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EP0403578B1 Expired / Lapsed EP ⏱️ 0.0 years remaining

Stable pharmaceutical composition

Assignee: Becton Dickinson Infusion Therapy UK
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Filing: 1989-05-04
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Granted: 1994-10-12
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Expires: 2009-05-04
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Abstract

Abstract An injectable, aqueous pharmaceutical composition for the treatment of cardiac conditions comprising an effective amount of methyl 3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride (esmolol) for treating such a cardiac condition, said composition comprising about 1 mg to 250 mg of esmolol per milliliter of said injectable pharmaceutical composition; 0.01 to 0.20 M buffer; said composition having a pH range of 4.5 to 5.5, the esmolol degrading in aqueous solution to produce 3-[4-(3-propionic acid)-phenoxy]-1-isopropylamino-2-propanol hydrochloride, said 3-[4-(3-propionic acid)-phenoxy]-1-isopropylamino-2-propanol hydrochloride having a pK in the pH range of said composition to thereby act as a secondary buffer to increase the buffer capacity and minimize the change in pH as degradation occurs, whereby the stability of esmolol in an aqueous composition is enhanced.

Inventors

  • 👤 Leonard S. Rosenberg
  • 👤 Cheryl K. Black
  • 👤 Earl R. Speicher
  • 👤 Dietmar M. Wagenknecht

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-25 23:54
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K31/00; A61K31/185; A61K31/19; A61K31/195; A61K31/21; A61K31/215; A61K47/00; A61K47/06; A61K47/08; A61K47/12; A61P; A61P25/00; A61P25/02; A61P9/00; A61P9/12

Claims Analysis

Total Claims: 8
Claim 1
Independent Claim 53 words
An injectable, aqueous pharmaceutical composition for the treatment of cardiac conditions comprising an effective amount of methyl 3-{4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl}propionate hydrochloride (esmolol) for treating such a cardiac condition, said composition comprising 1 mg to 250 mg of esmolol/mL of solution; 0.01 to 0.04 M buffer; said composition having a pH range of 4.5 to 5.5.
Claim 2
Dependent Claim 21 words
The composition of Claim 1 wherein the buffer is selected from the group comprising acetate, tartrate, lactate, gluconate and phosphate buffer.
Claim 3
Dependent Claim 11 words
The composition of Claim 2 wherein the buffer is acetate buffer.
Claim 4
Dependent Claim 10 words
The composition of Claim 3 including 10 mg/mL of solution.
Claim 5
Dependent Claim 14 words
The composition of Claim 4 wherein the concentration of acetate buffer is 0.05 M.
Claim 6
Dependent Claim 12 words
The composition of Claim 5 having a pH of 4.9 to 5.1.
Claim 7
Dependent Claim 49 words
A stable, injectable, aqueous pharmaceutical composition for the treatment of cardiac conditions comprising an effective amount of methyl 3-{4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl}propionate hydrochloride (esmolol) for treating such a cardiac condition, said composition comprising 10 mg of esmolol/mL of solution; 0.05 M buffer; said composition having a pH range of 4.5 to 5.5.
Claim 8
Dependent Claim 12 words
The composition of Claim 7 having a pH of 4.9 to 5.1.

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