Solid foamed active substance preparations

Details Solid foamed active substance preparations Solid foamed active substance preparations

1999-03-01

2000-11-21

Clardy, S. Mark

Drug, bio-affecting and body treating compositions

Designated organic nonactive ingredient containing other...

Solid synthetic organic polymer

5147725, A61K 4732

Patent

active

061504246

DESCRIPTION:

BRIEF SUMMARY
DESCRIPTION

The present invention relates to solid, partially or completely foamed active ingredient forms based on melt-processable polymers.
The invention furthermore relates to processes for producing active ingredient forms of this type.
It is generally known that foamed plastics can be produced by extruding melts comprising volatile blowing agents.
It is furthermore known, for example from EP-A 240 904, to prepare solid drug forms by extruding active ingredient-containing polymer melts with subsequent shaping.
Rapid-release drug forms are, as a rule, obtained by using insoluble but swellable disintegrants to bring about rapid disintegration of the drug form.
Rapid release can also be obtained with drug forms produced by melt extrusion by using relatively low molecular weight, water-soluble thermoplastic polymers as matrix polymers. However, the disadvantage of this is that on use of such polymers there are frequently problems with the storage stability of the finished drug forms.
It is an object of the present invention to find active ingredient-containing preparations which can be obtained by the economically attractive melt-extrusion process and permit controlled release of the active ingredient.
We have found that this object is achieved by the active ingredient forms defined at the outset. We have also found processes for producing such active ingredient forms.
The solid, foamed active ingredient preparations according to the invention may contain as active ingredients all the substances which can be incorporated without decomposition into the polymer melt under the processing conditions.
Examples of suitable active ingredients are:
acebutolol, acetylcysteine acetylsalicylic acid, aciclovir, alprazolam, albumin, alfacalcidol, allantoin, allopurinol, ambroxol, amikacin, amiloride, aminoacetic acid, amiodarone, amitriptyline, amlodipine, amoxicillin, ampicillin, ascorbic acid, aspartame, astemizole, atenolol, azemetacin [sic], beclometasone [sic], benscerazide [sic], benzalkonium hydroxide, benzocaine, benzoic acid, betametasone, bezafibrate, biotin, biperiden, bisoprolol, bromazepam, bromhexine, bromocriptine, budesonide, bufexamac, buflomedil, buspirone, caffeine, camphor, captopril, carbamazepine, carbidopa, carboplatin, cefachlor, cefalexin, cefadroxil, cefazolin, cefixime, cefotaxime, ceftazidine, ceftriaxone, cefuroxime, chloramphenicol, chlorhexidine, chlorpheniramine, chlortalidone, choline, ciclosporin, cilastatin, cimetidine, ciprofloxacin, cisapride, cisplatin, clarithromycin, clavulanic acid, clomibramine [sic], clonazepam, clonidine, clotrimazole, clozapine, codeine, colestyramine, cromoglicic [sic] acid, cyanocobalamin, cyproterone, desogestrel, dexamethasone, dexpanthenol, dexthromethorphan [sic], dextropropoxiphene, diazepam, diclofenac, digoxin, dihydrocodeine, dihydroergotamine, dilthiazem [sic], diphenhydramine, dipyridamole, dipyrone, disopyramide, domperidone, dopamine, doxocycline [sic], enalapril, enrofloxacin, ephedrine, epinephrine, ergocalciferol, ergotamine, erythromycin, estradiol, ethinylestradiol, etoposide, Eucalyptus Globulus [sic], famotidine, felodipine, fenofibrate, fenoterol, fentanyl, flavin mononucleotide, fluconazole, flunarizine, fluorouracil, fluoxetine, flurbiprofen, flutamide, furosemide, gemfibrozil, gentamicin, Ginkgo Biloba [sic], glibenclamine [sic], glipizide, Glycyrrhiza Glabra [sic], guaifenesin, haloperidol, heparin, hyaluronic acid, hydrochlorothiazide, hydrocodone, hydrocortisone, hydromorphone, hydroxytetracycline, ipratropium hydroxide, ibuprofen, imipenem, indomethacin, iohexol, iopamidol, isosorbide dinitrate, isosorbide mononitrate, isotredinoin [sic], kethotifen [sic], ketoconazole, ketoprofen, ketorolac, labetalon [sic], lactulose, lecithin, levocarnitine, levodopa, levoglutamide, levonorgestrel, levothyroxine, lidocaine, lipase, lisinopril, loperamide, lorazepam, lovastatin, medroxyprogesterone, menthol, methotrexate, methyldopa, methylprednisolone, metoclopramide, metoprolol, miconazole, midazolam, minocycline, minoxidil, misobrostol [si

REFERENCES:
patent: 4801460 (1989-01-01), Goertz et al.
patent: 4880585 (1989-11-01), Klimesch et al.
patent: 5369131 (1994-11-01), Poli et al.

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