Clonidine hydrochloride multivesicular liposome and preparation method thereof

A technology of clonidine hydrochloride and multivesicular liposomes, which is applied in liposome delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of unsuitable multivesicular liposome prescriptions and preparation processes, etc. Achieve the effects of reducing adverse reactions, reducing the number of medications, and good sustained-release effects

Inactive Publication Date: 2009-09-23
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, since different drugs have different physicochemical properties and mechanisms of a...

Method used

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  • Clonidine hydrochloride multivesicular liposome and preparation method thereof
  • Clonidine hydrochloride multivesicular liposome and preparation method thereof
  • Clonidine hydrochloride multivesicular liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Step 1: Accurately weigh 100 mg of lecithin, 77 mg of cholesterol, and 3.2 mg of glyceryl trioleate, dissolve and dilute to 5 ml with chloroform-ether (1:1; v / v), as the lipid phase;

[0046] Step 2: Accurately weigh 25 mg of clonidine hydrochloride and 400 mg of sucrose, ultrasonically dissolve with an appropriate amount of 80 mmol / L citric acid solution, and use the citric acid solution to dilute to 5 ml as the inner water phase;

[0047] Step 3: Slowly add the above-mentioned internal water phase to the upper layer of the lipid phase, and use a high-speed shear homogenizer to act on it at a speed of 13,000 rpm for 8 minutes to obtain a water-in-oil emulsion;

[0048] Step 4: Add the emulsion prepared in step 3 to 25ml of the external aqueous phase containing 3.2mg / ml glucose and 40mmol / L lysine, and use a high-speed shear homogenizer to act on it at a speed of 10,000rpm for 8 seconds Clock, forming water-in-oil-in-water type double emulsion;

[0049] Step 5: inject ...

Embodiment 2

[0052] Step 1: Precisely weigh 100 mg of lecithin, 26 mg of cholesterol, and 3.2 mg of glycerol trioleate, dissolve it in chloroform and set the volume to 5 ml, and use it as the lipid phase;

[0053] Step 2: Accurately weigh 75 mg of clonidine hydrochloride and 50 mg of sucrose, ultrasonically dissolve with an appropriate amount of 30 mmol / L citric acid solution, and use the citric acid solution to dilute to 5 ml as the inner water phase;

[0054] Step 3: with embodiment 1, make water-in-oil type emulsion;

[0055] Step 4: Add the emulsion prepared in step 3 to 25ml of the external aqueous phase containing 3.2mg / ml glucose and 20mmol / L lysine, and use a high-speed shear homogenizer to act on it at a speed of 10000rpm for 8 seconds Clock, forming water-in-oil-in-water type double emulsion;

[0056] Step 5: Same as Example 1, multivesicular liposome suspension.

[0057] The particle size of clonidine hydrochloride multivesicular liposomes was measured to be 8-45 μm; the encap...

Embodiment 3

[0059] Step 1: Accurately weigh 200 mg of lecithin, 77 mg of cholesterol, 30 mg of phosphatidylserine and 6.4 mg of glyceryl trioleate, dissolve and dilute to 5 ml with chloroform-ether (1:1, v / v) as the lipid phase;

[0060] Step 2: Accurately weigh 75mg of clonidine hydrochloride and 300mg of sucrose, ultrasonically dissolve with an appropriate amount of 100mmol / L hydrochloric acid solution, and use the citric acid solution to dilute to 10.0ml as the inner water phase;

[0061] Step 3: with embodiment 1, make water-in-oil type emulsion;

[0062] Step 4: Add the emulsion prepared in step 3 to 25ml of the external aqueous phase containing 3.2mg / ml glucose and 80mmol / L lysine, and use a high-speed shear homogenizer to act on it at a speed of 10000rpm for 8 seconds Clock, forming water-in-oil-in-water type double emulsion;

[0063] Step 5: Same as Example 1, multivesicular liposome suspension.

[0064] The particle size of clonidine hydrochloride multivesicular liposomes was m...

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Abstract

The invention discloses clonidine hydrochloride multivesicular liposome and a preparation method thereof. The clonidine hydrochloride multivesicular liposome comprises the following components by weight portion: 1 portion of active ingredient (clonidine hydrochloride), 1 to 10 portions of lipid component, 0.1 to 3.5 portions of acid regulator, 10 to 50 portions of osmotic pressure regulator, and 1.0 to 6.0 portions of lysine, wherein the lipid component comprises neutral phospholipid and cholesterol in a mol ratio of 1: 0.5-1: 2, and neutral lipid which accounts for 1 to 2 mol percent of the weight of the lipid component. The clonidine hydrochloride multivesicular liposome has high encapsulation rate and stability, and is shown in vivo and in vitro experiments to have a good slow release effect.

Description

technical field [0001] The invention relates to a sustained-release preparation of clonidine hydrochloride, in particular to a clonidine hydrochloride multivesicular liposome and a preparation method thereof. Background technique [0002] Clonidine hydrochloride is an imidazoline derivative synthesized in the early 1960s, which is 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. The analgesic effect of clonidine hydrochloride is caused by α 2 - Adrenoceptor mediated by activation of the spinal adrenergic descending inhibitory system. Clonidine hydrochloride is administered as an analgesic at a dose of 2 μg / kg or more per day by epidural or intrathecal injection, or in combination with an opioid analgesic. Clonidine hydrochloride is used for analgesia, without complications s...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4168A61P29/00
Inventor 陆伟根王培全陈亭亭李军虞丽芳
Owner SHANGHAI INST OF PHARMA IND
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