CA2513064A1 - Nanoparticulate topiramate formulations - Google Patents
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- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
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- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- A—HUMAN NECESSITIES
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Abstract
The present invention is directed to nanoparticulate compositions comprising topiramate. The topiramate particles of the composition have an effective average particle size of less than about 2 microns.
Claims (46)
1. A nanoparticulate topiramate composition comprising:
(a) particles of topiramate or a salt thereof; and (b) at least one surface stabilizer, wherein the topiramate particles have an effective average particle size of less than about 2 microns.
(a) particles of topiramate or a salt thereof; and (b) at least one surface stabilizer, wherein the topiramate particles have an effective average particle size of less than about 2 microns.
2. The composition of claim 1, wherein the effective average particle size of the nanoparticulate topiramate particles is selected from the group consisting of less than about 1900 nm, less than less than about 1800 nm, less than about 1700 nm, less than about 1600 nm, less than about 1500 nm, less than about 1400 nm, less than about 1300 nm, less than about 1200 nm, less than about 1100 nm, less than about 1000 nm, less than about 900 nm, less than about 800 nm, less than about 700 nm, less than about 600 nm, less than about 500 nm, less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 200 nm, less than about 150 nm, less than about 140 nm, less than about 130 nm, less than about 120 nm, less than about 110 nm, less than about 100 nm, less than about 90 nm, less than about 80 nm, less than about 70 nm, less than about 60 nm, and less than about 50 nm.
3. The composition of claim 1 or claim 2, wherein at least about 70%, at least about 90%, at least about 95%, or at least about 99% of the topiramate particles have a particle size less than the effective average particle size.
4. The composition of any one of claims 1-3, wherein the topiramate is selected from the group consisting of a crystalline phase, an amorphous phase, a semi-crystalline phase, a semi-amorphous phase, and mixtures thereof.
5. The composition of any one of claims 1-4, wherein the composition is formulated for administration selected from the group consisting of oral, pulmonary, rectal, opthalmic, colonic, parenteral, intracisternal, intravaginal, intraperitoneal, local, buccal, nasal, and topical administration.
6. The composition of any one of claims 1-5, wherein the composition further comprises one or more pharmaceutically acceptable excipients, carriers, or a combination thereof.
7. The composition of any one of claim, 1-6, wherein the topiramate is present in an amount selected from the group consisting of from about 99.5% to about 0.001%, from about 95% to about 0.1%, and from about 90% to about 0.5%, by weight, based on the total combined dry weight of the topiramate and at least one surface stabilizer, not including other excipients.
8. The composition of any one of claims 1-7, wherein the at least one surface stabilizer is present in an amount selected from the group consisting of from about 0.5%
to about 99.999%, from about 5.0% to about 99.9%, and from about 10% to about 99.5%, by weight, based on the total combined dry weight of the topiramate and at least one surface stabilizer, not including other excipients.
to about 99.999%, from about 5.0% to about 99.9%, and from about 10% to about 99.5%, by weight, based on the total combined dry weight of the topiramate and at least one surface stabilizer, not including other excipients.
9. The composition of any one of claims 1-8, comprising at least two surface stabilizers.
10. The composition of any one of claims 1-9, wherein the surface stabilizer is selected from the group consisting of an anionic surface stabilizer, a cationic surface stabilizer, a zwitterionic surface stabilizer, and an ionic surface stabilizer.
11. The composition of any one of claims 1-10, wherein the at least one surface stabilizer is selected from the group consisting of cetyl pyridinium chloride, gelatin, casein, phosphatides, dextran, glycerol, gum acacia, cholesterol, tragacanth, stearic acid, benzalkonium chloride, calcium stearate, glycerol monostearate, cetostearyl alcohol, cetomacrogol emulsifying wax, sorbitan esters, polyoxyethylene alkyl ethers, polyoxyethylene castor oil derivatives, polyoxyethylene sorbitan fatty acid esters, polyethylene glycols, dodecyl trimethyl ammonium bromide, polyoxyethylene stearates, colloidal silicon dioxide, phosphates, sodium dodecylsulfate, carboxymethylcellulose calcium, hydroxypropyl celluloses, hydroxypropyl methylcellulose, carboxymethylcellulose sodium, methylcellulose, hydroxyethylcellulose, hydroxypropylmethyl-cellulose phthalate, noncrystalline cellulose, magnesium aluminum silicate, triethanolamine, polyvinyl alcohol, polyvinylpyrrolidone, 4-(1,1,3,3-tetramethylbutyl)-phenol polymer with ethylene oxide and formaldehyde, poloxamers;
poloxamines, a charged phospholipid, dioctylsulfosuccinate, dialkylesters of sodium sulfosuccinic acid, sodium lauryl sulfate, alkyl aryl polyether sulfonates, mixtures of sucrose stearate and sucrose distearate, p-isononylphenoxypoly-(glycidol), decanoyl-N-methylglucamide; n-decyl .beta.-D-glucopyranoside; n-decyl .beta.-D-maltopyranoside; n-dodecyl .beta.-D-glucopyranoside; n-dodecyl .beta.-D-maltoside; heptanoyl-N-methylglucamide; n-heptyl-.beta.-D-glucopyranoside; n-heptyl .beta.-D-thioglucoside; n-hexyl .beta.-D-glucopyranoside;
nonanoyl-N-methylglucamide; n-noyl .beta.-D-glucopyranoside; octanoyl-N-methylglucamide; n-octyl-.beta.-D-glucopyranoside; octyl .beta.-D-thioglucopyranoside;
lysozyme, PEG-derivatized phospholipid, PEG-derivatized cholesterol, PEG-derivatized cholesterol derivative, PEG-derivatized vitamin A, PEG-derivatized vitamin E, and random copolymers of vinyl acetate and vinyl pyrrolidone.
poloxamines, a charged phospholipid, dioctylsulfosuccinate, dialkylesters of sodium sulfosuccinic acid, sodium lauryl sulfate, alkyl aryl polyether sulfonates, mixtures of sucrose stearate and sucrose distearate, p-isononylphenoxypoly-(glycidol), decanoyl-N-methylglucamide; n-decyl .beta.-D-glucopyranoside; n-decyl .beta.-D-maltopyranoside; n-dodecyl .beta.-D-glucopyranoside; n-dodecyl .beta.-D-maltoside; heptanoyl-N-methylglucamide; n-heptyl-.beta.-D-glucopyranoside; n-heptyl .beta.-D-thioglucoside; n-hexyl .beta.-D-glucopyranoside;
nonanoyl-N-methylglucamide; n-noyl .beta.-D-glucopyranoside; octanoyl-N-methylglucamide; n-octyl-.beta.-D-glucopyranoside; octyl .beta.-D-thioglucopyranoside;
lysozyme, PEG-derivatized phospholipid, PEG-derivatized cholesterol, PEG-derivatized cholesterol derivative, PEG-derivatized vitamin A, PEG-derivatized vitamin E, and random copolymers of vinyl acetate and vinyl pyrrolidone.
12. The composition of any one of claims 1-10, wherein the at least one cationic surface stabilizer is selected from the group consisting of a polymer, a biopolymer, a polysaccharide, a cellulosic, an alginate, a nonpolymeric compound, a phospholipid, zwitterionic stabilizers, poly-n-methylpyridinium, anthryul pyridinium chloride, chitosan, polylysine, polyvinylimidazole, polybrene, polymethylmethacrylate trimethylammoniumbromide bromide (PMMTMABr), hexyldesyltrimethylammonium bromide (HDMAB), polyvinylpyrrolidone-2-dimethylaminoethyl methacrylate dimethyl sulfate, 1,2 Dipalmitoyl-sn-Glycero-3-Phosphoethanolamine-N-[Amino(Polyethylene Glycol)2000] (sodium salt), Poly(2-methacryloxyethyl trimethylammonium bromide), poloxamines, lysozyme, alginic acid, carrageenan, POLYOX, cationic lipids, sulfonium, phosphonium, quarternary ammonium compounds, stearyltrimethylammonium chloride, benzyl-di(2-chloroethyl)ethylammonium bromide, coconut trimethyl ammonium chloride, coconut trimethyl ammonium bromide, coconut methyl dihydroxyethyl ammonium chloride, coconut methyl dihydroxyethyl ammonium bromide decyl triethyl ammonium chloride, decyl dimethyl hydroxyethyl ammonium chloride, decyl dimethyl hydroxyethyl ammonium bromide, C12-15dimethyl hydroxyethyl ammonium chloride, C12-15dimethyl hydroxyethyl ammonium bromide, coconut dimethyl hydroxyethyl ammonium chloride, coconut dimethyl hydroxyethyl ammonium bromide, myristyl trimethyl ammonium methyl sulphate, lauryl dimethyl benzyl ammonium chloride, lauryl dimethyl benzyl ammonium bromide, lauryl dimethyl (ethenoxy)4 ammonium chloride, lauryl dimethyl (ethenoxy)4 ammonium bromide, N-alkyl (C12-18)dimethylbenzyl ammonium chloride, N-alkyl (C14-18)dimethyl-benzyl ammonium chloride, N-tetradecylidmethylbenzyl ammonium chloride monohydrate, dimethyl didecyl ammonium chloride, N-alkyl and (C12-14) dimethyl 1-napthylmethyl ammonium chloride, trimethylammonium halide, alkyl-trimethylammonium salts, dialkyl-dimethylammonium salts, lauryl trimethyl ammonium chloride, ethoxylated alkyamidoalkyldialkylammonium salt, an ethoxylated trialkyl ammonium salt, dialkylbenzene dialkylammonium chloride, N-didecyldimethyl ammonium chloride, N-tetradecyldimethylbenzyl ammonium, chloride monohydrate, N-alkyl(C12-14) dimethyl 1-naphthylmethyl ammonium chloride, dodecyldimethylbenzyl ammonium chloride, dialkyl benzenealkyl ammonium chloride, lauryl trimethyl ammonium chloride, alkylbenzyl methyl ammonium chloride, alkyl benzyl dimethyl ammonium bromide, C12, C15, C17 trimethyl ammonium bromides, dodecylbenzyl triethyl ammonium chloride, poly-diallyldimethylammonium chloride (DADMAC), dimethyl ammonium chlorides, alkyldimethylammonium halogenides, tricetyl methyl ammonium chloride, decyltrimethylammonium bromide, dodecyltriethylammonium bromide, tetradecyltrimethylammonium bromide, methyl trioctylammonium chloride, POLYQUAT
10.TM., tetrabutylammonium bromide, benzyl trimethylammonium bromide, choline esters, benzalkonium chloride, stearalkonium chloride compounds, cetyl pyridinium bromide, cetyl pyrridinium chloride, halide salts of quaternized polyoxyethylalkylamines, MIRAPOL.TM., ALKAQUAT.TM., alkyl pyridinium salts, amines, protonated quaternary acrylamides, methylated quaternary polymers, and cationic guar.
10.TM., tetrabutylammonium bromide, benzyl trimethylammonium bromide, choline esters, benzalkonium chloride, stearalkonium chloride compounds, cetyl pyridinium bromide, cetyl pyrridinium chloride, halide salts of quaternized polyoxyethylalkylamines, MIRAPOL.TM., ALKAQUAT.TM., alkyl pyridinium salts, amines, protonated quaternary acrylamides, methylated quaternary polymers, and cationic guar.
13. The composition of claim 12, wherein the amine is selected from the group consisting of alkylamines, dialkylamines, alkanolamines, polyethylenepolyamines, N,N-dialkylaminoalkyl acrylates, vinyl pyridine, amine salts, lauryl amine acetate, stearyl amine acetate, alkylpyridinium salt, alkylimidazolium salt, amine oxides, and, imide azolinium salts.
14. The composition of any one of claims 1-10, wherein the cationic surface stabilizer is a nonpolymeric compound selected from the group consisting of benzalkonium chloride, a carbonium compound, a phosphonium compound, an oxonium compound, a halonium compound, a cationic organometallic compound, a quarternary phosphorous compound, a pyridinium compound, an anilinium compound, an ammonium compound, a hydroxylammonium compound, a primary ammonium compound, a secondary ammonium compound, a tertiary ammonium compound, behenalkonium chloride, benzethonium chloride, cetylpyridinium chloride, behentrimonium chloride, lauralkonium chloride, cetalkonium chloride, cetrimonium bromide, cetrimonium chloride, cethylamine hydrofluoride, chlorallylmethenamine chloride (Quaternium-15), distearyldimonium chloride (Quaternium-5), dodecyl dimethyl ethylbenzyl ammonium chloride(Quaternium-14), Quaternium-22, Quaternium-26, Quaternium-18 hectorite, dimethylaminoethylchloride hydrochloride, cysteine hydrochloride, diethanolammonium POE (10) oletyl ether phosphate, diethanolammonium POE (3)oleyl ether phosphate, tallow alkonium chloride, dimethyl dioctadecylammoniumbentonite, stearalkonium chloride, domiphen bromide, denatonium benzoate, myristalkonium chloride, laurtrimonium chloride, ethylenediamine dihydrochloride, guanidine hydrochloride, pyridoxine HCl, iofetamine hydrochloride, meglumine hydrochloride, methylbenzethonium chloride, myrtrimonium bromide, oleyltrimonium chloride, polyquaternium-1, procainehydrochloride, cocobetaine, stearalkonium bentonite, stearalkoniumhectonite, stearyl trihydroxyethyl propylenediamine dihydrofluoride, tallowtrimonium chloride, and hexadecyltrimethyl ammonium bromide.
15. The composition according to any one of claims 1-10, 12, 13, or 14, wherein the composition is bioadhesive.
16. The composition of any one of claims 1-10, comprising hypromellose, docusate sodium, or a combination thereof as surface stabilizers.
17. The composition of any one of claims 1-16, further comprising a topiramate composition having an effective average particle size of greater than about 2 microns.
18. The composition of any one of claims 1-17, further comprising at least one additional nanoparticulate topiramate composition having an effective average particle size of less than about 2 microns, wherein said additional nanoparticulate topiramate composition has an effective average particle size which is different than the effective average particle size of the nanoparticulate topiramate composition of claim 1.
19. The composition of any one of claims 1-18, additionally comprising at least one non-topiramate active agent.
20. The composition of claim 19, wherein said active agent is selected from the group consisting of amino acids, proteins, peptides, nucleotides, anti-obesity drugs, nutraceuticals, dietary supplements, central nervous symptom stimulants, carotenoids, corticosteroids, elastase inhibitors, anti-fungals, alkylxanthine, oncology therapies, anti-emetics, analgesics, opioids, antipyretics, cardiovascular agents, anti-inflammatory agents, anthelmintics, anti-arrhythmic agents, antibiotics, anticoagulants, antidepressants, antidiabetic agents, antiepileptics, antihistamines, antihypertensive agents, antimuscarinic agents, antimycobacterial agents, antineoplastic agents, immunosuppressants, antithyroid agents, antiviral agents, anxiolytics, sedatives, astringents, alpha-adrenergic receptor blocking agents, beta-adrenoceptor blocking agents, blood products, blood substitutes, cardiac inotropic agents, contrast media, corticosteroids, cough suppressants, diagnostic agents, diagnostic imaging agents, diuretics, dopaminergics, haemostatics, immunological agents, lipid regulating agents, muscle relaxants, parasympathomimetics, parathyroid calcitonin and biphosphonates, prostaglandins, radio- pharmaceuticals, sex hormones, anti-allergic agents, stimulants, anoretics, sympathomimetics, thyroid agents, vasodilators, vasomodulator, xanthines, Mu receptor antagonists, Kappa receptor antagonists, non-narcotic analgesics, monoamine uptake inhibitors, adenosine regulating agents, cannabinoid derivatives, Substance P antagonists, neurokinin-1 receptor antagonists, and sodium channel blockers.
21. The composition of claim 20, wherein said nutraceutical is selected from the group consisting of lutein, folic acid, fatty acids, fruit extracts, vegetable extracts, vitamin supplements, mineral supplements, phosphatidylserine, lipoic acid, melatonin, glucosamine/chondroitin, Aloe Vera, Guggul, glutamine, amino acids, green tea, lycopene, whole foods, food additives, herbs, phytonutrients, antioxidants, flavonoid constituents of fruits, evening primrose oil, flax seeds, fish oils, marine animal oils, and probiotics.
22. The composition of any one of claims 19, 20, or 21, wherein at least one non-topiramate active agent has an effective average particle size of less than about 2 microns.
23. The composition of any one of claims 19, 20, or 21, wherein at least one non-topiramate active agent has an effective average particle size of greater than about 2 microns.
24. The composition of any one of claims 1-23 formulated into a liquid dosage form, wherein the dosage form has a viscosity of less than about 2000 mPa.cndot.s at a shear rate of 0.1 (1/s).
25. The composition of claim 24 having a viscosity at a shear rate of 0.1 (1/s) selected from the group consisting of from about 2000 mPa.cndot.s to about 1 mPa.cndot.s, from about 1900 mPa.cndot.s to about 1 mPa.cndot.s, from about 1800 mPa.cndot.s to about 1 mPa.cndot.s, from about 1700 mPa.cndot.s to about 1 mPa.cndot.s, from about 1600 mPa.cndot.s to about 1 mPa.cndot.s, from about 1500 mPa.cndot.s to about 1 mPa.cndot.s, from about 1400 mPa.cndot.s to about 1 mPa.cndot.s, from about 1300 mPa.cndot.s to about 1 mPa.cndot.s, from about 1200 mPa.cndot.s to about 1 mPa.cndot.s, from about 1100 mPa.cndot.s to about 1 mPa.cndot.s, from about 1000 mPa.cndot.s to about 1 mPa.cndot.s, from about 900 mPa.cndot.s to about 1 mPa.cndot.s, from about 800 mPa.cndot.s to about 1 mPa.cndot.s, from about 700 mPa.cndot.s to about 1 mPa.cndot.s, from about 600 mPa.cndot.s to about 1 mPa.cndot.s, from about 500 mPa.cndot.s to about 1 mPa.cndot.s, from about 400 mPa.cndot.s to about 1 mPa.cndot.s, from about 300 mPa.cndot.s to about 1 mPa.cndot.s, from about 200 mPa.cndot.s to about 1 mPa.cndot.s, from about 175 mPa.cndot.s to about 1 mPa.cndot.s, from about 150 mPa.cndot.s to about 1 mPa.cndot.s, from about 125 mPa.cndot.s to about 1 mPa.cndot.s, from about 100 mPa.cndot.s to about 1 mPa.cndot.s, from about 75 mPa.cndot.s to about 1 mPa.cndot.s, from about 50 mPa.cndot.s to about 1 mPa.cndot.s, from about 25 mPa.cndot.s to about 1 mPa.cndot.s, from about 15 mPa.cndot.s to about 1 mPa.cndot.s, from about 10 mPa.cndot.s to about 1 mPa.cndot.s, and from about 5 mPa.cndot.s to about 1 mPa.cndot.s.
26. The composition of any one of claims 1-25 formulated into a liquid dosage form, wherein the viscosity of the dosage form is selected from the group consisting of less than about 1/200, less than about 1/100, less than about 1/50, less than about 1/25, and less than about 1/10 of the viscosity of a liquid dosage form of a conventional non-nanoparticulate topiramate composition, at about the same concentration per ml of topiramate.
27. The composition of any one of claims 1-26 formulated into a liquid dosage form, wherein the viscosity of the dosage form is selected from the group consisting of less than about 5%, less than about 10%, less than about 15%, less than about 20%, less than about 25%, less than about 30%, less than about 35%, less than about 40%, less than about 45%, less than about 50%, less than about 55%, less than about 60%, less than about 65%, less than about 70%, less than about 75%, less than about 80%, less than about 85%, and less than about 90% of the viscosity of a liquid dosage form of a conventional non-nanoparticulate topiramate composition at about the same concentration per ml of topiramate.
28. The composition of any one of claims 1-27, formulated into a liquid dosage form, wherein the amount of topiramate per ml is equal to or greater than the amount of topiramate per ml of a liquid dosage form of a conventional non-nanoparticulate topiramate composition.
29. The composition of any one of claims 1-23 formulated into a solid dosage form, wherein upon administration the dosage form redisperses such that the topiramate particles have an effective average particle size selected from the group consisting of less than about 2 microns, less than about 1900 nm, less than about 1800 nm, less than about 1700 nm, less than about 1600 nm, less than about 1500 nm, less than about 1400 nm, less than about 1300 nm, less than about 1200 nm, less than about 1100 nm, less than about 1000 nm, less than about 900 nm, less than about 800 nm, less than about 700 nm, less than about 600 nm, less than about 500 nm, less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 200 nm, less than about 150 nm, less than about 100 nm, less than about 75 nm, and less than about 50 nm.
30. The composition of any one of claims 1-23 formulated into a solid dosage form, wherein the dosage form redisperses in a biorelevant media such that the topiramate particles have an effective average particle size selected from the group consisting of less than about 2 microns, less than about 1900 nm, less than about 1800 nm, less than about 1700 nm, less than about 1600 nm, less than about 1500 nm, less than about 1400 nm, less than about 1300 nm, less than about 1200 nm, less than about 1100 nm, less than about 1000 nm, less than about 900 nm, less than about 300 nm, less than about 700 nm, less than about 600 nm, less than about 500 nm, less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 200 nm, less than about 150 nm, less than about 100 nm, less than about 75 nm, and less than about 50 nm.
31. The composition of any one of claims 1-30, wherein the composition does not produce significantly different absorption levels when administered under fed as compared to fasted conditions.
32. The composition of any one of claims 1-31, wherein upon administration the T max is less than that of a conventional non-nanoparticulate topiramate composition, administered at the same dosage.
33. The composition of any one of claims 1-32, wherein in comparative pharmacokinetic testing with a conventional non-nanoparticulate topiramate composition, administered at the same dosage, the nanoparticulate composition exhibits a T
max selected from the group consisting of less than about 100%, less than about 90%, less than about 80%, less than about 70%, less than about 60%, less than about 50%, less than about 40%, less than about 30%, less than about 25%, less than about 20%, less than about 15%, and less than about 10% of the T max exhibited by the non-nanoparticulate topiramate composition.
max selected from the group consisting of less than about 100%, less than about 90%, less than about 80%, less than about 70%, less than about 60%, less than about 50%, less than about 40%, less than about 30%, less than about 25%, less than about 20%, less than about 15%, and less than about 10% of the T max exhibited by the non-nanoparticulate topiramate composition.
34. The composition of any one of claims 1-33, wherein following administration the composition has a T max selected from the group consisting of less than about 2 hours, less than about 110 min., less than about 100 min., less than about 90 min., less than about 80 min. less than about 70 min., less than about 60 min., less than about 50 min., less than about 40 min., less than about 30 min., less than about 25 min., less than about 20 min., less than about 15 min., less than about 10 min., less than about 5 min., and less than about 3 min.
35. The composition of any one of claims 1-34, wherein upon administration the C max of the composition is greater than the C max of a conventional non-nanoparticulate topiramate composition, administered at the same dosage.
36. The composition of any one of claims 1-35, wherein in comparative pharmacokinetic testing with a conventional non-nanoparticulate topiramate composition, administered at the same dosage, the nanoparticulate composition exhibits a C
max selected from the group consisting of greater than about 5%, greater than about 10%, greater than about 15%, greater than about 20%, greater than about 30%, greater than about 40%, greater than about 50%, Beater than about 60%, greater than about 70%, greater than about 80%, greater than about 90%; greater than about 100%, greater than about 110%, greater than about 120%, greater than about 130%, greater than about 140%, and greater than about 150% than the C max exhibited by the non-nanoparticulate topiramate composition.
max selected from the group consisting of greater than about 5%, greater than about 10%, greater than about 15%, greater than about 20%, greater than about 30%, greater than about 40%, greater than about 50%, Beater than about 60%, greater than about 70%, greater than about 80%, greater than about 90%; greater than about 100%, greater than about 110%, greater than about 120%, greater than about 130%, greater than about 140%, and greater than about 150% than the C max exhibited by the non-nanoparticulate topiramate composition.
37. The composition of any one of claims 1-36, wherein the therapeutically effective amount of topiramate is selected from the group consisting of 1/6, 1/5, 1/4, 1/3rd, and 1/2 of the therapeutically effective amount of a conventional non-nanoparticulate topiramate composition.
38. The nanoparticulate topiramate composition of any one of claims 1-37 formulated into a dosage form for oral administration, wherein the relative bioavailability of the nanoparticulate topiramate composition compared to a solution is selected from the group consisting of greater than about 80%, greater than about 85%, greater than about 90%, and greater than about 95%.
39. method of making a nanoparticulate topiramate composition according to any one of claims 1 to 38, comprising contacting topiramate particles with at least one surface stabilizer for a time and under conditions sufficient to provide a nanoparticulate topiramate composition having an effective average particle size of less than about 2 microns.
40. The method of claim 39, wherein said contacting grinding.
41. The method of claim 40, wherein said grinding comprises wet grinding.
42. The method of claim 39, wherein said contacting comprises homogenzing.
43. The method of claim 39, wherein said contacting comprises:
(a) dissolving the topiramate particles in a solvent;
(b) adding the resulting topiramate solution to a solution comprising at least one surface stabilizer; and (c) precipitating the solubilized topiramate and at least one surface by the addition thereto of a non-solvent.
(a) dissolving the topiramate particles in a solvent;
(b) adding the resulting topiramate solution to a solution comprising at least one surface stabilizer; and (c) precipitating the solubilized topiramate and at least one surface by the addition thereto of a non-solvent.
44. Use of a nanoparticulate topiramate composition according to any one of claims 1 to 38 for the preparation of a medicament.
45. The use of claim 44, wherein the medicament is useful in, treating a subject having a condition selected from the group consisting of seizures, mood disorders, post traumatic stress syndrome (PTSD), Bipolar Disorder, mania, depression, personality disorders, bipolar mood instability, schizophrenia, psychosis, bipolar spectrum disorders, and rapid-cycling bipolar disorders.
46. The use of claim 45, wherein the wherein the medicament is useful in treating a subject having a mood disorder or a bipolar mood disorder which has nit been adequately controlled by other medications.
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CA2513064C (en) | 2009-11-10 |
EP1587499A1 (en) | 2005-10-26 |
US20040258758A1 (en) | 2004-12-23 |
JP4469846B2 (en) | 2010-06-02 |
WO2004078162A1 (en) | 2004-09-16 |
US7390505B2 (en) | 2008-06-24 |
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