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Antimicrobial preservatives to achieve multi-dose formulation using beta-cyclodextrins for liquid dosage forms

一种环糊精、防腐剂的技术，应用在环糊精和防腐剂的药物组合物,开发防腐的API组合物领域，能够解决抗菌效力丧失等问题

Inactive Publication Date: 2007-12-19
PFIZER PROD INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, studies have confirmed that SBE-CD can form complexes with antimicrobial preservatives (e.g., m-cresol) and compounds of formula Ia, resulting in competing binding interactions, often resulting in loss of antimicrobial efficacy

Method used

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  • Antimicrobial preservatives to achieve multi-dose formulation using beta-cyclodextrins for liquid dosage forms
  • Antimicrobial preservatives to achieve multi-dose formulation using beta-cyclodextrins for liquid dosage forms
  • Antimicrobial preservatives to achieve multi-dose formulation using beta-cyclodextrins for liquid dosage forms

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0147] preparation of formulations . Three different assay formulations were prepared, consisting of a single component control; a binary system containing drug or m-cresol, and SBE-CD; or a ternary system containing drug, m-cresol, and SBE-CD. Formulations were prepared in various ratios and concentrations at room temperature 24 hours prior to assay to confirm equilibrium binding. Formulations were prepared by first dissolving SBE-CD at the appropriate concentration, then adding the drug or m-cresol and dissolving it in the cyclodextrin solution.

[0148] Dialysis .1 mL of compound or control formulation was loaded on the supply side of the membrane. The receiving side was loaded with 1 mL of sodium citrate (pH 4.4) to maintain ion balance across the chamber. At various time points, 50 [mu]L aliquots were withdrawn from both the donor and recipient sides of the equilibrated dialysis chamber and analyzed using HPLC. Concentration (mM) data for each side ligand at differe...

Embodiment approach

[0211] A. A pharmaceutical composition comprising a therapeutically effective amount of an active pharmaceutical ingredient, β-cyclodextrin, a pharmaceutically acceptable preservative, a pharmaceutically acceptable carrier, and an optional pharmaceutically acceptable excipient, wherein the The preservatives described above demonstrate pharmaceutically acceptable antimicrobial preservative efficacy.

[0212] B. The pharmaceutical composition according to preferred embodiment A, wherein said β-cyclodextrin is 2-hydroxypropyl-β-cyclodextrin or sulfobutyl ether-β-cyclodextrin.

[0213] C. The pharmaceutical composition according to preferred embodiment B, wherein the preservative is selected from the group consisting of sodium ethylmercury thiosalicylate, propylene glycol, phenol, or m-cresol, or a combination thereof.

[0214] D. The pharmaceutical composition according to preferred embodiment B or C, wherein the binding value of the preservative to the cyclodextrin is less than ...

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Abstract

The present invention is directed to pharmaceutical compositions containing a therapeutically effective amount of an Active Pharmaceutical Ingredient (''API''), a pharmaceutically acceptable cyclodextrin and a pharmaceutically acceptable preservative. The invention is also directed to pharmaceutical compositions of the compounds of Formula (I) wherein R<2> is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl and a pharmaceutically acceptable cyclodextrin and preservative. Formula (I): In particular, the invention is directed to pharmaceutical compositions of the compound of Formula la, and a pharmaceutically acceptable cyclodextrin and a preservative.

Description

technical field [0001] The present invention relates to pharmaceutical compositions comprising a therapeutically effective amount of an active pharmaceutical ingredient ("API"), a pharmaceutically acceptable cyclodextrin, and a pharmaceutically acceptable preservative. The present invention also relates to a pharmaceutical composition containing a compound of formula I, a pharmaceutically acceptable cyclodextrin and a preservative, wherein R 2 selected from methyl, ethyl, isopropyl, sec-butyl and tert-butyl. [0002] [0003] In particular, the present invention relates to pharmaceutical compositions comprising a compound of formula Ia, a pharmaceutically acceptable cyclodextrin and a preservative. [0004] [0005] The present invention further relates to improving the injection site tolerance of aqueous injectable solutions containing a compound of formula I or a pharmaceutically acceptable salt thereof, β-cyclodextrin and a preservative. [0006] The present inventi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/10A61K47/40A61K47/48A61K9/00A61K47/00
CPCA61K9/0019A61K31/724A61K47/40A61K47/10A61K47/48969B82Y5/00A61K47/6951A61P1/06A61P25/00A61P29/02A61P31/04A61P31/10
Inventor R·C·阿达米F·戴维J·A·伍德
Owner PFIZER PROD INC
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