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Claims for Patent: 5,482,931

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Claims for Patent: 5,482,931

Title: Stabilized pharmaceutical peptide compositions
Abstract:Disclosed is a stabilized aqueous composition for administration to a patient comprising a biologically active peptide, a buffer, a quaternary amine-type preservative or disinfectant, and an osmotic pressure-controlling agent, which composition can be stored and used at room temperature. The buffer stabilizes the pH of the composition between about 4 and 6. The preferred buffer contains citrate and/or phosphate, and the preferred preservative or disinfectant is benzalkonium chloride. The composition protects the peptide contained therein from adhering to container surfaces, particularly in containers made of polymeric materials.
Inventor(s): Harris; Alan (Malmo, SE), Tennhammar-Ekman; Birgitta (Malmo, SE)
Assignee: Ferring AB (Malmo, SE)
Application Number:08/084,563
Patent Claims: 1. A stable, aqueous composition for administration to a patient of at least one biologically active peptide, consisting essentially of:

a) said biologically active peptide selected from the group consisting of oxytocin, vasopressin, an oxytocin analog, an oxytocin derivative, a vasopressin analog, and a vasopressin derivative;

b) a buffering agent;

c) a quaternary amine preservative or disinfectant; and

d) an osmotic pressure-controlling agent.

2. The composition according to claim 1, wherein said peptide is selected from the group consisting of terlipressin, atosiban, carbetocin, and triptorelin.

3. The composition according to claim 1, wherein said vasopressin analog is desmopressin.

4. The composition according to claim 1, wherein said buffering agent is a buffer which maintains the pH of said composition between 4.0 and 6.0.

5. The composition according to claim 4, wherein said buffer maintains said pH at about 5.0.

6. The composition according to claim 1, wherein said buffering agent comprises a buffer selected from the group consisting of citrate, phosphate, and a mixture of citrate and phosphate.

7. The composition according to claim 6, wherein said buffer mixture of citrate and phosphate contains sodium ions such that the molar ratio of citrate, phosphate and sodium ions is from about 1:3:3 to about 1:1:2.

8. The composition according to claim 1, wherein said quaternary amine preservative or disinfectant is benzalkonium chloride having the following structure:

where R.sup.1 and R.sup.2 are both methyl; R.sup.3 is benzyl; and R.sup.4 can be an alkyl group from C.sub.8 H.sub.17 to C.sub.18 H.sub.37.

9. The composition according to claim 1, wherein said administration is oral.

10. The composition according to claim 1, wherein said administration is parenteral.

11. An aqueous composition for nasal administration of a biologically active component, consisting essentially of:

a) said biologically active component selected from the group consisting of a peptide selected from the group consisting of oxytocin, vasopressin, an oxytocin analog, an oxytocin derivative, a vasopressin analog, and a vasopressin derivative;

b) a buffering agent;

c) a quaternary amine preservative of disinfectant; and

d) an osmotic pressure-controlling agent such the said composition is capable of maintaining said biologically active component in a functionally stable condition over extended periods and at room temperature.

12. The composition of claim 11, wherein said vasopressin analog is desmopressin.

13. The composition according to claim 11, wherein said buffering agent is a buffer which maintains the pH of said composition between 4.0 and 6.0.

14. The composition according to claim 13, wherein said buffer maintains said pH at about 5.0.

15. The composition of claim 11, wherein said buffering agent comprises a buffer selected from the group consisting of citrate, phosphate, and a mixture of citrate and phosphate.

16. The composition of claim 15, wherein said buffer comprises a mixture of citrate and disodium hydrogen phosphate such that the molar ratio of citrate, phosphate and sodium ions is from about 1:3:3 to about 1:1:2.

17. The composition according to claim 11, wherein said quaternary amine preservative or disinfectant is benzalkonium chloride having the following structure:

where R.sup.1 and R.sup.2 are both methyl; R.sup.3 is benzyl; and R.sup.4 can be an alkyl group from C.sub.8 H.sub.17 to C.sub.18 H.sub.37.

18. A stable aqueous composition for nasal application, comprising:

a) from 0.025 mg to 1.5 mg of desmopressin acetate;

b) from 1.35 mg to 1.75 mg of citric acid;

c) from 2.25 mg to 2.65 mg of disodium hydrogen phosphate;

d) from 0.05 mg to 0.20 mg of benzalkonium chloride; and

e) sodium chloride in an amount sufficient to provide said composition with an osmotic pressure comparable to that of human plasma.

19. The stable, aqueous composition of claim 1, wherein said buffering agent can also function as said osmotic pressure-controlling agent.

20. The stable, aqueous composition of claim 1, wherein said buffering agent in combination with sodium chloride can also function as said osmotic pressure-controlling agent.

21. The aqueous composition of claim 11, wherein said buffering agent can also function as said osmotic pressure-controlling agent.

22. The aqueous composition of claim 11, wherein said buffering agent in combination with sodium chloride can also function as said osmotic pressure-controlling agent.
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