Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Ion exchange resin
Reexamination Certificate
2000-07-12
2003-02-04
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Solid synthetic organic polymer as designated organic active...
Ion exchange resin
C424S078120, C424S078140, C424S400000, C424S464000, C424S451000, C424S474000, C424S486000
Reexamination Certificate
active
06514492
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to the formulation of oral liquid preparations of quinolones or derivatives thereof using ion exchange resins, such as a methacrylic acid polymer crosslinked with divinylbenzene, as the carrier. The formation of a quinolone-resin complex (resinate) eliminates the extreme bitterness of the quinolones to make the liquid oral dosage form palatable.
2. Description of Related Art
Quinolone antibiotics are widely used in the treatment of common infections. The current quinolone products on the market, including orbifloxacin, and ciprofloxacin, are administered as tablets or capsules. Since quinolones have an extremely bitter taste, development of palatable liquid oral dosage forms has always been challenging. Liquid oral dosage forms are useful for patients having difficulty swallowing capsules or tablets. The Journal of Pharm. Sciences, vol 60, No 10, pp 1523-1527 (October 1971) discloses polycarboxylic acid ion exchange resins as adsorbates for masking the bad taste of ephedrine, dextromethorphan, pseudoephedrine, and methapyrilene; EPO 225615, published Jun. 16, 1987, discloses liquid pharmaceutical compositions containing dextrometorphan, ion exchange resin (preferably a cationic resin) and acceptable pharmaceutical carriers, sweetners and formulation aids. Taste is not an issue. U.S. Pat. No. 4,808,411 issued Feb. 28, 1989 discloses antibiotic polymer compositions containing acrylic acid polymers and erythromycin. Said compositions can be prepared as liquids and are effective in masking the taste of the erythromycin antibiotic; U.S. Pat. No. 5,152,986, issued Oct. 6, 1992, discloses pharmaceutical compositions containing quinolone carboxylic acid derivatives (such as ciprofloxacin) and ion exchange resins (preferably cationic) which mask the bad taste of the quinolone in animal feeds. Said compositions are in solid form and paste form; EPO 622083, published Nov. 11, 1994, discloses a solid pharmaceutical preparation containing any number of therapeutic agents, such as &bgr;-lactam antibiotics, antihistamines, bronchodilators and antiinflammatories, and cationic or anionic ion exchange resins which decrease the unpleasant taste and odor of the therapeutic agent.
There is still a need in the art for oral liquid quinolone preparations with acceptable taste. Applicants have satisfied this need in the art by preparing liquid quinolone preparations with acceptable taste.
DEFINITIONS AND USAGES OF TERMS
The term “pharmaceutical composition”, as used herein, means a combination comprised of a safe and effective amount of the quinolone compound active ingredient, or mixtures thereof, and pharmaceutically-acceptable excipients.
The term “pharmaceutically acceptable excipients”, as used herein, means any physiologically inert, pharmacologically inactive material known to one skilled in the art, which is compatible with the physical and chemical characteristics of the particular quinolone compound active ingredient selected for use. Pharmaceutically-acceptable excipients include, but are not limited to, polymers, resins, plasticizers, fillers, binders, lubricants, glidants, disintegrants, solvents, co-solvents, buffer systems, surfactants, preservatives, sweetening agents, flavoring agents, pharmaceutical grade dyes or pigments, and viscosity agents.
The term “ion exchange resin”, as used herein, means anionic or cationic ion exchange resins.
The term “oral dosage form”, as used herein, means any pharmaceutical composition intended to be systemically administered to an individual by delivering said composition to the gastrointestinal tract of an individual, via the mouth of said individual. Oral dosage forms include, tablets, coated or non-coated; liquids, such as solutions and suspensions; or capsules, coated or non-coated.
All percentages are on a weight percent basis unless otherwise indicated.
BRIEF SUMMARY OF THE INVENTION
The present invention relates to an aqueous pharmaceutical composition comprising:
a. 0.01% to 30% by weight of a quinolone compound or derivative thereof;
b. 0.01% to 60% by weight of an ion exchange resin;
c. pharmaceutically acceptable excipients to equal 100%.
DETAILED DESCRIPTION OF THE INVENTION
The present invention relates to an aqueous pharmaceutical composition comprising:
a. 0.01% to 30% by weight of a quinolone compound or derivative thereof;
b. 0.01% to 60% by weight of an ion exchange resin;
c. pharmaceutically acceptable excipients to equal 100%.
Quinolones and Derivatives Thereof Useful in the Practice of the Present Invention
Quinolones and derivatives thereof useful in the practice of the present invention include, but are not limited to, orbifloxacin, ciprofloxacin, danofloxacin, enoxacin, grepafloxacin, levofloxacin,lomefloxacin, nalidixic acid, norfloxacin, ofloxacin,sparfloxacin, and trovafloxacin mesylate. The preferred quinolone is orbifloxacin available from Schering Plough, Kenilworth, N.J. as ORBAX®. Other quinolones useful in the practice of the present invention are described in WO 96/16055 published May 30, 1996; U.S. Pat. No. 5,104,868 issued Apr. 14, 1992; U.S. Pat. No. 5,496,947 issued Mar. 5, 1996; U.S. Pat. No. 5,498,615 issued Mar. 12, 1996; U.S. Pat. No. 5,770,597 issued Jun. 23, 1998; U.S. Pat. No. 5,840,333 issued Nov. 24, 1998; U.S. Pat. No. 5,672,600 issued Sep. 30, 1997; U.S. Pat. No. 5,491,139 issued Feb. 13, 1996; U.S. Pat. No. 5,530,116 issued Jun. 25, 1996; and U.S. Pat. No. 5,646,163 issued Jul. 8, 1997, all incorporated by reference herein.
The quinolone compounds useful in the practice of the present invention comprise from about 0.01% to about 30% by weight of the pharmaceutical compositions of the present invention. Preferably, the quinolone compounds useful in the practice of the present invention comprise from about 0.1% to about 10% by weight of the pharmaceutical compositions of the present invention. More preferably, the quinolone compounds useful in the practice of the present invention comprise from about 0.5% to 5% by weight of the pharmaceutical compositions of the present invention.
Ion Exchange Resins Useful in the Practice of the Present Invention Ion exchange resins useful in the practice of the present invention include, but are not limited to, anionic resins such as: DUOLITE® AP143/1083 (cholestyramine resin USP) and cationic resins such as: AMBERLITE® IRP-64 (a porous copolymers of methacrylic acid crosslinked with divinylbenzene), AMBERLITE® IRP-69 (Sodium polystyrene sulfonate USP) and AMBERLITE® IRP-88 (Polacrilin Potassium). AMBERLITE® IRP 64 is preferred resin. The DUOLITE® and AMBERLITE® resins are available from the Rohm and Haas Company, Philadelphia, Pa. The DOWEX® resins, available from the Dow Chemical Company, Midland, Mich. are also useful in the practice of the present invention. Said DOWEX® resins are strong cationic exchangers based upon polystyrenesulphonic acid with variable crosslinking (1-12% divinylbenzene) in a variety of particle sizes.
Further, said AMBERLITE® IRP 69 (sodium polystyrenesulfonate) is available commercially as a sodium salt. However, it is within the scope of the present invention to convert the sodium salt to other salt forms including, but not limited to, K and Li.
The ion exchange resins useful in the practice of the present invention comprise from about 0.01% to about 60% by weight of the pharmaceutical compositions of the present invention. Preferably the ion exchange resins useful in the practice of the present invention comprise from about 0.2% to about 20% by weight of the pharmaceutical compositions of the present invention. More preferably, the ion exchange resins useful in the practice of the present invention comprise from about 0.5% to 15% by weight of the pharmaceutical compositions of the present invention
Pharmaceutically Acceptable Excipients Useful in the Practice of the Present Invention
As stated hereinabove, pharmaceutically-acceptable excipients include, but are not limited to, resins, fillers, binders, lubricants, solvents, glidants, disintegrants, co-solv
Fan Allan Chor-Lun
Gao Rong
Shao Zezhi Jesse
Stewart Daniel Charles
Witchey-Lakshmanan Leonore Catherine
Fubara Blessing
Page Thurman K.
Schering-Plough Veterinary Corporation
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