Processes for making pharmaceutical oral ECB formulations and compositions

A technology for pharmaceutical preparations and compounds, which can be used in antifungal agents, resistance to vector-borne diseases, cyclic peptide components, etc., and can solve problems such as difficult preparations, short shelf life, and unstable echinocandin compounds.

Inactive Publication Date: 2002-04-17
ELI LILLY & CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The instability of echinocandin compounds makes them particularly difficult to formulate
Most formulations tested to date have a shelf life of less than 1 year at room temperature

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0113] Example 1 illustrates the in situ formation of echinocandin / saccharide complexes using a fluidized bed spray method.

[0114] Solution A was prepared by adding 523.70 g of fructose to 760.0 ml of warm purified water while stirring. The solution was then cooled to room temperature.

[0115] Solution B was prepared by adding 2,850.0 ml of acetone to 950.0 ml of purified water cooled to 20-25°C while stirring. 523.70 g of compound 1(a) was slowly added to the acetone / water solution with stirring.

[0116] Slowly add solution A to solution B while stirring. This clear solution was then sprayed into granulated Mannitol 2080 (available from SPI Polyols Co. , New Castle, DE) fluidized bed. The initial inlet temperature of the apparatus was set at 30°C and then increased to 45°C after spraying was complete to remove excess solvent. Once dry, shake the bag and transfer the contents to a plastic-lined container.

[0117] This procedure yielded 3,332.7 g (90.9% yield) of fin...

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Abstract

A fluid bed spray process is described where one or more carbohydrates are incorporated into an echinocandin formulation to provide a significant improvement in thermal stability. The carbohydrate is solubilized with an echinocandin compound or echinocandin/carbohydrate complex in a solvent(s) to form a pharmaceutical solution which is sprayed onto the surface of a granular diluent or carrier. Alternatively, a granulating agent is added to the pharmaceutical solution which is then sprayed onto the surface of a non-granular diluent or carrier. The resulting granular oral formulations and medicaments derived therefrom are also described.

Description

field of invention [0001] The present invention relates to a preparation method of a pharmaceutical preparation or a pharmaceutical composition containing an antifungal compound, in particular, incorporating an echinocandin / saccharide complex into an oral preparation or composition to enhance stability. Background of the invention [0002] Oral formulations of the drug can be administered to patients via cachets, chewable or conventional tablets, capsules, or oral solutions and suspensions, and the like. The formulation developed for a particular drug depends on many factors. For example, it is well known in the art that oral formulations should be sufficiently stable, have an acceptable appearance and be prepared with generally recognized safe excipients. [0003] Stability is an important consideration when designing formulations, especially for oral applications. For practical and commercial reasons, it is desirable that sufficient formulation stability be maintained fo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K38/12A61P31/10
CPCA61K9/1694A61K38/12A61K9/1623A61P31/10Y02A50/30A61K9/16
Inventor J·R·施维克J·泰勒
Owner ELI LILLY & CO
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