Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1999-04-26
2000-11-21
Spear, James M.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424468, 424474, 5147723, 514777, 514778, 514779, 514773, 514781, 514784, 514785, A61K 924, A61K 928, A61K 922
Patent
active
061499404
DESCRIPTION:
BRIEF SUMMARY
This applicatin is a 371 of PCT/FR97/01515 filed Aug. 27, 1997.
The present invention relates to a tablet with controlled release of alfuzosin hydrochloride and to a pharmaceutical composition containing one or more tablets.
Alfuzosin hydrochloride is an active substance that is known in the treatment of benign hypertrophy of the prostate. There is a wealth of data and experimental studies regarding the activity of the product. In particular, there is a large amount of data regarding the bioavailability of the product and the pharmacokinetics of the active substance. Indeed, it is an active substance which has a relatively short half-life and a more intense absorption at the duodenum-jejunum level, but the size of which decreases along the intestinal tract. Consequently, for an optimum effect, the administration of alfuzosin hydrochloride as conventional tablets (with rapid disintegration and dissolution) must be carried out several times a day. For these reasons, alfuzosin hydrochloride is a candidate for the production of a pharmaceutical preparation with controlled release in the promixal upper parts of the tract (duodenum and jejunum).
In the pharmaceutical field, noteworthy progress has been made in recent years in the production of increasingly improved systems for the release of active substances, which are capable of releasing the active substances conveyed per se according to kinetics and modes of release designed to allow optimum therapeutic effects.
Prolonged-release forms (or delayed-effect preparations) are characterized in that they convey a markedly larger amount of medicinal product than traditional pharmaceutical preparations, so as to allow the dosage to be simplified. That is to say that the administration decreases from two, three or more times a day to only one administration of a pharmaceutical preparation (or therapeutic system) capable of providing satisfactory therapeutic cover throughout the day.
Preparations of this type have been used and marketed for a long time, among which mention should be made of: chronoids, microcapsules and micro-matrices, tablets generically defined as "delayed-effect" tablets, gastro-resistent tablets and more complex preparations such as hydrophilic matrices which break down and/or swell. Recently, more refined therapeutic systems have been produced, for example so-called "reservoir" systems and the Geomatrix.RTM. systems as described in U.S. Pat. Nos. 4,839,177 and 5,422,123.
Most of these novel therapeutic systems are capable of releasing the active substance conveyed per se, at a constant rate (that is to say according to zero-order kinetics) up to complete release of the active substance, independently of the pH conditions of the gastrointestinal tract, and thus uniformly along the gastrointestinal tract. It results therefrom that these systems may be applied widely in the case of administration of medicinal products that are absorbed uniformly in the gastrointestinal tract. However, these pharmaceutical systems may have major drawbacks in the case where active substances per se would be conveyed, such as alfuzosin, having a more intense absorption at the duodenum-jejunum level which decreases thereafter in the tract. Indeed, in this case, only a very limited amount of the active substance conveyed may be absorbed and thus exert the desired therapeutic activity, whereas most of the medicinal product released by the pharmaceutical preparation cannot be absorbed since, in lower portions of the gastrointestinal tract, the biological barriers are relatively incapable of allowing the medicinal product to pass.
The subject of the present patent application is a tablet with controlled release of alfuzosin hydrochloride, which overcomes the drawbacks mentioned above.
The invention consists of a pharmaceutical tablet containing two or three layers, characterized in that it has the following structure: on contact with aqueous biological fluids, the said layer being produced by compression of a mixture or of a granulate comprising hydrophilic polymers constit
REFERENCES:
patent: 4661491 (1987-04-01), Regnier
patent: 4839177 (1989-06-01), Colombo et al.
patent: 5422123 (1995-06-01), Conte et al.
patent: 5589190 (1996-12-01), Andrieu et al.
Conte Ubaldo
Dufour Alain
Grenier Pascal
Jarreau Fran.cedilla.ois Xavier
Maggi Lauretta
Jagotec AB
Spear James M.
Synthelabo
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