Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
2000-04-20
2003-04-22
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S464000, C424S489000, C424S490000, C424S497000, C424S451000, C424S452000, C424S457000, C424S458000, C424S468000, C424S469000, C424S470000
Reexamination Certificate
active
06551617
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a coating applied to the outside of a pharmaceutically active ingredient. More particularly, the present invention relates to a coating that masks the taste of a pharmaceutically active ingredient.
2. Description of the Prior Art
In general, there are two types of tablet dosage forms that are available in the marketplace, one that can be swallowed as a whole entity and the other as a chewable tablet. If the tablet is swallowed whole, the unpleasant taste of the pharmaceutically active ingredient is greatly minimized or avoided altogether. However, tablets formulated in a chewable form are designed for young children and for people with difficulty swallowing. Hence, the undesirable taste of the chewable tablet is mainly due to the bad taste of the pharmaceutically active ingredient. This can ultimately create a feeling of reluctance to taking medicine.
The use of a coating as part of a medicament is known. The coating is typically applied for the ease of swallowing and provides a barrier, which prevents the undesirable taste of the drug ingredient from coming through, making the drug preparation more palatable. In addition, this type of coating can be designed to act as a time release mechanism to control the rate of release of the medicine in the body. This can be accomplished in various ways such as adjusting the thickness of the coating and selection of the coating polymers/components that are used in these types of specialized coating formulations.
Various types of coatings can be applied to the outside of tablets and drug powders to achieve a specific desired effect. Enteric coatings are designed to be soluble in the intestine, where the pH is 6.5 or higher, but insoluble in the stomach, where the pH is lower. On the other hand, reverse enteric coatings are designed to be partially soluble in the stomach, i.e. under acidic or lower pH conditions, thereby releasing the drug in the stomach. Coatings can also be used for masking purposes including taste masking of chewable products.
Several U.S. patents are directed to taste masking. However, none disclose the coating of the present invention.
U.S. Pat. No. 4,851,226 issued on Jul. 25, 1989 to Julian et al. It provides a chewable medicament tablet made from granules coated with a blend of cellulose acetate or cellulose acetate butyrate and polyvinyl pyrrolidone.
U.S. Pat. No. 5,075,114, which issued on Dec. 24, 1991 to Roche, provides a taste masking and sustained release coating applied to a tablet. The coating blend is made with cellulose acetate and/or cellulose acetate butyrate and hydroxypropyl cellulose.
U.S. Pat. No. 5,489,436 issued on Feb. 6, 1996 to Hoy et al. This patent provides chewable tablets that have a coating consisting essentially of dimethylaminoethyl methacrylate and neutral methacrylic acid ester, and a polymer selected from the group consisting of cellulose acetate, cellulose triacetate, and mixtures thereof.
SUMMARY OF THE INVENTION
It is an object of the present invention to provide a coating or coating composition that coats a pharmaceutically active ingredient or particle and, thus, is part of a medicament.
It is another object of the present invention to provide such a coating that masks the undesirable taste, without delaying the availability of the pharmaceutically active ingredients when consumed orally.
It is also an object of the present invention to provide such a coating that is substantially insoluble in water and in a neutral pH environment, e.g. the mouth.
It is still another object of the present invention to provide such a coating that rapidly breaks down in an acid environment, such as in the stomach, thereby releasing the drug.
It is yet another object of the present invention to provide such a coating that readily dissolves, yet the rate of dissolution can be modified based on the composition.
It is a further object of the present invention to provide a medicament comprising a pharmaceutical active agent and the coating.
It is a still further object of the present invention to provide such a medicament in a variety of forms.
It is a still yet a further object of the present invention to provide a pharmaceutical composition comprising one or more pharmaceutical active agents coated with the coating of the present invention, which has an alkaline component in the coat composition that enhances the performance of the coat.
To accomplish the foregoing objects and advantages, the present invention, in brief summary, is a coating composition that masks the taste of a drug ingredient or medicine taken orally. The composition has (a) polyvinyl acetate, and (b) a dimethylaminoethyl methacrylate and neutral methacrylic acid ester.
In another embodiment, the coating composition of the present invention not only masks the taste of the medicine, but readily dissolves at an enhanced rate in an acid environment. The coating composition of this embodiment has (a) polyvinyl acetate, (b) a dimethylaminoethyl methacrylate and neutral methacrylic acid ester, and (c) an alkaline modifier.
DETAILED DESCRIPTION OF THE INVENTION
In the present application, a medicament is defined as a drug ingredient that is coated with a coating composition. Taste masking is defined as a perceived reduction of an undesirable taste that would otherwise be there.
The mouth is, for the most part, a neutral environment where the pH is about 7. One can mask the unpleasant taste of a drug by surrounding the drug ingredient, drug particle, or an agglomeration of drug particles with a coating composition that is insoluble in the mouth. The coating must be formulated to rapidly break down in the stomach to release the pharmaceutically active ingredient into the body. The present invention accomplishes this by providing a coating composition that effectively masks the unpleasant taste of a pharmaceutically active ingredient, i.e., drug or medicine, taken orally and immediately dissolves in an acidic pH environment, thereby releasing the pharmaceutically active ingredient in the stomach. Moreover, there is no noticeable after taste.
The coating composition of the present invention has a taste masking blend. The blend is (a) polyvinyl acetate, and (b) a dimethylaminoethyl methacrylate and neutral methacrylic acid ester. Additionally, the composition may include an alkaline modifier.
In a preferred embodiment, the present invention is a medicament having a drug ingredient, and a coating composition for masking the taste of the drug ingredient. The blend has (a) polyvinyl acetate and (b) a dimethylaminoethyl methacrylate and neutral methacrylic acid ester. Optionally, the coating composition of the medicament may have an alkaline modifier that enhances the release of the drug ingredient into one's body. That is, the inclusion of the alkaline modifier in the coating composition quickens the release of the drug ingredient in the stomach.
Polyvinyl acetate is the first component in the coating composition of the present invention. The polyvinyl acetate is insoluble in water. This property gives a composition containing polyvinyl acetate resistance to dissolution in the mouth. The polyvinyl acetate can be provided in its pure form or as a blend. BASF Corporation provides such a blend, commercially available under the tradename KOLLIDON SR. KOLLIDON SR is a blend that contains primarily polyvinyl acetate, polyvinylpyrrolidone, and minor amounts of sodium lauryl sulfate and colloidal silica.
The coating composition of the present invention includes about 3 percentage by weight or weight percent (wt. %) to about 97 wt. % of polyvinyl acetate of the total weight of the composition. Preferably, the polyvinyl acetate is included in an amount about 10 wt. % to about 70 wt. %, and more preferably, about 15 wt. % to about 50 wt. %. Above 50 wt. %, the polyvinyl acetate may be difficult to dissolve.
The dimethylaminoethyl methacrylate and neutral methacrylic acid ester is the second component in the present coating composition. This compound is available comm
Corbo Michael
Desai Jatin
Patell Mahesh
Warrick Ronald
Bristol--Myers Squibb Company
Di Nola -Baron Liliana
Page Thurman K.
Provoost Jonathan N.
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