US20070020186A1 - Solid dosage formulations of narcotic drugs having improved buccal adsorption - Google Patents
Solid dosage formulations of narcotic drugs having improved buccal adsorption Download PDFInfo
- Publication number
- US20070020186A1 US20070020186A1 US11/186,925 US18692505A US2007020186A1 US 20070020186 A1 US20070020186 A1 US 20070020186A1 US 18692505 A US18692505 A US 18692505A US 2007020186 A1 US2007020186 A1 US 2007020186A1
- Authority
- US
- United States
- Prior art keywords
- solid dosage
- fentanyl
- formulations according
- dosage formulations
- narcotic
- 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.)
- Abandoned
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
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
-
- 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
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
-
- 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
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Definitions
- the present invention concerns solid dosage formulations of narcotic drugs having improved buccal adsorption.
- the formulations of the invention are characterized by the introduction in a buccal formulation of a soluble organic compound having a primary, secondary or tertiary amine group.
- buccal formulations are more and more popular for drug administrations. They exhibit in fact several advantages in comparison with other solid dosage forms; in particular, buccal formulations dissolve in the oral cavity without requiring water for ingestion, allowing the buccal adsorption of drugs coming into contact with the oral mucosa in dissolved form. Sometimes, buccal administration does not unfortunately always allow to obtain a fast onset of action of the drug, as the result of difficulties of the drug to cross the skin barrier of mucosa and to penetrate into the blood stream.
- the amount of amine required in the formulation ranges between 0.1 to 500% of the moles of active component(s), more preferably 0.5 to 300% and most preferably 1 to 200%.
- amines used in order to improve bioavailability according to the invention include Histidine, Arginine, Lysine, Triethanolamine, Trimethylamine, Betaine, Pyrrolidine, Guanidine, Cysteamine, Taurine and derivatives and analogues thereof.
- Arginine is a preferred non-toxic amine.
- Oral dispersible tablets containing 200 mcg of Fentanyl were obtained as follows:
- a pharmacokinetic study was carried out on 6 fasting healthy volunteers treated with a buccal formulation prepared in accordance with example # 1A containing 200 mcg of Fentanyl. The results were compared with a pharmacokinetic study carried out on 6 healthy volunteers treated with a buccal formulation prepared in accordance with example # 1B containing 400 mcg of Fentanyl.
Abstract
The present invention provides solid dosage formulations of narcotic drugs with improved buccal adsorption. These improved characteristics are provided by the combination of the narcotic drug with an additional non-toxic soluble organic compound. The soluble organic compound contains a primary, secondary or tertiary amine group. The addition of this organic compound favorably alters the kinetics of mucosal penetration such that mucosal penetration times are decreased. This provides for a faster onset of action of the drug.
Description
- The present invention concerns solid dosage formulations of narcotic drugs having improved buccal adsorption.
- The formulations of the invention are characterized by the introduction in a buccal formulation of a soluble organic compound having a primary, secondary or tertiary amine group.
- Buccal formulations are more and more popular for drug administrations. They exhibit in fact several advantages in comparison with other solid dosage forms; in particular, buccal formulations dissolve in the oral cavity without requiring water for ingestion, allowing the buccal adsorption of drugs coming into contact with the oral mucosa in dissolved form. Sometimes, buccal administration does not unfortunately always allow to obtain a fast onset of action of the drug, as the result of difficulties of the drug to cross the skin barrier of mucosa and to penetrate into the blood stream.
- Surprisingly, it has been found that adding a non-toxic amine to a buccal formulation, the penetration capacity of drugs is significantly improved, allowing to reach an higher and earlier blood concentration of drugs in comparison with formulations without amines.
- The amount of amine required in the formulation ranges between 0.1 to 500% of the moles of active component(s), more preferably 0.5 to 300% and most preferably 1 to 200%.
- Examples of amines used in order to improve bioavailability according to the invention include Histidine, Arginine, Lysine, Triethanolamine, Trimethylamine, Betaine, Pyrrolidine, Guanidine, Cysteamine, Taurine and derivatives and analogues thereof. Arginine is a preferred non-toxic amine.
- Examples of active components that may be advantageously formulated in solid dosage form according to the invention include:
- Alfentanil, Buprenorphine Butorphanol, Codeine, Diphenoxylate, Fentanyl, Heroin, Hydrocodone, Hydromorphone, Oxymorphone, Levophanol, Levallorphan, Loperamide, Meperidine, Morfine, Nalbuphine, Nalmefene, Nalorphine, Naloxone, Naltrexone, Remifentanyl, Sufentanil. Fentanyl is preferred.
- The invention is illustrated by the following Examples:
- Preparation of a Oral Dispersible Tablet Containing Amine (Arginine)
- Oral dispersible tablets containing 200 mcg of Fentanyl were obtained as follows:
- A) 1.05 g of Fentanyl and 50 g of PEG 600 were dissolved into 90 g of purified water.
- B) 335.62 g of Sorbitol, 516.67 g of Mannitol, 26.67 g of aspartame and 10 g of Citric acid, were granulated together with a water solution containing PEG and Fentanyl citrate.
- C) At the end of granulation and drying, 43.33 g of arginine free base and 16.67 g of magnesium stearate were added.
- D) The product was blended until homogeneity and compressed in toroidal tablets having a diameter of 10 mm and weighing 300 mg each
- Preparation of an Oral Dispersable Tablet without Amine (Arginine)
- Oral dispersible tablets containing 400 mcg of Fentanyl have been obtained as follows:
- E) 2.1 g of Fentanyl and 50 g of PEG 600 was dissolved into 90 g of purified water.
- F) 455.62 g of Sorbitol, 455.62 g of Mannitol, 26.67 g of aspartame and 10 g of Citric acid, were granulated together with a water solution containing PEG and Fentanyl citrate.
- G) The product was blended until homogeneity and compressed in toroidal tablets having a diameter of 10 mm and weighing 300 mg each
- A pharmacokinetic study was carried out on 6 fasting healthy volunteers treated with a buccal formulation prepared in accordance with example # 1A containing 200 mcg of Fentanyl. The results were compared with a pharmacokinetic study carried out on 6 healthy volunteers treated with a buccal formulation prepared in accordance with example # 1B containing 400 mcg of Fentanyl.
- The results are reported in the following Table:
Fentanyl strength per dosage Tmax Cmax AUC Example # 1A 200 mcg 48 minutes 496 pg/mL 2430 Example # 1B 400 mcg 35 minutes 491 pg/mL 3331 - Despite the dose of Fentanyl administered in the tablets described in example # 1A (200 mcg) is 50% of the dose described in example #1B (400 mcg), the pharmacokinetic parameters are similar, demonstrating a dramatic improvement of the Fentanyl bioavailability for the formulation of the invention.
Claims (6)
1. Solid dosage formulations of narcotic drugs in form of buccal tablets characterized by containing a non toxic amine.
2. Formulations according to claim 1 , wherein the non-toxic amine is selected from Histidine, Arginine, Lysine, Triethanolamine, Trimethylamine, Betaine, Pyrrolidine, Guanidine, Cysteamine, Taurine and derivatives and analogues thereof.
3. Formulations according to claim 2 wherein the non-toxic amine is arginine.
4. Formulations according to claim 1 wherein the non-toxic amine is present in amounts ranging between 0.1 to 500% of the moles of active component(s), more preferably 0.5 to 300% and most preferably 1 to 200%.
5. Formulations according to claim 1 wherein the narcotic drug is selected from Alfentanil, Buprenorphine, Butorphanol, Codeine, Diphenoxylate, Fentanyl, Heroin, Hydrocodone, Hydromorphone, Oxymorphone, Levophanol, Levallorphan, Loperamide, Meperidine, Morfine, Nalbuphine, Nalmefene, Nalorphine, Naloxone, Naltrexone, Remifentanyl, Sufentanil.
6. Formulations according to claim 5 wherein the active ingredient is Fentanyl.
Priority Applications (28)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US11/186,925 US20070020186A1 (en) | 2005-07-22 | 2005-07-22 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
ES06776336.7T ES2569228T3 (en) | 2005-07-22 | 2006-07-21 | Formulations of solid pharmaceutical forms of fentanyl that have better oral adsorption |
NZ563511A NZ563511A (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narocotic drugs having improved buccal adsorption |
PL06776336T PL1906961T3 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of fentanyl having improved buccal adsorption |
TW095126670A TW200727922A (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
UAA200713973A UA90518C2 (en) | 2005-07-22 | 2006-07-21 | Pharmaceutical composition in the form of a tablet suitable for dissolution in the buccal cavity, comprising a narcotic active ingredient and amine |
CA2607360A CA2607360C (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
US11/490,500 US8574552B2 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
RU2007149044/15A RU2408373C2 (en) | 2005-07-22 | 2006-07-21 | Solid dosage forms of narcotic drugs of enhanced absorption in transbuccal administration |
JP2008521904A JP5714797B2 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulation of anesthetic with improved absorption in the oral cavity |
KR1020087000576A KR101326206B1 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
CNA2006800232888A CN101208091A (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
AU2006271870A AU2006271870B2 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
RS20160214A RS54670B1 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of fentanyl having improved buccal adsorption |
PCT/EP2006/007189 WO2007009806A2 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
EP06776336.7A EP1906961B1 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of fentanyl having improved buccal adsorption |
HUE06776336A HUE027354T2 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of fentanyl having improved buccal adsorption |
SI200632040A SI1906961T1 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of fentanyl having improved buccal adsorption |
DK06776336.7T DK1906961T3 (en) | 2005-07-22 | 2006-07-21 | FIXED DOSAGE FORMS OF FENTANYL WITH IMPROVED BUCHAL ADSORPTION |
BRPI0613769-5A BRPI0613769A2 (en) | 2005-07-22 | 2006-07-21 | solid narcotic drug dosage formulations having improved buccal adsorption |
MX2007015480A MX2007015480A (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption. |
IL187387A IL187387A (en) | 2005-07-22 | 2007-11-15 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
ZA200710406A ZA200710406B (en) | 2005-07-22 | 2007-11-30 | Solid dosage formulations of narcotic drugs having improved buccal absorption |
NO20080827A NO20080827L (en) | 2005-07-22 | 2008-02-15 | Solid dosage formulations of narcotic drugs that have improved buccal adsorption |
MA30659A MA29744B1 (en) | 2005-07-22 | 2008-02-18 | SOLID DOSAGE FORMULATIONS OF MEDICAMENTS HAVING IMPROVED ORAL ADSORPTION |
US14/017,642 US10258693B2 (en) | 2005-07-22 | 2013-09-04 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
HRP20160327TT HRP20160327T1 (en) | 2005-07-22 | 2016-04-01 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
CY20161100346T CY1117470T1 (en) | 2005-07-22 | 2016-04-26 | SOLID DOSAGE PREPARATIONS WITH IMPROVED ANIMAL ADJUSTMENT |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US11/186,925 US20070020186A1 (en) | 2005-07-22 | 2005-07-22 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US11/490,500 Continuation-In-Part US8574552B2 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
Publications (1)
Publication Number | Publication Date |
---|---|
US20070020186A1 true US20070020186A1 (en) | 2007-01-25 |
Family
ID=37440618
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US11/186,925 Abandoned US20070020186A1 (en) | 2005-07-22 | 2005-07-22 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
US11/490,500 Active 2028-10-01 US8574552B2 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
US14/017,642 Active US10258693B2 (en) | 2005-07-22 | 2013-09-04 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
Family Applications After (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US11/490,500 Active 2028-10-01 US8574552B2 (en) | 2005-07-22 | 2006-07-21 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
US14/017,642 Active US10258693B2 (en) | 2005-07-22 | 2013-09-04 | Solid dosage formulations of narcotic drugs having improved buccal adsorption |
Country Status (26)
Country | Link |
---|---|
US (3) | US20070020186A1 (en) |
EP (1) | EP1906961B1 (en) |
JP (1) | JP5714797B2 (en) |
KR (1) | KR101326206B1 (en) |
CN (1) | CN101208091A (en) |
AU (1) | AU2006271870B2 (en) |
BR (1) | BRPI0613769A2 (en) |
CA (1) | CA2607360C (en) |
CY (1) | CY1117470T1 (en) |
DK (1) | DK1906961T3 (en) |
ES (1) | ES2569228T3 (en) |
HR (1) | HRP20160327T1 (en) |
HU (1) | HUE027354T2 (en) |
IL (1) | IL187387A (en) |
MA (1) | MA29744B1 (en) |
MX (1) | MX2007015480A (en) |
NO (1) | NO20080827L (en) |
NZ (1) | NZ563511A (en) |
PL (1) | PL1906961T3 (en) |
RS (1) | RS54670B1 (en) |
RU (1) | RU2408373C2 (en) |
SI (1) | SI1906961T1 (en) |
TW (1) | TW200727922A (en) |
UA (1) | UA90518C2 (en) |
WO (1) | WO2007009806A2 (en) |
ZA (1) | ZA200710406B (en) |
Cited By (13)
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US20070207207A1 (en) * | 2006-01-06 | 2007-09-06 | Acelrx Pharmaceuticals, Inc. | Bioadhesive drug formulations for oral transmucosal delivery |
US20070260491A1 (en) * | 2006-05-08 | 2007-11-08 | Pamela Palmer | System for delivery and monitoring of administration of controlled substances |
US20070299687A1 (en) * | 2006-06-23 | 2007-12-27 | Pamela Palmer | Inpatient system for patient-controlled delivery of oral transmucosal medications dosed as needed |
US20080147044A1 (en) * | 2006-01-06 | 2008-06-19 | Acelrx Pharmaceuticals, Inc. | Methods for administering small volume oral transmucosal dosage forms using a dispensing device |
US20080164275A1 (en) * | 2007-01-05 | 2008-07-10 | Acelrx Pharmaceuticals, Inc. | Storage and dispensing devices for administration of oral transmucosal dosage forms |
US20090131479A1 (en) * | 2006-01-06 | 2009-05-21 | Acelrx Pharmaceuticals, Inc. | Small-volume oral transmucosal dosage |
US8252329B2 (en) | 2007-01-05 | 2012-08-28 | Acelrx Pharmaceuticals, Inc. | Bioadhesive drug formulations for oral transmucosal delivery |
US8357114B2 (en) | 2006-01-06 | 2013-01-22 | Acelrx Pharmaceuticals, Inc. | Drug dispensing device with flexible push rod |
US8535714B2 (en) | 2006-01-06 | 2013-09-17 | Acelrx Pharmaceuticals, Inc. | Small volume oral transmucosal dosage forms containing sufentanil for treatment of pain |
US8753308B2 (en) | 2006-01-06 | 2014-06-17 | Acelrx Pharmaceuticals, Inc. | Methods for administering small volume oral transmucosal dosage forms using a dispensing device |
US8865743B2 (en) | 2006-01-06 | 2014-10-21 | Acelrx Pharmaceuticals, Inc. | Small volume oral transmucosal dosage forms containing sufentanil for treatment of pain |
US8945592B2 (en) | 2008-11-21 | 2015-02-03 | Acelrx Pharmaceuticals, Inc. | Sufentanil solid dosage forms comprising oxygen scavengers and methods of using the same |
US11058856B2 (en) | 2014-12-23 | 2021-07-13 | Acelrx Pharmaceuticals, Inc. | Systems, devices and methods for dispensing oral transmucosal dosage forms |
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MX337286B (en) | 2007-05-25 | 2016-02-22 | Indivior Uk Ltd | Sustained delivery formulations of risperidone compounds. |
US20110097401A1 (en) * | 2009-06-12 | 2011-04-28 | Meritage Pharma, Inc. | Methods for treating gastrointestinal disorders |
US9272044B2 (en) | 2010-06-08 | 2016-03-01 | Indivior Uk Limited | Injectable flowable composition buprenorphine |
GB2513060B (en) | 2010-06-08 | 2015-01-07 | Rb Pharmaceuticals Ltd | Microparticle buprenorphine suspension |
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- 2006-07-21 RS RS20160214A patent/RS54670B1/en unknown
- 2006-07-21 US US11/490,500 patent/US8574552B2/en active Active
- 2006-07-21 HU HUE06776336A patent/HUE027354T2/en unknown
- 2006-07-21 AU AU2006271870A patent/AU2006271870B2/en not_active Ceased
- 2006-07-21 NZ NZ563511A patent/NZ563511A/en not_active IP Right Cessation
- 2006-07-21 UA UAA200713973A patent/UA90518C2/en unknown
- 2006-07-21 SI SI200632040A patent/SI1906961T1/en unknown
- 2006-07-21 ES ES06776336.7T patent/ES2569228T3/en active Active
- 2006-07-21 PL PL06776336T patent/PL1906961T3/en unknown
- 2006-07-21 EP EP06776336.7A patent/EP1906961B1/en active Active
- 2006-07-21 DK DK06776336.7T patent/DK1906961T3/en active
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- 2006-07-21 RU RU2007149044/15A patent/RU2408373C2/en active
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2008
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2013
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