WO2007021168A1 - Formulaciones farmacéuticas sólidas sublinguales coneniendo meloxicam - Google Patents
Formulaciones farmacéuticas sólidas sublinguales coneniendo meloxicam Download PDFInfo
- Publication number
- WO2007021168A1 WO2007021168A1 PCT/MX2006/000047 MX2006000047W WO2007021168A1 WO 2007021168 A1 WO2007021168 A1 WO 2007021168A1 MX 2006000047 W MX2006000047 W MX 2006000047W WO 2007021168 A1 WO2007021168 A1 WO 2007021168A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- agents
- sodium
- solid pharmaceutical
- meloxicam
- pharmaceutical formulations
- Prior art date
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
- A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- 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
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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 is related to the pharmaceutical industry in general and to the pharmaceutical industry producing various solid sublingual pharmaceutical formulations containing Meloxicam
- the solid pharmaceutical forms are preparations containing the active ingredient or additives generally in discoid form, grooved or not grooved, molded and of vain size obtained by compression of powders or granules, in tablets, capsules, patches, ovules, pearls, suppositories , troches or pills
- Osteoart ⁇ tis is the eighth cause of disability in the world, according to studies conducted by the WHO It is the most frequent of joint diseases and their prevalence increases with age. The typical joint alterations of osteoarthritis begin in the second decade of life, affecting 90% of people over 40 years.
- the distribution of the disease is universal, although there are geographical differences, due in part to genetic, environmental factors and the different use of the joints.
- Rheumatoid arthritis is a condition that has the potential to severely affect the survival, functional capacity and quality of life of the individual who suffers, as well as the ability to maintain satisfactory employment. Mortality due to direct causes or complications derived from rheumatoid arthritis continues to be twice that observed in the control population, without modification of this trend in the last four decades. It affects 0.5 to 1.0% of the world's population.
- the present invention provides new formulations comprising: (a) Melox ⁇ cam, (b) one or more anti-inheriting agents, (c) one or more disintegrating agents, (d) one or more binding agents, ( e) one or more lubricating agents, (f) one or more diluting agents, (g) one or more solvents, (h) one or more solubilizing agents, (i) one or more sweetening agents, (j) one or more agents flavoring and / or essences, (k) one or more viscosity agents, (I) one or more antimicrobial agents (m) one or more surfactants, (n) one or more antioxidant agents, (or) one or more emulsifying agents, and (p) any other additive that favors the formulation.
- Meloxicam is 4-Hydroxy-2-methyl-N- (5-methyl-2-thiazolyl) -2H-1, 2- Benzothiazine-3-carboxamide-1, 1-Dioxide and can be represented by the formula (I ).
- the compound of the formula (I) is known for its anti-inflammatory, analgesic and antipyretic activity that acts by inhibiting the synthesis of prostaglandins with greater potency at the site of inflammation than on the kidney and gastric mucosa. It is currently indicated in the treatment of rheumatoid arthritis, osteoarthritis, periartritis in the scapulohumeral and coxofemoral joints, muscle strains and pain and inflammation in soft tissues and respiratory tract with inflammatory processes.
- the present invention can be reflected in a medication whose concentration of the drug in the formulation is in a proportion of 0.0001% to 95.0% w / w, preferably 0.5 to 50.0% w / w for Meloxicam.
- This drug present in it can be found as its anhydrous or hydrated base or as a physiologically acceptable salt such as Meloxicam base.
- This invention relates to solid sublingual formulations containing Meloxicam.
- the present invention provides new formulations comprising: (a) Meloxicam, (b) one or more non-stick agents, (c) one or more disintegrating agents, (d) one or more binding agents, (e) one or more lubricating agents, (f) one or more diluting agents, (g) one or more solvents, (h) one or more solubilizing agents, (i) one or more sweetening agents, (j) one or more flavoring agents and / or essences, (k) one or more viscosity agents, (I) one or more antimicrobial agents (m) one or more surfactants, (n) one or more anti-oxidant agents, (or) one or more emulsifying agents, and (p ) any other additive that favors the formulation.
- additives or excipients consist, for example, of the diluting agents in lactose, manltol, dextrose, sucrose, sucrose, calcium phosphate, microcrystalline cellulose, calcium sulfate, kaolin, compressible sugar, corn starch, among others.
- the diluting agent can of being in a proportion from 5% to 99%.
- the disintegrating agents are selected from corn starch, alginic acid, celluloses and their derivatives, povidone, croscarmellose sodium, sodium starch, sodium I, among others.
- the disintegrating agent can be found from 0.0001% to 25.0%.
- Binder agents such as Io are polyvinylpyrrolidone, tragacanth, acacia, starch, methylcellulose, among others.
- the binding agent can be found from 0.01% to 10.0%.
- the polar and non-polar solvent agent can be: water, ethyl alcohol, acetone, isopropyl myristate, polyoxypropylenes, pro pi I glycol, polyethylene glycol I, glycerol, 70% sorbitol, polyethylene glycols, mineral oils, petroate, lanolin, vegetable waxes, animal waxes, vegetable oils such as olive oil, cotton, corn oil, among others, or a combination thereof, those preferably used are ethyl alcohol, 70% sorbitol solution, vegetable oils and polar solvents such as Water.
- the final formulation may contain from 1% to 95% w / v of the solvent.
- Lubricating agents are selected from stearic acid, stearate and talc, among others.
- the lubricating agent can be in a proportion from 0.0001% to 10.0%.
- Non-stick agents such as Io, colloidal silicon dioxide, calcium sulfate, calcium chloride, talc, corn starch, among others.
- the non-stick agent can be in a proportion from 0.0001% to 10.0%.
- Solubilizing agents such as povidone, cyclodextrins, n-methylglucamine, lecithin, monoethanolamine, glycine, benzyl benzoate, poloxamers, polyoxyethylene alkyl elecres, among others.
- the solubilizing agent can be found in a proportion from 0.0001% to 50.0%.
- One or more surfactants such as Io are sodium laurate, sodium oleate, sodium lauryl sulfate, sodium cholate, sodium deoxycholate, sodium diamyl sulphosuccinate, dioctyl sulphosuccinate sodium, poloxamers, lecithin, tetradecyltrimethylammonium bromide, hexadecylpidium chloride, hexadecyl chloride polysorbate 20, polysorbate 60, among others.
- the surfactant can be found in a proportion from 0.0001% to 30%.
- Emulsifying agents such as Io are gum arabic, tragacanth, alginates, chondrus, pectin, aluminum silicate, bentonite, magnesium aluminum silicate, sodium dodecyl sulfate, benzalconium chloride, sorbitan polyoxyethylene monostearate, polyethylene glycol monostearate 400, ethylene glycol distearate, sorbitan triestearate, sorbitan monopalmitate, diethylene glycol monostearate, sodium oleate, potassium oleate, sodium lauryl sulfate, among others.
- the emulsifying agent can be found from 0.0001% to 10%
- Sweetening agents such as Io are aspartame, acesulfame k, dextrose, fructose, glucose, mannitol, sorbitol, sugar, sucrose, among others.
- the sweetening agent can be found in a proportion from O 0001% to 60 0% w / v
- Flavoring agents such as menthol, vanillin, cinnamon, sorbet, citric acid, cherry flavor essence, orange flavor essence, pine flavor essence, peach flavor essence, grape flavor essence, strawberry flavor essence, among others
- the flavoring agent can be found in a proportion from 0.0001% to 5 0% w / v
- Antioxidant agents such as Io are disodium edetate (EDTA), ascorbic acid, Butylhydroxytoluene (BHT), tocopherols, sodium bisulfite or metab is or If sodium mess, gallic acid, propylgalate, ascorbyl palmitate.
- EDTA disodium edetate
- BHT Butylhydroxytoluene
- tocopherols sodium bisulfite or metab is or If sodium mess, gallic acid, propylgalate, ascorbyl palmitate.
- the antioxidant agent can be found in a proportion from 0.0001% to 20 0%
- Antimicrobial agents such as Io are ⁇ orbic acid, potassium sorbate, potassium benzoate, chlorobutanol, methyl p-hydroxybenzoate, propyl p-hydroxybenzoate, thimerosal among others.
- the antimicrobial agent can be found in a proportion from 0.0001% to 5.0% w / v
- Viscosity agents such as acacia, agar, alginic acid, povidone, hydroxypropylmethylcellulose, sodium carboxymethylcellulose, calcium carboxymethylcellulose, pectin, gelatin, guar gum, xanthan gum, carbomer, bentonite, hydroxypropylcellulose, among others, preferably sodium carboxymethylcellulose.
- the final formulation may contain from 0.0001% to 10.0% w / v of the viscosity agent.
- the formulation may also contain other components such as Io are a flocculating agent such as sodium chloride or potassium chloride; a pH buffer system such as phosphates, phosphoric acid, citrates, citric acid, carbonates, bicarbonates, acetates, lactates among others; they can be found as their anhydrous or hydrated base or as a physiologically acceptable salt,
- the flocculating agent can be found in a proportion from 0.0001% - 5.0% w / v and the pH buffer system can be contained in a proportion ranging from 0.01% to 10% w / w.
- the present invention also provides a method for the treatment of processes that occur with inflammation and pain such as low back pain, cervicalgia, brachialgia, radiculitis, peripheral neuropathies of various ethiopathogenesis: facial neuralgia, trigeminal neuralgia, intercostal neuralgia, herpetic neuralgia, alcoholic neuropathy, diabetic neuropathy, carpal duct syndrome, fibromyalgia, spondylitis, rheumatoid arthritis, osteoarthritis, periarthritis of the scapulohumeral and coxofemoral joints, muscle strains and pain and inflammation in soft tissues and respiratory tract, caused by various etiologies, by administering adequate doses of the present formulations.
- the formulations may be contained in: containers of adequate capacity ranging from 5 mL to 150 mL, made of high and / or low density polyethylene, polyethylene terephthalate, polyvinyl chloride, polypropylene, polystyrene, type I, II glass, III and IV, among others, with or without color.
- the cover may be inviolable, threaded, cap to cap, child proof, made of high and / or low density polyethylene, polyethylene terephthalate, polyvinyl chloride, polypropylene, polystyrene, with or without color.
- PVDC polygidene chloride
- the preparation of the different pharmaceutical forms is carried out with the mixture of the active ingredients with the corresponding additives, in the appropriate concentrations.
- the administration of 15 mg of Meloxicam every 24 hours causes peak plasma concentrations of 1.6 ⁇ g / mL. Concentrations in steady state are achieved in 3 to 5 days. 99% of Meloxicam is linked to plasma proteins. The drug has a good distribution in the body but particularly achieves high penetration into synovial fluid, reaching equivalent levels. half of the plasma concentrations.
- the metabolism of Meloxicam is mainly by oxidation of the methyl group of the thiazolyl molecule. Approximately 50% of the dose is eliminated by urinary tract and the rest is excreted in feces. The elimination half-life is 20 hours.
- the present invention provides a solid sublingual pharmaceutical formulation that provides from 0.25 mg to 25 mg of Meloxicam in suitable doses.
- the tablet is prepared as follows: Meloxicam is mixed with the anhydrous lactose, separately, the alcohol and water are mixed; in this solution, sucrose is dissolved and gradually added to the first mixture. Finally we proceed to molding.
- formulations are indicated for the treatment of processes that occur with inflammation and pain such as lumbago, cerrhagia, brachialgia, radiculitis, peripheral neuropathies of various etiopathogenesis, facial neuralgia, trigeminal neuralgia, intercostal neuralgia, herpetic neuralgia, alcoholic neuropathy, diabetic neuropathy , carpal duct syndrome, fibromyalgia, spondylitis, rheumatoid arthritis, osteoart ⁇ tis, pe ⁇ art ⁇ tis in the scapulohumeral and coxofemoral joints, muscle strains and pain and inflammation in soft tissues and respiratory tract, caused by various etiologies, by administering appropriate doses of the present formulations
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
Claims
Priority Applications (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP06757780A EP1913936A4 (en) | 2005-08-12 | 2006-06-06 | SUBLINGUAL SOLID PHARMACEUTICAL FORMULATIONS WITH MELOXICAM |
BRPI0614585-0A BRPI0614585A2 (pt) | 2005-08-12 | 2006-06-06 | formulações farmacêuticas sólidas sublinguais contendo meloxicam |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
MXPA/A/2005/008575 | 2005-08-12 | ||
MXPA05008575A MXPA05008575A (es) | 2005-08-12 | 2005-08-12 | Formulaciones farmaceuticas solidas sublinguales conteniendo meloxicam. |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2007021168A1 true WO2007021168A1 (es) | 2007-02-22 |
WO2007021168A8 WO2007021168A8 (es) | 2008-02-21 |
Family
ID=37757792
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/MX2006/000047 WO2007021168A1 (es) | 2005-08-12 | 2006-06-06 | Formulaciones farmacéuticas sólidas sublinguales coneniendo meloxicam |
Country Status (6)
Country | Link |
---|---|
EP (1) | EP1913936A4 (es) |
BR (1) | BRPI0614585A2 (es) |
CR (1) | CR9726A (es) |
EC (1) | ECSP088174A (es) |
MX (1) | MXPA05008575A (es) |
WO (1) | WO2007021168A1 (es) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102065845A (zh) * | 2008-06-11 | 2011-05-18 | 阿斯利康(瑞典)有限公司 | 含有(2s)-(4e)-n-甲基-5-(5-异丙氧基吡啶-3-基)-戊-4-烯-2-胺的舌下组合物 |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1250921A1 (en) * | 2001-04-21 | 2002-10-23 | BOEHRINGER INGELHEIM INTERNATIONAL GmbH | Fast disintegrating meloxicam tablet |
US20030161875A1 (en) * | 2002-02-27 | 2003-08-28 | Deepak Murpani | Fast dissolving tablets of cyclooxygenase-2 enzyme inhibitors |
US20050119239A1 (en) * | 2003-11-27 | 2005-06-02 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition consisting of a beta-3-adrenoceptor agonist and an active substance which influences prostaglandin metabolism |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU750125B2 (en) * | 1997-08-27 | 2002-07-11 | Hexal Ag | New pharmaceutical compositions of meloxicam with improved solubility and bioavailability |
AU2004238321B2 (en) * | 2003-05-07 | 2009-08-27 | Samyang Biopharmaceuticals Corporation | Highly plastic granules for making fast melting tablets |
CN1233323C (zh) * | 2003-12-09 | 2005-12-28 | 成都圣诺科技发展有限公司 | 美洛昔康口腔崩解片及其制备方法 |
MXPA04009698A (es) * | 2004-10-04 | 2006-04-05 | Maria Elena Garcia Armenta | Formulaciones farmaceuticas solidas conteniendo diacereina y meloxicam. |
-
2005
- 2005-08-12 MX MXPA05008575A patent/MXPA05008575A/es active IP Right Grant
-
2006
- 2006-06-06 EP EP06757780A patent/EP1913936A4/en not_active Withdrawn
- 2006-06-06 WO PCT/MX2006/000047 patent/WO2007021168A1/es active Application Filing
- 2006-06-06 BR BRPI0614585-0A patent/BRPI0614585A2/pt not_active Application Discontinuation
-
2008
- 2008-02-12 CR CR9726A patent/CR9726A/es not_active Application Discontinuation
- 2008-02-12 EC EC2008008174A patent/ECSP088174A/es unknown
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1250921A1 (en) * | 2001-04-21 | 2002-10-23 | BOEHRINGER INGELHEIM INTERNATIONAL GmbH | Fast disintegrating meloxicam tablet |
US20030161875A1 (en) * | 2002-02-27 | 2003-08-28 | Deepak Murpani | Fast dissolving tablets of cyclooxygenase-2 enzyme inhibitors |
US20050119239A1 (en) * | 2003-11-27 | 2005-06-02 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition consisting of a beta-3-adrenoceptor agonist and an active substance which influences prostaglandin metabolism |
Non-Patent Citations (2)
Title |
---|
DAWOOD AL-WAILI N.S.: "Sublingual meloxicam for renal colic", UROLOGIA INTERNATIONALS, vol. 67, 2001, pages 119 - 120, XP008077043 * |
See also references of EP1913936A4 * |
Also Published As
Publication number | Publication date |
---|---|
BRPI0614585A2 (pt) | 2011-04-05 |
MXPA05008575A (es) | 2007-02-12 |
WO2007021168A8 (es) | 2008-02-21 |
EP1913936A1 (en) | 2008-04-23 |
CR9726A (es) | 2008-10-10 |
EP1913936A4 (en) | 2012-12-19 |
ECSP088174A (es) | 2008-05-30 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
US6017932A (en) | Pharmaceutical compositions containing at least one NSAID having increased bioavailability | |
RU2640418C2 (ru) | Ингибиторы цистатионин-г-лиазы (cse) | |
AU650706B2 (en) | Medicaments | |
EP0498069B1 (en) | New use of peptide derivative | |
ES2267111T3 (es) | Utilizacion de inhibidores de fosfodiesterasa-cgmp para el tratamiento de la impotencia. | |
EP1067927B1 (en) | Antioxidant stabilizer system for pharmaceutical formulations | |
ES2969344T3 (es) | Composiciones de profármaco de alta penetración y composición farmacéutica del mismo para el tratamiento de afecciones pulmonares | |
US20090023712A1 (en) | Pharmaceutical Compositions for the Treatment of Attention Deficit Hyperactivity Disorder Comprising Flibanserin | |
US20050261356A1 (en) | Methods and compositions for the treatment of chronic lymphocytic leukemia | |
ES2332225T3 (es) | Formulaciones farmaceuticas solidas conteniendo diacereina y meloxicam. | |
ES2549924T3 (es) | Análogos de ácido araquidónico y métodos para tratamiento analgésico usando el mismo | |
MXPA05010505A (es) | Forma farmaceutica que contiene metocarbamol, meloxicam y betametasona. | |
BR112019018615B1 (pt) | Composto antimicrobiano e sua composiqao farmaceutica | |
ES2332462T3 (es) | Composicion farmaceutica de derivados de piperazina. | |
US20170022179A1 (en) | Compositions, dosages, and methods of using tetrahydrocannabinol derivatives | |
EP0530311A1 (en) | The use of phenylpropanolamine as a mucus secretagogue in the upper airways | |
WO2007021168A1 (es) | Formulaciones farmacéuticas sólidas sublinguales coneniendo meloxicam | |
EP0935964A1 (en) | Pharmaceutical compositions containing NSAIDs and piperine | |
EP1632229B1 (en) | Medicaments for the treatment of urinary tract disorders comprising anticholinergic agents | |
LU82163A1 (fr) | Nouveaux derives d'acide penicillanique utile notamment comme antibiotiques et leurs procedes de preparation | |
WO2007021167A1 (es) | Formulaciones farmacéuticas sólidas, semisólidas, en suspensión, en solución, en emulsión o en jarabe conte niendo clindamicina y uno o más de los miembros de la familia de los azoles | |
MXPA05007032A (es) | Formulaciones farmaceuticas solidas, en suspension y en emulsion, conteniendo nimesulida y pseudoefedrina. | |
IE46581B1 (en) | Cromoglycic acid salts and compositions | |
WO2005058879A1 (ja) | 滲出性中耳炎の予防および/または治療剤 | |
MXPA05007025A (es) | Forma farmaceutica solida, semi-solida, en suspension, en emulsion, jarabe o en solucion que contiene amoxicilina, acido clavulanico y nimesulida. |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
121 | Ep: the epo has been informed by wipo that ep was designated in this application | ||
WWE | Wipo information: entry into national phase |
Ref document number: 08012143 Country of ref document: CO |
|
REEP | Request for entry into the european phase |
Ref document number: 2006757780 Country of ref document: EP |
|
WWE | Wipo information: entry into national phase |
Ref document number: CR2008-009726 Country of ref document: CR Ref document number: 2006757780 Country of ref document: EP |
|
NENP | Non-entry into the national phase |
Ref country code: DE |
|
ENP | Entry into the national phase |
Ref document number: PI0614585 Country of ref document: BR Kind code of ref document: A2 Effective date: 20080212 |