Selexipag polycystic lipidosome and preparation method thereof

A technology of multivesicular liposomes and Siripag, which is applied in the field of preparing Siripag multivesicular liposomes, can solve the problems of long-term medication, large fluctuations in blood drug concentration, and reduced patient compliance, etc., and achieve prolonged The effect of drug action time, reducing the number of medications, and prolonging the drug effect time

Active Publication Date: 2018-03-20
JIANGSU ALICORN PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its short half-life, patients need to take medicine for a long time, which reduces patient compliance
In addition, the drug needs to be taken for a long time in clinical treatment, and frequent administration for a long time brings inconvenience to the patient, and the blood drug concentration in the body fluctuates greatly, which is easy to cause toxic and side effects

Method used

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  • Selexipag polycystic lipidosome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Step 1: Accurately weigh 150mg of soybean lecithin, 15mg of cholesterol, and 70mg of triolein, dissolve it in chloroform-ether (volume ratio 1:1) to 5ml, and use it as the oil phase.

[0037] Step 2: Accurately weigh 2 mg of Siripag, 200 mg of sodium lauryl sulfate, and 200 mg of sucrose, and add 5 ml of water for ultrasonic dissolution as the inner water phase.

[0038] Step 3: Slowly add the above-mentioned internal water phase to the upper layer of the oil phase, and shear with a high-speed shear homogenizer for 5 minutes at 15,000 rpm to obtain W / O type colostrum.

[0039] Step 4: Add the colostrum prepared in step 3 to 30ml of the external aqueous phase containing 30mg of sodium chloride and 6mg of arginine, and cut it with a high-speed shear homogenizer for 1min at 5000rpm to form W / O / W Double milk.

[0040] Step 5: Transfer the double emulsion to a 250ml Erlenmeyer flask filled with 20ml of the external aqueous phase, blow nitrogen gas (5L / min), keep a constant ...

Embodiment 2

[0044] Step 1: Accurately weigh 100 mg of soybean lecithin, 20 mg of cholesterol, and 60 mg of glycerol trioleate, dissolve it in chloroform-ether (volume ratio 1:1) to 5 ml, and use it as the oil phase.

[0045] Step 2: Accurately weigh 2 mg of Siripag, 150 mg of sodium lauryl sulfate, and 100 mg of sucrose, and add 5 ml of water for ultrasonic dissolution as the inner water phase.

[0046] Step 3: Same as Example 1, prepare W / O type colostrum.

[0047]Step 4: Add the colostrum prepared in step 3 to 30ml of the external aqueous phase containing 25mg of sodium chloride and 4mg of arginine, and cut it with a high-speed shear homogenizer for 1min at 5000rpm to form W / O / W Double milk.

[0048] Step 5: Transfer the double emulsion to a 250ml Erlenmeyer flask filled with 20ml of the external aqueous phase, blow nitrogen gas (5L / min), keep a constant temperature water bath at 37°C, remove the chloroform-ether for 15min, and obtain a polyvesicular liposome suspension.

[0049] Step...

Embodiment 3

[0052] Step 1: Accurately weigh 180mg of lecithin, 45mg of cholesterol, and 90mg of glyceryl trioleate, dissolve and dilute to 5ml with chloroform-ether (volume ratio 1:1), as the oil phase.

[0053] Step 2: Accurately weigh 2 mg of Siripag, 180 mg of sodium lauryl sulfate, and 150 mg of sucrose, and add 5 ml of water for ultrasonic dissolution as the inner water phase.

[0054] Step 3: Same as Example 1, prepare W / O type colostrum.

[0055] Step 4: Add the colostrum prepared in step 3 to 30ml of the external aqueous phase containing 27mg of sodium chloride and 3mg of arginine, and cut it with a high-speed shear homogenizer for 1min at 5000rpm to form W / O / W Double milk.

[0056] Step 5: Transfer the double emulsion to a 250ml Erlenmeyer flask filled with 20ml of the external aqueous phase, blow nitrogen gas (5L / min), keep a constant temperature water bath at 37°C, remove the chloroform-ether for 15min, and obtain a polyvesicular liposome suspension.

[0057] Step 6: Same as ...

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Abstract

The invention belongs to the field of pharmaceutic preparations and particularly relates to a selexipag polycystic lipidosome and a preparation method thereof. The selexipag polycystic lipidosome comprises selexipag, lipids, a surfactant, an osmotic pressure regulator and an auxiliary emulsifier, wherein the lipids comprise amphiphilic lipids, neutral lipids and cholesterol. The selexipag polycystic lipidosome has relatively high encapsulation efficiency and stability, and shows a good slow release action in an in vitro test.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a method for preparing Silipag multivesicular liposomes. Background technique [0002] Selexipag (English name selexipag) is an oral prostacyclin receptor antagonist developed by Actelon in Switzerland for the treatment of pulmonary arterial hypertension. The U.S. FDA approved Siripag Tablets for marketing in December 2015, and its specifications are 200 μg, 400 μg, 600 μg, 800 μg, 1000 μg, 1200 μg, 1400 μg and 1600 μg. The EU EMA approved its listing in May 2016. However, due to its short half-life, patients need to take medicine for a long time, which reduces patient compliance. In addition, the drug needs to be taken for a long time in clinical treatment, and frequent administration for a long time brings inconvenience to patients, and the blood drug concentration in the body fluctuates greatly, which is easy to cause toxic and side effects. [0003] Liposome is mai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4965A61K47/28A61P9/12
CPCA61K9/127A61K31/4965A61K47/28
Inventor 谭欣周文亮周卫赛周祥陆平波
Owner JIANGSU ALICORN PHARMATECH CO LTD
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