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Claims for Patent: 7,776,314

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Claims for Patent: 7,776,314

Title:Abuse-proofed dosage system
Abstract:The invention relates to a solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid.
Inventor(s): Bartholomaus; Johannes (Aachen, DE), Kugelmann; Heinrich (Aachen, DE)
Assignee: Grunenthal GmbH (Aachen, DE)
Application Number:11/007,887
Patent Claims: 1. A parenteral abuse-proofed solid dosage form for oral administration, comprising, in addition to one or more active ingredients with potential for abuse selected from the group consisting of opiates, opioids, tranquillizers, stimulants and narcotics, at least one viscosity-increasing agent in a quantity equal to or greater than 5 mg per dosage form and such that an aqueous extract obtained from the dosage form with 10 ml of water at 25.degree. C. forms a gel which can still pass through a needle having a diameter of 0.9 mm and remains visually distinguishable when introduced by a needle into a further quantity of an aqueous liquid.

2. A dosage form according to claim 1, wherein the active ingredient is an opiate, opioid, tranquillizer or a narcotic selected from the group consisting of N-{1-[2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl]-4-methoxymethyl-4-piperid- yl}propionanilide(alfentanil), 5,5-diallylbarbituric acid(allobarbital), allylprodine, alphaprodine, 8-chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]-benzodiazepine(- alprazolam), 2-diethylaminopropiophenone(amfepramone), (.+-.)-.alpha.-methylphenethylamine(amphetamine), 2-(.alpha.-methylphenet-hylamino)-2-phenylacetonitrile(amphetaminil), 5-ethyl-5-isopentylbarbituri- c acid(amobarbital), anileridine, apocodeine, 5,5-diethylbarbituric acid(barbital), benzylmorphine, bezitramide, 7-bromo-5-(2-pyridyl)-1H-1,4-benzodiazepine-2(3H)-one (bromazepam), 2-bromo-4-(2-chlorophenyl)-9-methyl-l-6H-thieno[3,2-f][1,2,4]triazolo[4,3- -a][1,4]diazepine(brotizolam), 17-cyclopropylmethyl-4,5a-epoxy-7a[(S)-1-hydroxy-1,2,2-trimethyl-propyl]- -6-methoxy-6,14-endo-ethanomorphinan-3-ol(buprenorphine), 5-butyl-5-ethylbarbituric acid(butobarbital), butorphanol, (7-chloro-1,3-dihydro-1-methyl-2-oxo-5-phenyl-2H-1,4-benzodiazepin-3-yl)d- imethylcarbamate(camazepam), (1S,2S)-2-amino-1-phenyl-1-propanol(cathine/D- -norpseudoephedrine), 7-chloro-N-methyl-5-phenyl-3H-1,4-benzodiazepin-2-yl-amine 4-oxide(chlordiazepoxide), 7-chloro-1-methyl-5-phenyl-1H-1,5-benzodi-azepine-2,4(3H,5H)-dione(clobaz- am), 5-(2-chlorophenyl)-7-nitro-1H-1,4-benz-odiazepin-2(3H)-one(clonazepam- ), clonitazene, 7-chloro-2,3-dihydro-2-oxo-5-phenyl-1H-1,4-benzodiazepine-3-carboxylic acid(clorazepate), 5-(2-chlorophenyl)-7-ethyl-1-methyl-1H-thieno[2,3-e][1,4]diazepin-2(3H)-o- ne(clotiazepam), 10-chloro-11b-(2-chlorophenyl)-2,3,7,11b-tetrahydrooxazol-o [3,2-d][1,4]benzodiazepin-6 (5H)-one(cloxazolam), (-)-methyl-[3.beta.-benzoyloxy-2.beta.(1.alpha.H,5.alpha.H)-tropane carboxylate](cocaine), 4,5.alpha.-epoxy-3-methoxy-17-methyl-7-morphinen-6.alpha.-ol(codeine), 5-(1-cyclohexenyl)-5-ethyl barbituric acid(cyclobarbital), cyclorphan, cyprenorphine, 7-chloro-5-(2-chloropheny-l)-1H-1,4-benzodiazepin-2(3H)-one(delorazepam), desomorphine, dextromoramide, (+)-(1-benzyl-3-dimethylamino-2-methyl-1-phenylpropyl)pro-pionate(dextrop- ropoxyphene), dezocine, diampromide, diamorphone, 7-chloro-1-methyl-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one (diazepam), 4,5.alpha.-epoxy-3-methoxy-17-methyl-6.alpha.-morphinanol(dihydrocodeine)- -, 4,5.alpha.-epoxy-17-methyl-3,6a-morphinandiol(dihydromorphine), dimenoxadol, dimephetamol, dimethylthiambutene, dioxaphetyl butyrate, dipipanone, (6aR,10aR)-6,6,9-trimethyl-3-pentyl-6a,7,8,10a-tetrahydro-6H-benzo[c]chro- men-1-ol(dronabinol), eptazocine, 8-chloro-6-phenyl-4H-[1,2,4]-triazolo[4,3-(a)][1,4]benzodiazepine(estazol- am), ethoheptazine, ethylmethylthiambutene, ethyl[7-chloro-5-(2-fluorophenyl)-2,3-dihydro-2-oxo-1H-1,4-benzodiazepine- -3-carboxylate](ethyl loflazepate), 4,5.alpha.-epoxy-3-ethoxy-17-methyl-7-morphinen-6.alpha.-ol(ethylmorphine- -), etonitazene, 4,5.alpha.-epoxy-7.alpha.-(1-hydroxy-1-methylbutyl)-6-meth-oxy-17-methyl-- 6,14-endo-etheno-morphinan-3-ol(etorphine), N-ethyl-3-phenyl-8,9,10-trinorbornan-2-ylamine (fencamfamine), 7-[2-(.alpha.-methylphenethylamino)ethyl]-theophylline)(fenethylline), 3-(.alpha.-methylphenethylamino)propionitrile(fenproporex), N-(1-phenethyl-4-piperidyl)propionanilide(fentanyl), 7-chloro-5-(2-fluorophenyl)-1-methyl-1H-1,4-benzodiazepin-2(3H)-one (fludiazepam), 5-(2-fluorophenyl)-1-methyl-7-nitro-1H-1,4-benzodiazepin-2(3H)-one(flunit- razepam), 7-chloro-1-(2-diethylaminoethyl)-5-(2-fluoropheny-l)-1H-1,4-benz- odiazepin-2(3H)-one(flurazepam), 7-chloro-5-phenyl-1-(2,2,2-trifluoroethyl)-1H-1,4-benzodiazepin-2(3H)-one- (halazepam), 10-bromo-11b-(2-fluorophenyl)-2,3,7,11b-tetrahydro[1,3]oxazolyl[3,2-d][1,- -4]benzodiazepin-6(5H)-one (haloxazolam), heroin, 4,5.alpha.-epoxy-3-methox-y-17-methyl-6-morphinanone(hydrocodone), 4,5.alpha.-epoxy-3-hydroxy-17-methyl-6-morphinanone(hydromorphone), hydroxypethidine, isomethadone, hydroxymethylmorphinan, 11-chloro-8,12b-dihydro-2,8-dimethyl-12b-phenyl-4H-[1,3]oxazino[3,2-d][1,- 4]benzodiazepine-4,7(6H)-dione(ketazolam), 1-[4-(3-hydroxyphenyl)-1-methyl-4-piperidyl]-1-propanone(ketobemidone), (3S,6S)-6-dimethylamino-4,4-diphenylheptan-3-yl acetate (levacetylmethadol(LAAM)), (-)-6-dimethylamino-4,4-diphenol-3-heptanone(l-evomethadone), (-)-17-methyl-3-morphinanol (levorphanol), levophenacylmorphane, lofentanil, 6-(2-chlorophenyl)-2-(4-methyl-1-pipera-zinylmethylene)-8-nitro-2H-imidaz- o[1,2-a][1,4]-benzodiazepin-1(4H)-one(lop-razolam), 7-chloro-5-(2-chlorophenyl)-3-hydroxy-1H-1,4-benzodiazepin-2(3H)- -one(lorazepam), 7-chloro-5-(2-chlorophenyl)-3-hydroxy-1-methyl-1H-1,4-ben-zodiazepin-2(3H- )-one(lormetazepam), 5-(4-chlorophenyl)-2,5-dihydro-3H-imid-azo[2,1-a]isoindol-5-ol (mazindol), 7-chloro-2,3-dihydro-1-methyl-5-phenyl- -1H-1,4-benzodiazepine(medazepam), N-(3-chloropropyl)-.alpha.-methylphenet-hylamine(mefenorex), meperidine, 2-methyl-2-propyltrimethylene dicarbamate(meprobamate), meptazinol, metazocine, methylmorphine, N,.alpha.-dimethylphenethylamine(metamphetamine), (.+-.)-6-dimethylamino-4,4-diphenol-3-heptanone(methadone), 2-methyl-3-o-tolyl-4(3H)-quinazolinon-e(methaqualone), methyl [2-phenyl-2-(2-piperidyl)acetate](methylphenidate)-, 5-ethyl-1-methyl-5-phenylbarbituric acid(methylphenobarbital), 3,3-diethyl-5-methyl-2,4-piperidinedione(methyprylon), metopon, 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine- -(midazolam), 2-(benzhydrylsulfinyl)acetamide(modafinil), 4,5.alpha.-epoxy-17-methyl-7-morphinen-3,6.alpha.-diol(morphine), myrophine, (.+-.)-trans-3-(1,1-dimethylheptyl)-7,8,10,10.alpha.-tetrahydr-o-1-hydrox- y-6,6-dimethyl-6H-dibenzo-[b,d]pyran-9(6.alpha.H)-one(nabilone), nalbuphene, nalorphine, narceine, nicomorphine, 1-methyl-7-nitro-5-phenyl- -1H-1,4-benzodiazepin-2(3H)-one(nimetazepam), 7-nitro-5-phenyl-1H-1,4-benz-odiazepin-2(3H)-one(nitrazepam), 7-chloro-5-phenyl-1H-1,4-benzodiazepin-2(-3H)-one(nordazepam), norlevorphanol, 6-dimethylamino-4,4-diphenyl-3-hexano ne(normethadone), normorphine, norpipanone, the exudation from plants belonging to the species Papaver somniferum (opium), 7-chloro-3-hydroxy-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one(oxazepam), (cis-trans)-10-chloro-2,3,7,11b-tetrahydro-2-methyl-11b-phenyloxazolo[3,2- - -d][1,4]benzodiazepin-6-(5H)-one(oxazolam), 4,5.alpha.-epoxy-14-hydroxy-3--methoxy-17-methyl-6-morphinanone(oxycodone- ), oxymorphone, plants and parts of plants belonging to the species Papaver somniferum (including the subspecies setigerum) (Papaver somniferum), papaveretum, 2-imino-5-phenyl-4-oxazolidinone(pernoline), 1,2,3,4,5,6-hexahydro-6,11-d- imethyl-3-(3-methyl-2-butenyl)-2,6-methano-3-benzazocin-8-ol(pentazocine)- , 5-ethyl-5-(1-methylbutyl)-barbituric acid(pentobarbital), ethyl-(1-methyl-4-phenyl-4-piperidinecarboxylate)(pethidine), phenadoxone, phenomorphane, phenazocine, phenoperidine, piminodine, pholcodeine, 3-methyl-2-phenylmorpholine(phenmetrazine), 5-ethyl-5-phenylbarbituric acid(phenobarbital), .alpha., .alpha.-dimethylphenethylamine(phentermine), 7-chloro-5-phenyl-1-(2-propynyl)-1H-1,4-benzodiazepin-2(3H)-one(pinazepam- ), .alpha.-(2-piperidyl)benzhydryl alcohol(pipradrol), 1'-(3-cyano-3,3-diphenylpropyl)[1,4'-bipiperidine]-4'- -carboxamide(piritramide), 7-chloro-1-(cyclopropylmethyl)-5-phenyl-1H-1,4--benzodiazepin-2(3H)-one(p- razepam), profadol, proheptazine, promedol, properidine, propoxyphene, N-(1-methyl -2-piperidinoethyl)-N-(2-pyridyl)p- ropionamide, methyl {3-[4-methoxycarbonyl-4-(N-phenylpropanamido)piperidin-o]propanoate}(remi- fentanil), 5-sec-butyl-5-ethylbarbituric acid (secbutabarbital), 5-allyl-5-(1-methylbutyl)-barbituric acid(secobarbital), N-{4-methoxymethyl-1-[2-(2-thienyl)ethyl]-4-piperidyl}propionanilide (sufentanil), 7-chloro-2-hydroxy-methyl-5-phenyl-1H-1,4-be-nzodiazepin-2(3H)-one(temaze- pam), 7-chloro-5-(1-cyclohexenyl)-1-methyl-1H--1,4-benzodiazepin-2(3H)-one- (tetrazepam), ethyl (2-dimethylamino-1-phenyl-3- -cyclohexene-1-carboxylate)(tilidine (cis and trans)), tramadol, 8-chloro-6-(2-chlorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzod- - iazepine(triazolam), 5-(1-methylbutyl)-5-vinylbarbituric acid(vinylbital), (1R*,2R*)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol, (1R,2R,4S)-2-(dimethylamino)methyl-4-(p-fluorobenzyloxy)-1-(m-methoxyphen- yl)cyclohexanol and corresponding stereoisomeric compounds in each case and the corresponding derivatives thereof in each case, in particular esters or ethers, and the physiologically acceptable compounds thereof in each case, in particular salts and solvates.

3. A dosage form according to claim 1, comprising a stimulant selected from the group consisting of amphetamine, norpseudoephedrine, methylphenidate and in each case optionally the corresponding physiological compounds thereof, in particular the bases, salts and solvates thereof.

4. A dosage form according to claim 1, comprising one or more viscosity-increasing agents selected from the group consisting of microcrystalline cellulose with 11 wt. % carboxymethylcellulose sodium (Avicel.RTM. RC 591), carboxymethylcellulose sodium (Blanose.RTM., CMC--Na C300P.RTM., Frimulsion BLC-5.RTM., Tylose C300 P.RTM.), polyacrylic acid (Carbopol.RTM. 980 NF, Carbopol.RTM. 981), locust bean flour (Cesagum.RTM. LA-200, Cesagum.RTM. LID/150, Cesagum.RTM. LN-1), citrus pectin (Cesapectin.RTM. HM Medium Rapid Set), waxy maize starch (C*Gel 04201.RTM.), sodium alginate (Frimulsion ALG (E401).RTM.), guar flour (Frimulsion BM.RTM., Polygum 26/1-75.RTM.), iota-carrageenan (Frimulsion D021.RTM.), karaya gum, gellan gum (Kelcogel F.RTM., Kelcogel LT100.RTM.), galactomannan (Meyprogat 150.RTM.), tara stone flour (Polygum 43/1.RTM.), propylene glycol alginate (Protanal-Ester SDLB.RTM.), apple pectin, lemon peel pectin, sodium hyaluronate, tragacanth, tara gum (Vidogum SP 200.RTM.), fermented polysaccharide welan gum (K1A96) and xanthan gum (Xantural 180.RTM.).

5. A dosage form according to claim 1, in particulate form.

6. A dosage form according to claim 1, comprising at least one active ingredient at least partially in controlled release form.

7. A dosage form according to claim 1, comprising a coating resistant to gastric juices.

8. The dosage form of claim 1, wherein said tranquilizer is benzodiazepine.

9. A dosage form according to claim 1, comprising the at least one viscosity-increasing agent in a quantity of .gtoreq.5 mg per administration unit.

10. A dosage form according to claim 1 in multiparticulate form.

11. A dosage form according to claim 10, wherein said multiparticulate form is in the form of microtablets, microcapsules, micropellets, granules, spheroids, beads or pellets.

12. A dosage form according to claim 11 packaged in capsules or press-moulded into tablets.
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