IP Library Granted Patent US 10,563,270
Granted Patent B2
US 10,563,270 · App. 15/558,871 · Granted Feb 18, 2020

Solid forms of menaquinols

Inventors: Davide Bianchi (Desio, IT); Simona Daly (Desio, IT); Niccolo Miraglia (Desio, IT); Antonella Trentin (Desio, IT); Federica Colzani (Desio, IT); Francesca Bollini (Desio, IT); Cesare Ponzone (Desio, IT)
Assignee: Gnosis S.p.A.
C12R1/07A61K31/05C07C37/07C07C37/84C07C39/225C12P7/22C12R1/185C12R1/38
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Quick Facts
Patent No.
US 10,563,270
App. No.
15/558,871
Granted
Feb 18, 2020
Kind
B2
Abstract

Disclosed are solid forms of menaquinol and processes for obtaining them by chemical or enzymatic reduction of menaquinone. Said solid forms possess high stability to oxidation which allows effective use of menaquinol in the most common formulations wherein vitamin K2 is used.

Claims (12)

1. A process for the preparation of a crystalline form of menaquinol of formula (II)

wherein n is 0 or an integer from 1 to 11, comprising the following steps:

a) reducing menaquinone of formula (I)

wherein n is as defined above, in a biphasic system consisting of a water-immiscible solvent and an aqueous solution of sodium dithionite;

b) removing said solvent by evaporation to provide an aqueous phase;

c) Cooling and filtering the aqueous phase obtained in step b) at a temperature lower than 25° C., to give a crystalline form of menaquinol of formula (II).

2. The process of claim 1 wherein step a) is performed at a temperature between 2° C. and 75° C.

3. The process of claim 1 wherein the solution of sodium dithionite has a pH ranging between 3 and 8.

4. The process of claim 1 , further comprising washing of the crystalline form obtained in step c) with a solution of ascorbic acid followed by drying of the crystals at a temperature not exceeding 40° C.

5. The process of claim 1 wherein, in the compound of formula (II), n is 6.

6. The process of claim 1 wherein, in the compound of formula (II), n is 3.

7. A pharmaceutical or nutraceutical composition containing the product obtained from the process of claim 1 and a carrier.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 21, 2018
From: BIANCHI, DAVIDE; DALY, SIMONA; MIRAGLIA, NICCOLO; TRENTIN, ANTONELLA; COLZANI, FEDERICA; BOLLINI, FRANCESCA; PONZONE, CESARE
To: GNOSIS S.P.A.
Reel/Frame 045302/0463 →
Priority Claims (1)
IT 10201509450 · Mar 20, 2015 · national
Continuity (1)
Related Publication 20180066326A1 · Mar 8, 2018