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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

Inactive Publication Date: 2017-07-07
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The disadvantages of protein and polypeptide drugs, such as large molecular weight, poor stability, low bioavailability, short biological half-life in vivo, and easy decomposition by enzymes in vivo, limit their application in the field of therapeutics.
Due to the short half-life of terlipressin, the existing technology overcomes ordinary injections by preparing the drug into long-term circulating liposomes, but the action time of ordinary liposomes in the body is relatively short

Method used

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  • Terlipressinlipidosome and preparation method thereof
  • Terlipressinlipidosome and preparation method thereof
  • Terlipressinlipidosome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Dissolving 500 mg of the drug terlipressin in 20 mL of the aqueous phase to obtain an aqueous phase containing the active ingredient;

[0050] DSPE-PEG20002g was dissolved in 20mL of chloroform (oil phase), placed in a round bottom flask, and the organic phase was removed by rotary evaporation;

[0051] Add the water phase, prepare the pH between sodium bicarbonate and sodium hydroxide to be between 8.0, vortex to obtain rough liposomes, first homogenize and then pass through a 0.22 μm filter membrane, and use the dialysis membrane method to remove the free water phase, Promptly obtain the liposome solution of medicine.

Embodiment 2

[0053] Dissolving 5 mg of the drug terlipressin in 20 mL of the aqueous phase to obtain an aqueous phase containing the active ingredient;

[0054] 2g of PEG-PE and 1g of cholesterol were dissolved in 20mL of chloroform (oil phase), placed in a round bottom flask, and the organic phase was removed by rotary evaporation;

[0055] Add the water phase, the pH prepared by ammonium sulfate, sodium hydroxide, and sucrose is between 8.4 and 8.5, vortex to obtain rough liposomes, first homogenize and then pass through a 0.22 μm filter membrane, and use the dialysis membrane method to remove free liposomes Aqueous phase, promptly obtains the liposome solution of medicine.

Embodiment 3

[0057] Dissolving 5 mg of the drug terlipressin in 20 mL of the water phase to obtain the water phase;

[0058] Dissolve 2g of DSPE-PEG2000 and 1g of cholesterol in 20mL of chloroform (oil phase), put in a round bottom flask, and remove the organic phase by rotary evaporation;

[0059] Add the water phase, the pH prepared by sodium carbonate and citric acid is between 7.9 and 8.0, vortex to obtain rough liposomes, first homogenize and then pass through a 0.22 μm filter membrane, and use the dialysis membrane method to remove the free water phase. Promptly obtain the liposome solution of medicine.

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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.

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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Application Information

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IPC IPC(8): A61K38/11A61K9/127A61P7/04A61P1/16A61P7/10A61P9/00A61P17/02A61K38/095
CPCA61K38/095A61K9/127
Inventor 张伟明颜携国陶安进袁建成
Owner HYBIO PHARMA
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