Solid active extrusion compound preparations containing low-subs

Details Solid active extrusion compound preparations containing low-subs Solid active extrusion compound preparations containing low-subs

1997-07-30

1999-08-17

Webman, Edward J.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Matrices

514781, A61K 910, A61K 4738

Patent

active

059390999

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/EP96/00417 filed Feb. 1, 1996.
The present invention relates to solid preparations, obtainable by joint melt extrusion of water-soluble polymer, and hydroxypropylcellulose, and of one or more pharmaceutical auxiliaries.
The invention furthermore relates to a process for producing such preparations, and to their use as drugs.
Active compound-containing preparations which are produced by melt extrusion are generally known.
The extrusion of active compound-containing melts of water-soluble polymers, preferably of copolymers of vinylpyrrolidone, is described in EP-A 240 904 and EP-A 240 906.
JP-A 58-192817 and JP-A 58-79915 disclose the melt extrusion of active compound-containing preparations based on thermoplastic polymers such as hydroxypropylcellulose as binders.
Low-substituted hydroxypropylcellulose (L-HPC), which is prepared by partial etherification of cellulose with propylene oxide, is insoluble in water, but swells on contact with water. On account of this swelling behavior, L-HPC is employed as a disintegrant for accelerating the disintegration of the tablets. L-HPC can also be employed as a binder for tablets for increasing the tablet hardness.
Kawashima et al., Chem. Pharm. Bull. 41 (1933), 1827-31, describe that the use of L-HPC in granules for tableting is strongly dependent, on the one hand, on the particle size of the L-HPC, and on the other hand the active compound release profile is crucially affected by the pressing force during compaction.
In contrast to hydroxypropylcellulose having higher degrees of substitution, L-HPC, however, shows no thermoplastic processability.
It is an object of the present invention to find active compound preparations which can be produced by polymer-active compound melt extrusion and allow a specific adjustment of the release of active compound.
We have found that this object is achieved by the preparations defined at the outset, a process for their production, and their use as drugs.
Active compounds suitable as component A) are those which do not decompose under the processing conditions during melt extrusion.
Suitable active compounds are, for example: albumin, alfacalcidol, allantoin, allopurinol, ambroxol, amikacin, amiloride, aminoacetic acid, amiodarone, amitriptyline, amlodipine, amoxicillin, ampicillin, ascorbic acid, aspartame, astemizole, atenolol, beclomethasone, benserazide, benzalkonium hydroxide, benzocaine, benzoic acid, betamethasone, 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 axetil, chloramphenicol, chlorhexidine, chlorpheniramine, chlorthalidone, choline, ciclosporin, cilastatin, cimetidine, ciprofloxacin, cisapride, cisplatin, clarithromycin, clavulanic acid, clomipramine, clonazepam, clonidine, clotrimazole, clozapine, codeine, colestyramine, cromoglicic acid, cyanocobalamin, cyproterone, desogestrel, dexamethasone, dexpanthenol, dextromethorphan, dextropropoxiphene, diazepam, diclofenac, digoxin, dihydrocodeine, dihydroergotamine, diltiazem, diphenhydramine, dipyridamole, dipyrone, disopyramide, domperidone, dopamine, enalapril, ephedrine, epinephrine, ergocalciferol, ergotamine, erythromycin, estradiol, ethinylestradiol, etoposide, Eucalyptus globulus, famotidine, felodipine, fenofibrate, fenoterol, fentanyl, flavine mononucleotide, fluconazole, flunarizine, fluorouracil, fluoxetine, flurbiprofen, folinic acid, furosemide, gemfibrozil, gentamicin, Ginkgo biloba, glibenclamide, glipizide, Glycyrrhiza glabra, guaifenesin, haloperidol, heparin, hyaluronic acid, hydrochlorothiazide, hydrocodone, hydrocortisone, hydromorphone, ipratropium hydroxide, ibuprofen, imipenem, indomethacin, iohexol, iopamidol, isosorbide dinitrate, isosorbide mononitrate, isotretinoin, ketotifen, ketoconazole, ketoprofen, ketorolac, labetalol, lactulose, lecithin, levocarnitine,

REFERENCES:
patent: 4801460 (1989-01-01), Goertz et al.
patent: 4880585 (1989-11-01), Klimesch et al.
patent: 5194197 (1993-03-01), Munk et al.
Chem. & Phar. Bul. vol. 42, No. 9, Matsumura et al., Computer Optimization for the Formulation of . . .
Chem. Pharm. Bull. 41(10) 1827-1831 (1993) Kawashima et al.
Chem. Abst. J5 8079-915.
Chem. Abst. J5 8192-817.

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