EP1198227A1 - Procede de production de preparations pharmaceutiques solides se desagregeant rapidement - Google Patents

Procede de production de preparations pharmaceutiques solides se desagregeant rapidement

Info

Publication number
EP1198227A1
EP1198227A1 EP00942137A EP00942137A EP1198227A1 EP 1198227 A1 EP1198227 A1 EP 1198227A1 EP 00942137 A EP00942137 A EP 00942137A EP 00942137 A EP00942137 A EP 00942137A EP 1198227 A1 EP1198227 A1 EP 1198227A1
Authority
EP
European Patent Office
Prior art keywords
liquid
ingredients
shaping
water
parts
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
EP00942137A
Other languages
German (de)
English (en)
Inventor
Marco Schroeder
Klaus-Jürgen Steffens
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer AG
Original Assignee
Bayer AG
Bayer Healthcare AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=7913998&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EP1198227(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer AG, Bayer Healthcare AG filed Critical Bayer AG
Publication of EP1198227A1 publication Critical patent/EP1198227A1/fr
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007—Effervescent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing

Definitions

  • the invention relates to a process for the preparation of rapidly disintegrating solid preparations containing pharmaceutical active substances in aqueous liquids (such as water, saliva).
  • aqueous liquids such as water, saliva
  • Immediate drug formulations are expected to rapidly disintegrate into liquids and release the active ingredient. This goal is often attempted to be achieved by formulating the active ingredient without binders, but with auxiliaries which promote the disintegration of the preparations after the liquid has entered, into formulations such as Tablets, processed. However, satisfactory results are not always obtained.
  • a new generation of immediately effective pharmaceutical preparations is expected to disintegrate and release the active ingredient in the shortest possible time.
  • preparations in the presence of only small amounts of liquid such as e.g. given by oral application without the addition of liquid, disintegrate within a very short time without leaving behind coarse granulate particles which cause a "sand feeling" in the mouth.
  • Effervescent preparations such as effervescent powder and effervescent tablets are a form of formulation for active ingredients with a long absorption time and / or with limited gastric tolerance, which can significantly improve the disadvantageous properties of the active ingredient.
  • Effervescent preparations containing drugs are therefore becoming increasingly popular. It would therefore be desirable that the problem solution to be found can also be applied to pharmaceutical effervescent preparations.
  • the desired pharmaceutical preparations should also include the properties of the individual active ingredients, such as the frequently encountered sensitivity to water, duly take into account.
  • the problem solution to be found should lead to mechanically stable formulations (low abrasion, high breaking and compressive strength), which can be easily packaged and stored and transported under normal conditions.
  • JP-A 08291051 a method for tablet production is known, according to which the active ingredients, water-soluble binder and water-soluble filler are first tabletted under very low pressure; then the tablets obtained are moistened and then dried.
  • EP-A 192 460 describes tablets with a relatively hard shell made of pressed material which is relatively resistant to liquids, the tablet constituents rapidly dissolving in the presence of liquid after the tablet has broken.
  • EP-A 352 190 describes the production of porous tablets which disintegrate quickly in water and whose pores are produced by freeze-drying a dispersion.
  • the molding compound for the production of the tablets contains a certain amount of water
  • EP-A 450 141 relates to a quickly soluble carrier material, i.a. for active pharmaceutical ingredients, with porous, water-soluble, hydratable gel or foam material that has been hydrated with water, hardened in a hydrated state and then dehydrated in such a way that cavities remain instead of the hydrating liquid.
  • Disintegrants and / or swelling agents or tablets containing soluble substances are known from EP-PS 548 356, the (bad-tasting) active ingredient having a multi- is particulate and is in the form of coated microcrystals or coated microgranules.
  • EP-A 553 777 describes a process for the production of porous, rapidly disintegrating tablets, according to which granules containing an active ingredient and carbohydrate are moistened with water, a tablet is formed therefrom and this is dried.
  • the dissolution times (in the mouth) are between 0.2 and 1.5 minutes.
  • Matrix network structure made of mannitol and a natural rubber such as guar gum or acacia gum.
  • US Pat. No. 5,851,553 describes a process for producing rapidly disintegrating tablets, according to which a mixture comprising active ingredient and amorphous sugar is subjected to a so-called flash flow process ("flash flow process"), the sugar crystallizing in the form of a type of cotton candy.
  • flash flow process a so-called flash flow process
  • the voluminous mass containing cotton candy can be shaped into tablets with low forces (preferably not more than 80 psi) and then subjected to annealing, if appropriate in a humid atmosphere.
  • WO 98/23656 relates to a freeze-drying process for the production of rapidly disintegrating tablets using lipids and structure-forming agents.
  • WO 98/29137 describes rapidly disintegrating tablets which comprise a solid dispersion of a poorly soluble active ingredient in a gel-forming water-soluble polymer and contain an alkali salt of a weak acid or a strong acid with an endothermic standard solution enthalpy or heat of solution.
  • a technology is known from WO 98/46215, according to which granulation is dispensed with and the active ingredients and a matrix comprising a non-directly compressible filler ("a non-direct compression filier"), for example mannitol, and a lubricant are compressed into tablets Tablets should disintegrate quickly in the mouth and cause a minimal "sand feeling".
  • a non-direct compression filier for example mannitol
  • sucrose crystals are slightly moistened (residual moisture below 2% by weight) and dried after compression under high pressure, resulting in porous but stable moldings.
  • the invention relates to a process for the preparation of preparations comprising A) at least one active pharmaceutical ingredient and B) at least one auxiliary, but - apart from an optionally present effervescent set - no disintegrant, after which at least the major part of the total mass of
  • liquid C preferably water, ethanol and / or isopropanol
  • the solid preparations obtainable in this way are porous and are moistened immediately upon contact with aqueous liquid.
  • the disintegration and disintegration of preparations containing the broth set according to the invention take place almost simultaneously within a few seconds.
  • disintegration and dissolution are completed within 2 to 12 seconds, preferably within less than 8 seconds, in particular within less than 5 seconds (measured in a vessel filled with 150 ml of water at 20 ° C. or on the tongue without Addition of additional liquid);
  • Preparations according to the invention which are free of effervescent products have completely disintegrated during this time and have been at least half dissolved.
  • active ingredient in the sense of this invention includes pharmaceutical active ingredients in the narrower sense, i.e. preferably not food (such as dairy products) and vitamins only in pharmaceutical dosage.
  • Preferred active ingredients A) for the preparations to be produced according to the invention are, for example
  • Analgesics such as ibuprofen, ketoprofen, paracetamol, acetylsalicylic acid, COX 2 inhibitors such as nimesulide, meloxicam, naproxen, propyphenanzone, metamizole,
  • Antacids such as hydrotalcide, magaldrate, calcium carbonate, Anti-asthmatics / broncholytics such as salbutamol, tulobuterol, terbutaline, cromoglycic acid, ketotifen, theophylline,
  • Antibiotics such as quinolones, tetracyclines, cephalosporins, penicillins,
  • Macrolides sulfonamides, polypeptides, psychopharmaceuticals such as benzodiazepines, haloperidol, anitriptyline, carbamazepin,
  • Anti-rheumatic drugs such as phenylbutazone, indomethacin, diclofenac, piroxicam,
  • Antidiabetic agents such as metformin, glibenclamide, acarbose, glisoxepid,
  • Antiallergics / antihistamines such as astemizole, terfenadine, loratadine, clemastine, bamipine, cetrizine,
  • Antihypertensives such as etilefrin, norfenefrin, dihydroergotamine mesilate,
  • Antitussives such as codeine, dextromefhorphan, clobutinol, dopropizin,
  • Antihypertensives such as beta blockers such as propanolol, atenolol, metoprolol, prazosin, - antihypertensives such as calcium antagonists such as nifedipine, nitrendipine, diltiazem, verapamil, felodipine, nimodipine,
  • Laxantia such as sodium picosulfate, lactulose, lactitol,
  • Mucolytics / expectorants such as ambroxol, bromhexine, guaifenesin, acetyl cysteine, carbocysteine, H 2 blockers such as ranitidine, famotidine, pirenzepin,
  • Local anesthetics such as benzocaine, lidocaine, procaine,
  • Antiemetics / prokinetics such as metoclopramide, domperidone, meclozin, dimenhydinate,
  • Lipid-lowering agents such as fenofibrate, bezafibrate, pravastatin, fluvastatin, - anti-migraine agents such as caffeine, dihydroergotamine, ergotamine,
  • Sympathomimetics such as pseudoephedrine, pholedrine,
  • Vitamins and minerals In the case of active ingredients A) which are intrinsically poorly soluble, it is generally advantageous if the active ingredients A) are converted into water-soluble salts.
  • Preferred water-soluble ASA salts include ASA lysinate and ASA arginate.
  • Carriers such as monosaccharides, for example glucose, oligosaccharides, for example sucrose, polysaccharides, for example maltodextrin and
  • Polyols for example mannitol and sorbitol, binders such as glycol, maltodextrin, polyvinyl alcohol, polyvinylpyrrolidone, vinyl alcohol / vinylpyrrolidone copolymers, polyethylene glycol,
  • wetting agents such as di-octyl sodium sulfosuccinate, sodium lauryl sulfate, lubricants such as polyethylene glycol, disodium fumarate,
  • Fillers such as highly disperse silicon dioxide,
  • the auxiliaries B) are preferably water-soluble. “Water-soluble” in this sense means a solubility in water (20 ° C.) of at least 10, preferably at least 30 and in particular at least 40 g / 100 ml of water. A particularly preferred auxiliary B) is maltodextrin.
  • the auxiliaries B) further comprise the effervescent set necessary for effervescent preparations, comprising (i) CO 2 dispenser and (ii) acidic component.
  • Preferred CO donors (i) include alkali and alkaline earth carbonates and hydrogen carbonates, in particular sodium and potassium carbonate and hydrogen carbonate, and magnesium and calcium carbonate.
  • Suitable acidic component (ii), which serves to release carbon dioxide from the CO 2 dispenser (i) are all physiologically harmless acids (so-called “pleasure acids”) which are strong enough to release carbon dioxide from component (i). set; such acids have a first equilibrium exponent pKs from 1 to
  • Preferred acidic components (ii) include ascorbic acid and polybasic carboxylic acids having 3 to 8, preferably 4 to 6, C atoms and 2 to 4 carboxyl groups per molecule, e.g. Vitamin C, malic acid, citric acid, tartaric acid and their mixtures. Further preferred acidic components (ii) include the acidic salts of the above polybasic
  • the shower set preferably contains 30 to 70% by weight of CO 2 dispenser (i) and 70 to 30% by weight of acidic component (ii), in each case based on the sum of components (i) and (ii).
  • the shaped bodies obtainable according to the invention should - apart from the shower set which may be present - be free of so-called disintegrants (disintegration aids).
  • disintegrants include e.g. B. normal starch (such as corn or rice starch).
  • disintegrant also depends on the quantity of individual substances, such as starch, for example: during quantities of at least 5% by weight of starch (usually in powder form, ie avoiding contact with water), based on the finished product
  • Shaped bodies, which act as disintegrants, amounts of up to 3% by weight of starch, based on finished shaped bodies, are used as binders in the granulation.
  • disintegrant includes in particular the so-called “super disintegrants”; these include a) crosslinked polyvinylpyrrolidone, which is normally used in amounts of 2 to 5% by weight, based on the finished molded article; b) cross-linked carboxymethyl cellulose ("cross ceramellose-sodium”), which is usually in
  • L-HPC low-substituted hydroxypropyl cellulose
  • the preparations produced according to the invention contain less than 3% by weight, based on the finished molded article, of swellable binders.
  • “Swellable binders” in this sense are primarily natural starches, but not non-swelling water-soluble starches.
  • a particularly preferred preparation obtainable according to the invention contains an effervescent set and A) acetylsalicylic acid and / or ibuprofen or its water-soluble salts and B) maltodextrin and / or mannitol.
  • Water is the most preferred liquid C).
  • Preferred liquid C) are also ethanol and isopropanol and all conceivable mixtures which can be prepared from at least two members from the group consisting of water, ethanol and isopropanol.
  • the primary particles to be used for the granulation should be as small as possible and, if possible, be amorphous.
  • the primary particle size of the active ingredients can vary within wide limits, but will usually be between 100 and 600, preferably 150 and 500, in particular below 250 ⁇ m.
  • the granulation can be carried out in a manner known per se on granulation plates, in granulation drums, in the fluidized bed or by vibration. A particularly porous granulate can be obtained by pre-reacting the shower set with water.
  • the uniformity and the rate of disintegration of the preparations produced according to the invention are promoted by a narrow particle size distribution of the granules.
  • the preferred average particle diameter d 50 is 500 to
  • d 50 is the particle diameter, above and below it each 50% by weight of the particles lie.
  • the particle diameter dio-dgo is preferably in the range from 300 to 1300, in particular from 500 to 1000 ⁇ m. Because spherical granules offer optimum porosity and the number of possible contact points, spherical and almost spherical granules are preferred; a narrow particle size distribution is particularly preferred.
  • the liquid C) to be used according to the invention can be added before, during or after the granulation. Since the liquid C) acts as a lubricant during the deformation during the process according to the invention, other lubricants can be dispensed with.
  • Unwanted large agglomerates can be sieved, e.g. by forced sieving.
  • the mesh size can vary within wide limits; it is usually 0.5 to 2.0 mm, preferably 0.8 to 1.5 mm.
  • the residual moisture of the mass before shaping can be 2.5 to 15, preferably 5 to 10% by weight, based on the sum of solid ingredients and liquid. You can use a dry scale, e.g. with an MA 40 instrument from Sartorius, at 50 ° C. Any crystal water present should not be taken into account when determining moisture.
  • the bulk density of the granules is generally 0.5 to 1.8, preferably 0.7 to 1.5 g / cm 3 .
  • the porosity of the granules can be 0.3 to 0.7, preferably 0.4 to 0.6.
  • the shaping can take place, for example, on tabletting machines (in order to avoid undesired adhesion of the preparations to the tool, the tool can be coated with polytetrafluoroethylene, since the tool is only exposed to small forces). For tableting machines and form compactors, it is advisable to eject the shaped preparations downwards.
  • the method according to the invention makes it possible to dispense with so-called lubricating or mold release agents. If such agents are nevertheless to be used, very small amounts, such as, for example, 0.001 to 0.2, preferably 0.03 to 0.1,% by weight, based on the moist mass before shaping, are sufficient.
  • the height of the poured material in the die can serve as a reference for the degree of compaction.
  • the true density of the preparations obtainable according to the invention is generally 0.7 to 2.5, preferably 1.5 to 1.8 g / cm 3 .
  • the apparent density determination of the envelope volume in mercury (eg with a Pascal 440 porosimeter from Carlo
  • Drying can be carried out using customary methods, for example via contact, convection or radiation.
  • Preferred drying devices include duct dryers, convection cupboards, vacuum dryers, infrared, microwave and radio frequency devices.
  • the drying conditions depend on the size of the formulations. As a rule, temperatures of 20 to 80 ° C, in the presence of shower set lead from 20 to 50 ° C for good results. For example, forced air drying at 40 ° C is not a problem for most active ingredients.
  • the drying times can be 10 minutes to 6 hours, preferably 0.5 to 4 hours. If necessary, the drying can be followed by a cooling step.
  • the breaking strength of the preparations produced according to the invention reaches values of 10 to 110, preferably 20 to 50 N / cm 2 , determined in the breaking strength tester type 2E / 205 from Schleuniger / Switzerland.
  • active substances or auxiliary substances are hygroscopic, sensitive to air or light, this must be taken into account in the type of packaging.
  • the preparations produced according to the invention are also suitable for oral or rectal administration.
  • the moist granules were then fed to a tabletting machine, the form of which was coated with polytetrafluoroethylene.
  • the maximum pressure was 64 N / cm 2 , the compression 62%.
  • the ejected tablets (diameter 20 mm, height 7 mm) were then dried in a forced-air drying cabinet at 38 ° C. for 3 hours.
  • the tablets then had a compressive strength, measured in the type 2E / 205 breaking strength tester from Schleuniger / Switzerland, of 0.25 kg / cm 2 .
  • the tablet immediately sinks to the bottom, completely moistening it. Spontaneous decay is observed within 2 to 5 seconds with evolution of carbon dioxide. lung, whereby tablet parts created by the disintegration are driven to the surface. After 10 to 20 seconds, measured from the introduction of the tablet into the water, the dissolution of the tablet ingredients has ended.
  • Composition 21.0 parts sodium hydrogen carbonate
  • Composition 21.0 parts of potassium hydrogen carbonate

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

L'invention concerne un procédé simple de production de préparations se désagrégeant rapidement, contenant au moins un principe actif pharmaceutique et au moins une substance auxiliaire. Selon ledit procédé, on procède à la granulation d'au moins la partie prépondérante de la masse totale des composants de la préparation à produire, on moule le granulat obtenu et éventuellement le reste des composants, en présence d'un liquide, presque sans pression, et on sèche les corps moulés obtenus.
EP00942137A 1999-07-08 2000-06-27 Procede de production de preparations pharmaceutiques solides se desagregeant rapidement Ceased EP1198227A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19931708 1999-07-08
DE19931708A DE19931708A1 (de) 1999-07-08 1999-07-08 Verfahren zur Herstellung schnell zerfallender, fester pharmazeutischer Zubereitungen
PCT/EP2000/005938 WO2001003674A1 (fr) 1999-07-08 2000-06-27 Procede de production de preparations pharmaceutiques solides se desagregeant rapidement

Publications (1)

Publication Number Publication Date
EP1198227A1 true EP1198227A1 (fr) 2002-04-24

Family

ID=7913998

Family Applications (1)

Application Number Title Priority Date Filing Date
EP00942137A Ceased EP1198227A1 (fr) 1999-07-08 2000-06-27 Procede de production de preparations pharmaceutiques solides se desagregeant rapidement

Country Status (18)

Country Link
US (2) US6602520B1 (fr)
EP (1) EP1198227A1 (fr)
AR (1) AR024653A1 (fr)
AU (1) AU5686400A (fr)
BR (1) BR0012258A (fr)
CA (1) CA2375545A1 (fr)
CO (1) CO5190682A1 (fr)
DE (1) DE19931708A1 (fr)
GT (1) GT200000111A (fr)
MA (1) MA25418A1 (fr)
MX (1) MXPA02000130A (fr)
MY (1) MY128368A (fr)
PE (1) PE20010573A1 (fr)
PL (1) PL353171A1 (fr)
SV (1) SV2001000125A (fr)
TW (1) TWI253348B (fr)
UY (1) UY26234A1 (fr)
WO (1) WO2001003674A1 (fr)

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US20040057995A1 (en) 2004-03-25
US7208175B2 (en) 2007-04-24
TWI253348B (en) 2006-04-21
PL353171A1 (en) 2003-11-03
WO2001003674A1 (fr) 2001-01-18
US6602520B1 (en) 2003-08-05
CA2375545A1 (fr) 2001-01-18
DE19931708A1 (de) 2001-01-18
SV2001000125A (es) 2001-09-04
CO5190682A1 (es) 2002-08-29
BR0012258A (pt) 2002-03-12
GT200000111A (es) 2001-12-28
MY128368A (en) 2007-01-31
MA25418A1 (fr) 2002-04-01
MXPA02000130A (es) 2002-07-30
AR024653A1 (es) 2002-10-23
UY26234A1 (es) 2001-03-16
AU5686400A (en) 2001-01-30
PE20010573A1 (es) 2001-07-12

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