Furan-2,5-dione--methoxyethene (1/1) → 2-(6-Hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid

HRID 1681565

Reaktionsgleichung

Reaktionsgleichung von HRID 1681565
[CH:1]1[CH:6]=[C:5]2[C:7]([O:9][C:10]3([C:20]4[CH:21]=[CH:22][C:23]([O-:25])=[CH:24][C:19]=4[O:18][C:12]4[CH:13]=[C:14]([O-:17])[CH:15]=[CH:16][C:11]3=4)[C:4]2=[CH:3][CH:2]=1)=[O:8].[Na+].[Na+].COC=C.C1(=O)OC(=O)C=C1>FC1(F)C2(F)C(F)(C(F)(F)C(F)(F)C(F)(F)C2(F)F)C(F)(F)C(F)(F)C1(F)F>[CH:2]1[CH:1]=[CH:6][C:5]([C:7]([OH:9])=[O:8])=[C:4]([C:10]2[C:11]3[CH:16]=[CH:15][C:14]([OH:17])=[CH:13][C:12]=3[O:18][C:19]3[C:20]=2[CH:21]=[CH:22][C:23]([CH:24]=3)=[O:25])[CH:3]=1

Komponenten

4

Edukt 2

HCID 62708Furan-2,5-dione--methoxyethene (1/1)HCID 9885981Sodium 3-oxo-3H-spiro[isobenzofuran-1,9'-xanthene]-3',6'-bis(olate)

Produkt 1

HCID 33832-(6-Hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 9386PerfluorodecalinLösungsmittel

Versuchsvorschrift

In order to determine the temperature stability and release profile of the nonaqueous drug delivery vehicle suspensions of the present invention microparticulates containing 5% sodium fluorescein were prepared utilizing poly(methylvinylether/maleic anhydride) as the polymer matrix utilizing the manufacturing technique of Example 1 and were suspended in perfluorodecalin (PFC) as a 2% w/v suspension utilizing the technique of Example 4. This nonaqueous drug delivery vehicle suspension was divided in half and equal portions were stored at 23° C. and at 45° C. for thirty days. Samples were taken of each portion during the thirty days test period and fluorescein release profiles were obtained as is known in the art. More specifically, the dissolution tests were performed as follows. 500 ml of 7.4 pH phosphate buffer (0.05M) was added to the kettles in the standard USP dissolution apparatus set at 37° C. 10 ml of the 2% w/v suspension was slowly added to the dissolution medium and the propeller speed was set to 50 rpm. Over a seven hour time period, samples were taken from the dissolution medium and immediately centrifuged. The supernatant containing the released fluorescein was assayed for fluorescein content by UV spectrophotometry. Release profiles for the 23° C. and 45° C. samples are given in FIGS. 1 and 2. The control was freshly prepared microparticulates.

Aufarbeitung

  1. waitwere stored at 23° C. and at 45° C. for thirty days
  2. customwere taken of each portion during the thirty days
  3. waittest period

Quellen und Nachweise

ORD-Eintrag
ord-7c00c9d4ef4e4521935f717c83620a9e
Quelldatensatz
uspto-grants-1992_12
Patentnummer
US05173298

Verknüpfte Notizen

Wird geladen…