EP1855687A1 - Formes galeniques presentant une biodisponibilite controlee - Google Patents

Formes galeniques presentant une biodisponibilite controlee

Info

Publication number
EP1855687A1
EP1855687A1 EP06707140A EP06707140A EP1855687A1 EP 1855687 A1 EP1855687 A1 EP 1855687A1 EP 06707140 A EP06707140 A EP 06707140A EP 06707140 A EP06707140 A EP 06707140A EP 1855687 A1 EP1855687 A1 EP 1855687A1
Authority
EP
European Patent Office
Prior art keywords
vardenafil
polymer
acid
formulation according
active ingredient
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.)
Withdrawn
Application number
EP06707140A
Other languages
German (de)
English (en)
Inventor
Peter Serno
Roland Heinig
Kerstin Pauli
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 Intellectual Property GmbH
Original Assignee
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
Application filed by Bayer Healthcare AG filed Critical Bayer Healthcare AG
Priority to EP10177166A priority Critical patent/EP2255810A1/fr
Publication of EP1855687A1 publication Critical patent/EP1855687A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives

Definitions

  • the present application relates to novel drug formulations of Vardenafil, which dissolve quickly in the mouth and a. have controlled bioavailability and methods for their production.
  • Imidazotriazinone derivatives such as vardenafil and its use as a cGMP phosphodiesterase inhibitor and its spectrum of activity are known (for example WO 99/24433) and are commercially available under the name Levitra®.
  • Vardenafil hydrochloride may be administered orally and various oral dosage forms may be used such as, for example, tablets, hard gelatin capsules, soft gelatin capsules, powders, granules, chewable tablets or effervescent tablets.
  • Another administration option is fast-dissolving forms of oral administration. These can be taken by the patient quickly, discreetly and without fluid. These drug forms usually disintegrate in less than 3 minutes, preferably less than 1 minute in the mouth and the resulting solution or suspension is then swallowed. In the mouth quickly disintegrating dosage forms are therefore particularly suitable for patients who have trouble swallowing tablets.
  • the active ingredient can e.g. by coating the active ingredient, granules of active ingredient or coated
  • Aromas are easily masked or incorporated into a pleasant taste sensation.
  • Hydrochloride trihydrate - tablet differs. In particular, it comes to higher maximum plasma concentrations and the bioavailability of the active ingredient is higher than after administration of the commercial tablet. This can be reversed in patients who have been treated for a long time with commercial vardenafil hydrochloride trihydrate swallowing tablets and fast-dissolving tablets, or in patients who often switch between swallowing tablets and fast-disintegrating tablets, depending on their circumstances to be undesirable.
  • the rate of release of vardenafil is limited after administration of the rapid disintegration in the mouth. It has also been found that this limitation of drug release can be determined by measuring the dissolution rate of vardenafil in the USP Blattrritterapparatur in physiological saline at 37 0 C and 50 revolutions per minute and can be determined with this method of determination for the dosage form of the invention, a release rate, according to which no more than 50% of the dose may dissolve within the first 5 minutes.
  • vardenafil in the form of the vardenafil dihydrate or the anhydrous vardenafil.
  • Dä "s vardenafil dihydrate or anhydrous Vardenafil is processed according to one of the known methods for the preparation of pharmaceutical forms which rapidly disintegrate in the mouth as an active ingredient.
  • the disintegration time of the dosage form (method of the European Pharmacopoeia) shorter than 3 minutes, preferably shorter than 1 minute.
  • These dosage forms are prepared by mixing the active ingredient with sugars, sugar alcohols, disintegrants or other disintegration promoters, and other excipients such as surfactants, lubricants and lubricants. medium, flow control agents flavoring agents, dyes or fillers and compression produced on a tablet machine.
  • the anhydrous vardenafil or vardenafil dihydrate may be dissolved or suspended in an aqueous solvent together with adjuvants such as sugar alcohols, polymers or surfactants, and the solution or suspension is dosed into blister pots and subjected to a freeze-drying process.
  • anhydrous vardenafil or Vardena She dihydrate can be dissolved or suspended together with excipients such as film formers, plasticizers, flavoring and coloring agents in an organic solvent and processed into a film. Also a solvent-free film production with fusible film formulations is possible. After preparation, the films are cut to pieces corresponding to a single dose.
  • Another possibility for achieving the low dissolution rate of vardenafil in physiological saline solution according to the invention is the use of a salt of vardenafil with low water solubility.
  • the solubility of these salts and thus also the rate of dissolution can optionally be further suppressed by the addition of an equimolar addition.
  • a further possibility for achieving the slow dissolution rate of vardenafil in physiological saline solution according to the invention is to previously treat a water-soluble vardenafil salt in such a way that the release rate according to the invention is achieved.
  • coating the active substance salts with or embedding in polymers (n) is suitable for this purpose.
  • the vardenafil salts may be solvent-free or solvent-containing and in a different polymorphic form. Examples of water-soluble salts are vardenafil
  • phosphoric acid lactic acid, maleic acid, malic acid, phosphoric acid, lactobionic acid, malonic acid, naphthalenesulfonic acid, naphthalenedisulfonic acid or toluenesulfonic acid.
  • water soluble vardenafil salt (s) by co-processing vardenafil and acid in the dosage form.
  • the corresponding salt forms after access of aqueous medium in the mouth.
  • the release rate of the invention by coating or embedding with polymers can be achieved pH or time controlled.
  • physiologically acceptable polymers which are insoluble at neutral pH and are soluble at acidic pH, in particular basic butyl methacrylate copolymer (eg Eudragit ® E 100).
  • the time-controlled release is achieved by coating or embedding with physiologically acceptable polymers, by way of example and preferably with ethylcellulose.
  • To coat the active ingredient with polymer drug crystals, granules or pellets are coated with polymer solution or melt in a suitable apparatus and by suitable methods, such as in the fluidized bed or drum coater. Coating in spray-drying or spray-hardening processes is also possible. Coating of the active ingredient can also be achieved in a coacervation procedure. For embedding the active ingredient this is pressed together with polymer on a roller or tablet machine. Also, the joint precipitation of active ingredient and polymer in a Cooniacipitatvon are possible.
  • the polymer For processing the polymer preferably used poly (butyl methacrylate-co- (2-dimethyl-aminoethyl) methacrylate-co-methyl methacrylate) (Eudragit ® E 100), the polymer is dissolved either in acetone / isopropanol / water or it is an aqueous dispersion of fine milled substance which contains polymer and water as well as surfactants such as sodium lauryl sulfate and release agents such as magnesium stearate. The solution or dispersion thus obtained is sprayed onto the active substance-containing particles, for example a granulate.
  • fluidized bed processes are suitable, for example a coating in the Wurster tube or spraying in coaters.
  • a typical application amount is, for example, 1 mg of polymer per cm 2 surface area of the particles.
  • Another possibility for achieving the low dissolution rate in physiological saline solution according to the invention is the use of coarse particle size fractions of a Vardena tart salt, for example of Vardena tart hydrochloride trihydrate, in particular of Vardenafil Hydroc ⁇ orid trihydrate having an average particle size> 80 ⁇ m.
  • the particles can also be coated.
  • the vardenafil salt After the vardenafil salt has been pretreated in one of the described methods in such a way that the release rate according to the invention can be achieved, it is processed as an active ingredient according to one of the known methods for the preparation of dosage forms which disintegrate rapidly in the mouth.
  • the mixing of the pretreated active ingredient with sugars, sugar alcohols, disintegrants or other disintegration promoters and other excipients such as surfactants, lubricants, flow control agents flavoring agents, dyes or fillers and pressing on a tablet machine are suitable.
  • the pretreated vardenafil salt can be suspended together with excipients such as sugar alcohols, polymers or surfactants in an aqueous solvent, the suspension is metered into blister pots and subjected to a freeze-drying process. process.
  • the pretreated Vardena Stahl salt can be suspended together with adjuvants such as film formers, plasticizers, flavoring and coloring agents in an organic solvent and processed into a film. Also a solvent-free film production with fusible film formulations is possible. After preparation, the films are cut to pieces corresponding to a single dose.
  • tablets are prepared consisting of 23.7 mg Vardenaflu hydrochloride trihydrate, 0.748 mg yellow iron oxide, 0.102 mg red iron oxide, 1.02 mg apricot flavor, 0.17 mg neohesperidin dihydrochalcones, 3.40 mg aspartame 0,850 mg colloidal silicon dioxide, 4.25 mg of magnesium stearate and 135.76 mg of Pharmaburst ® (commercially available mixture of SPI) are made.
  • the drug release in 900 ml of physiological saline at 37 ° C and 50 rpm in the USP paddle stirrer apparatus is 85% in 5 minutes. Thus, the dissolution rate criterion according to the invention is not fulfilled.
  • Example 2 Evidence of approximately matching bioavailability of a erfmdungs-
  • An orally disintegrating tablet consisting of 10.7 mg vardenafildihydrate (equivalent to 10 mg vardenafil), 0.484 mg yellow iron oxide, 0.066 mg red iron oxide, 1.1 mg apricot flavor, 4.4 mg aspartame, 6.6 mg magnesium stearate and 196.65 mg Pharmaburst ® B2 (commercial excipient mixture from SPI) is prepared by vardenafil dihydrate, yellow iron oxide, red iron oxide, apricot flavor, aspartame, and pharmaceutical burst ® are mixed in a forced mixer, and this mixture is subsequently mixed with magnesium stearate in a free fall mixer.
  • the area under the plasma concentration time curve was used, which was 34.9 ⁇ g * h / L for the tablet according to the invention and 35.7 ⁇ g * h / L for the reference tablet (respectively geometric mean).
  • the maximum plasma concentration of the tablets according to the invention could be limited to 79% of the reference tablet.
  • Example 3 Evidence of approximately matching bioavailability of a rapid disintegrating tablet according to the invention with a swallowing tablet
  • Pharmaburst ® B2 (commercially available Hüfsstoffmischung - SPI) and sprayed 44.8 g of aspartame. The granulate is dried in a fluidized bed and with 2714 g Pharmaburst® ® B2
  • anhydrous Vardenafil is mixed commercially available with 24.7 g orange flavoring, 49.4 g of aspartame and 4563 g Pharmaburst® ® B2 (excipient mixture from SPI, sieved mm 0.5, mixed again and dry granulated on a roller.
  • the granules are 24.7 g fumed Silicon dioxide and 148.2 g of magnesium stearate are added and mixed in a free-fall mixer for 5 minutes.
  • the mixture is compressed on a tablet machine into tablets having a mass of 380 mg.
  • the rapidly disintegrating tablets meet the dissolution rate criterion according to the invention, since in 900 ml physiological Saline at 37 ° C within 5 minutes, only about 26% of the applied dose will be released.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Zoology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne de nouvelles formulations pharmaceutiques du Vardénafil qui se dissolvent rapidement dans la bouche et présentent une biodisponibilité contrôlée. Cette invention se rapporte en outre à des procédés de production de ces formulations.
EP06707140A 2005-03-01 2006-02-22 Formes galeniques presentant une biodisponibilite controlee Withdrawn EP1855687A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP10177166A EP2255810A1 (fr) 2005-03-01 2006-02-22 Formes galéniques comprenant du vardenafil et présentant une biodisponibilité contrôlée

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102005009241A DE102005009241A1 (de) 2005-03-01 2005-03-01 Arzneiformen mit kontrollierter Bioverfügbarkeit
PCT/EP2006/001573 WO2006092222A1 (fr) 2005-03-01 2006-02-22 Formes galeniques presentant une biodisponibilite controlee

Publications (1)

Publication Number Publication Date
EP1855687A1 true EP1855687A1 (fr) 2007-11-21

Family

ID=36178023

Family Applications (2)

Application Number Title Priority Date Filing Date
EP10177166A Withdrawn EP2255810A1 (fr) 2005-03-01 2006-02-22 Formes galéniques comprenant du vardenafil et présentant une biodisponibilité contrôlée
EP06707140A Withdrawn EP1855687A1 (fr) 2005-03-01 2006-02-22 Formes galeniques presentant une biodisponibilite controlee

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP10177166A Withdrawn EP2255810A1 (fr) 2005-03-01 2006-02-22 Formes galéniques comprenant du vardenafil et présentant une biodisponibilité contrôlée

Country Status (5)

Country Link
US (1) US20090017122A1 (fr)
EP (2) EP2255810A1 (fr)
CA (1) CA2599649C (fr)
DE (1) DE102005009241A1 (fr)
WO (1) WO2006092222A1 (fr)

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DE102007027067A1 (de) 2007-06-12 2008-12-18 Ratiopharm Gmbh Verfahren zur Herstellung eines Arzneimittels enthaltend Vardenafil Hydrochlorid Trihydrat
EP2205213A2 (fr) * 2007-10-01 2010-07-14 Laboratorios Lesvi, S.L. Comprimés orodispersibles
US9629806B2 (en) 2008-07-21 2017-04-25 Si Group, Inc. High content sodium ibuprofen granules, their preparation and their use in preparing non-effervescent solid dosage forms
DE102009020888A1 (de) 2009-05-12 2010-11-18 Ratiopharm Gmbh Schmelztablette, enthaltend ein Vardenafil-Salz
PL390079A1 (pl) * 2009-12-30 2011-07-04 Zakłady Farmaceutyczne POLPHARMA Spółka Akcyjna Sposób otrzymywania wardenafilu i jego izolacji jako soli z kwasem cytrynowym oraz krystaliczna postać tej soli
CA2894272A1 (fr) * 2012-12-14 2014-06-19 Si Group, Inc. Granules d'ibuprofene sodique a teneur elevee, leur preparation et leur utilisation dans la preparation de formes posologiques solides non effervescentes
SG10201808645TA (en) * 2013-12-16 2018-11-29 Massachusetts Inst Technology Fortified Micronutrient Salt Formulations
EP3142640A1 (fr) * 2014-05-16 2017-03-22 Vivus, Inc. Forme dosifiée à désintégration par voie orale pour l'administration d'avanafil, et procédés associés de fabrication et d'utilisation
BR112022024098A2 (pt) * 2020-05-26 2023-02-07 Strategic Drug Solutions Inc Formulações e métodos para tratar a disfunção erétil
WO2025048919A1 (fr) * 2023-08-30 2025-03-06 Dow Global Technologies Llc Mélanges d'excipients séchés par pulvérisation

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WO2004012702A1 (fr) * 2002-08-05 2004-02-12 Pfizer Health Ab Formulations pharmaceutiques a delai d'action rapide contenant un compose pour le dysfonctionnement sexuel contenant de la poudre de cacao et utilisation
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WO2005110419A1 (fr) * 2004-05-11 2005-11-24 Bayer Healthcare Ag Formulations a liberation controlee contenant du vardenafil
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Non-Patent Citations (1)

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Title
See also references of WO2006092222A1 *

Also Published As

Publication number Publication date
US20090017122A1 (en) 2009-01-15
CA2599649C (fr) 2013-11-12
EP2255810A1 (fr) 2010-12-01
WO2006092222A1 (fr) 2006-09-08
CA2599649A1 (fr) 2006-09-08
DE102005009241A1 (de) 2006-09-07

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