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Inhalation particles incorporating a combination of two or more active ingredients

a technology of inhalation particles and active ingredients, which is applied in the direction of drug compositions, immunological disorders, metabolism disorders, etc., can solve the problems of uncontrollable inflammation, patients often do not recognise immediate therapeutic effects, and the onset of action of the drug is relatively slow, so as to improve the dispersibility and stability, the effect of improving the dispersibility

Inactive Publication Date: 2008-10-16
ORION CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a method for preparing uncharged, spherical and crystalline inhalation particles that can deliver a combination of drugs in a controlled and constant ratio. The particles have improved dispersibility, stability, and are suitable for use in dry powder inhalers. The method is simple and can be easily scaled-up to higher production rates. The invention also provides an inhalation composition comprising the particles and pharmaceutically acceptable additives, diluents or carriers. The particles can be formulated into a dry inhalation powder for the treatment of asthma and other respiratory disorders.

Problems solved by technology

One of the drawbacks of anti-inflammatory drugs is that their onset of action is relatively slow.
Therefore, patients often do not recognise any immediate therapeutic effects and tend to stop the medication.
This could cause the inflammation uncontrollable.
However, there are currently debates on the safety of a regular use of β2-agonists as well as efficiency of long-acting β2-agonists.
Also, the short-acting nature of the drug requires more frequent drug administrations, which tend to cause patient compliance problem.
When these combinations are used in dry powder inhalers, the consistency of drug proportion in each dose cannot be easily controlled.
Hence, it is not easy to keep the ratio of the drugs in each dose constant.
The inconsistency of the dose could cause serious problems especially when a very potent drug is delivered in a much higher amount than expected.
However, the method produces amorphous particles, which have stability problems and a high, tendency toward moisture re-absorption, which is undesirable for pharmaceutical particles intended for administration by inhalation.
Furthermore the size and the morphology of the particles obtained are not optimal for pulmonary delivery.

Method used

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  • Inhalation particles incorporating a combination of two or more active ingredients
  • Inhalation particles incorporating a combination of two or more active ingredients
  • Inhalation particles incorporating a combination of two or more active ingredients

Examples

Experimental program
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Effect test

example 1

Preparation of Inhalation Particles Incorporating a Combination of Beclomethasone Dipropionate and Formoterol Fumarate

[0050]Preparation of the Liquid Feed Stock

[0051]Beclomethasone dipropionate is an anti-inflammatory glucocorticosteroid, which is practically insoluble in water, freely soluble in acetone and in chloroform, and sparingly soluble in alcohol. Thus, the solvent could be acetone, chloroform, methanol, ethanol, or other alcohols. In the current experiments, ethanol was used as a solvent, not only because ethanol is cheap and readily available but it is also recommended for use in production of pharmaceutical agents because it is non-toxic.

[0052]The beclomethasone dipropionate liquid feed stock was prepared by dissolving 1 gram of beclomethasone dipropionate powder in 40 ml of ethanol (99.5%) at room temperature.

[0053]Formoterol fumarate is a β2-agonist bronchodilator, which is freely soluble in glacial acetic acid, soluble in methanol, sparingly soluble in ethanol. Thus, ...

example 2

Dry Inhalation Powder

[0075]

Per doseFormoterol fumarate6μgBeclomethasone dipropionate200μgLactose monohydrate Ph. Eur.8mg

[0076]Particles of Example 1 and part of lactose is added into a blender. The powder mixture is mixed until it is homogenous. The mixture is sieved to reduce the number of particle clusters present. Thereafter the rest of lactose is added and the powder is again mixed until it is homogenous. Powder is poured into a supply chamber of the multi-dose powder inhaler Easyhaler (Orion Corporation trademark) for a supply of 200 doses.

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Abstract

Crystalline spherical inhalation particles incorporating a combination of two or more different active ingredients and a process for the preparation thereof. The particles have a narrow particle size distribution, rough surfaces and improved stability. The inhalation particles of the invention are particularly useful in the administration of a combination medicament, e.g. a combination of an anti-inflammatory agent and a bronchodilator, by inhalation in the treatment of asthma and other respiratory disorders.

Description

FIELD OF THE INVENTION[0001]The present invention relates to inhalation particles and inhalation compositions suitable for pulmonary drug delivery and to methods for the preparation thereof. In particular, the present invention relates to inhalation particles incorporating a combination of two or more different active ingredients. The inhalation particles of the invention are particularly useful in the treatment of asthma and other respiratory disorders.BACKGROUND OF THE INVENTION[0002]Inhalation has become the primary route of administration in the treatment of asthma. This is because, besides providing direct access to the lungs, medication delivered through the respiratory tract provides rapid and predictable onset of action and requires lower dosages compared to the oral route.[0003]There have been recent advances in the treatment of asthma resulting from the recognition that asthma is a chronic inflammatory disease. Current asthma drugs can be classified into two classes, namel...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/14A61K31/56A61P11/00A61K9/00A61K9/10A61K9/72A61K31/137A61K31/165A61K31/167A61K31/57A61K31/573A61K45/06A61K47/10A61L9/04A61P3/02A61P3/10A61P5/00A61P9/06A61P11/06A61P11/08A61P11/10A61P25/18A61P25/20A61P29/00A61P31/10A61P31/12A61P35/00A61P37/00A61P43/00
CPCA61K9/0075A61K31/165A61K31/167A61K31/57A61K31/573A61K45/06A61K2300/00Y10S514/826A61P11/00A61P11/06A61P11/08A61P11/10A61P25/18A61P25/20A61P29/00A61P3/02A61P3/10A61P31/10A61P31/12A61P35/00A61P37/00A61P43/00A61P5/00A61P9/06
Inventor WATANABE, WIWIKKAUPPINEN, ESKOAHONEN, PETRIBROWN, DAVIDMUTTONEN, ESA
Owner ORION CORPORATION
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