Self Nanoelmusifying Drug Delivery System of Rosuvastatin : Bioavailability Evaluation and In vitro - In vivo Correlation
Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net..
BACKGROUND: Rosuvastatin, most commonly used in the form of calcium salt, belongs to the statin groups of synthetic antihyperlipidemic agents. Rosuvastatin possesses high permeability, however, its aqueous solubility is poor, causing a slow dissolution rate in water. Consequently, this dissolution rate has a decisive role in the release and absorption of rosuvastatin in the gastrointestinal tube.
OBJECTIVE: The aims of this study were to evaluate the absorption of the drug from the self-nano emulsifying drug delivery system of rosuvastatin (Ros SNEDDS) compared to rosuvastatin substance and to develop a level-A in vitro-in vivo correlation (IVIVC) for Ros SNEDDS.
METHODS: An in-house developed LC-MS/MS method was used to determine the concentrations of rosuvastatin in dog plasma. Six beagle dogs received an intravenous dose, Ros SNEDDS, rosuvastatin substance. In vitro dissolution of the Ros SNEDDS was carried out with different conditions. Correlation models were developed from the dissolution and absorption results of Ros SNEDDS.
RESULTS: The results showed a 1.7-fold enhanced oral bioavailability and 2.1-time increase of rosuvastatin Cmax in Ros SNEDDS form, compared to the rosuvastatin substance. A 900 ml dissolution medium of pH of 6.6 has demonstrated its suitability, the in vitro dissolution model was studied and supported by the Weibull equation with a weighting factor of 1/y2 as it presented the lowest values of AIC.
CONCLUSION: Ros SNEDDS demonstrated higher bioavailability of rosuvastatin in comparison to rosuvastatin substance and established a level A IVIVC used in future bioequivalence trials.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2024 |
|---|---|
| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:21 |
|---|---|
| Enthalten in: |
Current drug delivery - 21(2024), 5 vom: 10., Seite 734-743 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Phan, Nghia Thi [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
83MVU38M7Q |
|---|
| Anmerkungen: |
Date Completed 11.01.2024 Date Revised 11.01.2024 published: Print Citation Status MEDLINE |
|---|
| doi: |
10.2174/1567201820666221220104244 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM350573115 |
|---|
| LEADER | 01000caa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM350573115 | ||
| 003 | DE-627 | ||
| 005 | 20240114233714.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231226s2024 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.2174/1567201820666221220104244 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1256.xml |
| 035 | |a (DE-627)NLM350573115 | ||
| 035 | |a (NLM)36545742 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Phan, Nghia Thi |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Self Nanoelmusifying Drug Delivery System of Rosuvastatin |b Bioavailability Evaluation and In vitro - In vivo Correlation |
| 264 | 1 | |c 2024 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 11.01.2024 | ||
| 500 | |a Date Revised 11.01.2024 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net. | ||
| 520 | |a BACKGROUND: Rosuvastatin, most commonly used in the form of calcium salt, belongs to the statin groups of synthetic antihyperlipidemic agents. Rosuvastatin possesses high permeability, however, its aqueous solubility is poor, causing a slow dissolution rate in water. Consequently, this dissolution rate has a decisive role in the release and absorption of rosuvastatin in the gastrointestinal tube | ||
| 520 | |a OBJECTIVE: The aims of this study were to evaluate the absorption of the drug from the self-nano emulsifying drug delivery system of rosuvastatin (Ros SNEDDS) compared to rosuvastatin substance and to develop a level-A in vitro-in vivo correlation (IVIVC) for Ros SNEDDS | ||
| 520 | |a METHODS: An in-house developed LC-MS/MS method was used to determine the concentrations of rosuvastatin in dog plasma. Six beagle dogs received an intravenous dose, Ros SNEDDS, rosuvastatin substance. In vitro dissolution of the Ros SNEDDS was carried out with different conditions. Correlation models were developed from the dissolution and absorption results of Ros SNEDDS | ||
| 520 | |a RESULTS: The results showed a 1.7-fold enhanced oral bioavailability and 2.1-time increase of rosuvastatin Cmax in Ros SNEDDS form, compared to the rosuvastatin substance. A 900 ml dissolution medium of pH of 6.6 has demonstrated its suitability, the in vitro dissolution model was studied and supported by the Weibull equation with a weighting factor of 1/y2 as it presented the lowest values of AIC | ||
| 520 | |a CONCLUSION: Ros SNEDDS demonstrated higher bioavailability of rosuvastatin in comparison to rosuvastatin substance and established a level A IVIVC used in future bioequivalence trials | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Absorption | |
| 650 | 4 | |a deconvolution | |
| 650 | 4 | |a dissolution | |
| 650 | 4 | |a in vitro-in vivo correlation | |
| 650 | 4 | |a pharmacokinetics | |
| 650 | 4 | |a rosuvastatin. | |
| 650 | 7 | |a Rosuvastatin Calcium |2 NLM | |
| 650 | 7 | |a 83MVU38M7Q |2 NLM | |
| 650 | 7 | |a Reactive Oxygen Species |2 NLM | |
| 650 | 7 | |a Emulsions |2 NLM | |
| 700 | 1 | |a Tran, Yen Thi Hai |e verfasserin |4 aut | |
| 700 | 1 | |a Nguyen, Linh Tran |e verfasserin |4 aut | |
| 700 | 1 | |a Hoang, Yen Kieu |e verfasserin |4 aut | |
| 700 | 1 | |a Bui, Cuong Khac |e verfasserin |4 aut | |
| 700 | 1 | |a Nguyen, Hoa Dang |e verfasserin |4 aut | |
| 700 | 1 | |a Vu, Giang Thi Thu |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Current drug delivery |d 2004 |g 21(2024), 5 vom: 10., Seite 734-743 |w (DE-627)NLM159100232 |x 1875-5704 |7 nnns |
| 773 | 1 | 8 | |g volume:21 |g year:2024 |g number:5 |g day:10 |g pages:734-743 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.2174/1567201820666221220104244 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 21 |j 2024 |e 5 |b 10 |h 734-743 | ||