반응 #2267052

ord-c3aa9180f2134a2c87d4796fe89c9112

반응 방정식

O=P([O-])(O)O.O=P([O-])([O-])O.[Cl-].[Cl-].[K+].[K+].[Na+].[Na+].[Na+]
phosphate-buffered saline
CC[C@H]1OC(=O)C[C@@H](O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)[C@@H](O)[C@H](N(C)C)[C@H]2O)[C@@H](CCN2C[C@H](C)C[C@H](C)C2)C[C@@H](C)C(=O)/C=C/C(C)=C/[C@@H]1CO[C@@H]1O[C@H](C)[C@@H](O)[C@@H](OC)[C@H]1OC
tilmicosin
CC[C@H]1OC(=O)C[C@@H](O)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)[C@@H](O)[C@H](N(C)C)[C@H]2O)[C@@H](CCN2C[C@H](C)C[C@H](C)C2)C[C@@H](C)C(=O)/C=C/C(C)=C/[C@@H]1CO[C@@H]1O[C@H](C)[C@@H](O)[C@@H](OC)[C@H]1OC
tilmicosin
CCCCCCCCCCCC(=O)O
lauric acid
CCCCCCCCCC(=O)O
decanoic acid

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타to obtain a clear solution
  2. 2
    기타One ml aliquots of these solutions were sealed in dialysis bags
  3. 3
    기타the bags were suspended in flasks
  4. 4
    기타to precipitate in the bag within about 1 hour
  5. 5
    기타Aliquots of saline were removed at various intervals and tilmicosin

실험 절차

10 grams (0.0115 moles) of tilmicosin and 0.0253 moles of various carboxylic acids (such as, for example, decanoic, lauric, linoleic, or myristic acids, in individual assays) were taken in a flask and made up to a final volume of 100 ml with N-methyl-pyrrolidone and stirred for 60 minutes to obtain a clear solution. One ml aliquots of these solutions were sealed in dialysis bags, and the bags were suspended in flasks containing 150 ml of phosphate-buffered saline, pH 7.4. The salt was observed to precipitate in the bag within about 1 hour. Aliquots of saline were removed at various intervals and tilmicosin was determined by HPLC. The results with decanoic acid (C-10) and lauric acid (C-12) salts in FIG. 3 show that tilmicosin continued to diffuse out of the bag for more than 120 hours. Longer chain length acids caused a slower release of tilmicosin. Micotil® (Eli Lilly, Indianapolis, Ind.), a phosphate salt of tilmicosin, is readily soluble and rapidly diffuses from the bag.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US06887487B2uspto-grants-2005_05