Sterilized nanoparticulate glucocorticosteroid formulations

A technology of glucocorticoids and granules, applied in nanostructure manufacturing, nanotechnology, nanotechnology, etc., can solve problems such as contaminated drugs, difficulties, and time-consuming processes

Inactive Publication Date: 2009-05-27
ELAN PHRMA INT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this technique requires elimination of residual ethylene oxide from the product, a time-consuming and difficult process that could contaminate the final drug product

Method used

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  • Sterilized nanoparticulate glucocorticosteroid formulations
  • Sterilized nanoparticulate glucocorticosteroid formulations
  • Sterilized nanoparticulate glucocorticosteroid formulations

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0181] D. Preparation method of the composition of the present invention

[0182]In another aspect of the present invention, a method for preparing the nanoparticle glucocorticoid preparation of the present invention is provided. The method includes one of the following methods: grinding or milling (including but not limited to wet milling), homogenization, precipitation, freezing, template emulsion method, supercritical fluid method, nano electrospray method, or any combination thereof. Exemplary methods of preparing nanoparticle compositions are described in US Patent No. 5,145,684. Methods of preparing nanoparticle compositions are also described in U.S. Pat. No. 5,518,187 "Method of Grinding Pharmaceutical Substances", U.S. Pat. 5,862,999 "Method of Grinding Pharmaceutical Substances (method of grinding drugs)", US Patent No. 5,665,331 "Co-Microprecipitation of Nanoparticulate Pharmaceutical Agents with Crystal Growth Modifiers (co-microprecipitation of nanoparticle drugs...

Embodiment 1

[0250] The purpose of this example was to evaluate the particle size of budesonide nanoparticle dispersions with polysorbate 80 as non-ionic surface stabilizer in the presence and absence of the amphipathic lipid lecithin.

[0251] Budesonide has the following formula:

[0252]

[0253] Budesonide is known chemically as an acetal of (RS)-11,16,17,21-tetrahydroxy-pregna-1,4-diene-3,20-dionecyclo16,17-diol and butyraldehyde . Budesonide is provided as a mixture of two epimers (22R and 22S). The empirical formula for budesonide is C 25 h 34 o 6 , and its molecular weight is 430.5.

[0254] Budesonide is a white to off-white odorless powder, almost insoluble in water and heptane, slightly soluble in ethanol, and easily soluble in chloroform.

[0255] A drug containing 30% (w / w) budesonide and 1.5% (w / w) polysorbate was prepared by adding 10 g polysorbate-80 to 456.7 g sterile water for injection (Abbott Labs) and 200 g budesonide (Farmabios) Aqueous colloidal dispersion ...

Embodiment 2

[0266] The purpose of this example is to determine the effects of different amounts of nonionic surface stabilizers and amphiphilic lipids on the particle size of nanoparticle budesonide dispersions after high pressure heat treatment.

[0267] A separate portion of the 30% budesonide, 1.5% polysorbate-80 milled dispersion described in Example 1 was further diluted and various levels of sterile water for injection (SWFI), lecithin NF and polysorbate-80 were added. 80 was compounded to examine the effect of different percentages of polysorbate-80 and lecithin NF on the particle size of budesonide after autoclaving heat treatment. The effect of different hyperbaric exposure temperatures is also listed in Table II ("API" is active pharmaceutical ingredient or budesonide). All in Table II are percent by weight.

[0268] Table II: Particle size of budesonide dispersions after autoclave heat treatment: effect of different percentages of polysorbate-80 and lecithin NF

[0269]

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Abstract

The invention is directed sterile to compositions of glucocorticosteroids useful in the prophylaxis and chronic treatment of asthma and other allergic and inflammatory conditions in adults and pediatric patients.

Description

field of invention [0001] The present invention generally relates to sterile compositions for the prophylaxis and long-term treatment of asthma in adult and pediatric patients and for the relief of symptoms of allergic conjunctivitis and seasonal allergic rhinitis in adult and pediatric patients. The sterile composition comprises a glucocorticoid. The present invention also relates to a glucocorticoid pharmaceutical composition for parenteral, inhalation and topical administration in the treatment of various inflammatory and allergic diseases. Background of the invention [0002] a. Background on glucocorticoids [0003] Corticosteroids have been shown to be effective as preventive therapy for the maintenance treatment of asthma, management of nasal symptoms of seasonal and perennial allergic and non-allergic rhinitis, and relief of signs of seasonal allergic conjunctivitis in adult and pediatric patients and symptoms. [0004] US Patent No. 6,392,036 "Dry Heat Steriliza...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/57A61K47/48
CPCA61K9/145A61K47/14A61K9/146A61K9/0043A61K31/57A61K31/573A61K47/10A61K9/0078A61K47/34A61K9/10A61K45/06A61P11/00A61P11/06A61P11/08A61P17/02A61K2300/00A61P27/02A61P27/16A61P29/00A61P37/00B82B3/00H01L21/20
Inventor J·M·肖D·斯利菲尔S·B·拉迪J·普勒伊特R·克瓦尔拉马尼
Owner ELAN PHRMA INT LTD
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