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
  • A61K9/0048—Eye, e.g. artificial tears
  • A61K9/0051—Ocular inserts, ocular implants
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61F—FILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
  • A61F9/00—Methods or devices for treatment of the eyes; Devices for putting-in contact lenses; Devices to correct squinting; Apparatus to guide the blind; Protective devices for the eyes, carried on the body or in the hand
  • A61F9/0008—Introducing ophthalmic products into the ocular cavity or retaining products therein
  • A61F9/0017—Introducing ophthalmic products into the ocular cavity or retaining products therein implantable in, or in contact with, the eye, e.g. ocular inserts

Definitions

• the invention relates to a new compressed product for local ophthalmic use.
• Isters or other sheet-like or lamellar shaped bodies which are inserted into the lower conjunctival sac and which delay the release of active ingredient can only be produced with considerable outlay in terms of process technology and are often unsuitable for long-term use due to a lack of compatibility.
• Even new therapeutic systems propagated in recent years - eg Ocuserr- 'for ophthalmology - have not been able to solve the existing problems, the manufacture of such chamber-like molded articles consisting of plastics is very complex, and the question must also be asked whether an extension of the effect over a period of seven days makes any sense.
• An inadequate chemical stability often speaks against an excessively long residence time of active substances in the tear fluid, for example in the case of pilocarpine.
• the object of the invention is to provide pharmaceutical preparations for local ophthalmic use which can be obtained in a relatively simple and inexpensive manner and which guarantee an effect lasting from about 12 to 24 hours.
• compressed tablets can be produced with the aid of tablet machines, which are largely adapted to the anatomical conditions of the eye when water-insoluble ophthalmologically acceptable carriers are used.
• the invention relates to a compressed product for local ophthalmic use of 8 to 14 mm in length, 3 to 14 mm in width and 0.05 to 1 mm in height, comprising at least one water-insoluble ophthalmologically acceptable carrier and at least one ophthalmologically acceptable active ingredient.
• Suitable carrier substances are, in particular, polymer substances which are indifferent to water and tear fluid, for example the polymethyl methacrylic acid esters (PMMA) which are also used for the production of contact lenses, and other polymethacrylates and the corresponding polyacrylates.
• PMMA polymethyl methacrylic acid esters
• polyacrylic acid derivatives with acidic, e.g. Carboxyl, or basic, e.g. Ammonium groups are used, which may also be in the form of their salts.
• the compressed products according to the invention are thin slices of 8 to 14, preferably 10 to 12 mm in length, 3 to 14, preferably 4 to 8 mm in width and 0.05 to 1, preferably 0.1 to 0.5 mm web height.
• You can use any, for example angular, for example square, pentagonal or hexagonal, or in rounded, for example circular, oval or - preferably - kidney-shaped form. They can be flat or curved, in particular adapted to the shape of the eye; they can preferably have curvature radii of 11 to 14 mm, expediently 12 to 13 mm.
• aqueous dispersions which have an average molecular weight of the polymer substance of 0.5 to 1.5 million, preferably of about 800,000, and a
• Adhesion of the molding compound to the punches can generally be added by adding approx. 2 to 20. ⁇ , preferably 8 to 12 ?. Water can be avoided. It is also possible to improve the tabletting ability by adding about 0.5 to 5, preferably 0.5 to 2?? Of highly disperse silica - for example Aerosil ⁇ ' 200 - without adversely affecting the compressed product or the active ingredient enter.
• Suitable basic components which are also suitable as additives, are Eudragit ⁇ RS and Eudragit ⁇ L. If these substances are not used in the form of aqueous dispersions, e.g. the anionic compound (Eudragit ⁇ - L) after adjustment to a pH of> 7 by drying, e.g. Spray drying, convert into a powder product. Not only aqueous dispersions or aqueous solutions, but also solutions in organic solvents can be subjected to spray drying. It is advisable, for example, to use chloroform-methanol when incorporating Eudragit® RS as a solvent, preferably in a volume ratio of 7: 3.
• the compressions according to the invention can in particular contain active substances from the following groups: Antibacterial agents, for example antibiotics such as chloramphenico gentamycin, neomycin; Sulfonamides such as sulfisomidine, sulfadicram sulfathiazole; quaternary salts such as benzalkonium chloride, cetylpyridinium chloride; Antihistamines such as tetryzolin, antazolin; Antiphlogistics such as hydrocortisone acetate, prednisolone acetate, dexamethasone and its ester, betamethasone and its ester; Berberine chloride; Miotics such as pilocarpine, physostigmine; ⁇ -receptor blockers such as propranolol, timolol or bisoprolol; Mydriatics such as atropine, scopolamine.
• Antibacterial agents for example antibiotics such as chloram
• the active substance (s) can be incorporated into the carrier (s) either by mixing or after drying a solution of the carrier in which the active substance is dissolved or suspended.
• the starting material for tableting can also be obtained by spray drying the carrier and active ingredient together.
• plasticizers such as triacetin, citric acid or sebacic acid esters etc. can be included. Incorporation can be carried out by immersing the compressed products in a solution of the plasticizer in a volatile organic solvent such as ethanol and then drying them.
• kidney-shaped compresses of 10 mg total weight - 10 mm length, 3 mm width, 0.15 mm web height - which have a total duration of action of about 12 to 20 hours are obtained with the aid of a conventional tablet machine .
• compositions are available analogously:
• Example 4 Dexamethasone 0.1? _ Finely divided silica 1

Landscapes

• Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Ophthalmology & Optometry (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Heart & Thoracic Surgery (AREA)
• Vascular Medicine (AREA)
• Biomedical Technology (AREA)
• Engineering & Computer Science (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)

Applications Claiming Priority (2)

Publications (1)

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• 1985
  • 1985-01-30 DE DE19853502962 patent/DE3502962A1/de not_active Withdrawn
• 1986
  • 1986-01-21 JP JP61501209A patent/JPS62501564A/ja active Pending
  • 1986-01-21 WO PCT/EP1986/000019 patent/WO1986004502A1/de not_active Application Discontinuation
  • 1986-01-21 EP EP86901366A patent/EP0211072A1/de not_active Withdrawn
  • 1986-01-21 HU HU861490A patent/HUT42937A/hu unknown
  • 1986-01-29 IE IE860259A patent/IE860259L/xx unknown
  • 1986-01-29 ES ES551375A patent/ES551375A1/es not_active Expired
  • 1986-01-30 ZA ZA86701A patent/ZA86701B/xx unknown
  • 1986-02-21 AU AU55167/86A patent/AU5516786A/en not_active Abandoned

Non-Patent Citations (1)

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