Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Patent
1987-11-10
1989-09-05
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
424 78, 424 81, 424923, A61L 904
Patent
active
048637203
DESCRIPTION:
BRIEF SUMMARY
The invention relates to a pharmaceutical preparation with benzodiazepines as active ingredients and to methods for its production.
Benzodiazepines, in particular the 1,3-Dihydro-7-nitro-5-phenyl-2H-1,4-benzodiazepine-2-one or Diazepam (7-Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepine-2-one) or Flurazepam 7-Chloro-1-2-(diethylamino)ethyl-5-(2-fluoro-phenyl)-1H-1,4-benzodiazepine -2(3H)-one or Triazolam, 8-Chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo-[4,3-a]-[1,4]benzodiaze pine or Alprazolam (8-chloro-1-methyl-6-phenyl-4H-1,2,4-triazolo[4,3-a][1,4]-benzodiazepine) or Midazolam (8-chloro-6-(2-fluoro-phenyl)-1-methyl-4 H-imidazolo[1,5]-[1,4]-benzodiazepine) are widely distributed as sedatives and are used especially in the case of disturbed sleep, anxiety states in a status epilepticus, spasms of central nervous origin etc. Benzodiazepines are generally used in form of tablets, whereby the onset of activity usually occur with a delay. Especially the previous ingestion of food may lead to a significant retardation of the therapeutic effect. A formulation with a more rapid absorption and thus a more rapid onset of activity was proposed in form of drops. Such drops require a not trembling hand for dosage and are therefore not intended for many patients especially by using it in connection with status epilepticus or spasms of central nervous origin. Pharmaceutical preparations containing benzodiazepines which are applicated in form of drops or soft gelatine capsules have already been described in the DE-OS No. 28 30 044.
The aim of the present invention is to prepare a form of administration of these well known drugs which guarantees a higher precision of the dosage, a more rapid bioavailability and especially an independence of the absorption from the previous intake of food. Moreover the preparation should be largely protected against manipulation. Because of the wide-spreading use of these drugs attempts of adding toxic substances to presentations like tablets or drops are possible. Moreover a relative slow onset of activity as in the case of a tablet formulation may cause an unnecessary high drug level in the patient, which can be prevented by an acceleration of the onset of effect. Especially patients suffering from insomnia and anxiety states tend to increase the dose in the case of an insufficient onset of activity. Similarly an inaccurate counting by administering the drug in form of drops may cause an overdosage.
Thus the present invention aims at avoiding the above mentioned disadvantages and in particular preparing a formulation with a very rapid onset of activity, a minimum risk of manipulation, an improvement of the precision of the dosage and altogether a reduction of the patient strain caused by an unnecessary high dosage.
To fulfil these demands the preparation of the present invention with benzodiazepines as active ingredients consists essentially of a solution of the active ingredient in polyalkylene glycol, and/or polyethylene glycol, and/or glycerine-polyethylene glycol oxy fatty acid esters such as glycerine-polyethyleneglycol oxyoleate and/or glycerine-polyethylene glycol oxystearate, and/or partial fatty acid esters of sorbitol and polyhydroxyethylene-sorbitol respectively, and/or polyvinylpyrrolindones, and/or polyvinyl alcohols, and/or polyhydroxyethylene fatty alcohol ethers and polyhydroxyethylene fatty acid esters respectively and/or polyhydroxyethylene-polyhydroxypropylene condensates and/or propylene carbonate which is filled in aerosol containers in combination with ethanol, which can be replaced at least in part by medium-chain fatty acid di-and/or -triglycerides and a pharmacologically inert propellant, in particular halogenated hydrocarbons and can be sprayed as a metered dose aerosol.
Due to the selection of the solvent proposed in the present invention such an aerosol surprisingly has shown an extremely rapid absorption, a much more rapid onset of activity and a more uniform action than other forms of administration. Due to the more rapid onset of activity the
Burghart Kurt
Burghart Walter
Page Thurman K.
Prater P. L.
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