Micronized pharmaceutical or nutraceutical powder with immediate release

• US 20050118272A1
• Filed: 12/27/2002
• Published: 06/02/2005
• Est. Priority Date: 12/27/2001
• Status: Abandoned Application

• Current Assignee: Besins International Belgique, Galenix Innovations
• Original Assignee: Besins International Belgique, Galenix Innovations
• Inventors: Besse, Jerome, Besse, Laurence
• Application Number:
  US10/500,213
• Publication Number:
  US 20050118272A1
• Time in Patent Office: Days
• US Class Current: 424/489
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals

Abstract

The invention concerns a micronized pharmaceutical or nutraceutical powder with immediate release having a grain size distribution of not more than 100 μm, and comprising the combination of at least an active substance, at least a wetting agent and at least a diluent.

Claims

1. Immediate-release pharmaceutical or nutraceutical micronized powder having a particle size of at most 100 μ

m and comprising a combination of at least one active substance, at least one wetting agent and at least one diluent.

2. Powder according to claim 1, characterized in that it has a particle size of at most 50 μ

m.

3. Powder according to claim 1, characterized in that it has a particle size of at most 10 μ

m.

4. Powder according to claim 1, characterized in that it allows the dissolution of all of the active substance(s) in less than 30 seconds, when it is administered mucosally.

5. Powder according to claim 1, characterized in that the active substance is in a micronized form.

6. Powder according to claim 1, wherein the active substance is at least one member selected from the group consisting of cyproterone acetate, norethisterone acetate, progesterone, 3-keto-desogestrel, norgestimate, laevonorgestrel, desogestrel, gestodene, a natural estrogens a synthetic estrogen, Δ

-4-androstenedione, testosterone, dihydrotestosterone, or androstanolone, DHEA, trinitrine, fentanyl, nitroglycerine, nicotine (nicotine S(−

)), scopolamine, clonidine, isosorbide dinitrate, alclometasone dipropionate, phloroglucinol, molsidomine, acetazolamide, acyclovir, adapalene, alclomethasone dipropionate, amcinonide, ameline, bamethan sulphate+escin, betamethasone valerate, betamethasone dipropionate, bufexamac, caffeine, calcipotriol monohydrate, cetrimonium bromide, clobetasol propionate, crilanomer, desonide, dexpanthenol, diclofenac, diflucortolone, valerate, difluprednate, diphenydramine hydrochloride, econazole nitrate, erythromicin, flumetasone pivalate, fluocinolone acetonide, fluocinodine, fluocortolone, fluocortolone hexanoate, fluocortolone pivalate, hydrocortisone, hydrocortisone acetate, ibacitabine, ibuprofen, imiquimod, ketoconazole, ketoprofen, lidocaine, metronidazole, miconazole nitrate, minoxidil, nifluminic acid, penciclovir, benzoyl peroxide, piroxam, iodinated povidone, promestriene, pyrazinobutazone, roxithromycin, sulphacetamide, triamcinolone, tazarotene, tretinoin and isotretinoin, triclocarban, vidarabine monophosphate, β

-3-adrenergic agonist, growth hormone, oxybutinin, buprenorphine, pergolide, nestorone, 7α

-methyl-19-nortesterone, mecamylamine, salbutamol, clenbuterol, selegiline, buspirone, ketotifen, lidocaine, ketorolac, eptazocine, insulin, α

-interferon, prostaglandins, 5-aminolevulinic acid, benzodiazepine alprozolam, diclofenac, fenoprofen, flubiprofen, ketoprofen, methyl phenidate, miconazole, piroxicam, bruprenorphine, alprozolam, dexmedetomidine, prazosin (α

-adrenergic antagonist), alprostadil, tulobuterol (β

-adrenergic agonist), ethinyl oestradiol+norelgestromin, ketorolac, physostigmine, medindolol (β

-adrenergic agonist), rotigotine (dopamine D2 antagonist), thiatolserine, Esomeprazole, Melagatran (in the case of thrombosis), Rosuvastatin, Ezetimide, Pitavastatin (hyperlipidaemia), Mitiglinide (type II diabetes), Cilomilast, Viozan (asthma), Aripipazole (psychiatry), Omapatrilat (hypertensive), Orzel (cancerology), Caspofongin acetate, Voriconazole (infections), a new COX inhibitor, Valdecoxib (arthritis) and Parecoxib, Substance P antagonist (depression), Darifenacin (urology), Eletriptan (migraine), Alosetron, Tegaserod, Capravirine (HIV), Finasteride (5-alpha reductase inhibitor).

7. Powder according to claim 1 wherein the active substance is at least one member selected from the group consisting of a vitamin, an inorganic salt, and brewer'"'"'s yeast.

8. Powder according to claim 1, wherein wetting agent is at lease one member selected from the group consisting of a polyol, triacetin, a hydrogenated vegetable oil, a polyoxy(ethylene)polyoxy(propylene) copolymer, and a polyoxyethylene alkyl ether.

9. Powder according to claim 1, wherein the diluent is at least one member selected from the group consisting of calcium or sodium carbonate or bicarbonate, sucrose, mannitol, xylitol, sorbitol, lactose, maltotol, glucose, cellulose, a microcrystalline cellulose powder, starch, a starch derivative, dibasic calcium phosphate, tribasic calcium phosphate, calcium sulphate, a dextrate, a dextrin, a dextrose excipient, fructose, kaolin, and lactitol.

10. Powder according to claim 1, characterized in that it further comprises an antistatic agent.

11. Powder according to claim 10, characterized in that the antistatic agent is selected from the group consisting of colloidal silica, magnesium silicate, talc, calcium silicate and tribasic calcium phosphate and mixtures thereof.

12. Powder according to claim 1, which further comprises a binder which is at least one member selected from the group consisting of acacia, alginic acid, carboxymethyl cellulose sodium, microcrystalline cellulose, a dextrin, ethyl cellulose, gelatin, glucose, guar gum, hydroxypropyl methyl cellulose, methyl cellulose, polyethylene oxide, povidone, and pregelatinized starch.

13. Powder according to claim 1, which further comprises an absorption enhancer selected from the group consisting of an aliphatic fatty acid ester, a fatty acid, an alcohol or polyol, a component of an essential oil, a terpene derivative, a surfactant, a moisturizer, a keratolytic agent, 23-lauryl ether, aprotinin, azone, benzalkonium chloride, cetylpyridinium chloride, cetyltrimethylammonium bromide, a cyclodextrin, dextran sulphate, lauric acid, lysophosphatidylcholine, a menthol, methoxysalicylate, methyl oleate, oleic acid, phosphatidylcholine, polyoxyethylene, polysorbate 80, sodium EDTA, sodium glycocholate, sodium glycodeoxycholate, sodium lauryl sulphate, sodium salicylate, sodium taurocholate, sodium taurodeoxycholate, a sulphoxides, and an alkyl glycoside.

14. Powder according to claim 1, characterized in that it further comprises an edulcorant agent and/or a flavoring agent.

15. Powder according to claim 14, characterized in that the edulcorant agent is selected from the group consisting of aspartam, dextrates, dextrose, fructose, mannitol, sodium or calcium saccharinate, sorbitol, sucralose, sucrose, and mixtures thereof.

16. Powder according to claim 14, wherein the flavoring agent is at least one member selected from the group consisting of a flavor of synthetic, semi-synthetic or natural origin.

17. Powder according to claim 1, characterized in that it is in a form suitable for its application on the buccal mucosa, the nasal mucosa or the vaginal mucosa.

18. Powder according to claim 1 characterized in that it is in a form suitable for its application to the buccal mucosa sublingually.

19. Powder according to claim 1, characterized in that it is in a sprayable form.

20. Powder according to claim 1, characterized in that it is packaged in a single-dose packet.

21. Powder according to claim 1, characterized in that it is packaged in a thermally moulded capsule provided with a peelable operculum.

22. Powder according to claim 1, characterized in that it is in a packaging suitable for powder administration known to those skilled in the art.

24. Powder according to claim 6 wherein the active substance is at least one member selected from the group consisting of estradiol, a natural estradiol derivative, ethinylestradiol, and Etoricoxib (inflammation).

25. Powder according to claim 8 wherein the wetting agent is at least one member selected from the group consisting of PEG, hexylene glycol, triacetin, and a hydrogenated vegetable oil.

26. Powder according to claim 13 wherein the absorption enhancer is at least one member selected from the group consisting of isopropylmyristate, oleic acid, ethanol, propylene glycol, polyethylene glycol, eugenol, geraniol, nerol, eucalyptol, menthol, polyoxyethylene sorbitan, polyoxyethylene alkyl ether, polyoxyethylene derived from castor oil, glycerin, urea, and an alpha-hydroxy acid.

23. (canceled)

27. A method for manufacturing an immediate-release pharmaceutical or nutraceutical composition, said method comprising a step of micronizing a composition comprising a combination of at least one active substance, at least one wetting agent and at least one diluent.