# US 5,350,582 A · Stable formulation of enalapril salt, a process for the preparation thereof and the use thereof

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- Number: US 5,350,582 A
- Document ID: US5350582A
- Status: Granted
- Kind: A
- Application number: 07/980,956
- Filed: 1992-11-24
- Granted: 1994-09-27
- Earliest claimed: 1991-11-25
- Assignees: KRKA, tovarna zdravil, p.o.
- Inventors: Marjo Merslavic; Jozica Razen; Ales Rotar
- Web page: https://patentgrep.com/patent/US5350582A

## CPC

- A61K 38/556: {Angiotensin converting enzyme inhibitors}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

There is disclosed a stable formulation of enalapril salt of the formula I ##STR1## which is prepared in such manner that a compound of formula II ##STR2## is suspended in demineralized water and a stoichiometric amount of the corresponding sodium compound such as sodium carbonate, sodium hydrogen carbonate or sodium hydroxide is added thereto, to this enalapril sodium salt prepared in situ of the formula I ##STR3## formulating additives are added, the whole is homogenized and formulated.

## Claims

### Claim 1

Process for preparing stable formulation of enalapril sodium salt of the formula I ##STR7## characterized in that enalapril mileate of formula II ##STR8## is suspended in demineralized water and a stoichiometric amount of the corresponding sodium compound selected from the group consisting of sodium carbonate, sodium hydrogen carbonate and sodium hydroxide is added thereto, to this enalapril sodium salt prepared in situ of the formula I ##STR9## formulating additives are added, the whole is homogenized and formulated.

### Claim 2 (depends on 1)

Stable formulation of enalapril sodium salt obtained according to the process of claim 1.

### Claim 3 (depends on 2)

Formulation according to claim 2, characterized in that it is in the form of a tablet.

### Claim 4 (depends on 1)

Pharmaceutical composition comprising an effective amount of enalapril sodium of formula 1 ##STR10## obtained in accordance with the process of claim 1.

### Claim 5 (depends on 1)

A method for treating cardiovascular disease which comprises administering to a patient suffering from cardiovascular disease a pharmaceutical composition comprising an effective amount for treating cardiovascular disease of enalapril sodium of formula 1 ##STR11## obtained in accordance with the process of claim 1.

### Claim 6 (depends on 5)

The method of claim 5 wherein said cardiovascular disease is hypertension.

### Claim 7 (depends on 5)

The method of claim 5 wherein said pharmaceutical composition is a tablet.

### Claim 8 (depends on 7)

The method of claim 7 wherein said tablet contains 2 to 16 mg of said enalapril sodium.

### Claim 9 (depends on 5)

The method of claim 5 wherein the daily dosage of said enalapril sodium is 4 to 64 mg.

### Claim 10 (depends on 1)

The process of claim 1 which further comprises drying at 40.degree. C. to 50.degree., subsequent to adding said sodium compound.

### Claim 11 (depends on 4)

The composition of claim 4 being in the form of a tablet.

### Claim 12 (depends on 11)

The composition of claim 11 wherein said tablet contains 2 to 16 mg of said enalapril sodium.

### Claim 13 (depends on 4)

The composition of claim 4 which further comprises at least one member selected from the group consisting of cellulose, lactose, alcohol, acid, base, dyestuff, starch, talc, polyvinyl pyrolidone and magnesium stearate.