EP0045655A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Solubilization of ivermectin in water
Assignee: Merck and Co Inc
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Filing: 1981-08-03
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Granted: —
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Expires: 2001-08-03
Abstract
Abstract lvermectin, 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 water-miscible organic 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 Albert Lo
- 👤 James B. Williams
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-01 19:30
CPC Classifications
A; A61; A61K; A61K47/00; A61K9/00; A61K9/10; A61K9/107; A61K9/1075; A61K31/00; A61K31/33; A61K31/335; A61K31/35; A61P; A61P33/00; A61P33/10
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
41 words
A stabilized aqueous formulation comprising Ivermectin in a solution of a surface-active agent and water and including one or more water-miscible organic cosolvents suitable for parenteral or oral administration, and/or one or more substrates also suitable for parenteral or oral administration.
Claim 2
Dependent Claim
41 words
A stabilized aqueous formulation comprising Ivermectin in a solution of a surface-active agent and water and including one or more water-miscible organic cosolvents suitable for parenteral or oral administration, and/or one or more substrates also suitable for parenteral or oral administration.
Claim 3
Dependent Claim
56 words
A formulation as claimed in Claim 1 that contains from 0.1 to 7.5% w/v of Ivermectin for parenteral administration or from 0.01 to 2.0% w/v of Ivermectin for oral administration; from 4 to 25% w/v of the surface-active agent; from 10 to 40% v/v of the cosolvent; and from 1 to 5% w/v of the substrate.
Claim 4
Dependent Claim
50 words
A formulation as claimed in Claim 1 or 2, in which the surface-active agent is a polyoxyethylated vegetable oil, polyoxyethylene sorbitan monoisostearate, polyoxyethylene sorbitan monostearate or polysorbate 80; the cosolvent is glycerol formal, propylene glycol, glycerine, or polyethylene glycol; and the substrate from benzyl alcohol, lidocaine, a paraben, or choline.
Claim 5
Dependent Claim
18 words
A formulation as claimed in Claim 1, in which a cosolvent is present but no substrate is included.
Claim 6
Dependent Claim
63 words
A formulation as claimed in Claim 4 containing from 0.1 to 7.5% w/v of Ivermectin for parenteral administration or from 0.01 to 2.0% w/v of Ivermectin for oral administration, from 4 to 25% w/v of a polyethylated vegetable oil, polyoxyethylene sorbitan monoisostearate, polyoxyethylene sorbitan monostearate or polysorbate 80; and from 10 to 40% v/v of glycerol formal, propylene glycol, glycerine or polyethylene glycol.
Claim 7
Dependent Claim
18 words
A formulation as claimed in Claim 1, in which a substrate is present but no cosolvent is included.
Claim 8
Dependent Claim
66 words
A formulation as claimed in Claim 6 comprising from 0.1 to 7.5% w/v of Ivermectin for parenteral administration or from 0.01 to 2.0% w/v of Ivermectin for oral administration; from 4 to 25% w/v of a polyoxyethylated vegetable oil, polyoxyethylene sorbitan monoisostearate, polyoxyethylene sorbitan monostearate or polysorbate 80; and from 1 to 5% w/v of one or more of benzyl alcohol, lidocaine, a paraben, or choline.
Claim 9
Dependent Claim
70 words
A process for preparing a stabilized aqueous formulation containing Ivermectin, which comprises dissolving Ivermectin in a surface-active agent containing one or both of (1) a cosolvent comprising one or more water-miscible organic solvents suitable for parenteral administration and (2) one or more of a substrate suitable for parenteral or oral administration; adding water to the thus prepared solution to make up the desired volume and adjusting the pH if necessary.
Claim 10
Dependent Claim
70 words
A process for preparing a stabilized aqueous formulation containing Ivermectin, which comprises dissolving Ivermectin in a surface-active agent containing one or both of (1) a cosolvent comprising one or more water-miscible organic solvents suitable for parenteral administration and (2) one or more of a substrate suitable for parenteral or oral administration; adding water to the thus prepared solution to make up the desired volume and adjusting the pH if necessary.
Claim 11
Dependent Claim
35 words
A process as Claimed in Claim 8, in which the final solution has a pH adjusted to be in the range 6 to 6.5 and is a solution as claimed in Claim 2 or 3.
Claim 12
Dependent Claim
35 words
A process as claimed in Claim 9, in which the surface-active agent is polysorbate 80, the cosolvent is glycerol formal or propylene glycol and the substrate is one or both of benzyl alcohol or lidocaine.
References Cited (Backward Citations)
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