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Priority claimed from DE3843239Aexternal-prioritypatent/DE3843239C1/de
Pharmaceuticals Containing Other Organic And Inorganic Compounds
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Medicines That Contain Protein Lipid Enzymes And Other Medicines
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Acyclic And Carbocyclic Compounds In Medicinal Compositions
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Abstract
The invention refers to the procedure for the preparation of transdermal therapeutic system for the application of physostigmine to the skin consisting of the cover layer impermeable to the active ingredient, of the clinging and sticking reservoir layer and possibly removable protective layer. It is characterised by the fact that the active substance physostigmine together with the ingredients of the clinging and sticking reservoir layer, possibly in the solution is homogeneously mixed and applied to the cover layer that is impermeable to the active substance, possibly the solvent is removed and the sticking reservoir layer is covered with the protective layer, where the reservoir layer contains 10-90 % by weight of polymer material gathered from the groups consisting of bloccopolymers on the basis of styrol and 1,3 dienen, polyisobutylene, polymers on acrylate and/or methacrylate basis and esters of hydrated colophony, 0-30 % by weight of softeners on the basis of hydrocarbons and/or esters and 0.1-20 % by weight of physostigmine.
Claims (15)
POSTOPEK ZA IZDELAVO TRANSDERMALNEGA TERAPEVTSKEGA SISTEMA S FIZOSTIGMINOM KOT DEJAVNO SESTAVINO PATENTNI ZAHTEVKI 1 Postopek za izdelavo transdermalnega terapevtskega sistema za dajanje fizostigmina na kožo iz za dejavno snov nepropustnega pokrivnega sloja, oprijemno-lepljivega rezervoamega sloja in eventualno ponovno odstranljivega varovalnega sloja, označen s tem, da rezervoami sloj, izhajajoč iz raztopine v topilu z nizkim vreliščem ali zmesi topil, vsebuje sledeče dele v homogeni fini disperziji: - 10 - 90 masnih % polimernega materiala, izbranega iz skupin, obstoječih iz blokkopolimerov na bazi stirola in 1,3 dienena, poliizobutilena, polimerov na akrilatni in/ali metakrilatni bazi in estrov hidriranega kolofonija, - 0 - 30 masnih % mehčalcev na bazi ogljikovodikov in/ali estrov, in - 0,1 - 20 masnih % fizostigmina.PROCESS FOR THE MANUFACTURE OF A TRANSDERMAL THERAPEUTIC SYSTEM WITH PHYSOSTIGMIN AS AN ACTIVE INGREDIENT PATENT APPLICATIONS 1 the reservoir layer resulting from the solution in a low-boiling solvent or mixture of solvents contains the following parts in a homogeneous fine dispersion: - 10 - 90% by weight of the polymeric material selected from the group consisting of styrene-based block copolymers and 1,3 dienene, polyisobutylene, polymers based on acrylate and / or methacrylate and esters of hydrogenated rosin, - 0 - 30% by weight of hydrocarbon and / or ester softeners, and - 0,1 - 20% by weight of physostigmine.2 Postopek po zahtevku 1, označen s tem, da polimerni material vsebuje linearni stiren-izopren-stirol blokkopolimer.Process according to Claim 1, characterized in that the polymeric material contains a linear styrene-isoprene-styrene block copolymer.3 Postopek po zahtevku 1, označen s tem, da polimerni material vsebuje linearni stiren-butadien-stirol blokkopolimer.Process according to Claim 1, characterized in that the polymeric material contains a linear styrene-butadiene-styrene block copolymer.4 Postopek po zahtevku 1, označen s tem, da polimerni material vsebuje samo-omrežujoči akrilatkopolimer iz 2-etilheksilakrilata, vinilacetata, akrilne kisline in estra titankelata. -2-Process according to Claim 1, characterized in that the polymeric material comprises a self-crosslinking acrylate polymer of 2-ethylhexyl acrylate, vinyl acetate, acrylic acid and titanium ester. -2-5 Postopek po zahtevku 1, označen s tem, da polimerni material vsebuje ne-samo-omrežujoči akrilatkopolimer iz 2-etiIheksilakrilata, vinilacetata in akrilne kisline.Process according to Claim 1, characterized in that the polymeric material comprises a non-self-crosslinking acrylate copolymer of 2-ethylhexyl acrylate, vinyl acetate and acrylic acid.6 Postopek po zahtevku 1, označen s tem, da polimerni material vsebuje, kot polimer na bazi metakrilatov, kopolimer na bazi dimetilaminoetilmetakrilata in nevtralnega estra metakrilne kisline.Process according to Claim 1, characterized in that the polymeric material contains, as a methacrylate-based polymer, a copolymer based on dimethylaminoethyl methacrylate and a methacrylic acid neutral ester.7 Postopek po zahtevku 1, označen s tem, da polimerni material vsebuje, kot ester hidriranega kolofonija, njegov metilester.Process according to Claim 1, characterized in that the polymeric material contains, as the ester of hydrogenated rosin, its methyl ester.8 Postopek po zahtevku 1, označen s tem, da polimerni material vsebuje, kot ester hidriranega kolofonija, njegov glicerinester.Process according to Claim 1, characterized in that the polymeric material contains, as the ester of hydrogenated rosin, its glycerol ester.9 Postopek po zahtevku 1, označen s tem, da rezervoarni sloj vsebuje, kot mehčalec, dioktilcikloheksan.Process according to Claim 1, characterized in that the reservoir layer contains, as a plasticizer, dioctylcyclohexane.10 Postopek po zahtevku 1, označen s tem, da rezervoarni sloj vsebuje, kot mehčalec, di-n-butiladipat.Process according to Claim 1, characterized in that the reservoir layer contains, as a plasticizer, di-n-butyladipate.11 Postopek po zahtevku 1, označen s tem, da rezervoarni sloj vsebuje, kot mehčalec, trigliceride.Process according to Claim 1, characterized in that the reservoir layer contains, as a plasticizer, triglycerides.12 Postopek po zahtevku 1, označen s tem, da rezervoarni sloj vsebuje, kot mehčalec, izopropilmiristat.Process according to Claim 1, characterized in that the reservoir layer contains, as a plasticizer, isopropyl myristate.13 Postopek za izdelavo transdermalnega terapevtskega sistema po enem od zahtevkov 1 do 12, označen s tem, da so sestavine rezervoarnega sloja raztopljene v topilu z nizkim vreliščem, ki omogoča sušenje do maksimalne preostale vlage manj kot 0,4 masnih %.Process for manufacturing a transdermal therapeutic system according to one of Claims 1 to 12, characterized in that the components of the reservoir layer are dissolved in a low-boiling solvent which allows drying to a maximum residual moisture content of less than 0.4% by weight.14 Postopek za izdelavo transdermalnega terapevtskega sistema po zahtevku 13 -3- označen s tem, da se uporabi zmes topil iz butanona in n-heptana.Process for the preparation of a transdermal therapeutic system according to Claim 13 -3 - characterized in that a solvent mixture of butanone and n-heptane is used.15 Nosilec za uporabo pri transdermalnem dajanju fizostigmina, sestavljen iz za dejavno snov nepropustnega hrbtnega sloja, oprijemno-lepljivega sloja, zmožnega absorbirati dejavno snov, kakor tudi, eventualno, iz ponovno odstranljivega varovalnega sloja, označen s tem, da je rezervoami sloj oprijemno-lepljiv in da vsebuje 50 - 90 masnih % polimernega materiala kakor tudi 0-30 masnih % mehčalca.15 Carrier for use in transdermal administration of physostigmine, consisting of an active impermeable backing layer, an adhesive-adhesive layer capable of absorbing the active substance as well as, optionally, a removable protective layer, characterized in that the reservoir layer is an adhesive-adhesive layer. and that it contains 50-90% by weight of polymeric material as well as 0-30% by weight of plasticizer.
SI8912407A1988-12-221989-12-19Process for the preparation of transdermal therapeutic system having physostigmine as the active ingradient
SI8912407B
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