Terlipressinlipidosome and preparation method thereof

A technology of terlipressin and liposomes, which is applied in liposome delivery, pharmaceutical formulations, peptide/protein components, etc., can solve the problem of short half-life, low bioavailability, and short biological half-life of terlipressin, etc. problems, to achieve the effect of low incidence of adverse reactions, stable blood concentration and long action time
CN106924715AInactive Publication Date: 2017-07-07HYBIO PHARMA

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
HYBIO PHARMA
Publication Date
2017-07-07
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to the field of medicines, in particular to terlipressinlipidosome and a preparation method thereof. The invention provides the terlipressinlipidosome, and the pH value of the internal water phase thereof is 7.9 to 8.9. The lipidosomepreparation overcomes the defect that the medicine action time is short. The isoelectric point of the terlipressin is weakly alkaline, the internal pH value of the lipidosome is adjusted to be weakly alkaline, the medicine is deposited under the weakly alkaline condition, and the medicine can be slowly released, so that a bettersustained release effect is achieved. The lipidosome provided by the invention can maintain long action time, the plasma concentration is stable and the occurrence rate of adverse effects is low.
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Description

technical field

[0001] The invention relates to the field of medicines, in particular to a terlipressin liposome and a preparation method thereof. Background technique

[0002] Terlipressin, triglycyllysine vasopressin acetate, is a novel synthetic analogue of vasopressin. Produced and marketed by the Swedish company Ferring in the early 1980s, it is a prodrug of vasopressin. After injection into the blood, the glycyl group in the molecule is hydrolyzed by enzymes to produce a sustained low level of vasopressin. Its chemical name is N-α-triglycyl-8-lysine-vasopressin, and its structure is shown in Formula I:

[0003]

[0004] It is mainly used for hemostasis of hemorrhage from cirrhotic varices, and is now widely used in the treatment of hepatorenal syndrome, cirrhotic ascites, septic shock, burns, acute liver failure, and cardiac arrest. For Hanwei currently on the market, the initial injection dosage is 2mg. Dissolve each 1 mg of injection powder with 5 ml of sodium ...

Claims

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