Perfluorooctyl bromide → Tobramycin

HRID 1182655

Reaktionsgleichung

Reaktionsgleichung von HRID 1182655
CCCCCCCCCCCCCCCCCC(OC[C@@H](OC(CCCCCCCCCCCCCCCCC)=O)COP(OCC[N+](C)(C)C)([O-])=O)=O.O.O.[Cl-].[Ca+2].[Cl-].FC(Br)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)F.[CH2:86]1[C@@H:91]([NH2:92])[C@H:90]([O:93][C@H:94]2[O:99][C@H:98]([CH2:100][OH:101])[C@@H:97]([OH:102])[C@H:96]([NH2:103])[C@H:95]2[OH:104])[C@@H:89]([OH:105])[C@H:88]([O:106][C@H:107]2[O:112][C@H:111]([CH2:113][NH2:114])[C@@H:110]([OH:115])[CH2:109][C@H:108]2[NH2:116])[C@H:87]1[NH2:117].OS(O)(=O)=O>O>[CH2:86]1[C@@H:91]([NH2:92])[C@H:90]([O:93][C@H:94]2[O:99][C@H:98]([CH2:100][OH:101])[C@@H:97]([OH:102])[C@H:96]([NH2:103])[C@H:95]2[OH:104])[C@@H:89]([OH:105])[C@H:88]([O:106][C@H:107]2[O:112][C@H:111]([CH2:113][NH2:114])[C@@H:110]([OH:115])[CH2:109][C@H:108]2[NH2:116])[C@H:87]1[NH2:117]

Komponenten

6

Edukt 4

HCID 9873Perfluorooctyl bromideHCID 62005Tobramycin Sulphate SaltHCID 941901,2-Distearoyl-sn-glycero-3-phosphocholineHCID 6093260Calcium chloride, dihydrate

Produkt 1

HCID 36294Tobramycin

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 962WaterLösungsmittel2×

Versuchsvorschrift

A tobramycin sulfate dry powder composition is prepared according to the following procedure. Sterile Water for Irrigation (SWFI) is heated above the gel to liquid crystal temperature (about 80° C.) of disteroyl phosphatidylcholine (DSPC). DSPC and calcium chloride dihydrate are then added to the heated water. The resulting lipid dispersion is mixed in an UltraTurrax T-50 (IKA Labortechnik) at 8,000 rpm for 5 min. Perfluorooctyl bromide (PFOB) is then added dropwise (15 ml/min) to the lipid dispersion under mixing. After the addition is complete the resulting PFOB-in-water emulsion is mixed for an additional 10 min at 10,000 rpm. Emulsification in the UltraTurrax produces droplets in the micron-size range. Tobramycin sulfate is then dissolved in the continuous phase of the emulsion and the resulting dispersion is used as the feedstock for spray drying. The feedstock is then spray dried to obtain a dry powder formulation having the composition set forth in Table 1 below.

Aufarbeitung

  1. dry with materialA tobramycin sulfate dry powder composition
  2. customis prepared
  3. additionThe resulting lipid dispersion is mixed in an UltraTurrax T-50 (IKA Labortechnik) at 8,000 rpm for 5 min
  4. additionunder mixing
  5. additionAfter the addition
  6. additionis mixed for an additional 10 min at 10,000 rpm
  7. customEmulsification in the UltraTurrax produces droplets in the micron-size range
  8. customdrying
  9. customThe feedstock is then spray dried
  10. customto obtain a dry powder formulation

Quellen und Nachweise

ORD-Eintrag
ord-2178096666c84924908923167b0ca2c0
Quelldatensatz
uspto-grants-2014_03
Patentnummer
US08664187B2

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