Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1995-03-17
1999-05-11
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424465, 424489, 5147722, 5147723, 514773, 514774, 514775, 514776, 514777, 514778, 514779, 514782, 514783, A61K9/14;9/20
Patent
active
059026065
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a formulation comprising sparingly water-soluble medicinal substances, which has a molecularly disperse distribution of the sparingly water-soluble medicinal substance in a hydrophilic peptide having a molecular weight above 100 D.
The invention furthermore relates to a process for the preparation of such formulations comprising sparingly water-soluble medicinal substances.
The invention also relates to pharmaceutical formulations which comprise such formulations of sparingly water-soluble medicinal substances.
The problem of imparting solubility to or solubilizing sparingly water-soluble substances is sufficiently known, for example, in pharmaceutical technology. The presence of the substance in the dissolved and non-dissociated state is an essential prerequisite for absorption of the substance in the organism. To remedy this problem, a number of possibilities exist:
Changes to the molecule itself include measures such as salt formation or introduction of a hydrophilic molecular radical. Although such interventions lead to compounds which have a better water-solubility, these are dissociated or changed in their original molecular structure.
The use of organic solvents, such as, for example, ethanol or polyethylene glycols, for example in liquid formulations, is not always desirable or promising bearing in mind that, on aqueous dilution in the physiological medium, the substances thus kept in solution may precipitate and are therefore not absorbable.
If surfactants are employed as solubilizing agents, or water-soluble complexes (for example cyclodextrin inclusion compounds) are prepared, possible undesirable side effects, such as, for example, the membrane-damaging cellular action of such substances, must be borne in mind.
Finally, the hydrotropic substances, such as urea or N-methylacetamide, may also be mentioned, but these have to be used in concentrations of 20-30% in order to obtain a true solution.
Summarizing, it can thus be said that the prior art to date offers no satisfactory solutions and in many cases adequate solubilization has still not been found for substances which present particular problems.
This fact means that medicinal formulations of sparingly water-soluble medicinal substances are to be evaluated critically in respect of their preparation and use in treatment.
The invention is therefore based on the object of converting sparingly water-soluble medicinal substances into a form such that the dissolved (molecularly disperse) state of the medicinal substance is ensured in a simple manner both during storage and during use of the formulation by the user or patient, without being associated directly with the presence of organic solvents or of solubilizing agents which cause undesirable side effects.
It is a particular object of the present invention to develop medicaments which comprise sparingly water-soluble medicinal substances and which avoid the disadvantages mentioned for the prior art and therefore improve the efficacy and bioavailability of such substances, in order to achieve an effective therapeutic utilization of such drugs.
This object is achieved by a formulation comprising sparingly water-soluble medicinal substances, which has a molecularly disperse distribution of the sparingly water-soluble medicinal substance in a hydrophilic peptide having a molecular weight above 100 D.
This object is furthermore achieved by a process for the preparation of such formulations comprising sparingly water-soluble medicinal substances as claimed in claim 24. Embodiments of the formulations according to the invention and of the process for their preparation are mentioned and claimed in the subclaims.
Finally, this object is achieved by pharmaceutical formulations which comprise such formulations of sparingly water-soluble medicinal substances.
The present invention is thus based on the completely surprising finding that a hydrophilic peptide having a molecular weight above 100 D is of itself sufficient to stabilize sparingly water-soluble medicinal substances
REFERENCES:
patent: 5080907 (1992-01-01), Iijima et al.
Freidenreich Jurgen
Schick Ursula
Werry Jurgen
Wunderlich Jens-Christian
Alfatec-Pharma GmbH
Page Thurman K.
Spear James M.
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