Effervescent composition containing iodinated polyvinylpyrrolido

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills

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424489, 5147723, 514777, A61K 946

Patent

active

058465642

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/FR96/00157 filed Jan. 30, 1996.
This invention relates to an iodinated polyvinylpyrrolidone-based effervescent composition.
It relates to the use of this composition for the purposes of disinfection.
Iodine has long been used in various pharmaceutical forms (solution, tincture) in the fine disinfection of small wounds. Despite its efficacy, application of the product is limited due to the fact that it presents a certain number of side effects.
Iodinated polyvinylpyrrolidone (IPVP) is a complex of polyvinylpyrrolidone (PVP) and iodine. Owing to its complexation with the polyvinylpyrrolidone molecule, the iodine contained in the complex is released slowly and gradually.
IPVP is characterized by a wide range of applications, principally in the prophylactic field:
This compound is a broad-spectrum antiseptic:
Iodinated polyvinylpyrrolidone (IPVP) is generally presented in the form of a solution.
There are, however, notable disadvantages with this formulation due to its poor conservation properties, high manufacturing price and storage and handling problems.
IPVP tablets have already been described but with specific reference to mucoadhesive and local use.
To the best of the applicant's knowledge, no IPVP preparation permitting the extemporaneous production of solutions, in the form of granules, tablets or any other solid form, has ever been described.
Owing to the particularly strong binding power of the PVPs, the IPVP tablets present in fact the major drawback of dissolving very slowly in aqueous media.
Thus, the abstracts of patent JP 63 225 308 (SANYO CHEMICAL CORPORATION Ltd.) describe compositions notably containing an iodine carrier which may be polyvinylpyrrolidone, an iodide or an iodine compound, an oxidizing agent, an acid or a base in powder form. The latter two compounds form an effervescent couple. This composition does not, however, comprise iodinated polyvinylpyrrolidone, a complex which has to be formed before it can be integrated in a composition. Moreover, the composition does not contain a disintegrating agent and consequently cannot be used for the extemporaneous production of IPVP solutions, but only for forming foam, as indicated in the abstracts hereabove mentioned.
Patent GB-A-2 108 386 (AUCHINCLOSS) describes compositions in dry forms containing an iodine source, such as a complex of polyvinylpyrrolidone and iodine, a non-reducing acid and a tensioactive agent capable of combining with iodine to form an iodophor. This patent makes no mention of the presence of a disintegrating agent nor even an effervescent couple.
Patent application PCT/GB 90 01 423 (AUCHINCLOSS) discloses a composition comprising an inorganic halide soluble in water, a strong oxidizing agent which will react with the halide so as to generate hypohalic ions, sulfamic acid, and a carbonate or bicarbonate soluble in water in order to produce, in reaction with the acid, an effervescent effect. The presence of a disintegrating agent is not mentioned in this application which preferentially concerns chlorine-based tablets.
U.S. Pat. No. 3,136,692 (STRONG CORB ARNER, INC.) concerns effervescent compositions containing polyvinylpyrrolidone, a solid organic acid and a therapeutic agent or a flavoring agent. Neither iodinated polyvinylpyrrolidone nor a disintegrating agent is mentioned in this patent.
It therefore emerges from an analysis of the current state of the art, and to the best of the applicant's knowledge, that none of the compositions described make it possible to obtain extemporaneously iodinated polyvinylpyrrolidone solutions.
It will also be noted that, with the compositions of the current state of the art, it is not possible to obtain reproducible solutions of IPVP presenting determined free iodine levels. This is particularly true in the case of the Japanese patent which associates free PVP and free iodine in foams, and which does not use a previously formed IPVP complex.
The applicant therefore endeavored to develop compositions which contain IPVP and which also permit extempor

REFERENCES:
patent: 5089606 (1992-02-01), Cole et al.

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