Classifications

• • B—PERFORMING OPERATIONS; TRANSPORTING
  • B82—NANOTECHNOLOGY
  • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
  • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
• • 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
  • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• • 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
  • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
  • A61K47/69—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
  • A61K47/6949—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
  • A61K47/6951—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
• • 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
• • 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

Definitions

• the present invention relates to liquid pharmaceu ⁇ tical compositions for the oral topical treatment, containing non steroidal anti-inflammatory drugs as the active ingredients.
• Therapeutical treatment of inflammations of the oral cavity such as aspecific odontostomatologic af ⁇ fections, gingivitis, glossitis, stomatitis and the like, is particularly complex and, until the specific pathogenic agent has precisely been determined, treat- ment can be restricted to the use of disinfectants of the general type.
• Said drugs besides showing negative characteri ⁇ stics (remarkable side-effects) can cause severe and diffused allergy phenomena, so as to compel to immedia- tely interrupt treatment and to take suitable restora ⁇ tion measures.
• compositions comprising non steroidal anti-inflammatory drugs (FANS) in form of solutions intended for the oral topical tre ⁇ atment (collutories) , allow to obtain very good thera ⁇ Promotionical results without causing sensitization pheno ⁇ mena.
• FANS non steroidal anti-inflammatory drugs
• the compositions of the invention are characteri ⁇ zed by the presence of a specific excipient, dimethyl isosorbide, giving them advantageous antiseptic proper ⁇ ties together with an antiplaque action which is parti- cularly desired in this kind of preparations.
• Anti-in ⁇ flammatory properties of the active ingredients also turn out to be surprisingly enhanced through a synerge- tic interaction with dimethyl isosorbide.
• compositions of the present invention can con- tain the active ingredient in amounts ranging from 0.001 to 20% by weight, whereas dimethyl isosorbide can be present in amounts ranging from 1 to 40% by weight.
• compositions of the invention can also contain other excipients and/or coadjuvants, such as surfactants, flavouring and sweetening agents, in order to give the preparation suitable organoleptic characteristics.
• excipients and/or co ⁇ adjuvants conventionally used for the preparation of collutories are described in "Remington's Pharm. Scien- ces Handbook", Mack Pub. Co., NY.
• the compositions of the invention will preferably contain natural and/or synthetic sweetening agents such as saccharine, ammo ⁇ nium glycyrrhizinate, cycla ate or, more preferably, not cariogenic carbohydrates such as xylitol and sorbi- tol.
• non steroidal anti- inflammatory drugs such as ketoprofen, ibuprofen, ibu- profen lysine salt, naproxen, suprofen, diclofenac, al- clofenac, indomethacin, acemethacin, benzidamine, flur- biprofen, piroxicam and the like, can be used as active ingredients, either in the free form or salified, in order to improve the solubility thereof.
• the active ingredients are present in combination with cyclodextrins or derivatives thereof, for example in form of physical admixtures, inclusion products or co- precipitates.
• Cyclodextrins or derivatives thereof such as hydroxypropyl beta-cyclodextrins, involve fa ⁇ vourable pharmacokinetic effects and, moreover, are useful to increase solubility and stability, or to im- prove the organoleptic characteristics of the medica ⁇ ment.
• Cyclodextrin contents can range from 0.5 to 50% by weight of the finished composition, but equimolecular ratios of active ingredient to cyclodextrin are prefe- rably used.
• cyclodex ⁇ trins (o , ⁇ , -) and the already cited hydroxypropyl ⁇ - cyclodextri ⁇ , dimethylcyclodextrins or other derivati ⁇ ves, possibly in a mixture thereof can also be used.
• polymers having an adhesive power towards ucosae are used as excipients.
• examples of said polymers are provided by carboxyvinyl polymers, ethyle e oxide - propylene oxide copolymers, cellulose derivatives such as carboxymethyl cellulose, calcium carboxymethyl cellulose, hydroxy- propylethyl cellulose, hydroxyethyl cellulose, hydroxy ⁇ propyl cellulose, carrageenan, dextrins, natural or synthetic gums and the like.
• Said excipients, which can be def ned bioadhesive polymers can be present in per ⁇ centages ranging from 0.5 to 30%, preferably from 1 to 5%.
• excipients allows to obtain sli ⁇ ghtly viscous solutions having adhesiveness towards mu- cosae, so as to achieve a better persistence of the preparation in contact with the area to be treated, thus obtaining a more effective and lasting action.
• compositions can also contain no dimethyl isosor- bide : said compositions also fall within the scope of the present invention.
• Each 15 ml ampoule contains: Active ingredient: ketoprofen Excipients:
• Ketoprofen is dissolved in an ethanol solution containing dimethyl isosorbide and Tween 60, the solu ⁇ tion is heated to 35 C C under stirring, to obtain a clear solution which is added with the other components. After filtration, a clear homogeneous solution (collutory) is obtained.
• Ketoprofen is added to a ⁇ -cyclodextrin aqueous solution (about 50 ml), which is heated to 30-40 e C for 30 hours. A solution is obtained which is added with dimethyl isosorbide and the other components, then fil ⁇ tered.
• EXAMPLE 4 Collutory containing ketoprofen, dimethyl isosorbide and bioadhesive polymers (in form of solution) 100 ml of collutory contain (% composition): Active ingredient: ketoprofen 0.05 Excipients:
• Each 15 ml ampoule contains : Active ingredient: Benzidamine 2 to 20 mg ExciDients: Tween 60 5 mg alpine herb flavor 52,503 T 15 mg dimethyl isosorbide 1500 mg
• Collutory containing piroxicam (in form of solution) 100 ml of collutory contain (% composition) : Active ingredient:
• Each 15 ml ampoule contains: Active ingredient: Piroxicam Excipients:

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Engineering & Computer Science (AREA)
• General Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• Animal Behavior & Ethology (AREA)
• Epidemiology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Molecular Biology (AREA)
• Physiology (AREA)
• Nanotechnology (AREA)
• Nutrition Science (AREA)
• General Engineering & Computer Science (AREA)
• Crystallography & Structural Chemistry (AREA)
• Medical Informatics (AREA)
• Biotechnology (AREA)
• Biophysics (AREA)
• Biochemistry (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Oil, Petroleum & Natural Gas (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Priority Applications (1)

Applications Claiming Priority (2)

Publications (1)

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ID=11174427

Family Applications (1)

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Cited By (23)

Citations (3)

• 1990
  • 1990-07-13 IT IT02094490A patent/IT1243342B/it active IP Right Grant
• 1991
  • 1991-07-04 CA CA002066731A patent/CA2066731A1/en not_active Abandoned
  • 1991-07-04 AU AU80935/91A patent/AU8093591A/en not_active Abandoned
  • 1991-07-04 EP EP91911791A patent/EP0491897A1/en not_active Withdrawn
  • 1991-07-04 ES ES199191911791T patent/ES2034926T1/es active Pending
  • 1991-07-04 WO PCT/EP1991/001245 patent/WO1992000725A1/en not_active Application Discontinuation
• 1993
  • 1993-04-28 GR GR930300021T patent/GR930300021T1/el unknown

Patent Citations (3)

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