Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
1998-09-14
2003-07-29
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S465000, C424S488000, C514S676000, C514S678000, C514S689000, C514S772000, C514S781000
Reexamination Certificate
active
06599530
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to a new pharmaceutical composition comprising a catechol derivative and croscarmellose sodium as a dissolution enhancing agent. Accordingly, the present invention relates to an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof, and croscarmellose sodium (Ac—Di—Sol) as a dissolution enhancing agent. Particularly, the invention relates to an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof and croscarmellose sodium, wherein the amount of croscarmellose sodium in the composition is at least 6% by weight, more preferably from about 8% to about 16% by weight, especially from about 10% to 14% by weight. Preferably the oral compacted composition is in the form of a tablet. Further, the present invention relates to a method of preparing an oral compacted composition comprising entacapone, nitecapone, or pharmaceutically acceptable salt thereof, and croscarmellose sodium. The present invention also relates to the use of croscarmellose sodium in the manufacture of an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof.
The chemical names of entacapone and nitecapone are (E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2-propenamide and 3-(3,4-dihydroxy-5-nitrobenzylidene)-2,4-pentanedione, respectively. Entacapone and nitecapone are described in U.S. Pat. No. 5,446,194 as catechol-O-methyltransferase (COMT) inhibitors. Enteral and parenteral routes of administration are discussed in U.S. Pat. No. 5,446,194.
It is desirable that entacapone, nitecapone, or a pharmaceutically acceptable salt thereof, is released from the oral composition as soon as possible after ingesting it. This can normally be achieved by using a dissolution enhancing agent in the pharmaceutical composition. The dissolution enhancing agent may be a disintegrant or any other agent that enhances the dissolution. There is a vast selection of different dissolution enhancing agents, including disintegrants, on the market, which have different chemical and physical characteristics. When selecting the best dissolution enhancing agent to be used in a pharmaceutical composition in combination with an active agent, numerous factors have to be considered, e.g., the chemical and physical characteristics of the active agent and the dissolution enhancing agent, the chemical and physical characteristics of the auxiliary agents, such as diluents and binders, the method of preparing the composition, etc.
Croscarmellose sodium is a cross-linked polymer of carboxymethyl-cellulose sodium. According to the Handbook of Pharmaceutical Excipients (Ainley Wade and Paul J. Weller, Second Edition, The Pharmaceutical Press, London, 1994), it is used in oral pharmaceutical formulations as a disintegrant for tablets, capsules, and granules. Typically, concentrations from 0.5 to 5% w/w are used as a tablet disintegrant.
Neither the above-cited patent nor any other patent or publication of which applicants are aware describes an oral compacted composition comprising entacapone, nitecapone, or pharmaceutically acceptable salt thereof, and croscarmellose sodium.
SUMMARY OF THE INVENTION
Applicants have discovered that croscarmellose sodium is a superior disintegrant to be used in an oral compacted composition comprising entacapone, nitecapone, or pharmaceutically acceptable salt thereof. Accordingly, an object of the invention is to provide an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof and croscarmellose sodium. The composition is premised on the discovery that croscarmellose sodium essentially increases the release rate of entacapone or nitecapone from an oral compacted composition. Particularly, an object of the invention is to provide an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof and croscarmellose sodium, wherein the amount of croscarmellose sodium in the composition is at least 6% by weight, more preferably from about 8% to about 16% by weight, especially from about 10% to 14% by weight.
Preferably, the oral compacted composition is in the form of a tablet and, therefore, an object of the invention is to provide a tablet comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof and croscarmellose sodium.
A further object of the invention is to provide a tablet comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof and croscarmellose sodium, wherein the amount of croscarmellose sodium is at least 6% by weight, more preferably from about 8% to about 16% by weight, especially from about 10% to about 14% by weight.
An object of the invention is also to provide a method for preparing an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof, and croscarmellose sodium, wherein said method comprises mixing a pharmaceutically effective amount of entacapone, nitecapone, or a pharmaceutically acceptable salt thereof, one or more auxiliary agents, and croscarmellose sodium to obtain a first mixture; compacting and crushing the first mixture one or more times to obtain a plurality of granules; adding a lubricant, a glidant or a mixture thereof to the granules to obtain a second mixture; and compressing the second mixture into a plurality of tablets.
An object of the invention is to provide a method of inhibiting catechol-O-methyltransferase by administering to a patient in need thereof an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof.
A further aspect of the invention relates to the use of croscarmellose sodium in the manufacture of an oral compacted composition comprising entacapone, nitecapone, or a pharmaceutically acceptable salt thereof.
Additional objects and advantages of the invention will be set forth in part in the description which follows, and in part will be obvious from the description, or may be learned by practice of the invention. The objects and advantages of the invention will be realized and attained by means of the elements and combinations particularly pointed out in the appended claims.
It is to be understood that both the foregoing general description and the following detailed description are exemplary and explanatory only and are not restrictive of the invention, as claimed.
REFERENCES:
patent: 5380535 (1995-01-01), Geyer et al.
patent: 5446194 (1995-08-01), Backstrom et al.
patent: 5489614 (1996-02-01), Korkolainen et al.
Remington: The science and practive of pharmacy. 19thEdition 1995. Mack Publishig Company Ed: Gennaro. pp. 1619-1626.*
A. Wade and P. J. Weller, Croscarmellose Sodium,Handbook of Pharmaceutical Excipients, Second Edition, The Pharmaceutical Press, London, 1994, 141-142.
Co-pending U.S. application No. 09/787,027, filed on Jun. 25, 2001.
Fielder, “Lexikon Der Hilfsstoffe” Editio Canteor Verlag, Aulendorf, Germany XP 002126381, 1996.
Co-pending U.S. application No. 09/605,529, filed on Jun. 29, 2000.
Channavajjala Lakshimi
Finnegan Henderson Farabow Garrett & Dunner LLP
Orion Corporation
Page Thurman K.
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