SEPARATION AND DETECTS
2 AIM OF THE
PROJECT.............................................................................................................19
3 RESULTS AND
DISCUSSION..................................................................................................21
3.1 LIPOPHLLICLTY OF
COMPOUNDS.....................................................................................21
3.1.1 CALCULATION OF CLOGP AND CLOGD
VALUES..........................................................21
3.1.2 MICRO SHAKE FLASK
METHOD...............................................................................23
3.2 PLASMA PROTEIN
BINDING...........................................................................................
34
3.2.1 DETERMINATION OF PLASMA PROTEIN BINDING BY HIGH PERFORMANCE
AFFINITY
CHROMATOGRAPHY....................................................................................34
3.2.2 DETERMINATION OF THE PLASMA PROTEIN BINDING BY
MICRODIALYSIS . ,. 45
3.3 IN SILICO, IN VITRO AND BIOMIMICRY METABOLISM STUDY 50
3.3.1 IN SILICO METABOLISM STUDY OF MMPIS 1-5 WITH
FAMF
50
3.3.2 IN VITRO METABOLISM STUDIES OF MMPIS 1 -5
...................................................
58
3.3.3 INSIGHTS INTO THE OXIDATIVE BIOTRANSFORMATICJN OF MINI-PEG CHAIN
CONTAINING MMPIS 4 AND
5...............................................................................94
4
SUMMARY......................................................................................................................119
4.1 DETERMINATION OF LOGDPH VALUES BY A MICRO SHAKE FLASK LC-MS METHOD
.YY_ 119
4.2 DETERMINATION OF PLASMA PROTEIN BINDING
..........................................................
120
4.3 IN SILICO AND IN VITRO METABOLISM STUDIES OF MMPIS 1-5
.YYYY..YY..YYYYYY.... 122
4.4 BIOTRANSFORMATION OF THE MN-PEG CHAINS OF MMPIS 4 AND
5.................... 123
5 EXPERIMENTAL
PART.......................................................................................................125
5.1
GENERAL....................................................................................................................125
5.1.1 PREPARATION OF DMSO STOCK SOLUTIONS
......................................................
125
5.1.2 PREPARATION OF
ALIQUOTS..................................................................................125
5.1.3 UPLC-UV
YY
QUADRUPOLE MASS SPECTROMETER
.................................................
126
5.1.4
HPLC-DAD-QTOF..........................................................................................126
5.2 DETERMINATION OF THE LIPOPHILICITY OF
COMPOUNDS..............................................127
5.2.1 IN SILICO PREDICTION OF THE LOGD
VALUE............................................................127
5.2.2 DETERMINATION OF THE LOGD VALUE WITH MICRO SHAKE FLASK AND
LC/MS... 127
5.3 PROTEIN
BINDING........................................................................................................131
5.3.1 HIGH PERFORMANCE AFFINITY
CHROMATOGRAPHY...............................................131
5.3.2
MICRODIALYSIS...................................................................................................132
5.4 METABOLISM
STUDY.................................................................................................135
5.4.1 IN SILICO PREDICTION OF POTENTIALLY METABOLIC LABILE POSITIONS OF
A.................
MOLECULE..........................................................................................................135
5.4.2 IN VITRO METABOLISM STUDY WITH MOUSE LIVER MICROSOME SUSPENSIONS
135
5.4.3 IN VITRO METABOLISM STUDY WITH RAT LIVER MICROSOME
SUSPENSION...YY 141
5.4.4 IN VITRO INCUBATION PROCEDURE WITH HUMAN LIVER MICROSOME
SUSPENSION143
5.4.5 IN VITRO STUDY OF METABOLITE
5-VII..................................................................145
5.4.6 MOUSE MICROSOMAL STABILITY OF MMP11
YY
4 AND 5 146
5.4.7 ANALYSIS OF BIOTRANSFORMATION OF MINI-PEG CHAIN OF MMPI 4 AND
5..... 147
6 IDENTIFICATION
PART..........................................................................................................152
6.1 IN SILICO ANALYSIS OF SOFT SPOTS OF METABOLISM
(SOM).YY.YYYYYYYYYY YY...YYYY... . 152
6.1.1
SOMSOFMMPI2........................................................................YYYYYYYY152
6.1.2
SOMSOFMMPI3..................................................YYYYYYYYYYYYYYYYYYYYYYYYYY153
6.1.3 SOM OF MMPI 5
..............................................................................................154
6.2 IN VITRO STUDY WITH IJVER MICROSOME
SUSPENSION...............................................155
6.2.1 IMIPRAMINE (11) AND ITS
METABOLITES............................................................155
6.2.2 BUFEXAMAC AND YYTS
METABOLITE......................................................................157
6.2.3 MMPI LAND ITS
METABOLITES...........................................................................159
6.2.4 MMPI 2 AND ITS
METABOJTESYY.YYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYY162
6.2.5 MMPI 3 AND ITS
METABOLITES...........................................................................165
6.2.6 MMPI 4 AND ITS
METABOLITES...........................................................................170
6.2.7
IP
X 5 AND TS
METABOLITES...........................................................................177
6.2.8 BIOTRANSFORMATION OF MINI-PEG CHAIN OF MMPI .............. 186
7 LIST OF
ACRONYMS...........................................................................................................
191
8
LITERATURE........................................................................................................................193
9 CURRICULUM
VITAE............................................................................................................204
|
| any_adam_object | 1 |
| author | Galla, Fabian 1987- |
| author_GND | (DE-588)1084809206 |
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| building | Verbundindex |
| bvnumber | BV043605527 |
| ctrlnum | (OCoLC)952060677 (DE-599)DNB1100197702 |
| discipline | Medizin |
| format | Thesis Book |
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| spelling | Galla, Fabian 1987- Verfasser (DE-588)1084809206 aut Analytical tools for the determination of pharmacokinetic parameters in vitro case study with matrix metalloproteinase inhibitors vorgelegt von Fabian Galla Münster 2016 205 Seiten Illustrationen 21 cm txt rdacontent n rdamedia nc rdacarrier Dissertation Westfälische Wilhelms-Universität Münster 2016 Biotransformation (DE-588)4006908-4 gnd rswk-swf Lipophiles Verhalten (DE-588)4279756-1 gnd rswk-swf Proteinbindung (DE-588)4047524-4 gnd rswk-swf Metalloproteinaseninhibitor (DE-588)4305228-9 gnd rswk-swf Pharmazeutische Analyse (DE-588)4174139-0 gnd rswk-swf (DE-588)4113937-9 Hochschulschrift gnd-content Pharmazeutische Analyse (DE-588)4174139-0 s Metalloproteinaseninhibitor (DE-588)4305228-9 s Lipophiles Verhalten (DE-588)4279756-1 s Proteinbindung (DE-588)4047524-4 s Biotransformation (DE-588)4006908-4 s DE-604 B:DE-101 application/pdf http://d-nb.info/1100197702/04 Inhaltsverzeichnis DNB Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=029019615&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Galla, Fabian 1987- Analytical tools for the determination of pharmacokinetic parameters in vitro case study with matrix metalloproteinase inhibitors Biotransformation (DE-588)4006908-4 gnd Lipophiles Verhalten (DE-588)4279756-1 gnd Proteinbindung (DE-588)4047524-4 gnd Metalloproteinaseninhibitor (DE-588)4305228-9 gnd Pharmazeutische Analyse (DE-588)4174139-0 gnd |
| subject_GND | (DE-588)4006908-4 (DE-588)4279756-1 (DE-588)4047524-4 (DE-588)4305228-9 (DE-588)4174139-0 (DE-588)4113937-9 |
| title | Analytical tools for the determination of pharmacokinetic parameters in vitro case study with matrix metalloproteinase inhibitors |
| title_auth | Analytical tools for the determination of pharmacokinetic parameters in vitro case study with matrix metalloproteinase inhibitors |
| title_exact_search | Analytical tools for the determination of pharmacokinetic parameters in vitro case study with matrix metalloproteinase inhibitors |
| title_full | Analytical tools for the determination of pharmacokinetic parameters in vitro case study with matrix metalloproteinase inhibitors vorgelegt von Fabian Galla |
| title_fullStr | Analytical tools for the determination of pharmacokinetic parameters in vitro case study with matrix metalloproteinase inhibitors vorgelegt von Fabian Galla |
| title_full_unstemmed | Analytical tools for the determination of pharmacokinetic parameters in vitro case study with matrix metalloproteinase inhibitors vorgelegt von Fabian Galla |
| title_short | Analytical tools for the determination of pharmacokinetic parameters in vitro |
| title_sort | analytical tools for the determination of pharmacokinetic parameters in vitro case study with matrix metalloproteinase inhibitors |
| title_sub | case study with matrix metalloproteinase inhibitors |
| topic | Biotransformation (DE-588)4006908-4 gnd Lipophiles Verhalten (DE-588)4279756-1 gnd Proteinbindung (DE-588)4047524-4 gnd Metalloproteinaseninhibitor (DE-588)4305228-9 gnd Pharmazeutische Analyse (DE-588)4174139-0 gnd |
| topic_facet | Biotransformation Lipophiles Verhalten Proteinbindung Metalloproteinaseninhibitor Pharmazeutische Analyse Hochschulschrift |
| url | http://d-nb.info/1100197702/04 http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=029019615&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
| work_keys_str_mv | AT gallafabian analyticaltoolsforthedeterminationofpharmacokineticparametersinvitrocasestudywithmatrixmetalloproteinaseinhibitors |
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