Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
1999-07-15
2004-02-24
Travers, Russell (Department: 1619)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S468000, C424S465000, C424S474000, C424S478000, C424S466000, C424S472000, C424S475000, C424S487000
Reexamination Certificate
active
06696085
ABSTRACT:
This is a continuation of a French Application 98 09221 filed on Jul. 20, 1998.
The present Application generally relates to the use of a polymer of acrylic type as a break-up or disintegration agent. It relates in particular to the use of a copolymer of acrylic type as disintegration agent or co-agent in a galenic form of tablet type, as well as a process for producing galenic forms of tablet type using such a copolymer as a disintegration agent or co-agent.
The agents most generally used for the production of galenic forms intended to disintegrate correspond to agents known as distintegration agents of the sodium carboxymethyl cellulose type, or to agents known as swelling agents of crospovidone or modified starch type.
While some of these agents allow tablets to be obtained which have a disintegration speed suited to the conditions in which they are used, while presenting acceptable pharmacotechnical characteristics (in particular hardness, friability and stability), this involves long and complex processes. In fact, the use of these agents as disintegration agents requires for example the creation of specific sub-structures such as microparticles or microgranules before the tablet is turned into its final galenic form, or the use of effervescent type reactions, which reactions themselves require the tablets to be manufactured in a low humidity medium.
SUMMARY OF INVENTION
The invention which is a subject of the present Application proposes a new use of a polymer of acrylic type and a new process which aims to remedy the drawbacks involved in the techniques of the prior art. The new use and the new process according to the invention also shows particularly appreciable performances for obtaining tablets which display appropriate disintegration properties under conditions of use or equivalent to this use while displaying very good pharmacotechnical characteristics (in particular hardness, friability, stability) before use and in particular during storage.
The polymers of acrylic type are, for their part, generally used in the prior art for the manufacture of sustained release tablets and/or for the production of enteric coatings. Among the different polymers of acrylic type known to a person skilled in the art, the US Pharmacopea National Formulary (USP/NF) makes a distinction in particular between methacrylic acid copolymers of type A, B or C and ammonium methacrylate copolymers of type A or B. It is in particular known that methacrylic acid copolymers of type A or B and ammonium methacrylate copolymers of type A or B can be used in the production of delay matrices (pH-dependent in the case of the first copolymers; pH-independent in the case of the second). The methacrylic acid copolymers of type C are for their part known as being able to be used in the production of different coatings: enteric coatings due to their gastro-resistent properties and their solubility in an intestinal medium at pH 5.5-7.5; insulation coatings intended to protect active ingredients in a tropical type environment; or also coatings intended to mask taste or smell.
DETAILED DESCRIPTION OF THE PREFFERED EMBODIEMENTS
The inventors have demonstrated that certain polymers of acrylic type, namely the methacrylic acid copolymers of type C according to the USP/NF, are, unexpectedly, capable of very significantly improving the disintegration speed of a tablet, while allowing a tablet to be obtained which has very good pharmacotechnical characteristics, and in particular very good cohesion. The use of a methacrylic acid copolymer of type C according to the invention has the particular advantage of allowing rapid disintegration tablets to be obtained, and in particular immediate type disintegration, which display, before use, very good pharmacotechnical characteristics (in particular, very good hardness and friability characteristics).
These very good pharmacotechnical characteristics simplify the packaging and storage of the tablets produced in this way: the tablets produced by means of the use or the process according to the invention do not require packaging specifically adapted to the protection of the structure of these tablets such as packaging with a peel-off film so as to avoid the extraction of the tablet from its cell by pushing with a finger.
These very good pharmacotechnical characteristics are also at the origin of the very good storage characteristics of said tablets over time (stability). These specific polymers of acrylic type according to the invention, in addition to the surprising disintegration effectiveness they offer, also have the notable advantage of being easy to use for producing tablets. In fact, they do not of themselves require the implementation of specific technologies to produce cohesive rapid disintegration tablets: any technology known to a person skilled in the art can be used, providing the other elements of the galenic form are chosen in such a manner as to allow this. In particular, they allow the production of cohesive rapid disintegration tablets by simple direct compression, without requiring the implementation of exacting technologies such as wet granulation.
A subject of the present Application is therefore, in general, the use of at least one methacrylic acid copolymer of type C according to the USP/NF as an agent or co-agent allowing the improvement of the disintegration speed of a tablet while allowing a tablet with a good cohesion to be obtained, in particular by simple direct compression. It relates in particular to the use of at least one methacrylic acid copolymer of type C according to the USP/NF as an agent or co-agent allowing or participating in the disintegration of a tablet, as well as a production process for tablets involving the use of at least one copolymer as a disintegration agent or co-agent in a tablet.
It relates in particular to the use of at least one methacrylic acid copolymer of type C according to the USP/NF as an agent or co-agent allowing or participating in rapid disintegration of immediate type of a tablet as well as a production process for rapid disintegration tablets, and in particular immediate disintegration tablets, using such a copolymer as a disintegration agent or co-agent.
The tablet disintegration effect observed according to the invention does not correspond to a simple erosion of mechanical type, but rather to an effect of the swelling type after appropriate hydration of the tablet.
By “tablet disintegration agent” is understood in the present Application an agent allowing an improvement in the disintegration speed observed for this tablet in the absence of this agent.
This improvement in tablet disintegration speed can naturally be optimized by choosing the other tablet characteristics (such as type and quantity of the tablet's components, mass, format, hardness of the tablet) such that they do not oppose or even that they enhance the disintegration phenomenon.
By “rapid tablet disintegration agent” is thus understood in the present Application an agent offering a significant improvement in the tablet's disintegration speed, as indicated above. The term “significant” can be appreciated using any statistical tool known to a person skilled in the art. Appropriate conditions for observing this significant improvement include those which consist in placing said tablet in medium conditions and in particular in composition, pH and temperature conditions suited to the disintegration of the tablet in question.
By “immediate type tablet disintegration agent” is understood an agent allowing the disintegration of said tablet over a period lasting approximately 25 seconds or less, preferably approximately 20 seconds or less, even more preferably approximately 10 seconds or less, when the tablet is tested under conditions appropriate for its disintegration, and when the other components of the tablet and its structure (mass, format, hardness) are chosen in such a way that they do not oppose, or they even enhance, the disintegration phenomenon. Appropriate conditions for testing the disintegration of a tablet include conditi
Pionnier Etienne
Rault Isabelle
Antares Pharma IPL AG
Sharareh Shahnam
Travers Russell
Winston & Strawn LLP
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