Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1996-10-22
1998-08-25
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514885, 514924, A61K 3114
Patent
active
057983917
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/FR95/00070, filed Jan. 23, 1995.
The invention concerns a solution which can be administered intravascularly consisting of at least one benzalkonium fluoride.
EP-A-0,308,564 already mentions the use of benzalkonium fluoride to obtain a composition for general or parenteral administration with between 0.05% and 7%, more particularly of the order of 1% in weight of benzalkonium fluoride, intented to act against viruses and retroviruses, particularly herpes or the LVAs responsible for AIDS.
Nevertheless, benzalkonium fluoride is supposed, as with all the benzalkonium salts which are tensio-active, to have a strong h.ae butted.molytic effect, prohibiting its intravascular administration. Thus, although general or parenteral administration of benzalkonium fluoride are mentionned in EP-A-0,308,564, its use in practice comes up against this difficulty, until now considered insurmountable for two reasons: the concentration to reach in the blood to arrive at an activity was itself supposed to lead to h.ae butted.molysis of the blood; injection, even administered very slowly, supposes the local creation of a high, thus h.ae butted.molytic, concentration of benzalkonium fluoride. In particular, injection of this salt at concentrations of the order of 1% weight appeared to be impossible. Now this concentration was considered indispensable to obtain a sufficient activity. We thus renounced the use of benzalkonium salts, and particularly benzalkonium fluoride, by intravascular administration, considering that the concentrations of the injected solutions would suppress all virucidal and bactericidal activity, taking into account the minimal inhibiting concentration measured in vitro, and that, even at these low concentrations, a very high risk of h.ae butted.molysis, and thus immediate death, persists. Thus until now, intravascular administration of benzalkonium salts, and notably benzalkonium fluoride in man or animals was considered purely and simply forbidden.
A constant need makes itself felt for a shock treatment against viral or infectious affections, notably of immunodeficient origin, and in particular in the treatment of patients suffering from AIDS in the declared or evolutive phase which present severe opportunistic infections leading rapidly to dehydration and death.
Such a shock treatment poses a series of apparently contradictory problems, however: for the deteriorated clinical state of the patient, but equally against the virus responsible for the immunodeficiency (the case of AIDS), variety of affections which may be involved in the case of an immunodeficiency, not irritate or attack healthy organs or cells in an already considerably weakened organism.
The invention thus aims in a general way at finding a solution to this general problem which has not, until now, been resolved. It thus aims at offering a treatment to patients suffering from viral or severe infectious affections, particularly multiple ones, such as those due to an immunodeficiency.
More particularly, the inventors discovered with surprise that, among the quaternary ammoniums, benzalkonium fluoride can be effectively injected intravascularly without risk of h.ae butted.molysis within a precise range of concentrations with which an effective activity is, nevertheless, noted.
The invention thus aims more particularly at offering an injectable solution of an antiviral or anti-infectious agent such as a benzalkonium salt.
For this, the invention concerns a solution administerable intravascularly, characterised by a content of the order of 0.23% or less in weight of a benzalkonium fluoride having the formula: ##STR2## where R is an alkyl radical which may vary between C.sub.8 H.sub.17 and C.sub.18 H.sub.37, dissolved in an excipient injectable intravascularly.
We could in effect note that when the proportions by weight of benzalkonium fluoride are of the order of 0.23% or less, and more particularly of the order of 0.20% of weight, no h.ae butted.molysis is to be feared in general, contrary to the previous general
REFERENCES:
patent: 5026561 (1991-06-01), Bourbon et al.
Bourbon Pierre
Lagny Pierre
Aromafarm Limited
Jordan Kimberly
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