Clonidine hydrochloride multi-vesicular liposome and preparation method thereof

A clonidine hydrochloride and liposome technology, which is applied in liposome delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of preparation encapsulation rate and drug release differences, and reduce the total dosage , good sustained-release effect, good analgesic effect

Inactive Publication Date: 2008-06-04
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, due to the different physical and chemical properties and mechanism of action of different drug active ingredients, their preparation encapsulation e

Method used

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  • Clonidine hydrochloride multi-vesicular liposome and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0032] Step 1: Precisely weigh 200 mg of lecithin, 50 mg of cholesterol, 40 mg of phosphatidyl glycerol and 17.4 mg of triolein, dissolve with 5 ml of dichloromethane, and use it as the lipid phase;

[0033] Step 2: Precisely weigh 5 mg of clonidine hydrochloride and 100 mg of sucrose, dissolve with an appropriate amount of hydrochloric acid solution (0.1 mol / L) ultrasonically, and dilute to 5 ml, as the inner water phase, slowly add the upper layer of the lipid phase;

[0034] Step 3: use a high-speed shearing homogenizer (Fluko, ATS Industrial Systems Co., Ltd.) to act on the mixture obtained in step 2 at a rotational speed of 10,000 rpm for 9 minutes to prepare W / O type colostrum;

[0035] Step 4: To prepare the dichloromethane microsphere suspension, add 20 mL of the outer water phase containing 3.2 g / 100 ml of glucose and 40 mM lysine to the upper layer of the W / O colostrum, and act at 4500 rpm for 15 seconds clock to form a suspension of dichloromethane microspheres;

...

Embodiment 2

[0039] Step 1: Accurately weigh 200 mg of lecithin, 50 mg of cholesterol, 10 mg of phosphatidic acid and 15.6 mg of glyceryl triolein, and dissolve them in 5 ml of dichloromethane as the lipid phase;

[0040] Step 2: Accurately weigh 50 mg of clonidine hydrochloride and 200 mg of sucrose, ultrasonically dissolve with an appropriate amount of hydrochloric acid solution (0.1 mol / L), and set the volume to 5 ml, as the inner water phase, slowly add to the upper layer of the lipid phase;

[0041] Step 3: with embodiment 1;

[0042] Step 4: To prepare the dichloromethane microsphere suspension, add 20mL of the external aqueous phase containing 6.0g / 100ml glucose and 40mM lysine to the upper layer of W / O colostrum, and act for 15 seconds at a speed of 4500rpm Clock, form the suspension of dichloromethane microsphere;

[0043] Step 5: Same as Example 1.

[0044] The particle size of clonidine hydrochloride multivesicular liposomes was measured to be 5-50 μm; the encapsulation effici...

Embodiment 3

[0046] Step 1: Accurately weigh 100 mg of dioleoylphosphatidylcholine, 50 mg of cholesterol, 20 mg of phosphatidylserine and 3.4 mg of glyceryl trioleate, dissolve them in 5 ml of chloroform-ether mixture (1:1 by volume), and use them as lipid Mutually;

[0047] Step 2: Accurately weigh 2.5mg of clonidine hydrochloride, dissolve it ultrasonically with an appropriate amount of hydrochloric acid solution (0.1mol / L), and set the volume to 5ml, as the inner water phase, slowly add to the upper layer of the lipid phase;

[0048] Step 3: with embodiment 1;

[0049] Step 4: To prepare the chloroform-ether microsphere suspension, add 60mL of the external aqueous phase containing 3.2g / 100ml glucose and 40mM lysine to the upper layer of W / O colostrum, and act for 15 seconds at a speed of 4500rpm Clock, form the suspension of chloroform-ether microsphere;

[0050] Step 5: Same as Example 1.

[0051] The particle size of clonidine hydrochloride multivesicular liposomes was measured to ...

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Abstract

The invention discloses a clonidine hydrochloride bubbly liposome and a preparation method of the clonidine hydrochloride bubbly liposome. The preparation method includes the following steps: (1) lipid comprising neutral phospholipids, cholesterin and neutral lipid is dissolved in organic solvent, and the content of the neutral phospholipids is controlled to be from 20 to 40 mg/ml as a lipid phase; (2) the clonidine hydrochloride is dissolved in injection-used water and concentration of the clonidine hydrochloride is regulated to be from 20 to 10,000Mug/ml as an internal-water phase; (3) the equal-volume internal-water phase is added to the upper layer of the lipid to be mixed and emulsified to get water-in-oil type initial emulsion; (4) external-water containing osmotic pressure regulator is added into the upper layer of the water-in-oil type initial emulsion to be stirred to form water-in-oil-in-water type compound emulsion; (5) organic solvent in the compound emulsion is removed to get the clonidine hydrochloride bubbly liposome. The clonidine hydrochloride bubbly liposome has higher encapsulation rate, better slow release effect and better pain-killing 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. 2 Adrenergic receptor agonists are widely used in the clinical treatment of hypertension as central antihypertensive drugs. Additionally, studies have found that systemic or topical application of alpha 2 Adrenergic receptor agonists also have analgesic effects, which can reduce the behavioral response of animals to painful stimuli, and only by spinal alpha 2 Receptor-mediated by activating the spinal adrenergic descending inhibitory system. Due to the short half-life of clonidine hydrochloride, the clinical use of existing preparations requires multiple doses. Therefore, the development of a sustained-release preparation of clonidine hydrochloride for i...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4168A61P9/12
Inventor 陆伟根陈亭亭
Owner SHANGHAI INST OF PHARMA IND
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