US4389397A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Solubilization of ivermectin in water
Assignee: Merck and Co Inc
•
Filing: 1981-09-21
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Granted: 1983-06-21
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Expires: 2001-09-21
Abstract
Abstract Ivermectin, an antiparasitic agent which is insoluble and unstable in water, is solubilized by the formation of colloidal particles, called micelles, with surface active agents as solubilizers and stabilized by using cosolvents and/or appropriate substrates in the aqueous formulation. The liquid formulations are suitable for use as parenteral or oral administration for the treatment of parasitic infections.
Inventors
- 👤 Pak-Kan A. Lo
- 👤 James B. Williams
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 14:02
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/335; A61K31/35; B; B82; B82Y; B82Y5/00
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
80 words
A stabilized aqueous formulation which comprises from 0.1 to 7.5% w/v of an avermectin for parenteral administration or from 0.01 to 2.0% w/v of an avermectin for oral administration; from 0.5 to 2.5% of a surface active agent selected from polyoxyethylene sorbitan monoisostearate, polyoxyethylene sorbitan monostearate and polysorbate 80; from 10 to 60% of a cosolvent selected from glycerol formal, glycerine and polyethyleneglycol; and from 1 to 5% w/v of a substrate selected from benzyl alcohol, lidocaine, parabens and choline.
Claim 2
Dependent Claim
80 words
A stabilized aqueous formulation which comprises from 0.1 to 7.5% w/v of an avermectin for parenteral administration or from 0.01 to 2.0% w/v of an avermectin for oral administration; from 0.5 to 2.5% of a surface active agent selected from polyoxyethylene sorbitan monoisostearate, polyoxyethylene sorbitan monostearate and polysorbate 80; from 10 to 60% of a cosolvent selected from glycerol formal, glycerine and polyethyleneglycol; and from 1 to 5% w/v of a substrate selected from benzyl alcohol, lidocaine, parabens and choline.
Claim 3
Dependent Claim
12 words
A stabilized aqueous formulation of claim 1 wherein the avermectin is ivermectin.
Claim 4
Dependent Claim
31 words
The stabilized aqueous formulation of claim 1 wherein the surface active agent is present at from 4 to 25% w/v and the cosolvent is present at from 10 to 40% v/v.
Claim 5
Dependent Claim
28 words
The stabilized aqueous formulation of claim 2 wherein the surface active agent is polysorbate 80; the cosolvent is glycerol formal; and the substrate is benzyl alcohol or lidocaine.
Claim 6
Dependent Claim
13 words
The stabilized aqueous formulation of claim 1 which is prepared for parenteral administration.
Claim 7
Dependent Claim
13 words
The stabilized aqueous formulation of claim 1 which is prepared for oral administration.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1986-06-20 | 1986-12-20 | 1987-06-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-06-20 | 1990-12-20 | 1991-06-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-06-20 | 1994-12-20 | 1995-06-21 | $7700.00 | Window Closed / Lapsed |