You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 29, 2024

Claims for Patent: 5,540,930


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 5,540,930
Title: Suspension of loteprednol etabonate for ear, eye, or nose treatment
Abstract:The invention provides novel compositions of matter containing water-insoluble steroid drugs suitable for therapeutic use. The invention provides stable aqueous suspensions of water-insoluble steroid drugs of particle sizes of .ltoreq.15 .mu.m which remain in such a state so as to allow for immediate suspension, when desired, even after extended periods of settling.
Inventor(s): Guy; Yaacov J. (Rehovot, IL), Friedman; Doron I. (Carmei Yosef, IL)
Assignee: Pharmos Corporation (New York, NY)
Application Number:08/142,743
Patent Claims: 1. A composition for ophthalmic or otolaryngological anti-inflammatory use comprising:

(A) a corticosteroid having a particle size of 0.1 to 30 microns in diameter in an amount of about 0.2 to 2% by weight;

(B) a nonionic polymer in an aqueous medium;

(C) a nonionic surface active agent in an amount sufficient to retain the corticosteroid in suspension; and

(D) a nonionic tonicity agent in an amount sufficient to achieve isotonicity, wherein the molar ratio of (A):(B):(C) is between about 1:20:1 and about 1:0.01:0.5.

2. The composition of claim 1 wherein the corticosteroid is selected from the group consisting of soft steroids having anti-inflammatory activity.

3. The composition of claim 1 wherein the corticosteroid is loteprednol etabonate and is present in an amount of about 0.5 to 1% by weight.

4. The composition of claim 3 wherein said corticosteroid has a particle size less than about fifteen microns.

5. The composition of claim 1 further including a preservative for preventing microbial formation in said composition and in an amount of about 0.01 to 0.025% by weight.

6. The composition of claim 5 wherein said preservative is benzalkonium chloride.

7. The composition of claim 6 further comprising disodium edetate.

8. The composition of claim 1 wherein said nonionic polymer is selected from the group consisting of polyvinylpyrrolidone, polyvinyl alcohol, or dextran and is present in an amount of about 0.2 to 2% by weight and wherein the nonionic surfactant is present in an amount of about 0.05 to 1% by weight.

9. The composition of claim 1 wherein said nonionic polymer is polyvinylpyrrolidone and is present in an amount of about 0.4 to 1% by weight.

10. The composition of claim 1 wherein said nonionic surface active agent is tyloxapol and is present in an amount of about 0.1 to 0.6% by weight.

11. The composition of claim 1 further comprising an additional therapeutic drug in admixture with said corticosteroid, wherein said additional therapeutic drug is selected from the group consisting of betaxalol, athenolol, livobanolol, epinenephrin, dipivalyl, oxonolol, acetazilumide-base, methazalomide, tobramycin, gentamycin, piroxicam, indomethacin, naproxen, phenylbutazone, ibuprofen, and diclofenac-acid.

12. A composition for ophthalmic or otolaryngological anti-inflammatory use according to claim 1 in which the nonionic tonicity agent is glycerol in an amount 2 to 2.8%.

13. A composition for ophthalmic or otolaryngological anti-inflammatory use comprising a nonionic polymer in an aqueous medium, a nonionic tonicity agent in an amount effective to product isotonicity, and a nonionic surface active agent in an amount sufficient to retain the polymer and tonicity agent in the aqueous medium, and further comprising a corticosteroid having a particle size of 0.1 to 30 microns in diameter in an amount of about 0.2 to 2% by weight, wherein the molar ratio of corticosteroid to nonionic polymer to nonionic surface active agent is between about 1:20:1 and about 1:0.01:0.05.

14. The composition of claim 13 wherein said nonionic tonicity agent is a nonionic diol and is present in an amount of about 2 to 2.8% by weight.

15. The composition of claim 13 wherein the nonionic polymer is present in an amount of about 0.2 to 2% by weight; the nonionic tonicity agent is present in an amount of about 2 to 2.8% by weight; and the nonionic surface active agent is present in an amount of about 0.05 to 1% by weight.

16. The composition of claim 13 further comprising a preservative of benzalkonium chloride, disodium edetate, and mixtures thereof in an amount of about 0.01 to 0.025% by weight.

17. The composition of claim 13 wherein the nonionic polymer is polyvinyl pyrrolidone and is present in an amount of about 0.4 to 1% by weight, the nonionic tonicity agent is mannitol or a diol and is present in an amount of about 2 to 2.8% by weight, and the nonionic surface active agent is tyloxapol and is present in an amount of about 0.1 to 0.6% by weight.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.