USE FOR THE MANUFACTURE OF ORAL FORMS OF NADOLOL FOR TREATING GLAUCOMA

Abstract: Nadolol compositions are provided for treating glauco­ ma and for inhibiting the onset of migraine headaches.

Description: The present invention relates to the use of nadolol or an ester thereof or a pharmaceutically acceptable acid-addition salt for the preparation of drugs for oral administration for treating glaucoma or lowering intraocular pressure. The term "nadolol" as employed herein refers to the beta blocker 2,3-cis-1,2,3,4-tetrahydro-5-[2-hydroxy-3-(tert-butylamino)propoxy]-2,3-naphthalenediol (and pharmaceutically acceptable acid-addition salts thereof) which is disclosed in U.S. Patent Nos. 3,935,267 and 3,982,021. Esters or nadolol included herein are the mono-, di- and tri-esters (and pharmaceutically acceptable acid-addition salts thereof). The di-esters have the structure wherein both R₁ groups are acyl, preferably acetyl, and R₂ is hydrogen. Esters or nadolol wherein both R₁ groups are hydrogen and R₂ is acyl (mono-ester), preferably acetyl, and wherein both R₁ groups are acyl, preferably acetyl, and R₂ is acyl, preferably acetyl (tri-esters) are disclosed in British Patent Specification GB-A-1,559,987. In carrying out the method of the present invention, the nadolol or nadolol ester or a physiologically acceptable acid-addition salt may be administered to mammalian species, such as monkeys, dogs, cats and rats and as such may be incorporated in a conventional dosage form such as a tablet, capsule or elixir, along with the necessary carrier material, excipient, lubricant or buffer. Single or divided doses of about 8 to about 120 mg, preferably about 20 to 80 mg/one to four times daily may be administered in dosage forms as described above. Example 1 A nadolol formulation suitable for oral administration in the treatment of glaucoma is set out below. The nadolol is blended with the microcrystalline cellulose in a Hobart-type mixer for 5 minutes. Thereafter, the magnesium stearate is added with mixing for 2-3 minutes. The final mix is compressed in a Strokes D3 tablet press to form a 40 mg tablet which is used for treating glaucoma or reducing intraocular pressure.

Claims: The use of nadolol or an ester thereof or a pharmaceutically acceptable acid-addition salt for the preparation of drugs for oral administration for treating glaucoma or lowering intraocular pressure. The use as defined in claim 1 wherein said ester is a mono-, di- or tri-ester. The use as defined in claim 2 wherein said ester is a monoacetate, diacetate or triacetate. The use as defined in claim 1 wherein said nadolol or ester thereof is administered in a dosage of from about 8 to about 120 mg. The use as defined in claim 4 wherein said nadolol or ester thereof is administered in a dosage of from about 20 to about 80 mg. The use as defined in claim 1 wherein said nadolol or ester thereof is in the form of a pharmaceutically acceptable acid-addition salt thereof.

Inventors: MUIR, JOHN GORDON, SUDILOVSKY, ABRAHAM
Applicants: E.R. SQUIBB & SONS, INC.
Application year: 1982
Main classification: A61K31
IPC codes: A61K31