Ocular insert housing steroid in two different therapeutic forms

• US 4,304,765 A
• Filed: 10/14/1980
• Issued: 12/08/1981
• Est. Priority Date: 10/14/1980
• Status: Expired due to Term

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Shell, John W., Gale, Robert M.
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/196,608
• Time in Patent Office: 420 Days
• Field of Search: 424/14, 424/19-22, 424/239
• US Class Current: 424/427
• CPC Class Codes: A61K 9/0051 Ocular inserts, ocular implants

Abstract

An ocular insert and an ocular composition are disclosed. The insert and the composition comprises a steroid in two different forms.

Claims

1. An ocular therapeutic insert sized, shaped and adapted for easy insertion and comfortable retention in an eye, the insert comprising a reservoir formed of non-toxic polymer, and a medication in the reservoir, said medication comprising a dosage amount of a pharmaceutically acceptable steroid selected from the group consisting of corticosteroids, glucocorticoid and antiinfammatory steroids, said steroid present in the insert in two different pharmaceutic and chemical forms selected from an alcohol and ester, alcohol and ether, ester and ether, acetal and ester and ester and ester, that are dispensed from the insert in a therapeutically effective amount to the tear fluid, with the amount of one form of the steroid dissolved in the fluid being independent of the amount of the different form of the same steroid dissolved in the fluid and their rate of penetration into eye tissue, which leads to a therapeutic and beneficial effect over a prolonged period of time.

2. The ocular therapeutic insert for dispensing the medication comprising the same steroid in two different forms according to claim 1, wherein the reservoir is a polymeric matrix.

3. The ocular therapeutic insert for dispensing the medication comprising the same steroid in two different forms according to claim 1, wherein the reservoir is a container and the medication is present therein.

4. The ocular therapeutic insert for dispensing the medication comprising the same steroid in two different forms according to claim 1 wherein the reservoir comprises depots of the medication dispersed in and surrounded substantially individually by the polymeric material.

5. The ocular therapeutic insert according to claim 1 wherein the same steroid in the insert comprises betamethasone acetate and betamethasone valerate.

6. The ocular therapeutic insert according to claim 1 wherein the same steroid in the insert comprises dexamethasone and dexamethasone sodium phosphate.

7. The ocular therapeutic insert according to claim 1 wherein the same steroid in the insert comprises triamcinolone and triamcinolone acetonide.

8. The ocular therapeutic insert according to claim 1 wherein the same steroid in the insert is selected from the group consisting of hydrocortisone and hydrocortisone acetate, hydrocortisone sodium phosphate and hydrocortisone sodium succinate, and hydrocortisone and hydrocortisone cyclopentylpropionate.

9. The ocular therapeutic insert according to claim 1 wherein the same steroid in the insert is selected from the group consisting of prednisolone and prednisolone acetate, prednisolone sodium phosphate and prednisolone sodium succinate, methylprednisolone and methylprednisolone acetate.

10. The ocular therapeutic insert according to claim 1 wherein the same steroid in the insert in fluormetholone and fluormetholone acetate.

11. A method for treating ocular inflammation which method comprises positioning in the eye the ocular insert of claim 1, said insert releasing the same steroid in two different forms to the eye in a therapeutically effective amount for treating said inflammation.

12. A method for treating diseases of the eye, which method comprises placing in the eye the ocular insert of claim 1, and releasing a dosage unit amount of same steroid in two different forms to the eye in a therapeutically effective amount for treating the diseases of the eye.