Title of Invention	NOVEL AEROSOL COMPOSITIONS OF SODIUM FUSIDATE
Abstract	Disclosed herein are stable aerosol pharmaceutical compositions for topical application, comprising therapeutically effective amount of Sodium Fusidate in association with pharmaceutically acceptable excipients.

Full Text

FORM 2 THE PATENT ACT 1970 (39 of 1970) & The Patents Rules, 2003 COMPLETE SPECIFICATION (See section 10 and rulel 3) 1. TITLE OF THE INVENTION: "Novel Aerosol compositions of Sodium Fusidate" 2. APPLICANT (S) (a) NAME: Salgaocar, Dilip Ramcrisna (b)NATIONALITY: Indian (c) ADDRESS: Sharvani, Pedem, Mapusa, Goa - 403507, India. 3. PREAMBLE TO THE DESCRIPTION The following specification particularly describes the invention and the manner in which it is to be performed: Technical Field of the invention: The present invention relates to novel aerosol pharmaceutical composition for topical application of Sodium Fusidate. Background and Prior Art: In recent years, Sodium Fusidate has been increasingly used as an anti-infective. It is also used as an agent to treat strains resistant to antibiotics. WOOI17506 discloses a mixed liposome pharmaceutical formulation with multilamellar vesicles, wherein the formulation can be administered as a metered dose aerosol mainly for oral administration wherein the formulation comprises an active ingredient selected from a large group including fiisidic acid. However there are no topical dosage forms of Sodium Fusidate reported in prior art or marketed in aerosol spray form which has substantial therapeutic benefits over conventional ointments, creams and gels. The aerosol spray based dosage form is a technological advancement with economic benefit as well as advantages of patient convenience and comfort over conventional dosage forms. Sodium Fusidate formulated as aerosol form for topical application is useful for treating infections due to staphylococci, especially strains resistant to other antibiotics and sanitisation of body surface prior to surgery. Such formulations can be used for geriatric. Paediatric, bed-ridden and in-tubated patients. It is clear from the above text, that a pharmaceutical I y stable and biologically equivalent formulation of Sodium Fusidate for topical application is required for a large section of patient population. However, no such stable formulation of Sodium Fusidate for local administration is available for convenient delivery. The present invention of aerosol dosage form for topical application fulfils this unmet need. 2 The major challenges of formulating Sodium Fusidate aerosol include a) atomisation of Sodium Fusidate, b) maintaining optimum solubility of the drug, c) ensuring long term stability, and d) ensuring bioequivalence. Summary of the invention: Sodium Fusidate is formulated in an aerosol spray composition for use in topical treatment of staphylococal and other infections, especially antibiotic resistant infections. Detailed Description of the invention: The present invention is directed to an aerosol pharmaceutical composition for topical application to a subject in need thereof which comprises of therapeutically effective amount of Sodium Fusidate in association with a pharmaceutically acceptable liquid carrier. In a preferred embodiment, the present invention is directed to a liquid formulation of Sodium Fusidate, wherein the formulation comprises of therapeutically effective amount of Sodium Fusidate in a liquid carrier, in association with pharmaceutical acceptable liquid vehicle which is free spraying and uniform, with ensured long term chemical stability, and established pharmacokinetic equivalency. The said liquid carrier comprises of one or more excipients selected from isopropyl alcohol, propylene glycol, ethyl alcohol, polyvinyl pyrolidone, isopropyl myristate, and buffering agent or combination thereof. It is most preferred that it contains all these components. The said liquid vehicle comprises liquefied petroleum gas. One such embodiment containing Sodium Fusidate and other carefully selected excipients shows : a) good physical stability of the Sodium Fusidate and other excipients upon storage under normal and stress conditions, b) maintains solubility of Sodium Fusidate and other excipients in the formulation and c) excellent chemical stability upon storage under normal and stress condition; maintains more than 95% of its initial content when exposed to 45°C for three months or more, 98% of its initial content when exposed to 40°C/75% Relative Humidity for three months or more, and more than 98% of its initial content when stored at room temperature for two years or more. 3 Such embodiment containing Sodium Fusidate formulated as aerosol spray formulation for topical application is useful for treating infections due to staphylococci especially strains resistant to other antibiotics and sanitisation of body surface prior to and after surgery. Such embodiment is especially useful in a patient population consisting of geriatric, paediatric, bed-ridden, and/or in-tubated patients, and others who experience difficulty in swallowing oral dosage forms or who cannot be administered ointment or creams/gels. The aerosol formulation has been shown to be chemically compatible with many other common applications and can be applied with ease. Other major attributes of such embodiment of Sodium Fusidate aerosol formulation is its proven bioavailability with a commercially available leading brand of cream and ointment dosage forms, as also disinfectants. One such embodiment of Sodium Fusidate aerosol spray formulation was investigated in a relative bioavailability study in which comparison with a leading brand formulation was performed. Proof of such bioequivalence of the subject embodiment is extremely important in clinical as well as pharmacy practice, since switchover from topical gel cream or ointment to topical aerosol spray formulation for local application can occur automatically without the need for physician's approval. In a more preferred embodiment, the formulation of the present invention contains at least one or more of the following components along with 2% by weight of Sodium Fusidate. One or more components includes; about 5% to about 40% by weight of propylene glycol, about 40% to about 70% by weight of ethyl alcohol, about 5% to about 20% by weight of isopropy alcohol, about 5% to about 20% by weight of isoproyl myristate, 0.1 to 1% polyvinyl pyrolidone. The vehicle liquefied petroleum gas (LPG) (deodorised) is used in about 30% to about 40%. In another embodiment, the formulation comprises a therapeutically effective amount of Sodium Fusidate in carrier that comprises of about 40% to about 65% by weight of isopropyl alcohol about 5% to about 20% by weight of ethyl alcohol, about 5% to about 20% by weight of propylene glycol, about 5% to about 20% by weight of isopropyl 4 myristate, 0.1 to 1.5% poly vinyl pyrolidone and 30 to 40% deodorised liquefied petroleum gas as a vehicle. In yet another embodiment, the formulation comprises a therapeutically effective amount of Sodium Fusidate in carrier that comprises about 40% to about 95%% by weight of ethyl alcohol, about 5% to about 20% by weight of isopropyl alcohol, about 5% to about 20% by weight of propylene glycol, about 5% to about 20% by weight of isopropyl myristate, 1 to 5% poly vinyl pyrolidone and 30 to 40% deodorised liquefied petroleum gas as a vehicle. The following examples, which include preferred embodiments, will serve to illustrate the practice of this invention, it being understood that the particulars shown are by way of example and for purpose of illustrative discussion of preferred embodiments of the invention. Example 1: In a suitable manufacturing container, 15gms of purified isopropyl alcohol was added. To this 2% by weight of Sodium Fusidate # 200 was added and mixed to dissolve. To this 5 gms of propylene glycol, lgm of isopropyl myristate, 0.1 gm poly vinyl pyrolidone, 10 gm deodorised liquefied petrolium gas was added mixed in a container for 15 minutes. Example 2: In a suitable manufacturing container, 15gms of purified ethyl alcohol was added. To this 2% by weight of Sodium Fusidate # 200 was added and mixed to dissolve. To this 5 gms of propylene glycol, lgm of isopropyl myristate, 0.1 gm poly vinyl pyrolidone, 10 gm liquefied petroleum gas was added mixed in a container for 15 minutes. Example 3: In a suitable manufacturing container, 7.5gms of purified ethyl alcohol and 7.5 gms of isopropyl alcohol was added. To this 2% by weight of Sodium Fusidate # 200 was added and mixed to dissolve. To this 5 gms of propylene glycol, lgm of isopropyl myristate, 0.1 gm poly vinyl pyrolidone, 10 gm liquefied petroleum gas was added mixed in a container for 15 minutes. 5 'e Claim, MP* \^ fj £- 1. Stable aerosol pharmaceutical compositions for topical application comprising $$v therapeutically effective amount of Sodium Fusidate in association with v r? pharmaceutically acceptable excipients. 2. The aerosol composition as claimed in claim 1, wherein said application is a liquid formulation. 3. The aerosol composition as claimed in claim 1 and 2, wherein Sodium Fusidate is present in an amount of 2% by weight of the total composition. 4. The aerosol composition as claimed in claims 1 to 3, wherein said excipients comprise liquid carrier for Sodium Fusidate and a liquid vehicle. 5. The aerosol composition as claimed in claims 1 to 4, wherein said liquid carrier is selected from isopropyl alcohol, propylene glycol, ethyl alcohol, polyvinyl pyrrolidone and isopropyl myristate and combination thereof. 6. The aerosol composition as claimed in claims 1 to 5, wherein isopropyl alcohol present in an amount of 5-65% by weight of the total composition; propylene glycol present in an amount of 5-40% by weight of the total composition; ethyl alcohol present in an amount of 5-95% by weight of the total composition; polyvinyl pyrolidone present in an amount of 0.1-5% by weight of the total composition and isopropyl myristate present in an amount of 5-20%. 7. The aerosol composition as claimed in claim 1 to 4, wherein said vehicle comprises deodorized liquefied petroleum gas present in an amount of 30-40% by weight of the total composition. 8. The aerosol composition as claimed in any of the preceding claims, wherein said composition optionally comprises buffering agent. 6 9. A stable aerosol pharmaceutical composition of Sodium Fusidate as substantially exemplified in examples 1 to 3 useful for treating infections due to staphylococci, especially strains resistant to other antibiotics and sanitisation of body surface prior to and after surgery. Dated this 13th day of April 2006 Dr. Gopakumar G. Nair Agent for the Applicant 7 ABSTRACT: Disclosed herein are stable aerosol pharmaceutical compositions for topical application, comprising therapeutically effective amount of Sodium Fusidate in association with pharmaceutically acceptable excipients. 8

Documents:

1621-MUM-2005-ABSTRACT(13-4-2006).pdf

1621-mum-2005-abstract(granted)-(10-1-2008).pdf

1621-MUM-2005-CANCELLED PAGES(20-6-2007).pdf

1621-mum-2005-claim(granetd)-(13-04-2005).pdf

1621-MUM-2005-CLAIMS(13-4-2006).pdf

1621-MUM-2005-CLAIMS(AMENDED)-(20-6-2007).pdf

1621-mum-2005-claims(granetd)-(13-04-2005).doc

1621-mum-2005-claims(granted)-(10-1-2008).pdf

1621-mum-2005-correspondence(13-04-2006).pdf

1621-MUM-2005-CORRESPONDENCE(26-5-2006).pdf

1621-MUM-2005-CORRESPONDENCE(29-7-2009).pdf

1621-mum-2005-correspondence(ipo)-(05-04-2007).pdf

1621-MUM-2005-CORRESPONDENCE(IPO)-(2-4-2008).pdf

1621-MUM-2005-DESCRIPTION(COMPLETE)-(13-4-2006).pdf

1621-mum-2005-description(granted)-(10-1-2008).pdf

1621-MUM-2005-DESCRIPTION(PROVISIONAL)-(26-12-2005).pdf

1621-mum-2005-form 1(23-12-2005).pdf

1621-mum-2005-form 18(26-05-2006).pdf

1621-MUM-2005-FORM 2(COMPLETE)-(13-4-2006).pdf

1621-mum-2005-form 2(granetd)-(13-04-2005).doc

1621-mum-2005-form 2(granetd)-(13-04-2005).pdf

1621-mum-2005-form 2(granted)-(10-1-2008).pdf

1621-MUM-2005-FORM 2(PROVISIONAL)-(26-12-2005).pdf

1621-MUM-2005-FORM 2(TITLE PAGE)-(COMPLETE)-(13-4-2006).pdf

1621-mum-2005-form 2(title page)-(granted)-(10-1-2008).pdf

1621-MUM-2005-FORM 2(TITLE PAGE)-(PROVISIONAL)-(26-12-2005).pdf

1621-mum-2005-form 3(23-12-2005).pdf

1621-MUM-2005-FORM 3(26-12-2005).pdf

1621-mum-2005-form 5(13-04-2006).pdf

1621-MUM-2005-FORM 5(13-4-2006).pdf

1621-mum-2005-form 9(13-04-2006).pdf

1621-MUM-2005-REPLY TO FIRST EXAMINATION REPORT(20-6-2007).pdf