Water soluble powder form compositions and their applications th

Details Water soluble powder form compositions and their applications th Water soluble powder form compositions and their applications th

1997-12-22

1999-08-10

Weddington, Kevin E.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

514199, 514200, 514311, 514600, 514951, A61K 914, A61K 3143, A61K 31545, A61K 3147

Patent

active

059356030

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to pulverulent and water-soluble compositions which are suitable for completely and rapidly dissolving active ingredients which are normally only soluble in water in the presence of basic salts, such as antibiotics of the beta-lactamide family, such as penicillins or their derivatives, cephalosporins or their derivatives, or other active ingredients such as sulfamides and quinolones, so that they can be absorbed by the oral route. Such compositions enable the active ingredients to be dissolved very rapidly, whatever the nature of the water employed, and, at the same time, provide an aqueous solution of active ingredient which is stable for from one to several days, thereby enabling them to be stored and therefore used over a period of one or more days.
The abovementioned active ingredients are known to lead rapidly, following oral absorption, to high concentrations in the blood. Given their broad spectrum of activity against both Gram-positive bacteria and Gram-negative bacteria, they have many therapeutic indications in human pharmacy or in the veterinary field: calves, pigs, poultry and others.
Soluble derivatives of the penicillins, such as the sodium or potassium salts of penicillin G, or the sodium salt of amoxicillin, or else the sodium salt of cefalexin, exist and have been very amply described in the literature. While being very soluble, these compounds suffer from the major drawback of at the same time exhibiting: generate, and
Thus, they are generally obtained by salifying in aqueous, frequently hot, solution and then evaporating the water using a standard technique such as lyophilization or spray drying; these different operations set in train well known reactions which degrade these molecules in alkaline medium, as soon as they have been prepared, with the said degradation reactions continuing even when the said compounds are in the pulverulent state.
In order to obtain aqueous solutions which can be administered by the oral route, the soluble salts of the penicillins are, for example, employed directly or formed in situ using pharmaceutically acceptable inorganic (solubilizing) salts of sodium, potassium, magnesium, ammonium or substituted ammonium. In these two cases, if the solubility is acceptable, the active ingredient is observed to be destroyed rapidly due to the alkaline character of the solution. This degradation is more substantial in the case of mixtures of antibiotics and inorganic (solubilizing) salts since, in order to achieve the desired solubility, it is necessary to have an excess of the solubilizing agent; however, on the one hand, the inorganic salt has a very basic character and, on the other hand, the stoichiometric ratio of 1:1, which is required in order to obtain dissolution, has to be modified in order to obtain the best solubility possible, leading to a particularly high pH being obtained. Nevertheless, mixtures of antibiotics and inorganic salts are more stable in the pulverulent state than are the soluble salts of penicillins.
Consequently, the object of the present invention is to make available a pulverulent composition which makes it possible to achieve, at one and the same time: latter,
The present invention relates to pulverulent, water-soluble compositions which are characterized in that they comprise, in combination and in pulverulent form: at alkaline pH, suitable for maintaining the pH of the medium at a value which is lower than the normal pH for solubilizing the said active ingredient.
Unexpectedly, such pulverulent compositions, which comprise, in combination, a salt of a strong base, which is employed in excess, and a buffer, that is to say a substance, or, more precisely, a mixture of substances, which maintains the pH of the medium in a precise pH range during and after dissolution, make it possible to solubilize the active ingredient very rapidly while preserving its integrity in solution over a period of from one to several days. The quantities of salt of a strong base and of buffer depend on the quantity and the nature

REFERENCES:
patent: 4726951 (1988-02-01), Panoz et al.
patent: 4933334 (1990-06-01), Shimizu et al.
patent: 5595762 (1997-01-01), Derrieu et al.

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