Drug – bio-affecting and body treating compositions – Inorganic active ingredient containing – Aluminum – calcium or magnesium element – or compound containing
Reexamination Certificate
2001-05-29
2003-02-04
Jones, Dwayne C. (Department: 1614)
Drug, bio-affecting and body treating compositions
Inorganic active ingredient containing
Aluminum, calcium or magnesium element, or compound containing
C514S892000, C514S574000
Reexamination Certificate
active
06514537
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to a novel magnesium citrate solution.
BACKGROUND OF THE INVENTION/Description of the Prior Art
The therapeutic use of magnesium citrate as a gentle laxative is well known. Magnesium citrate oral solutions are considered saline laxatives that are widely available over the counter. Magnesium citrate attracts and retains water in the intestine, softening stools and inducing the urge to defecate. A typical dose for adults is about 10 to 14 ounces daily in 1 or more doses.
Relevant background information and prior art oral solutions are discussed below.
U.S. Pat. No. 2,363,108 to Kane et al., issued on Nov. 21, 1944, incorporated herein by reference, describes a stable laxative composition comprising magnesium fumarate, fumaric acid and sodium bicarbonate. See Example 3, which describes the solution as having similar properties as magnesium citrate.
U.S. Pat. No. 4,664,920 to Saleeb et al., issued on May 12, 1987, incorporated herein by reference, discloses a method for fixing a water-soluble water-dispersible or water-emulsifiable food ingredient that comprises magnesium salts of citric acid. See examples 5 and 6 where aqueous magnesium citrate solutions were prepared.
U.S. Pat. No. 5,219,889 to Walsdorf et al., issued on Jun. 15, 1993, incorporated herein by reference, describes a potassium magnesium citrate used as dietary supplement.
U.S. Pat. No. 5,432,200 to Walsdorf et al., issued on Jul. 11, 1995, incorporated herein by reference, is a division of U.S. Pat. No. 5,219,889.
U.S. Pat. No. 5,780,046 to Humber et al., issued on Jul. 14, 1998, incorporated herein by reference, describes an oral formulation of ibuprofen comprising citric acid, sodium benzoate and disodium edetate. See Examples 1 and 2.
U.S. Pat. No. 5,811,131 to Mackles et al., issued on Sep. 22, 1998, incorporated herein by reference, describes a tasteless liquid composition. The loperamide suspension of Example 1 contains magnesium hydroxide and citric acid.
U.S. Pat. No. 5,958,445 to Humber et al., issued on Sep. 28, 1999, incorporated herein by reference, describes an oral formulation comprising citric acid, sodium benzoate and disodium edetate. See Examples 1 and 2.
U.S. Pat. No. 3,211,614 to Embring et al., issued on Oct. 12, 1965, incorporated herein by reference, describes a laxative composition consisting essentially of the following ingredients: an alkali salt of an aliphatic polybasic hydroxy acid such as citric acid; an alcohol; and water.
U.S. Pat. No. 4,716,153 to Morishita et al., issued on Dec. 29, 1987, incorporated herein by reference, describes citric acid is used as dissolution accelerator to prepare stable oral antibiotic formulation.
U.S. Pat. No. 5,858,403 to Borody et al., issued on Jan. 12, 1999, incorporated herein by reference, describes an osmotic colonic evacuant in solid dosage form comprising a phosphate/sulfate based laxative, sodium picosulfate and an antacid, for example, magnesium citrate/magnesium oxide with citric acid. See col. 6 table and lines 56-58. The patent describes a powder formulation that can be encapsulated. According to the disclosure, the capsules can also be used as a laxative.
U.S. Pat. No. 5,213,838 to Sheikh, issued on May 25, 1993, incorporated herein by reference, describes a sodium-free composition prepared from a solution containing sufficient citric acid to provide an initial solution pH equal to or less than about 3.5. The composition has primary components of potassium citrates, calcium citrates, and mixtures thereof. The composition may additionally contain amounts of magnesium citrate suitable for therapeutic use as a gentle dietary laxative. The solutions of this disclosure are added to citric acid in an amount to raise the pH to about 3.5. See example 1 and claim
1
.
SUMMARY OF THE INVENTION
The present invention relates to a magnesium citrate formulation that has an increased citric acid level. In another embodiment of the present invention, the magnesium citrate oral solution has an increased citric acid level and the incorporation of a suitable preservative.
As stated above, the therapeutic use of magnesium citrate as a gentle laxative is well known. The inventor has developed an improved magnesium citrate solution that has a lower crystallization level, does not require pasteurization, requires less filtering during production, and is less expensive to produce. Furthermore, the magnesium citrate solution of the present invention is less susceptible to microbial contamination and has a longer shelf live than traditional magnesium citrate solutions.
As discussed above, the novel magnesium citrate solution of the present invention has a therapeutic use as a gentle laxative and has many benefits over traditional oral magnesium citrate solutions.
One embodiment of the present invention, a magnesium citrate oral solution comprises citric acid in an amount greater than 10% weight/volume; magnesium hydroxide in an amount ranging from about 1.5-5% weight/volume; and water. Most preferably, the citric acid is present in an amount of about 10.9% weight/volume. Additionally, preferably the magnesium hydroxide is present in an amount of from 1.5 to 3.0% weight/volume. More preferably, the magnesium hydroxide is present in an amount of from 2.0 to 3.0% weight/volume.
Another embodiment of the present invention is a method of treating constipation in a patient in need thereof. The method of this embodiment comprises administering an effective amount of an oral composition that comprises citric acid in an amount greater than 10% weight/volume. Preferably, the composition of this embodiment comprises citric acid in an amount of 10.9% weight/volume.
DETAILED DESCRIPTION OF THE INVENTION
The magnesium citrate solution of the present invention comprises a citric acid level of over 10% w/v. The present inventor has found that increasing the citric acid level, among other things, eliminates the propensity of the active ingredient of the solution to crystallize in the bottle upon aging. Additionally, the magnesium citrate solution of the present invention is less susceptible to microbial contamination. For example,
Staph. hominis
and
Bacillus coagulans
organisms have been recovered from commercial magnesium citrate solutions. The present invention is much less susceptible to such contamination.
Current United States Pharmacopoeia standards do not specify a maximum level for citric acid. The USP standard only sets forth a minimum of 7.59% weight/volume. The current industry practice is approximately 8.95% weight/volume.
Additionally, the current practice with respect to magnesium citrate solutions is to require a pasteurization step. This is because a non-pasteurized solution may crystallize in a very short period of time. In some instances, crystallization will occur in two months or less. The present inventor has discovered a formula for an oral solution that will not crystallize in the absence of a pasteurization step.
In one embodiment of the present invention, benzoic acid is added as a preservative. The addition of preservatives is preferred because, even though typically directed to, in many cases consumers do not ingest an entire bottle in a single dose. That is, even though magnesium citrate solutions are typically packaged as single dose units, they are many times only partially ingested and the remaining product is saved for a later application. The incidence of microbial contamination (including mold and yeast contamination) is greater in the remaining portion of the unpreserved product than with a preserved product. Pasteurization reduces the microbial load in the product, but does not prevent microbes from being introduced after the bottle is opened. Unfortunately, a typical magnesium citrate formula provides microbes with an ideal environment to grow and flourish. However, these embodiments of the present invention provide a continual defense against the growth of microbes in a partially used unit.
Additionally, the uniqueness of these embodiments allows for the use of plastic bottles instead of
Cumberland Swan Holdings, Inc.
Delacroix-Muirheid C.
Jones Dwayne C.
Schelling Douglas W.
Waddey & Patterson , P.C.
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