Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form
Reexamination Certificate
1998-09-17
2001-03-06
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
C424S451000, C424S456000, C424S464000, C424S474000, C424S475000, C424S477000, C424S479000
Reexamination Certificate
active
06197314
ABSTRACT:
The present invention relates to oral administration forms from which the active ingredients can be isolated only with difficulty.
Amphetamines and ephedrones are dependency-forming drugs frequently used in the drug scene. The starting materials for preparing these substances are, inter alia, the active ingredients which are used in medicines for colds, racemic, (+)- and (−)-ephedrine, racemic, (+)- and (−)-pseudoephedrine and the corresponding phenylpropanolamines which are unsubstituted on the amino group. Since distribution of these substances is subject to strict international regulation and control, attempts are frequently made to isolate the starting materials from medicines and process them further to the corresponding drugs.
An aqueous solution of said active ingredients can easily be obtained from commercially available medicinal products, for example by comminution, acidic aqueous extraction and filtration, and they can be isolated therefrom by extraction with organic solvents after addition of alkali.
We have now found a way of making it possible to impede the isolation of said starting materials from medicines.
The present invention relates to solid oral pharmaceutical administration forms from which the active ingredients can be isolated only with difficulty, which comprise, besides conventional ingredients, as addition a mixture of pharmacologically suitable fats or gel formers with surfactants in an amount such that, when the forms are introduced into aqueous media, there is formation of a poorly filterable liquid which forms a creamy emulsion on extraction with organic solvents.
The present invention furthermore relates to the use of mixtures of pharmacologically suitable fats or gel formers with surfactants to impede the extraction of active ingredients out of solid oral pharmaceutical administration forms.
Active ingredients to be particularly considered are racemic ephedrine, (+)-ephedrine, (−)-ephedrine, racemic pseudoephedrine, (+)-pseudoephedrine and (−)-pseudoephedrine, and the corresponding phenylpropanolamines which are unsubstituted on the amino group, such as norephedrine and norpseudoephedrine. As a rule, the active ingredients are present in the medicines in the form of their salts with physiologically tolerated acids, in particular as hydrochlorides or sulfates.
Solid oral administration forms which may be mentioned are tablets, coated tablets (film- or sugar-coated tablets) and capsules (hard and soft gelatin capsules).
Pharmacologically suitable fats are: palm oil, hardened palm oil (P058), apricot kernel oil, cottonseed oil, carnauba wax, glycerol monostearate, mono- and diglycerides, cetyl alcohol, cetyl palmitate, hard fat USPXXII, coconut oil and arachis oil.
Pharmacologically suitable gel formers are xanthans, alginic acid and alkali metal alginates, gum arabic, agar, ghatti gum, karaya gum, tragacanth, guar gum, locust bean gum, pectin, chitin, amylopectin, gelatin, hydroxymethylpropylcellulose, methylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, ethylcellulose, sodium carboxymethylcellulose, sodium carboxyethylcellulose, montmorillonite, polyacrylic acid and its methyl and ethyl esters, sodium carboxymethylstarch and sodium carboxyethylstarch. Pharmacologically suitable surfactants which may be mentioned are: sodium alkylsulfonates (RO—CO—CH
2
—SO
3
Na; R=C
6
-Cl
6
-alkyl radical), in particular sodium lauryl sulfoacetate; sodium laurylammonium sulfate, sodium lauryl sulfate, sodium dioctyl sulfosuccinate, s odium stearate, Aerosol® OT, glycerol monostearate, Span® 8.6HLB, Span® 4.7HLB, Arlacel® 20, 60, 80, 83, Tween® 20, 60, 80, Cremophor® O, Myrj® 45, 52, 59, poloxamer 188 (=Pluronic® F68), Cremophor® RH 40, 60, RH, EL, lecithin, lecithin S75-3 and S20-10. In the case of a tablet or coated tablet, the liquid and semisolid surfactants must before processing be processed with Aerosil® 200 to a solid and free-flowing composition.
The mixtures comprise the surfactants and fats in an amount such that, when the forms are introduced into aqueous media, there is formation of a poorly filterable liquid which forms a creamy emulsion on extraction with organic solvents. Suitable examples are mixtures which comprise the surfactants and fats in the ratio of from 95:1 to 1:95, preferably of (5 to 60):(40 to 90). A ratio of (20 to 60):(40 to 80) is particularly preferred.
The mixtures are incorporated into the administration forms in an amount such that their proportion relative to the amount of active ingredient in the administration form is from 1 to 300, preferably from 10 to 150 and, in particular, from 20 to 100%.
Addition of said mixtures to the administration forms impedes the isolation of the active ingredients out of the administration forms greatly and moreover considerably reduces the yield. The results on use of only the individual substances of the mixtures for this purpose are unserviceable.
The following examples show the possibilities for satisfactory use of the mixture.
REFERENCES:
patent: 3169092 (1965-02-01), Petraglia et al.
patent: 9428870 (1994-12-01), None
patent: 9608252 (1996-03-01), None
The Physicians' Desk Reference, 52 Edition (Medical Economics Company 1998).
Federman Evan J.
McQueeney P. E.
Page Thurman K.
Warner & Lambert Company
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