COUGH SYRUP CONTAINING AMBROXOL HYDROCHLORIDE

Abstract

The present invention relates to cough syrups containing ambroxol hydrochloride, characterised in that they are substantially free from glycerol, and their use for mucolytic treatment in acute and chronic diseases of the bronchi and/or lungs.

Claims

1. A cough syrup containing ambroxol hydrochloride, characterised in that it is substantially free from glycerol.

2. The cough syrup according to claim 1, characterised in that it is also substantially free from sugar alcohols.

3. The cough syrup according to claim 1, also containing a suitable thickener.

4. The cough syrup according to claim 1, having a viscosity in the range from 1 mPa.Math.s to 30 Pa.Math.s at a temperature of 20 C.

5. The cough syrup according to claim 1, containing a suitable sweetener.

6. The cough syrup according to claim 5, present in an amount of 0.01 g to 10 g based on 100 ml of the cough syrup.

7. The cough syrup according to claim 1, having a water content of at least 77% by weight.

8. The cough syrup according to claim 1, consisting of: a) ambroxol hydrochloride in an amount of 0.1 g to 1.0 g, b) thickener in an amount of 0.01 g to 1.0 g, c) sweetener in an amount of 0.01 g to 10 g, d) preservative in an amount of 0 to 1.0 g and d) flavourings in an amount of 0 to 10 g and e) water ad 100 ml.

9. (canceled)

Description

EXAMPLES

[0042] In order to investigate their stability, two cough syrups according to the invention (composition (A) and (B)) and two compositions corresponding to standard commercial cough syrups (compositions (C) and (D)) were transferred into standard commercial brown glass bottles. The stability of the composition under controlled storage conditions (6 months at 40 C., 75% rel. humidity) was evaluated on the basis of the amount of three decomposition products of ambroxol hydrochloride present. For this purpose, the content of decomposition products (1) to (3) in the samples was determined by HPLC and UV detection.

TABLE-US-00001 (A) (B) (C) (D) Composition content [mg/ml] Ambroxol hydrochloride 3 6 3 3 Benzoic acid 0.5 0.5 1.7 1.7 Hydroxyethylcellulose 4 4 2 2 Acesulfame potassium 1 1 Sucralose 1 1.26 Sorbitol 350 350 (70% solution) Glycerol 150 150 (85% solution) (synthetic) (vegetable) Flavourings 4.4 4.8 2.2 2.4 Water ad 1 ml ad 1 ml ad 1 ml ad 1 ml

[0043] Decomposition product (1): Molecular weight: 424.6 g/mol

C.sub.14H.sub.16Br.sub.2N.sub.2O*HCl Total formula (empirical)

[0044] Decomposition product (2): Molecular weight: 426.6 g/mol;

C.sub.14H.sub.18Br.sub.2N.sub.2O*HCl Total formula (empirical)

[0045] Decomposition product (3): Molecular weight: 487.6 g/mol

C.sub.16H.sub.22Br.sub.2N.sub.2O.sub.3*HCl Total formula (empirical)

[0046] The results of this investigation are summarised below.

[0047] Composition (A)

TABLE-US-00002 Amount (based on 3 mg Decomposition product ambroxol hydrochloride/ml) A <0.05% B 0.07% C <0.05% Total 0.07%

[0048] Composition (B)

TABLE-US-00003 Amount (based on 6 mg Decomposition product ambroxol hydrochloride/ml) A <0.05% B <0.05% C <0.05% Total <0.05%

[0049] Composition (C) (Comparison example)

TABLE-US-00004 Amount (based on 3 mg Decomposition product ambroxol hydrochloride/ml) A 0.19% B 0.17% C 0.16% Total 0.52%

[0050] Composition (D) (Comparison example)

TABLE-US-00005 Amount (based on 3 mg Decomposition product ambroxol hydrochloride/ml) A 0.27% B 0.32% C 0.12% Total 0.71%

[0051] The test results show that the cough syrups according to the invention are distinguished from the standard commercial compositions containing ambroxol by a particularly low rate of decomposition of ambroxol hydrochloride.