Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Reexamination Certificate
2000-10-31
2002-09-10
Dees, Jose′ G. (Department: 1616)
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
C424S046000, C424S489000, C514S003100, C514S012200
Reexamination Certificate
active
06447750
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to a medicinal aerosol formulation, and more particularly, to a medicinal aerosol formulation comprising a rosiglitazone maleate.
2. Description of the Related Art
Delivery of drugs to the lung by way of inhalation is an important means of treating a variety of conditions, including such common local conditions as cystic fibrosis, pneumonia, bronchial asthma and chronic obstructive pulmonary disease and some systemic conditions, including hormone replacement, pain management, immune deficiency, erythropoiesis, diabetes, etc. Anti-diabetic drugs, e.g. an insulin, are among the drugs that are administered to the lung for such purposes. Such drugs are commonly administered to the lung in the form of an aerosol of particles of respirable size (less than about 10 &mgr;m in diameter). The aerosol formulation can be presented as a liquid or a dry powder. In order to assure proper particle size in a liquid aerosol, particles can be prepared in respirable size and then incorporated into a colloidial dispersion either containing a propellant as a metered dose inhaler (MDI) or air, such as in the case of a dry powder inhaler (DPI). Alternatively, formulations can be prepared in solution form in order to avoid the concern for proper particle size in the formulation. Solution formulations must nevertheless be dispensed in a manner that produces particles or droplets of respirable size.
For MDI application, once prepared an aerosol formulation is filled into an aerosol canister equipped with a metered dose valve. In the hands of the patient the formulation is dispensed via an actuator adapted to direct the dose from the valve to the patient.
What is needed and desired is a stable aerosol formulation for the treatment of diabetes and conditions related thereto.
SUMMARY OF THE INVENTION
It has surprisingly been found that a novel and stable medicinal aerosol formulation of an anti-diabetic or hypoglycemic medicament can be obtained without the use of a surfactant, such as sorbitan trioleate. The medicament is rosiglitazone and its salts or esters, such as, for example, maleate, hydrochloride, etc., or other pharmaceutically acceptable forms. This medicament may be used alone or combined with a suitable &bgr;-cell hypoglycemic selected from the group consisting of an amylin and insulin; as well as other medicament agents possessing antidiabetic activity, including the &agr;-cell hypoglycemic glucagon, acetohexamide, chlorpropamide, tolazamide, tolbutamide, and glipizide, as well as any mixture of any two or three of the foregoing &bgr;-cell hypoglycemic medicaments may be generally included.
DETAILED DESCRIPTION OF THE INVENTION
This application makes reference to U.S. application serial No. 09/209,228 filed Dec. 10, 1998, which is incorporated hereinto by reference in its entirety.
This invention involves a stable aerosol formulation suitable for delivery which comprises (a) a rosiglitazone maleate, such as rosiglitazone maleate (AVANDIA®), and (b) a suitable fluid carrier. The rosiglitazone maleate may be present as a single drug or in combination with a suitable &bgr;-cell hypoglycemic such as an amylin and an insulin and their derivatives, and the &agr;-cell hypoglycemic glucagon.
A suitable &bgr;-cell hypoglycemic medicament is one selected from either an amylin or insulin and any of their derivatives. A suitable synthetic, antidiabetic agent is one selected from an acetohexamide, chlorpropamide, tolazemide, tolbutamide, glipizide, glyburide, glucophage, phentolamine, etc., and a mixture of any two or three of the foregoing medicaments.
The term “insulin” shall be interpreted to encompass natural extracted human insulin, recombinantly produced human insulin, insulin extracted from bovine and/or porcine sources, recombinantly produced porcine and bovine insulin and mixtures of any of these insulin products. The term is intended to encompass the polypeptide normally used in the treatment of diabetics in a substantially purified form but encompasses the use of the term in its commercially available pharmaceutical form, which includes additional excipients. The insulin is preferably recombinantly produced and may be dehydrated (completely dried) or in solution.
The terms “insulin analog,” “monomeric insulin” and the like are used interchangeably herein and are intended to encompass any form of “insulin” as defined above wherein one or more of the amino acids within the polypeptide chain has been replaced with an alternative amino acid and/or wherein one or more of the amino acids has been deleted or wherein one or more additional amino acids has been added to the polypeptide chain or amino acid sequences which act as insulin in decreasing blood glucose levels. In general, the “insulin analogs” of the present invention include “insulin lispro analogs,” as disclosed in U.S. Pat. No. 5,547,929, incorporated hereinto by reference in its entirety, insulin analogs including LysPro insulin and humalog insulin, and other “super insulin analogs”, wherein the ability of the insulin analog to affect serum glucose levels is substantially enhanced as compared with conventional insulin as well as hepatoselective insulin analogs which are more active in the liver than in adipose tissue. Preferred analogs are monomeric insulin analogs, which are insulin-like compounds used for the same general purpose as insulin, such as insulin lispro, i.e., compounds which are administered to reduce blood glucose levels.
An “amylin” includes natural human amylin, bovine, porcine, rat, rabbit amylin, as well as synthetic, semi-synthetic or recombinant amylin or amylin analogs, including pramlintide and other amylin agonists, as disclosed in U.S. Pat. No. 5,686,411, and U.S. Pat. No. 5,854,215, both of which are incorporated hereinto by reference in their entirety.
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Parks et al, Differential activity of rosiglitazone enentiomers at PPARy, Bioorganic & medicinal chemistry letters 8 (1998) 3657-3658.*
.Evans et al. Recent Development and Emerging Therapies for Type 2 Diabetes Millitus, Drugs R&D 1999, vol. 2 No. 2.
Adjei Akwete L.
Cutie Anthony J.
Sexton Frederick A.
Aeropharm Technology Incorporated
Dees Jose′ G.
Frommer & Lawrence & Haug LLP
Haghighatian M.
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