Use of an immediate-release powder in pharmaceutical and nutraceutical compositions

• US 20030124191A1
• Filed: 03/25/2002
• Published: 07/03/2003
• 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:
  US10/106,923
• Publication Number:
  US 20030124191A1
• 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 present invention relates to the use of a powder comprising at least one active substance, at least one surfactant, at least one wetting agent and at least one diluent, for preparing a pharmaceutical or nutraceutical composition, this composition allowing rapid and immediate release of the active substance.

Claims

1. Method for administering a pharmaceutical or nutraceutical composition to a subject, said method comprising contacting said pharmaceutical or nutraceutical composition with a mucosal surface, said pharmaceutical or nutraceutical composition containing a powder comprising at least one active substance, at least one surfactant, at least one wetting agent and at least one diluent, whereby rapid and immediate release of the active substance is obtained.

2. Method according to claim 1, wherein at least the active substance is in micronized form.

3. Method according to claim 1, wherein the powder is in micronized form.

4. Method according to claim 1, wherein the active substance is selected from the group consisting of oestradiol and derivatives thereof, norethisterone acetate, progesterone, testosterone, dihydrotestosterone, trinitrine, fentanyl, nitroglycerine, nicotine (nicotine S(−

)), scopolamine, clonidine, isosorbide dinitrate, laevonorgestrel in combination with ethinyl oestradiol or with oestradiol, androstanolone, alclometasone dipropionate, 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, fluocinolon acetonide, fluocinodine, fluocortolone, fluocortolone hexanoate, fluocortolone pivalate, hydrocortisone, hydrocortison 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, P-3-adrenergic agonist, growth hormone, oxybutinin, buprenorphine, pergolide, oestradiol+nestorone, nestorone, 7α

-methyl-19-nortesterone, mecamylamine (nicotine antagonist)+nicotine, salbutamol, selegiline, buspirone, ketotifen, lidocaine, testosterone+oestradiol, ketorolac, eptazocine, insulin, a-interferon, prostaglandins, 17-p-oestradiol+norethindrone acetate, 5-aminolevulinic acid, the benzodiazepine alprozolam, diclofenac, fenoprofen, flubiprofen, ketoprofen, methyl phenidate, miconazole, piroxicam, bruprenorphine, dexmedetomidine, prazosin (α

-adrenergic antagonist), gestodene+ethinyl oestradiol, alprostadil, tulobuterol (β

-adrenergic agonist), ethinyl oestradiol+norelgestromin, physostigmine, lidocaine, medindolol (α

-adrenergic agonist), rotigotine (dopamine D2 antagonist), ethinyl oestradiol+norethindrone acetate, thiatolserine, phlorglucinol, molsidomine, 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), new COX inhibitors such as etoricoxib (inflammation), valdecoxib (arthritis) and parecoxib, substance P antagonist (depression), darifenacin (urology), eletriptan (migraine), alosetron, tegaserod, capravirine (HIV) and combinations thereof.

5. Method according to claim 1, wherein the active substance is selected from the group consisting of vitamins, mineral salts and brewer'"'"'s yeast.

6. Method according to claim 1, wherein the surfactant is selected from the group consisting of non-ionic surfactants, such as polyoxyethylene sorbitan (fatty acid ester), polyoxyethylene alkyl ether, the polyoxyethylene derived from castor oil, and mixtures thereof.

7. Method according to claim 1, wherein the wetting agent is selected from the group consisting of polyols such as sorbitol, glycerol or polyethylene glycol, and mixtures thereof.

8. Method according to claim 1, wherein the diluent is selected from the group consisting of sodium, calcium carbonate or bicarbonate, sucrose, mannitol, xylitol, sorbitol, lactose, microcrystalline cellulose or cellulose powder, starch and derivatives thereof, dibasic calcium phosphate, tribasic calcium phosphate, calcium sulphate, dextrates, dextrins, dextrose excipients, fructose, kaolin, lactitol and mixtures thereof.

9. Method according to claim 1, wherein the powder comprises a binding agent selected from the group consisting of acacia, alginic acid, sodium carboxymethylcellulose, microcrystalline cellulose, dextrins, ethylcellulose, gelatin, glucose, guar gum, hydroxypropylmethylcellulose, methylcellulose, polyethylene oxide, povidone, pregelatinized starch, and mixtures thereof.

10. Method according to claim 1, wherein the powder comprises a penetration enhancer selected from the group consisting of aliphatic fatty acid esters such as isopropyl myristate;

fatty acids such as oleic acid;

alcohols or polyols, such as ethanol, propylene glycol or polyethylene glycol;

the components of essential oils and terpene derivatives (such as eugenol, geraniol, nerol, eucalyptol or menthol);

surfactants;

moisturizers such as glycerol or urea;

keratolytic agents, such as alpha-hydroxy acids, 23-lauryl ether, aprotinin, azone, benzalkonium chloride, cetylpyridinium chloride, cetyltrimethylammonium bromide, cyclodextrins, dextran sulphate, lauric acid, lysophosphatidylcholine, 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, sulphoxides, alkyl glycosides, and mixtures thereof.

11. Method according to claim 1, wherein the powder has a particle size of between 0.01 μ

m and 1000 μ

m.

12. Method according to claim 11, wherein the powder has a particle size between 0.1 μ

m and 100 μ

m.

13. Method according to claim 12, wherein the powder has a particle size between 1 μ

m and 50 μ

m.

14. Method according to claim 1, wherein the pharmaceutical or nutraceutical composition is applied on the buccal mucous membrane, the nasal mucous membrane or the vaginal mucous membrane.

15. Method according to claim 14, wherein the composition is applied to the buccal mucous membrane sublingually.

16. Method according to claim 1, wherein the composition is in a sprayable form.

17. Method according to claim 1, wherein the composition is contained in a sachet.