US4857552A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Stable pharmaceutical composition
Assignee: Datex Ohmeda Inc
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Filing: 1988-06-08
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Granted: 1989-08-15
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Expires: 2008-06-08
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 0.02M 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)-phenoxyl]-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 Black
- 👤 Earl R. Speicher
- 👤 Dietmar Wagenknecht
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 05:17
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: 10
Claim 1
Independent Claim
118 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]phenylpropionate hydrochloride (esmolol) for treating such a cardiac condition, said composition comprising about 1 mg to about 250 mg of esmolol/mL of solution; 0.01 to 0.04 M buffer; said composition having a pH range of about 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 without the addition of buffer and minimize the change in pH as degradation occurs, whereby the stability of esmolol in an aqueous composition is enhanced.
Claim 2
Dependent Claim
118 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]phenylpropionate hydrochloride (esmolol) for treating such a cardiac condition, said composition comprising about 1 mg to about 250 mg of esmolol/mL of solution; 0.01 to 0.04 M buffer; said composition having a pH range of about 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 without the addition of buffer and minimize the change in pH as degradation occurs, whereby the stability of esmolol in an aqueous composition is enhanced.
Claim 3
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 4
Dependent Claim
11 words
The composition of claim 2 wherein the buffer is acetate buffer.
Claim 5
Dependent Claim
11 words
The composition of claim 3 including about 10 mg/mL of solution.
Claim 6
Dependent Claim
15 words
The composition of claim 4 wherein the concentration of acetate buffer is about 0.05 M.
Claim 7
Dependent Claim
14 words
The composition of claim 5 wherein a pH of about 4.9 to about 5.1.
Claim 8
Dependent Claim
114 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]phenylpropionate hydrochloride (esmolol) for treating such a cardiac condition, said composition comprising about 10 mg of esmolol/mL of solution; about 0.05 M buffer; said composition having a pH range of about 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 without the addition of buffer and minimize the change in pH as degradation occurs, whereby the stability of esmolol in an aqueous composition is enhanced.
Claim 9
Dependent Claim
114 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]phenylpropionate hydrochloride (esmolol) for treating such a cardiac condition, said composition comprising about 10 mg of esmolol/mL of solution; about 0.05 M buffer; said composition having a pH range of about 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 without the addition of buffer and minimize the change in pH as degradation occurs, whereby the stability of esmolol in an aqueous composition is enhanced.
Claim 10
Dependent Claim
14 words
The composition of claim 7 having a pH of about 4.9 to about 5.1.
References Cited (Backward Citations)
US4454154A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-08-14 | 1993-02-13 | 1993-08-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-08-14 | 1997-02-13 | 1997-08-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-08-14 | 2001-02-13 | 2001-08-15 | $7700.00 | Window Closed / Lapsed |