WO2000007597A1 - Systeme de traitement transmuqueux pour l'utilisation de sildenafil - Google Patents

Systeme de traitement transmuqueux pour l'utilisation de sildenafil Download PDF

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Publication number
WO2000007597A1
WO2000007597A1 PCT/EP1999/005465 EP9905465W WO0007597A1 WO 2000007597 A1 WO2000007597 A1 WO 2000007597A1 EP 9905465 W EP9905465 W EP 9905465W WO 0007597 A1 WO0007597 A1 WO 0007597A1
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WO
WIPO (PCT)
Prior art keywords
therapeutic system
sildenafil
sodium
transmucosal therapeutic
cyclodextrin
Prior art date
Application number
PCT/EP1999/005465
Other languages
German (de)
English (en)
Inventor
Thomas Strüngmann
Original Assignee
Hexal 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 Hexal Ag filed Critical Hexal Ag
Priority to AU52898/99A priority Critical patent/AU5289899A/en
Publication of WO2000007597A1 publication Critical patent/WO2000007597A1/fr

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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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/0043—Nose
    • 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
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin

Definitions

  • the invention relates to an active substance-containing transmucosal system for the use of sildenafil or its pharmaceutically acceptable salts.
  • Sildenafil [1- (4-ethoxy-3- (6,7-dihydro-1-methyl-7-oxo-3-propyl 1H-pyazolo (4,3-d) pyrimidin-5-yl) phenylsulfonyl) -4-methyl piperazin] is a very selective cyclic guanosine monophosphate (cGMP) -specific phosphodiesterase (PDE) type 5 inhibitor, which was developed for the treatment of both organic and psychological impotence.
  • cGMP cyclic guanosine monophosphate
  • PDE phosphodiesterase
  • the active ingredient sildenafil is known only in the form of an orally administered tablet with an active ingredient content of 25 mg, 50 mg or 100 mg, the bioavailability being only 40%.
  • the active substance content normally administered is 50 mg, with max. one tablet may be taken once a day.
  • the tablet should be taken at least one hour to show its therapeutic effect, and 1.5 hours before consumption if fatty foods are consumed beforehand.
  • the patient's sexual behavior is therefore somewhat spontaneous, which is a very considerable limitation for them.
  • taking this active ingredient is sometimes an insurmountable hurdle.
  • the object of the invention is to provide a transmucosal therapeutic system for the use of sildenafil or its pharmaceutically acceptable salts, the disadvantages of the oral dosage form being avoided and patient compliance being improved.
  • sildenafil or its pharmaceutically active salts are so effectively absorbed by the mucous membranes that a therapeutically effective blood plasma level is reached very quickly without causing irritation to the mucous membranes.
  • the rapid and complete absorption through the mucous membrane achieves the same therapeutic effect as with the oral dosage form, only much faster and without causing the frequently occurring side effects.
  • the active ingredient has a direct systemic effect, which considerably increases the bioavailability and reduces the amount of the dosage.
  • Patient compliance is also improved because the difficulties that may arise when taking tablets are avoided and the freedom and spontaneity in love life is guaranteed by the immediate attainment of a therapeutically effective blood plasma level.
  • transmucosal therapeutic system containing sildenafil or its pharmaceutically acceptable salts.
  • Possible addition salts are acid addition salts such as Hydrochloride or the halides, sulfates, phosphates, citrate acetates, maleates, succinates, ascorbates and carbonates in question.
  • Sildenafil or its pharmaceutically acceptable salts can also be used in combination with other known active compounds, especially specific and non-specific cytochrome P450 (C YP) inhibitors.
  • C YP cytochrome P450
  • sildenafil By combining sildenafil with a CYP inhibitor such as erythromycin, cimetidine, ketoconazole, itraconazole or mibefradil, the concentration in the blood plasma is increased and the breakdown or excretion is delayed. The rapid flooding is thus maintained or accelerated with a reduced amount of sildenafil.
  • a CYP inhibitor such as erythromycin, cimetidine, ketoconazole, itraconazole or mibefradil
  • the transmucosal therapeutic system addresses the nasal, buccal and rectal mucous membranes, the buccal and nasal mucous membranes being more permeable.
  • the transmucosal therapeutic system according to the invention which is used for nasal administration, can be in the form of sprays (solution and suspension), drops, gels, powders or creams.
  • Propellant and pump sprays can be used as spray forms.
  • the transmucosal therapeutic system according to the invention which is used for buccal administration, can be in the form of sprays (solution and suspension), lozenges, lozenges, tablets or wafers adhering to the oral mucosa and chewing gum.
  • the transmucosal therapeutic system according to the invention which is used for rectal administration, can be in the form of a suppository, the additives corresponding to the prior art, e.g. Hard fat and phospholipids are used.
  • the solutions or suspensions according to the invention used for nasal and / or buccal administration can be present as an aqueous system or as a liposome system or as an almost anhydrous oily system.
  • constituents of the nasal and / or buccal dosage forms can be solubilizers, antioxidants, preservatives, humectants, gelling agents, buffers and flavoring or flavoring agents as well as other customary auxiliaries.
  • Suitable solubilizers can glycol, ethanol, isopropanol, propylene glycol, Polyetyhlenglycol, Transcutol, medium chain glycerides, Genapol®, sodium dodecyl sulfate, sodium cetylstearyl sulfate, sodium dioctyl sulfosuccinate, cetyl stearyl alcohol, cetyl alcohol, stearyl alcohol, cholesterol, sorbitan monooleate, sorbitan monopalmitate, sorbitan monostearate, sorbitan trioleate, sorbitan tristearate, sorbitan monolaurate, polysorbate 20 , Polysorbate 60, polysorbate 80, polysorbate 40, macrogol 1500 glycerol triricinnoleate, macrogol glycerol hydroxystearate, macrogol 1000 glycerol monolaurate, macrogol
  • Lysophosphatidylcholine lysophosphatidylglycerol, phosphatidylethanolamine
  • Phosphatidylserine, phosphatidylinositol (ol) e, spingophospholipids and / or labrosol can be used.
  • antioxidants sodium metabisulfate, sodium bisulfate, ⁇ -tocopherol, ⁇ -tocopherol ester ( ⁇ -tocopherol propylene glycol succinate, ⁇ -tocopherol acetate, ⁇ -tocopherol succinate), ascorbic acid, ascorbic acid ester (myristate, palmitate and ß-stearate), Carotene, cysteine, acetylcysteine, folic acid (vitamin B 2 group), phytic acid, ice and / or trans-urocanoic acid, carnosine (N-ß-alanine-L-histidine), histidine, flavones, flavonoids, lycopene, tyrosine, Gluthation, glutation ester, ⁇ -lipoic acid, ubiquinone, nordihydroguaiaretic acid (NDGA), gallic acid ester (ethyl, propyl, octyl, dodecyl
  • Paraben, benzalkonium chloride, chlorobutanol and benzyl alcohol can be added in small quantities as preservatives against bacteria.
  • glycerin, sorbitol, dextran and mannitol can be added as humectants.
  • the better localization of the transmucosal system is achieved by adding gelling agents such as methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, carbopol, gelatin, agar-agar, alginate, tragacanth, xanthan and polyvinyl alcohol.
  • gelling agents such as methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, carbopol, gelatin, agar-agar, alginate, tragacanth, xanthan and polyvinyl alcohol.
  • sweeteners, aromatic oils and flavoring agents can be added as taste enhancers, e.g. Cyclamate, saccharin, aspartame, peppermint oil, fennel oil, caramel, vanilla, raspberry, forest berry, orange, cherry, lemon, strawberry, lime and multivitamin aroma.
  • taste enhancers e.g. Cyclamate, saccharin, aspartame, peppermint oil, fennel oil, caramel, vanilla, raspberry, forest berry, orange, cherry, lemon, strawberry, lime and multivitamin aroma.
  • the pH of an aqueous transmucosal system is between 3 and 8, in particular between 4.5 and 6.5.
  • the aqueous transmucosal system can optionally be present as an isotonic solution with a maximum concentration of sodium chloride of 0.462M.
  • glucose can also be added to achieve isotonicity.
  • the osmotic pressure of the aqueous transmucosal system can be between 150 and 850 milliosmoles (mOsm), in particular between 200-400 mOsm.
  • the transmucosal therapeutic system has an active substance content that is between 1-100 mg / dose.
  • 0.9 g of sodium chloride are dissolved in 94.1 g of water with 5 g of sildenafil citrate (corresponding to 3.44 g of sildenafil).
  • sildenafil citrate corresponding to 3.44 g of sildenafil.
  • 0.9 ml of a 1% benzalkonium chloride solution are added to the mixture and adjusted to a pH of 4.5 with 1N HCl.
  • sildenafil citrate (equivalent to 100 mg of sildenafil) are dissolved in 50 ml of water.
  • 480 mg of the starch microspheres are dispersed in 20 ml of the sildenafil citrate solution and 12 ml of water are added.
  • the suspension obtained is stirred for one hour and then freeze-dried to obtain a powder formulation. This powder is applied intranasally.
  • Paraben solution 2.4 g of methyl p-oxybenzoate and 600 mg of propyl p-oxybenzoate are dissolved in 2000 ml of water at a temperature of 80 ° C.
  • a suitable vessel which is equipped with a mixer and a heating spiral, 4 liters of purified water are heated to a temperature of 80 ° C. 10 g of nipagin and 1 g of EDTA disodium are dissolved in this solution with stirring and then cooled to room temperature. Then 500 g of sildenafil citrate (corresponding to 356 g of sildenafil) are dissolved and the entire solution is adjusted to a pH of 6.5 with 5% tromethamine solution. In a separate vessel, 200 g of glycerin are mixed with 10 g of Carbopol 940 until a homogeneous dispersion of the glycerin has formed. Then 4 l of water are added and the mixture is stirred until the polymer is completely hydrated. The two solutions are combined and filled with the remaining 21 water.
  • This solution is placed in a bottle with a metered dose aerosol device or in a
  • Compressed gas pack or filled into a nasal drop bottle Compressed gas pack or filled into a nasal drop bottle.
  • 0.9 g of sodium chloride are dissolved in 89.1 g of water with 5 g of sildenafil citrate (corresponds to 3.44 g of sildenafil) and 5 g of dexpanthenol.
  • sildenafil citrate corresponds to 3.44 g of sildenafil
  • dexpanthenol 5 g
  • 0.9 ml of a 1% benzalkonium chloride solution are added to the mixture and adjusted to a pH of 5.5 with 1N HCl.
  • sildenafil (corresponds to 3.44 g of sildenafil) are dissolved in 95 g of a (vegetable) oil that is liquid at room temperature.
  • This active substance-containing, oily solution can be applied either by spray or in the form of nose drops.
  • sildenafil citrate (corresponds to 6.88 g sildenafil), 1 g EDTA disodium, 0.9 g sodium chloride and 3 g hydroxymethyl cellulose are processed with 85.1 g water to a homogeneous solution. Then the pH is adjusted to 6.5 with anhydrous citric acid and buffered with Na 2 HPO 4 . The solution can be applied as a nasal spray or in the form of nasal drops.
  • composition is used to prepare 1000 tablets (240 mg, 50 mg sildenafil) adhering to the oral mucosa:
  • Sildenafil citrate 140.45 mg (corresponds to 100 mg sildenafil) highly disperse silicon dioxide 121.40 mg

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Gynecology & Obstetrics (AREA)
  • Otolaryngology (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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Abstract

L'invention concerne un système de traitement transmuqueux renfermant du sildenafil ou un de ses sels pharmaceutiquement acceptables.
PCT/EP1999/005465 1998-07-31 1999-07-30 Systeme de traitement transmuqueux pour l'utilisation de sildenafil WO2000007597A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU52898/99A AU5289899A (en) 1998-07-31 1999-07-30 Transmucosal therapeutic system for administering sildenafil

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19834506A DE19834506A1 (de) 1998-07-31 1998-07-31 Transmucosales therapeutisches System zur Anwendung von Sildenafil
DE19834506.2 1998-07-31

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WO2000007597A1 true WO2000007597A1 (fr) 2000-02-17

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PCT/EP1999/005465 WO2000007597A1 (fr) 1998-07-31 1999-07-30 Systeme de traitement transmuqueux pour l'utilisation de sildenafil

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AU (1) AU5289899A (fr)
DE (1) DE19834506A1 (fr)
WO (1) WO2000007597A1 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001035926A2 (fr) * 1999-11-18 2001-05-25 Natco Pharma Limited Composition pharmaceutique amelioree pour traiter la dyserection masculine
WO2001041807A2 (fr) * 1999-12-10 2001-06-14 Vivus, Inc. Administration a travers les muqueuses d'inhibiteurs de la phosphodiesterase dans le traitement de la dyserection
US6403597B1 (en) 1997-10-28 2002-06-11 Vivus, Inc. Administration of phosphodiesterase inhibitors for the treatment of premature ejaculation
JP2010241843A (ja) * 2002-08-29 2010-10-28 Novadel Pharma Inc 心血管薬剤または腎臓薬剤を含む口腔内用極性および非極性スプレーまたはカプセル
EP2575765A2 (fr) * 2010-06-07 2013-04-10 Novadel Pharma Inc. Formulations pour pulvérisation orale et méthodes d'administration de sildenafil
US9186321B2 (en) 2011-12-05 2015-11-17 Suda Ltd. Oral spray formulations and methods for administration of sildenafil

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BRPI0003386B8 (pt) 2000-08-08 2021-05-25 Cristalia Produtos Quim Farmaceuticos Ltda pró-droga homo ou heterodiméricas úteis no tratamento de doenças ou disfunções mediadas por fosfodiesterases; composições farmacêuticas contendo a pró-droga ou seus sais farmacêuticos aceitáveis; processo de obtenção destas pró-drogas
CA2425539C (fr) * 2000-10-12 2007-04-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Monohydrate cristallin, procedes permettant sa preparation et son utilisation pour la preparation d'une composition pharmaceutique
EP1404336A1 (fr) * 2001-06-14 2004-04-07 Sampad Bhattacharya Compositions comprenant un inhibiteur de cgmp pde5 pour administration transdermique au tissu erectile du penis
US20060035905A1 (en) * 2004-02-06 2006-02-16 Becton, Dickinson And Company Formulations of phosphodiesterase 5 inhibitors and methods of use
CN100463668C (zh) * 2005-05-09 2009-02-25 凌沛学 可逆性热凝胶化水性药物组合物
GB0606234D0 (en) * 2006-03-29 2006-05-10 Pliva Istrazivanje I Razvoj D Pharmaceutically acceptable salts and polymorphic forms
WO2008019106A1 (fr) * 2006-08-04 2008-02-14 Artesian Therapeutics, Inc. Méthodes et compositions pour le traitement d'hypertension pulmonaire utilisant une combinaison d'un agent bloquant de canal calcium et un inhibiteur de phosphodiestérase
US20100104624A1 (en) * 2008-06-11 2010-04-29 Peter Langecker Combination therapy using phosphodiesterase inhibitors
GB2497933B (en) * 2011-12-21 2014-12-24 Londonpharma Ltd Drug delivery technology

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Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6403597B1 (en) 1997-10-28 2002-06-11 Vivus, Inc. Administration of phosphodiesterase inhibitors for the treatment of premature ejaculation
US6548490B1 (en) 1997-10-28 2003-04-15 Vivus, Inc. Transmucosal administration of phosphodiesterase inhibitors for the treatment of erectile dysfunction
WO2001035926A2 (fr) * 1999-11-18 2001-05-25 Natco Pharma Limited Composition pharmaceutique amelioree pour traiter la dyserection masculine
WO2001035926A3 (fr) * 1999-11-18 2001-12-27 Natco Pharma Ltd Composition pharmaceutique amelioree pour traiter la dyserection masculine
WO2001041807A2 (fr) * 1999-12-10 2001-06-14 Vivus, Inc. Administration a travers les muqueuses d'inhibiteurs de la phosphodiesterase dans le traitement de la dyserection
WO2001041807A3 (fr) * 1999-12-10 2002-02-14 Vivus Inc Administration a travers les muqueuses d'inhibiteurs de la phosphodiesterase dans le traitement de la dyserection
JP2010241843A (ja) * 2002-08-29 2010-10-28 Novadel Pharma Inc 心血管薬剤または腎臓薬剤を含む口腔内用極性および非極性スプレーまたはカプセル
EP2575765A2 (fr) * 2010-06-07 2013-04-10 Novadel Pharma Inc. Formulations pour pulvérisation orale et méthodes d'administration de sildenafil
EP2575765A4 (fr) * 2010-06-07 2014-08-27 Suda Ltd Formulations pour pulvérisation orale et méthodes d'administration de sildenafil
US9186321B2 (en) 2011-12-05 2015-11-17 Suda Ltd. Oral spray formulations and methods for administration of sildenafil

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DE19834506A1 (de) 2000-02-03

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