Clonidine multivesicular liposome and preparation method thereof

A multivesicular liposome and clonidine technology, applied in the field of clonidine multivesicular liposome and its preparation, can solve the problems of low utilization rate of raw materials, low utilization rate of drugs, etc., and achieve high utilization rate of raw materials and less waste Effect

Inactive Publication Date: 2010-06-30
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The raw material utilization rate of this method is low, and the drug utilization rate is usually less than 40%.

Method used

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  • Clonidine multivesicular liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Step 1: In a clean glass vessel add 1 mL containing 19.8mM (14.85mg) lecithin, 4.2mM (3.13mg) dipalmitoylphosphatidylglycerol, 30mM (11.61mg) cholesterol and 3.75mM (3.32mg) trioleic acid Chloroform solution of glycerides. This solution is called the lipid phase.

[0055] Step 2: Add 1mL of the internal water phase of the aqueous solution of 120mM (15.86mg) ammonium sulfate into the above-mentioned glass container containing the lipid phase, and stir at a speed of 10,000rpm for 10 minutes with a high-speed shearer to obtain W / O type colostrum.

[0056] Step 3: 5 mL of a solution containing 5% (w / v) (250 mg) glucose and 40 mM (29.36 mg) lysine was placed on the colostrum layer, and then mixed at a speed of 7500 rpm for 10 seconds to obtain W / O / W type double milk.

[0057] Step 4: Transfer the double emulsion to a 250mL Erlenmeyer flask containing 7mL containing 5% (w / v) (350mg) glucose and 40mM (40.93mg) lysine, in a constant temperature water bath at 37°C, and make ...

Embodiment 2

[0062] Step 1: Add 1 mL of 5 mM (3.96 mg) Hydrogenated Soy Lecithin, 0.5 mM (0.38 mg) Dipalmitate Phosphatidylserine, 10 mM (3.87 mg) Cholesterol and 0.155 mM (0.073 mg) Tricaprylic Glycerin to a clean glass container Esters in chloroform-ether solution. This solution is called the lipid phase.

[0063] Step 2: Add 0.5mL of the inner water phase of the aqueous solution of 10mM manganese sulfate (0.845mg) and 6% (w / v) (600mg) sucrose into the above-mentioned glass container containing the lipid phase, and use a high-speed shearing machine to Stir at a speed of 10,000 rpm for 10 minutes to obtain W / O colostrum.

[0064] Step 3: 7.5 mL of a solution containing 0.5% (w / v) (37.5 mg) mannitol and 80 mM (87.71 mg) lysine was placed on the colostrum layer, and then mixed at a speed of 4500 rpm for 40 seconds to obtain W / O / W type double emulsion.

[0065] Step 4: Transfer the double emulsion to a 250mL Erlenmeyer flask containing 9mL containing 0.5% (w / v) (45mg) mannitol and 80mM (...

Embodiment 3

[0070] Step 1: Add 1 mL of a dichloromethane solution containing 100 mM (75 mg) lecithin, 20 mM (8.49 mg) phosphatidic acid, 10 mM (3.87 mg) cholesterol and 13 mM (11.51 mg) triolein into a clean glass container. This solution is called the lipid phase.

[0071] Step 2: Add 1mL of the inner water phase of the aqueous solution with 1000mM (192.1mg) citric acid into the above-mentioned glass container containing the lipid phase, and stir at a speed of 10,000rpm for 10 minutes with a high-speed shearer to obtain a W / O type colostrum.

[0072] Step 3: 20 mL of a solution containing 10% (w / v) (2000 mg) mannitol and 20 mM (58.48 mg) lysine was placed on the colostrum layer, and then mixed at a speed of 7500 rpm for 20 seconds to obtain W / O / W type double milk.

[0073] Step 4: Transfer the double emulsion to a 1000mL Erlenmeyer flask containing 22mL containing 10% (w / v) (2200mg) mannitol and 20mM (64.32mg) lysine. Flow through the suspension in the Erlenmeyer flask, slowly evapor...

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Abstract

The invention discloses a clonidine multivesicular liposome and a preparation method thereof. The clonidine multivesicular liposome comprises clonidine serving as a medicinal active ingredient and an empty multivesicular liposome serving as a carrier. The empty multivesicular liposome comprises the following components in part by mass: 1 part of lipid component and 0.1 to 50 parts of ion gradient regulator, wherein the lipid component comprises amphiphilic lipids and neutral lipids in a molar ratio of 5-36:1. The clonidine multivesicular liposome is obtained by adopting the empty multivesicular liposome enveloped with the gradient regulator and using a transmembrane gradient active loading method to enable the clonidine to enter the aqueous phase of the empty multivesicular liposome through a phospholipid membrane. The clonidine multivesicular liposome has high utilization rate of raw materials and high loading concentation, shows good slow release effect in in vivo and in vitro experiments, and has better analgesic effect.

Description

technical field [0001] The invention relates to the field of sustained-release preparations, in particular to a clonidine multivesicular liposome and a preparation method thereof. Background technique [0002] Clonidine and its salts are imidazoline derivatives synthesized in the early 1960s, which are α 2 - Adrenergic receptor agonists, as central antihypertensive drugs are widely used in the clinical treatment of hypertension. Because of its powerful analgesic effect, it has been deeply studied and widely used in the treatment of various pains. In clinical studies, single-dose epidural administration reduced postoperative pain, post-cesarean analgesia, refractory cancer pain, and chronic non-cancer pain. Clonidine hydrochloride is currently clinically used as an analgesic at a dose of 2 μg / kg or more per day, administered by epidural or intrathecal injection, and can also be used in combination with opioid analgesics. The drug is available in tablets, transdermal patche...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4168A61P29/00A61P25/04
Inventor 陆伟根陈亭亭杨耀杰虞丽芳李军王莉莉
Owner SHANGHAI INST OF PHARMA IND
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