Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
1998-10-06
2001-02-13
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S958000, C514S826000, C424S043000, C424S045000
Reexamination Certificate
active
06187765
ABSTRACT:
INTRODUCTION TO THE INVENTION
The present invention relates to aqueous suspensions of water-insoluble pharmaceutical substances, and more particularly to suspensions of substances intended for inhalation therapy.
Use of inhaled therapeutic substances has become common for the treatment of airway disorders, such disorders including, without limitation thereto, asthma, infections, emphysema and various inflammatory conditions. Substances commonly delivered to the lower airway surfaces, that is, the trachea, bronchial tree and lungs, by oral or nasal inhalation include bronchodilators, corticosteroids, anti-infectives and anti-inflammatory medicaments. Various methods have been used for such delivery, including pressurized metered dose inhalers, dry powder inhalers and nebulizers.
Nebulizers are considered to be instruments generating very fine particles of a liquid in a gas. As is very well known, particles intended for treatment of the lower airway, i.e., the bronchial tree or the lungs, will generally be less than 10 micrometers in the largest dimension, to prevent unwanted deposition onto surfaces of the mouth and pharynx, and more preferably will be less than 5 &mgr;m. In addition, particles much smaller than about 0.5 &mgr;m in the largest dimension frequently are not easily deposited at the desired location, and a large fraction of these simply will be exhaled by a patient. For these reasons, it is generally desired to produce particles which average 1-7 &mgr;m in their largest dimension, while preferably minimizing production of particles having sizes either less than about 0.5 or greater than about 10 &mgr;m. The more preferred average particle sizes are in the range of 0.5-5 &mgr;m.
Nebulization, although used more infrequently than other drug delivery techniques, has certain advantages for special patient groups, such as young children and the very infirm. Although somewhat cumbersome equipment is needed and there may be more stringent cleaning requirements than exist for some of the more popular delivery techniques, no particular patient skill or coordination is required: the patient merely needs to breathe normally to introduce the medication into the airway. Thus, treatment can be delivered even to an unconscious patient or an infant. It is also considered an advantage of nebulizers that quantities of moisture are delivered to the airway; this may help to fluidize secretions and tends to increase patient comfort.
The typical nebulized medication is a water-soluble substance which can form relatively dilute aqueous solutions. This is desired, due to the relatively large volumes of solution which will be entrained in an inhaled air stream, and to the very small quantities of drug which will typically be delivered in a single treatment. Handling of a drug solution is quite uncomplicated: a desired volume of a solution (usually aqueous) is either nebulized directly or is measured into a larger volume of sterile water for nebulization.
However, some very useful inhalation drugs have little or essentially no water solubility. Examples of such drugs are corticosteroids, typically administered in the treatment of asthma by inhalation from pressurized metered dose inhalers, either in alcohol solution or as suspended micronized particles, or from dry powder inhalers of various types.
It is also known to form an aqueous suspension of drug particles, for nebulization. Commercial products, which have not been made available in all countries, currently include beclomethasone dipropionate (sold by Glaxo under the trade name BECOTIDE) and budesonide (formulated with a citrate-citric acid buffer and Polysorbate 80 surfactant, and sold by Astra under the trade name PULMICORT). Corticosteroids have also been formulated in liposome suspensions in aqueous media, for nebulizer delivery, as in U.S. Pat. No. 5,192,528.
The therapeutic advantages of the corticosteroid mometasone furoate for treating disorders of the lower airway make this drug a desirable candidate for delivery by nebulization. Since this drug is not soluble in aqueous media, it has become necessary to develop aqueous suspensions for nebulization.
SUMMARY OF THE INVENTION
The invention comprises an aqueous suspension of micronized mometasone furoate monohydrate, also containing a nonionic surfactant, a soluble salt and optionally a pH buffer. Preferred surfactants are those known as polysorbates. The soluble salt may be sodium chloride, in amounts needed to render the solution phase isotonic. When the buffer is present, it preferably will be chosen to maintain a solution pH between about 3 and about 7.
REFERENCES:
patent: 5192528 (1993-03-01), Radhakrishnan et al.
patent: 5837699 (1998-11-01), Sequeira et al.
patent: 5889015 (1999-03-01), Sequeira et al.
patent: WO 9204365 (1992-03-01), None
Chaudry Imtiaz A.
Harris David
Sequeira Joel A.
Franks Robert A.
Page Thurman K.
Pulliam Amy E
Schering Corporation
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