Title:  Method of preventing retinopathy of prematurity in a neonate

United States Patent:  6,344,479

Assignee:  Farmacon-Il, LLC (Westport, CT)

Filed:  March 20, 2001

A method is disclosed of preventing retinopathy of prematurity in a prematurely born neonate susceptible to developing retinopathy of prematurity, which comprises the step of parenterally administering to said prematurely born neonate, a therapeutically effective amount of a water-soluble, pharmaceutically effective salt of ibuprofen as an active ingredient to promote retinal and choroidal blood flow autoregulation in said neonate.

SUMMARY OF THE INVENTION

We have discovered that administration of a water-soluble, pharmaceutically effective salt of ibuprofen prevents retinopathy of prematurity when given to preterm infants, preferably during the first month of life. We have discovered a method of preventing retinopathy of prematurity in a prematurely born neonate susceptible to developing retinopathy of prematurity, which comprises the step of parenterally administering to said prematurely born neonate, a therapeutically effective amount of a water-soluble, pharmaceutically effective salt of ibuprofen as an active ingredient to promote retinal and choroidal blood flow autoregulation in said neonate.

The ibuprofen is in the form of a pharmaceutically acceptable salt of the free acid. Salts that are preferred include salts of a basic amino acid such as lysine or arginine. The basic amino acid forming the salt may be in the form of the L-isomer or in the form of the racemate. Also salts such as the methylglucamine salt are within the scope of the invention as well as pharmaceutically acceptable carboxylate-forming salts such as the alkali metal, alkaline earth metal and ammonium salts.

Administration of the water-soluble, pharmaceutically acceptable salt of ibuprofen is parenteral administration, preferably by intravenous, intramuscular or subcutaneous injection. The daily dosage of the ibuprofen salt is expressed in terms of the ibuprofen content and not in terms of the salt-forming acid administered to the prematurely born neonate is 1 to 20 mg/kg of body weight, preferably about 10 mg/kg of body weight per day. In order to have the best chance of preventing development of retinopathy of prematurity, the ibuprofen salt is preferably administered during the first month of life.

The ibuprofen salt is preferably administered to the premature neonates in 2 ml ampoules. The preferred concentration of the pharmaceutically acceptable ibuprofen salt is 1 to 20 mg, preferably 10 mg per ml of sterile aqueous solution calculated on the basis of the ibuprofen content only and not on the basis of the salt forming moiety as well.

A preferred course of administration of the ibuprofen or pharmaceutically effective salt thereof to a prematurely born neonate in need of such a treatment is carried out over three days. In the first day of treatment 10 mg of the ibuprofen salt in terms of the ibuprofen content are parenterally administered to the neonate per kg of body weight. One day later a second dose of the ibuprofen salt is administered, but the second dose is only 5 mg per kg of body weight. One day later still a third dose of the ibuprofen salt is administered, and the third dose is also 5 mg per kg of body weight. This course of administration may be repeated one or more times during the first month of life.

A typical composition for parenteral administration includes a vial or ampoule holding 20 mg of ibuprofen salt. The composition includes 20 mg of ibuprofen dissolved in 2 ml of distilled water. The composition may further include an excipient such as mannitol.

Claim 1 of 10 Claims

What is claimed is:

1. A method of preventing retinopathy of prematurity in a prematurely born neonate susceptible to developing retinopathy of prematurity, which comprises the step of parenterally administering to said prematurely born neonate, a therapeutically effective amount of a water-soluble, pharmaceutically effective salt of ibuprofen as an active ingredient to promote retinal and choroidal blood flow autoregulation and stimulate normal retinal development and retinal vascularity in said neonate.

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