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
  • A61K31/74—Synthetic polymeric materials
  • A61K31/80—Polymers containing hetero atoms not provided for in groups A61K31/755 - A61K31/795
• • 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
  • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
  • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/04—Antibacterial agents

Definitions

• Dimeticone as a Transport and Carrier System and/or Drug Delivery System
• the invention relates to dimethylpolysiloxane (dimeticone) to be used as a transport and carrier system and/or a drug delivery system for pharmaceutical drugs for instance for the treatment of gastro-intestinal diseases. Moreover, the invention relates to pharmaceutical compositions containing dimethylpolysiloxane as a transport and carrier system and/or as a drug delivery system in combination with an active ingredient and methods related thereto.
• dimeticone-containing preparations are used to treat symptoms such as flatulence, sensation of repletion (bloating) and meteorism. Moreover, the use of dimeticone for treating inflammatory and ulcerous diseases of the esophagus, the stomach and the duodenum has been described.
• the galenics of a pharmaceutical composition should be such that only the
• the therapeutically active ingredient right at the site where it is to produce its effect or at the site where it is absorbed so as to increase the local bioavailability and/or general bioavailability of the active ingredient (for instance by averting a first pass effect in the liver) or so as to avoid systemic side effects as much as possible.
• the continuous peristalsis, the variation of the chemical conditions over the length of the digestive tract, and the morphology of the surface of the GI tract are obstacles to a prolonged residence time in the different sections of the tract (such as the esophagus, stomach, duodenum, and colon) .
• the present invention provides a carrier that lends itself for use in particular galenic pharmaceutical forms for oral, rectal and intraoperative applications which release and/or fix the active ingredient continuously at the very site where it is to produce its effect or is absorbed.
• dimeticone because of its unique physico-chemical properties is ideally suited for such purposes.
• Dimeticone has a very wide range of viscosities, depending on the degree of polymerization.
• the viscosity of dimeticone to be used in accordance with the invention may vary, depending on the therapeutical purpose, the nature and location of the condition to be treated as well as the drug to be administered.
• dimeticone having a kinematic viscosity in the range of 10 to 100,000 mm .S -1 is used.
• dimeticone having a kinematic viscosity in the range of 300 to 1,500 mm .S "1 is particularly preferred. Dimeticone may also be supplemented with silicone dioxide as it is for example contained in the product Simeticone.
• Dimeticone was found to show a particular association with or affinity to the surface structure of the GI tract. Because of an increased adhesion resulting from the adhesive properties of dimeticone, the residence time of an active ingredient in a region of the GI tract can be substantially prolonged if dimeticone is used as a transport or carrier system.
• dimeticone because of the different chemical, morphological and physiological conditions along the GI tract, the affinity and association of dimeticone with the epithelial cells of the GI tract is not uniform. Thus, in order to optimize the effect of dimeticone as a transport and carrier system and/or drug delivery system for any particular drug at any particular site of the GI tract, dimeticone with the appropriate viscosity should be chosen, depending on the nature of the therapy and drug as well as the location in the GI tract. This may readily be determined' by experimentation.
• dimeticone is not limited to the treatment of the GI tract. It may also be used in the treatment of the cardiovascular system the lungs, the brain and all hollow organs.
• dimeticone was found to be particularly suitable as a transport and carrier system or a drug delivery system for cytostatic drugs, immunosup- pressants, immunomodulating and immunostimulative substances, biological response modifying (BRM) substances, radio-, chemo- and photosensitizers, anti-inflammatory substances, such as corticoids, antibiotics, analgesics, locally effective anestetics, antiphlogistics, non-steroidal antirheumatics, antiviral substances, bismuth preparations and motility inhibiting and motility enhancing substances.
• BRM biological response modifying
• dimeticone as a carrier for the photo- sensitizer ⁇ 5-amino levulinic acid (ALA) , the H-, antagonists (such as ranitidine and cimetidine) and the proton pump inhibitors (such as omeprazole and lansoprazole) is particularly preferred.
• the pharmaceutical compositions which contain dimeticone in combination with one of the afore-mentioned substances therefore lend themselves particularly well for the treatment of inflammatory, infectious, ulcerous and neoplastic diseases of the GI tract.
• the dimeticone-containing pharmaceutical composition may be formulated in an enteral form according to conventional methods in order to prevent dimeticone and the active ingredient from remaining in the upper zone of the GI tract.
• the properties of the pharmaceutical composition should be so adjusted that it has an increased affinity for the lower part of the GI tract.
• Direct application for instance via the bioptic channel of an endoscope, bronchoscope or proctoscope, intraoperative or by instillation, is particularly preferred.
• the dimeticone-containing pharmaceutical composition should also contain highly dispersed silicon dioxide and/or a pharmaceutically acceptable surface-active agent.
• the ratio of dimethylpolysiloxane to the surface-active agent is preferably 3 to 10 : 1, in particular 4 to 6 : 1, and the ratio of highly dispersed silicon dioxide to dimethylpolysiloxane is preferably 3 to 50% (wt/wt) .
• a preferred range for the latter ratio is 30 to 40% (wt/wt) , the value of 35 to 36% being particularly preferred.
• the concentration of the surface active agent is preferably at least 1.5 % (wt/wt).
• a particularly preferred dimeticone formulation contains 8-10% (wt/wt) of the surface active agent.
• Stearic salts or long chain alkanoic acids in particular C- j ⁇ -C- ⁇ g alkanoic acids, such as myristic acid, palmitic acid and stearic acid, and their salts, such as magnesium or calcium salts and mixtures thereof can be suitably used as pharmaceutically acceptable surface active agents.
• ALA ⁇ -amino levulinic acid containing emulsion
• colloidal magnesium aluminum silicate
• the emulsion of the Example is intended for the photodynamic therapy of tumors of the GI tract, the emulsion being applied by means of an endoscope at the very site where the effect is to be elicited.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• Medicinal Chemistry (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• General Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Oncology (AREA)
• Proteomics, Peptides & Aminoacids (AREA)
• Inorganic Chemistry (AREA)
• Communicable Diseases (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

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• 1994
  • 1994-03-18 DE DE4409357A patent/DE4409357C2/de not_active Expired - Fee Related
• 1995
  • 1995-03-15 PL PL95316307A patent/PL316307A1/xx unknown
  • 1995-03-15 CN CN95192553A patent/CN1244129A/zh active Pending
  • 1995-03-15 AU AU20713/95A patent/AU699199B2/en not_active Ceased
  • 1995-03-15 CZ CZ963007A patent/CZ300796A3/cs unknown
  • 1995-03-15 SK SK1324-96A patent/SK132496A3/sk unknown
  • 1995-03-15 EP EP95913130A patent/EP0804242A1/de not_active Withdrawn
  • 1995-03-15 NZ NZ282805A patent/NZ282805A/en not_active IP Right Cessation
  • 1995-03-15 WO PCT/EP1995/000973 patent/WO1995025545A1/en not_active Application Discontinuation
  • 1995-03-15 JP JP7524363A patent/JPH09510466A/ja not_active Withdrawn
  • 1995-03-15 HU HU9602839A patent/HU215595B/hu not_active IP Right Cessation
  • 1995-03-15 CA CA002185882A patent/CA2185882A1/en not_active Abandoned
• 1996
  • 1996-09-17 FI FI963682A patent/FI963682A/fi unknown
  • 1996-09-17 NO NO963893A patent/NO963893L/no not_active Application Discontinuation

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