Springs and parachutes: development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe
Gespeichert in:
| 1. Verfasser: | |
|---|---|
| Format: | Abschlussarbeit Buch |
| Sprache: | English |
| Veröffentlicht: |
Würzburg
2017
|
| Schlagworte: | |
| Online-Zugang: | Inhaltsverzeichnis Volltext Inhaltsverzeichnis |
| Beschreibung: | VIII, 147 Seiten Illustrationen, Diagramme 30 cm |
Internformat
MARC
| LEADER | 00000nam a2200000 c 4500 | ||
|---|---|---|---|
| 001 | BV044734105 | ||
| 003 | DE-604 | ||
| 005 | 20180625 | ||
| 007 | t | ||
| 008 | 180129s2017 gw a||| m||| 00||| eng d | ||
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| 040 | |a DE-604 |b ger |e rda | ||
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| 100 | 1 | |a Terveer, Nils |d ca. 21. Jh. |e Verfasser |0 (DE-588)1151450839 |4 aut | |
| 245 | 1 | 0 | |a Springs and parachutes |b development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe |c vorgelegt von Nils Terveer aus Kiel |
| 246 | 1 | 1 | |a Sprungfedern und Fallschirme |
| 264 | 1 | |a Würzburg |c 2017 | |
| 300 | |a VIII, 147 Seiten |b Illustrationen, Diagramme |c 30 cm | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
| 338 | |b nc |2 rdacarrier | ||
| 502 | |b Dissertation |c Julius-Maximilians-Universität Würzburg |d 2017 | ||
| 546 | |a Zusammenfassung in deutscher und englischer Sprache | ||
| 650 | 0 | 7 | |a Wirkstoff |0 (DE-588)4066383-8 |2 gnd |9 rswk-swf |
| 650 | 0 | 7 | |a Imatinib mesilat |0 (DE-588)4709581-7 |2 gnd |9 rswk-swf |
| 650 | 0 | 7 | |a Wasserlöslichkeit |0 (DE-588)4273707-2 |2 gnd |9 rswk-swf |
| 650 | 0 | 7 | |a Arzneimittelforschung |0 (DE-588)4003120-2 |2 gnd |9 rswk-swf |
| 653 | |a Springs and Parachutes | ||
| 653 | |a Formulation development | ||
| 653 | |a Poorly water soluble drugs | ||
| 653 | |a ionic liquids | ||
| 653 | |a Imatinib | ||
| 655 | 7 | |0 (DE-588)4113937-9 |a Hochschulschrift |2 gnd-content | |
| 689 | 0 | 0 | |a Wirkstoff |0 (DE-588)4066383-8 |D s |
| 689 | 0 | 1 | |a Wasserlöslichkeit |0 (DE-588)4273707-2 |D s |
| 689 | 0 | 2 | |a Arzneimittelforschung |0 (DE-588)4003120-2 |D s |
| 689 | 0 | 3 | |a Imatinib mesilat |0 (DE-588)4709581-7 |D s |
| 689 | 0 | |5 DE-604 | |
| 776 | 0 | 8 | |i Erscheint auch als |n Online-Ausgabe |o urn:nbn:de:bvb:20-opus-154311 |a Terveer, Nils |t Springs and Parachutes - Development and Characterization of Novel Formulations for Poorly Water-Soluble Drugs |d Würzburg : Universität Würzburg, 2017 |h Online-Ressource |
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| 856 | 4 | 1 | |u https://nbn-resolving.org/urn:nbn:de:bvb:20-opus-154311 |x Resolving-System |z kostenfrei |3 Volltext |
| 856 | 4 | 2 | |m DNB Datenaustausch |q application/pdf |u http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=030130114&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |3 Inhaltsverzeichnis |
| 912 | |a ebook | ||
| 999 | |a oai:aleph.bib-bvb.de:BVB01-030130114 | ||
Datensatz im Suchindex
| _version_ | 1804178232336973824 |
|---|---|
| adam_text | TABLE OF CONTENTS
TABLE OF
CONTENTS..........................................................................................................
ILL
1
INTRODUCTION.................................................................................................................3
1.1 SPRINGS &
PARACHUTES..................................................................................................
4
1.2 FORMULATION STRATEGIES FOR POORLY WATER-SOLUBLE
DRUGS......................................4
1.2.1 IONIC LIQUID A
PPROACH........................................................................................5
1.2.2 COMPLEXATION WITH
CYCLODEXTRINS...................................................................
6
1.2.3 MICROEMULSION ORAL FORMULATIONS
...................
9
1.2.4 SOLID
DISPERSIONS..............................................................................................
10
1.2.5
COCRYSTALS..................................................................
11
1.3 REFERENCES
..................
13
2 AIM OF THE TH E S IS
.......................................................................................................23
3
RESULTS...........................................................................................................................
27
3.1 IONIC LIQUID CONCEPT TO IMPROVE THE SOLUBILITY PROFILE OF THE
TYROSINE-KINASE
INHIBITOR
IMATINIB........................................................................................................27
A
BSTRACT.......................................................................................................................
27
INTRODUCTION................................................................................................................
28
MATERIALS AND
METHODS.............................................................................................
29
MATERIALS...........................................................................................................29
PREPARATION OF IMATINIB FREE BASE
29
PREPARATION OF
ILS..............................................................................................30
PREPARATION OF SODIUM SALTS OF THE COUNTERIONS
..............................................
30
NUCLEAR MAGNETIC RESONANCE MEASUREMENTS
.................................................
30
X-RAY POWDER
DIFFRACTOMETRY.............................................................................31
DIFFERENTIAL SCANNING
CALORIMETRY......................................................................31
WATER VAPOUR
SORPTION......................................................................................32
PHOTOMETRICAL DETERMINATION OF DISSOLUTION RATES
..........................................
32
24 H SOLUBILITY
PROFILES.......................................................................................32
DETERMINATION OF PKA VALUES OF COUNTERIONS AND IMATINIB MESYLATE
...............
33
EXTRAPOLATION OF PKA VALUES OF THE COUNTERIONS TO METHANOL ACCORDING TO
THE
PROCEDURE OF YASUDA AND SHEDLOVSKY[17,18]
.......................................................
33
STABILITY TESTING OF
ILS.......................................................................................33
RESULTS..........................................................................................................................
34
PREPARATION AND PHYSICOCHEMICAL CHARACTERISTICS OF IMATINIB ILS
...................
34
DISSOLUTION RATE AND 24 H SOLUBILITY
.................................................................
40
DISCUSSION....................................................................................................................43
CONCLUSION....................................................................................................................46
ACKNOWLEDGMENTS.....................................................................................................
46
REFERENCES,
47
3.2 OVERCOMING SOLUBILITY CHALLENGES OF TRIAZOLOPYRIMIDINE
NOX-INHIBITORS
......
51
A
BSTRACT.......................................................................................................................51
INTRODUCTION................................................................................................................
52
MATERIALS AND
METHODS............................................................................................
53
MATERIALS..........................................................................................................
53
PHYSICOCHEMICAL CHARACTERIZATION OF THE STARTING PRODUCTS
...........................
54
EXECUTION OF THREE DIFFERENT FORMULATION APPROACHES
...................................
56
CYCLODEXTRIN FORMULATION FOR I.V.
APPLICATION...................................................64
STATISTICS...........................................................................................................64
RESULTS.........................................................................................................................65
PHYSICOCHEMICAL CHARACTERIZATION OF VAS
COMPOUNDS..................................65
CHARACTERIZATION OF THE SPRAY DRIED
FORMULATIONS...........................................66
DISSOLUTION OF VAS3947 FROM SPRAY DRIED
FORMULATIONS.................................67
EXCIPIENT SCREENING AND CHARACTERIZATION OF MICROEMULSIONS
.........................
71
DISSOLUTION OF VAS3947 FROM
MICROEMULSIONS.................................................72
NUCLEAR MAGNETIC RESONANCE
MEASUREMENTS.................................................79
VAS3947 - CYCLODEXTRIN FORMULATION FOR I.V. APPLICATION
.................................
81
DISCUSSION.......................................................................................
82
CONCLUSION..................................................................................................................
86
ACKNOWLEDGEMENTS..................................................................................................
86
REFERENCES..................................................................................................................
87
3.3 APPENDIX TO CHAPTER 3.2 - OVERCOMING SOLUBILITY CHALLENGES OF
TRIAZOLOPYRIMIDINE
NOX-INHIBITORS.........................................................................
91
MATERIALS AND
METHODS..............................................................................................
91
MATERIALS............................................................................................................
91
INSTRUMENTS........................................................................................................
92
CHROMATOGRAPHIC CONDITIONS FOR THE GUANTITATIVE DETERMINATION OF VAS3947
92
METHOD
VALIDATION.............................................................................................93
PREPARATION OF
VAS3947....................................................................................95
RESULTS...........................................................................................................................
97
DEVELOPMENT AND VALIDATION OF AN HPLC METHOD FOR THE GUANTITATIVE
DETERMINATION OF
VAS3947................................................................................97
REFERENCES..................................................................................................................100
3.4 TRIAZOLOPYRIMIDINES AS NOX-INHIBITORS: LIMITED DRUG STABILITY OF
VAS3947
HINDERING INVESTIGATION OF ROS FORMATION BY NADPH OXIDASES AND
PREVENTING FURTHER CLINICAL
DEVELOPMENT...........................................................
101
A B
STRACT......................................................................................................................
101
INTRODUCTION................................................................................................................102
MATERIALS AND
METHODS............................................................................................103
MATERIALS..........................................................................................................
103
INSTRUMENTS
.................................................................................
104
STABILITY
TESTING...............................................................................................
105
PRODUCTION AND ISOLATION OF DEGRADATION PRODUCTS
........................................
106
CHROMATOGRAPHIC CONDITIONS FOR MASS ANALYSIS
............................................
106
MICROSOMAL
ASSAY..........................................................................................
107
PLASMA STABILITY
ASSESSMENT.........................................................................
107
CACO-2 CELL
ASSAY..........................................................................................
108
CYTOTOXICITY....................................................................................................
109
NUCLEAR MAGNETIC RESONANCE MEASUREMENTS
...............................................
110
RESULTS.......................................................................................................................
111
PHOTOSTABILITY..................................................................................................
111
MICROSOMAL
ASSAY..........................................................................................
112
PLASMA
STABILITY..............................................................................................
113
CACO-2 CELL
ASSAY..........................................................................................
115
CYTOTOXICITY....................................................................................................
116
DISCUSSION.................................................................................................................117
CONCLUSION.................................................................................................................118
ACKNOWLEDGEMENTS................................................................................................
119
REFERENCES.................................................................................................................119
4 FINAL
DISCUSSION......................................................................................................125
5 SU M M A R Y
..................................
135
5.1
ZUSAMMENFASSUNG..............................................................................................
137
6 APPENDIX
................................................................................
;......................................143
6.1 DOCUMENTATION OF AUTHORSHIP
.................................................................................
143
6.2 LIST OF
ABBREVIATIONS..................................................................................................146
|
| any_adam_object | 1 |
| author | Terveer, Nils ca. 21. Jh |
| author_GND | (DE-588)1151450839 |
| author_facet | Terveer, Nils ca. 21. Jh |
| author_role | aut |
| author_sort | Terveer, Nils ca. 21. Jh |
| author_variant | n t nt |
| building | Verbundindex |
| bvnumber | BV044734105 |
| classification_rvk | VX 5070 |
| collection | ebook |
| ctrlnum | (OCoLC)1136410148 (DE-599)DNB1148786643 |
| discipline | Chemie / Pharmazie |
| format | Thesis Book |
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| id | DE-604.BV044734105 |
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| indexdate | 2024-07-10T08:00:42Z |
| institution | BVB |
| language | English |
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| physical | VIII, 147 Seiten Illustrationen, Diagramme 30 cm |
| psigel | ebook |
| publishDate | 2017 |
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| spelling | Terveer, Nils ca. 21. Jh. Verfasser (DE-588)1151450839 aut Springs and parachutes development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe vorgelegt von Nils Terveer aus Kiel Sprungfedern und Fallschirme Würzburg 2017 VIII, 147 Seiten Illustrationen, Diagramme 30 cm txt rdacontent n rdamedia nc rdacarrier Dissertation Julius-Maximilians-Universität Würzburg 2017 Zusammenfassung in deutscher und englischer Sprache Wirkstoff (DE-588)4066383-8 gnd rswk-swf Imatinib mesilat (DE-588)4709581-7 gnd rswk-swf Wasserlöslichkeit (DE-588)4273707-2 gnd rswk-swf Arzneimittelforschung (DE-588)4003120-2 gnd rswk-swf Springs and Parachutes Formulation development Poorly water soluble drugs ionic liquids Imatinib (DE-588)4113937-9 Hochschulschrift gnd-content Wirkstoff (DE-588)4066383-8 s Wasserlöslichkeit (DE-588)4273707-2 s Arzneimittelforschung (DE-588)4003120-2 s Imatinib mesilat (DE-588)4709581-7 s DE-604 Erscheint auch als Online-Ausgabe urn:nbn:de:bvb:20-opus-154311 Terveer, Nils Springs and Parachutes - Development and Characterization of Novel Formulations for Poorly Water-Soluble Drugs Würzburg : Universität Würzburg, 2017 Online-Ressource B:DE-101 application/pdf http://d-nb.info/1148786643/04 Inhaltsverzeichnis https://nbn-resolving.org/urn:nbn:de:bvb:20-opus-154311 Resolving-System kostenfrei Volltext DNB Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=030130114&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Terveer, Nils ca. 21. Jh Springs and parachutes development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe Wirkstoff (DE-588)4066383-8 gnd Imatinib mesilat (DE-588)4709581-7 gnd Wasserlöslichkeit (DE-588)4273707-2 gnd Arzneimittelforschung (DE-588)4003120-2 gnd |
| subject_GND | (DE-588)4066383-8 (DE-588)4709581-7 (DE-588)4273707-2 (DE-588)4003120-2 (DE-588)4113937-9 |
| title | Springs and parachutes development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe |
| title_alt | Sprungfedern und Fallschirme |
| title_auth | Springs and parachutes development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe |
| title_exact_search | Springs and parachutes development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe |
| title_full | Springs and parachutes development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe vorgelegt von Nils Terveer aus Kiel |
| title_fullStr | Springs and parachutes development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe vorgelegt von Nils Terveer aus Kiel |
| title_full_unstemmed | Springs and parachutes development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe vorgelegt von Nils Terveer aus Kiel |
| title_short | Springs and parachutes |
| title_sort | springs and parachutes development and characterization of novel formulations for poorly water soluble drugs sprungfedern und fallschirme entwicklung und charakterisierung neuer formulierungen fur schlecht wasserlosliche wirkstoffe |
| title_sub | development and characterization of novel formulations for poorly water-soluble drugs = Sprungfedern und Fallschirme : Entwicklung und Charakterisierung neuer Formulierungen für schlecht wasserlösliche Wirkstoffe |
| topic | Wirkstoff (DE-588)4066383-8 gnd Imatinib mesilat (DE-588)4709581-7 gnd Wasserlöslichkeit (DE-588)4273707-2 gnd Arzneimittelforschung (DE-588)4003120-2 gnd |
| topic_facet | Wirkstoff Imatinib mesilat Wasserlöslichkeit Arzneimittelforschung Hochschulschrift |
| url | http://d-nb.info/1148786643/04 https://nbn-resolving.org/urn:nbn:de:bvb:20-opus-154311 http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=030130114&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
| work_keys_str_mv | AT terveernils springsandparachutesdevelopmentandcharacterizationofnovelformulationsforpoorlywatersolubledrugssprungfedernundfallschirmeentwicklungundcharakterisierungneuerformulierungenfurschlechtwasserloslichewirkstoffe AT terveernils sprungfedernundfallschirme |
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