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

Definitions

• Ophthalmic ointments roust meet certain U.S. preservative efficacy testing standards in order to be marketed.
• ophthalmic ointment preservation has been achieved by organic-based chemical preservatives such as chlorobutanol, methylparaben and propylparaben.
• organic preservatives irritate ocular tissu and are discomforting.
• Ointments by nature are not particularly susciptable to single dose packaging because of the difficulty in expressing material from such a small package. Ointment materials are inherently not self-preserving so some preservative means is needed to meet most health agency preservative standards. ""
• High salt concentration ophthalmic ointments are known (5% sodium chloride formulations) .
• a hypertonic ointment of sodium chloride 5% in a base of mineral oil, lanolin, white petrolatum and water is marketed by Muro Pharmaceuticals, Inc.
• a similar sodium chloride 5% ointment is also produced by Akorn, Inc.
• This high level of salt in these ointments is used to provide temporary relief of corneal swelling or edema by dehydrating the tissue. So though these ointments are non-preserved, no one has previously determined that low levels of salt could be used to effect preservation of ointments.
• Salts at low concentrations are non-irritating and non-discomforting. Nor do they cause adverse reaction which is particularly useful for ocular preparations. It has now been found that using between about 0.01% and 0.9% (w/w) salt in ointments provides a composition which meets USP PET standards and does not involve a chemical preservative which may be irritating or discomforting to ocular tissue. Such means for preserving ointments is particularly useful for ophthalmic ointments where the greatest likelyhood of reaction to organic preservatives is encountered.
• This invention relates to an improved ointment which does not require use of an organic preservative, particularly an ophthalmic ointment, wherein the improvement comprises adding 0.01%-0.9% weight/weight of a pharmaceutically acceptable inorganic salt to an ointment formulation.
• this invention relates to a method for preparing preservative free ointments which method comprises adding between 0.01%-0.9% w/w of a pharmaceutically acceptable inorganic salt to an ointment formulation.
• a pharmaceutically acceptable inorganic salt is any salt derived from the reaction of an inorganic acid and base, which at the concentrations recited herein does not have deleterious or untoward effect when administered to mammal.
• Preferred salts are those derived from lithium, sodium, potassium, calcium, magnesium, or iron (the cation) and chloride, bromide, iodide, sulfate, carbonate and phosphate in its various forms (anions). Borate salt may also be used.
• Particularly preferred salts are sodiu - chloride, potassium chloride, calcium chloride, magnesium chloride, sodium or potassium salts of phosphates and sulfates, calcium sulfate, magnesium sulfate and sodium o potassium carbonate.
• Salt concentrations may vary between 0.1 and 0.9% by weight. Concentrations between 0.05 and 0.3% are preferred.
• Salts may be introduced into ointment bases by any means so long as a intimate and even distribution of the salt is effected.
• Salt, in powder form, or in a concentrated aqueous solution are the two primary forms - ⁇ -
• Esarople 1 Five ointment samples were prepared containing a range of sodium chloride concentration. The formulation is as follows:
• USP sodium chloride

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• Health & Medical Sciences (AREA)
• Ophthalmology & Optometry (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Medicinal Preparation (AREA)

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• 1988
  • 1988-05-18 AU AU19367/88A patent/AU1936788A/en not_active Abandoned
  • 1988-05-18 WO PCT/US1988/001708 patent/WO1988009665A1/en not_active Ceased
  • 1988-05-18 EP EP19880905291 patent/EP0362277A4/en not_active Ceased

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