Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1993-05-17
1995-07-11
Griffin, Ronald W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514180, 514969, 514975, 514 29, 514152, 514159, 514420, 514785, A61K 4700, A61K 4726, A61K 4714
Patent
active
054321700
DESCRIPTION:
BRIEF SUMMARY
The invention relates to a process for the production of semisolid preparations containing micronized active ingredients, characterized in that a mixture of one or two nonionic surfactants with an HLB of 9 to 18 with 2.3 to 100 times the amount by weight of a fatty acid ester of general formula with 12 to 32 carbon atoms, or of a mixture of these fatty acid esters is heated until it melts, the melt with stirring is put into 10 to 200 times the amount by weight of a semisolid preparation, which is heated approximately to the same temperature, the mixture is allowed to cool with stirring and mixed with the micronized active ingredient or active ingredient mixture as well as optionally with scents.
The semisolid preparations produced according to the process of the invention make possible a better availability of the active ingredient or active ingredient mixture than the semisolid formulations containing micronized active ingredients produced in a conventional way. This has the result that the preparations according to the invention require significantly lower active ingredient concentrations to show the same effectiveness than the formulations produced in the conventional way.
The actual substance mixture promoting the availability (designated below as "substance mixture") is a mixture of one or two nonionic surfactants with an HLB of 9 to 18 and 2.3 to 100 times the amount by weight (especially 2.4 to 30 times the amount by weight) of a fatty acid ester of general formula an alkyl group or an alkenyl group with 12 to 32 carbon atoms or a mixture of these fatty acid esters.
Nonionic surfactants, which are suitable for the production of the "substance mixture," are described, for example, in Ullmanns Enzyklopadie der technischen Chemie [Ullmann's Encyclopedia of Industrial Chemistry], 4th Edition, Volume 22 (Verlag Chemie; DE-Weinheim et al., 1982, pp. 488-496) and 1983 in "International McCutcheon's Emulsifiers/Detergents/Functional Materials" (Glen Rock N.J. 07452; USA).
Suitable surfactants are in particular ethoxylates soluble in water and insoluble in paraffin oil and within them preferably ethoxylates, which are terminally blocked.
Such surfactants are, for example: Chemical Products])
If a mixture of 2 surfactants is used for the production of the "substance mixture," this mixture has to have an HLB of 9 to 18, but the individual components can have a lower or higher HLB. Suitable surfactant mixtures are, for example, those which in addition to the above-mentioned ethoxylates, also contain fatty acid esters of polyhydroxy compounds (such as glycerol, sorbitol, saccharose or pentaerythritol).
A fatty acid ester is, for example, the pentaerythritol monostearate.
Fatty acid esters of the already mentioned formula preferably those which have a total of 28 to 58 carbon atoms and especially those which have 32 to 48 carbon atoms.
Such fatty acid esters are, for example, the octadecanoic acid-octadecenyl ester, the hexadecanoic acid-eicosyl ester, the octadecanoic acid-octadecyl ester, the eicosenoic acid-docosenyl ester, the 13-docosenoic acid eicosyl ester, the 9-octadecenoic acid-tetracosyl ester, the 12-triacontenoic acid-dodecyl ester, the eicosanoic acid-docosyl ester, the octadecanoic acid-tetracosyl ester and the 10-octacosenoic acid-eicosyl ester.
For the production of the "substance mixture," the surfactant or a mixture of two surfactants is mixed with 2.3 to 100 times the amount by weight--preferably with 24 to 30 times the amount by weight--of the fatty acid ester or fatty acid ester mixture and the mixture is heated with stirring until it melts. The melting temperature depends, of course, on the selection of the components and their quantitative ratio and is normally at about 40.degree. C. to 70.degree. C.
The melt of the "substance mixture" is then introduced with stirring in 10 to 200 times the amount by weight--preferably 20 to 120 times the amount by weight--of a semisolid preparation, which was heated approximately to the same temperature (.+-.about 5.degree. C.) as the "substance mixture"
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Dargel Erwin
Leitner Erich
Stindl Wolfgang
Tack Johannes
Griffin Ronald W.
Schering Aktiengesellschaft
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