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Claims for Patent: 5,674,850

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Claims for Patent: 5,674,850

Title: High purity desmopressin produced in large single batches
Abstract:A process for the manufacture of high purity desmopressin produced in single batches of substantial size and a method of treating diabetes insipidus with the high purity desmopressin produced therefrom.
Inventor(s): Larsson; Krister (Malmo, SE), Mellbrand; Thomas (Malmo, SE), Mornstam; Birgitta (Bunkeflostrand, SE), Roschester; Jan (Lund, SE), Skoldback; Jan-Ake (Malmo, SE)
Assignee: Ferring AB (Malmo, SE)
Application Number:08/524,761
Patent Claims: 1. A process for production of single batches of desmopressin having a weight of at least about 500 g containing at least 98.5% by weight of desmopressin (C.sub.46 H.sub.64 N.sub.14 O.sub.12 S.sub.2) in respect of other adjoining matter than water and acetic acid, consisting of a final synthetic step, in which at least about 1 kg of mercapto-propionyl-Tyr-Phe-Gln-Asn-Cys-Pro-D-Arg-Gly-NH.sub.2 (SEQ ID NO: 2) or a derivative thereof, said derivative being stable at neutral or slightly acidic conditions, are dissolved in a protic solvent at neutral or slightly acidic conditions to form a reactant solution into which a second solution of iodine in a protic solvent or solvent mixture is introduced under agitation to form a reactant/reagent solution in which desmopressin is being formed.

2. A single batch of desmopressin produced according to the method of claim 1, said batch having a size of at least about 50 g, containing at least 44 g of desmopressin (C.sub.46 H.sub.64 N.sub.14 O.sub.12 S.sub.2) .

3. The desmopressin batch according to claim 2 containing no more than a total of 1.5% of adjoining matter other than acetic acid and water.

4. A single batch of desmopressin produced according to the method of claim 1, said batch having a size of at least about 100 g, containing at least 98.5% by weight of desmopressin (C.sub.46 H.sub.64 N.sub.14 O.sub.12 S.sub.2) in respect of adjoining matter other than water and acetic acid.

5. A single batch of desmopressin produced according to the method of claim 1, said batch having a size of at least about 100 g, containing at least 88 g of desmopressin (C.sub.46 H.sub.64 N.sub.14 O.sub.12 S.sub.2) containing no more than a total of 1.5% by weight of adjoining matter other than acetic acid and water.

6. A single batch of desmopressin produced according to the method of claim 1, said batch having a size of at least about 500 g and containing at least 440 g of desmopressin (C.sub.46 H.sub.64 N.sub.14 O.sub.12 S.sub.2) and containing no more than a total of 1.5% by weight of adjoining matter other than acetic acid and water.

7. The process according to claim 1, wherein the amount of iodine is at least about stoichiometric in respect of said mercaptopropionyl-Tyr-Phe-Gln-Asn-Cys-Pro-D-Arg-Gly-NH.sub.2 (SEQ ID NO: 2) or derivative thereof.

8. The process according to claim 1, wherein upon substantial completion of the desmopressin-forming reaction the reactant/reagent solution is applied to a separation column containing cation exchange resin equilibrated with acid, desmopressin is eluted, and the eluted desmopressin is isolated.

9. The process of claim 8, wherein desmopressin is eluted with a buffered solution comprising ammonium acetate and acetic acid.

10. The process of claim 8, wherein the cation exchange resin is a resin based on cross-linked agarose substituted with methylsulfonyl groups.

11. The process of claim 1, wherein said derivative is .beta.-acetamido-metylmercapto-propionyl-Tyr-Phe-Gln-Asn-Cys-(S-acetamido- methyl)-Pro-D-Arg-Gly-NH.sub.2 (SEQ ID NO: 1).

12. A single oral dose from 25 to 2,000 .mu.g of desmopressin (C.sub.46 H.sub.64 N.sub.14 O.sub.12 S.sub.2) for producing a physiological effect for the treatment of diabetes insipidus, hemophilia A and von Willebrand's disease, said dose prepared from a batch obtained by a process for producing single batches of desmopressin having a weight of at least about 500 g containing at least 98.5% by weight of said desmopressin (C.sub.46 H.sub.64 N.sub.14 O.sub.12 S.sub.2) in respect of adjoining matter other than water and acetic acid, said process consisting of a final synthetic step in which at least about 1 kg of mercapto-propionyl-Tyr-Phe-Gln-Asn-Cys-Pro-D-Arg-Gly-NH.sub.2 SEQ ID NO: 2) or a derivative thereof, said derivative being stable at neutral or slightly acidic conditions, is dissolved in a protic solvent at neutral or slightly acidic conditions to form a reactant solution into which a second solution of iodine in a protic solvent or solvent mixture is introduced under agitation to form a reactant/reagent solution in which desmopressin is being formed.

13. A single oral dose from 25 to 2,000 .mu.g of desmopressin (C.sub.46 H.sub.64 N.sub.14 O.sub.12 S.sub.2) effective to produce a physiological effect for treatment of diabetes insipidus, hemophilia A, and von Willebrand's disease, said dose prepared from a single batch containing no less than 44 g of desmopressin (C.sub.46 H.sub.64 N.sub.14 O.sub.12 S.sub.2) and no more than a total of 1.5% by weight of adjoining matter with respect to desmopressin (C.sub.4 H.sub.64 N.sub.14 O.sub.12 S.sub.2) other than water and acetic acid.

14. A single dose for intranasal administration of an amount of desmopressin effective to produce a physiological effect for the treatment of diabetes insipidus, hemophilia A, and von Willebrand's disease, said desmopressin obtained from a desmopressin batch prepared by the process according to claim 1.

15. The single dose of claim 14, wherein the dose size is from 5 to 200 .mu.g desmopressin (C.sub.46 H.sub.64 N.sub.14 OS.sub.2).
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