Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Patent
1993-12-09
1995-12-12
Griffin, Ronald W.
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
424 46, 422 34, 422 37, 514826, A61K 972, C09K 330
Patent
active
054747597
DESCRIPTION:
BRIEF SUMMARY
INTRODUCTION TO THE INVENTION
The present invention is directed at aerosol formulations which are substantially free of chlorofluorocarbons (CFC's). More specifically, the present invention is directed at formulations substantially free of CFC's and having particular utility in medicinal applications, especially in metered dose pressurized inhalators (MDI's).
Metered dose inhalators have proven to be an effective method for delivering medicaments orally and nasally. They have been used extensively for delivering bronchodilating and steroidal compounds to asthmatics and may also be useful for delivering other compounds such as pentamidine and non-bronchodilator anti-inflammatory drugs. The rapid onset of activity of compounds administered in this manner and the absence of any significant side effects have resulted in a large number of compounds being formulated for administration via this route. Typically, the drug Is delivered to the patient by a propellant system generally comprising one or more propellents which have the appropriate vapor pressure and which era suitable for oral or nasal administration, The more preferred propellant systems typically comprise propellant 11, propellant 12, propellant 114 or mixtures thereof. Often the vapor pressure of the propellant systems is adjusted by admixing a liquid excipient with the propellant.
However, propellants 11, 12 and 114 belong to a class of compounds known as chlorofluorocarbons, which have been linked to the depletion of ozone in the atmosphere. It has been postulated that ozone blocks certain harmful UV rays and the a decrease in the atmospheric ozone content will result in an increase in the incidence of skin cancer. In the 1970's certain steps were taken to reduce the CFC emissions from aerosols. Other propellents, such as hydrocarbons, were used, or the product was delivered in a different manner. Because CFC usage in medicine; applications is relatively low i.e. less than 1% of total CFC emissions, and because of the health benefits associated with metered dose Inhalators, steps were not taken at that time to restrict the use of CFC propellents in metered dose inhalators.
However, continuing and more sophisticated ozone measurements have indicated that the earlier restrictions in CFC usage were insufficient and that additional, significant steps should be taken to drastically reduce CFC emissions. Recently, recommendations have been made that CFC production be virtually discontinued by the end of this century. As a result, it may not be possible to continue to use CFC propellents in the Intermediate and long term. While some efforts have been made to use non-pressurized metered dose inhalators, many of these devices have not been completely successful. Many do not deliver uniform doses, are mechanically complex, do not provide the 100-200 doses per unit of current aerosol containers, are difficult for individuals to utilize, and are bulky and/or cumbersome for the patients to use, particularly when they have an acute need for the medication.
As a result, there is a need for aerosol formulations which are substantially free of CFC's. Non-CFC propellents systems must meet several criteria for pressurized metered dose inhalators. They must be non-toxic, stable and non-reactive with the medicament and the other major components in the valve/actuator. One propellant which has been found to be suitable is CF.sub.3 --CH.sub.2 F--CF.sub.3, also known as Freon 227, HFA 227, HFC 227 or 1,1,1,2,3,3,3 heptafluoropropane. However, certain physical properties, i.e., polarity and solubility, of HFC 227 differ from those of commonly used CFC propellents. Commonly used surfactants may be insoluble in HFA 227. Moreover, where the medicament is to be delivered as a solution, the medicament may not be readily soluble In this propellant, The polarity difference between HFC 227 and the previously used CFC propellents may result in a different delivery of the medicament when HFC 227 replaces a CFC propellant. The medicament may cream, settle or agglomerate in the non-
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Chaudry Imtiaz A.
Fassberg Julianne
Kopcha Michael
Sequeira Joel A.
Franks Robert A.
Griffin Ronald W.
Hoffman Thomas D.
Mazer Edward H.
Schering Corporation
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