Tramadol multivesicular liposome and preparation method thereof

A technology of tramadol and liposome, which is applied in the field of tramadol vesicle liposome and its preparation, can solve the problems of preparation encapsulation efficiency and drug release difference, and achieves reduction of total dosage, reduction of medication times, Good sustained release effect

Inactive Publication Date: 2010-07-21
NANJING HAILING TRADITIONAL CHINESE MEDICINE RES CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the current problem is that because different drug active ingredients have different physical and chemical properties and mechanisms of action, their encapsulation ef

Method used

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  • Tramadol multivesicular liposome and preparation method thereof
  • Tramadol multivesicular liposome and preparation method thereof
  • Tramadol multivesicular liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] 1. Weigh 50 μmol of soybean lecithin, 80 μmol of dioleoylphosphatidylcholine (DOPC), 50 μmol of dipalmitoylphosphatidylglycerol (DPPG), 100 μmol of cholesterol (CH), and 12 μmol of triolein (To) in proportion. In the volumetric flask, add 5ml of chloroform to make it dissolve completely and become the organic phase;

[0029] 2. Prepare 5ml of tramadol hydrochloride solution with a concentration of 500mmol / L as the inner aqueous phase;

[0030] 3. Take 5ml of the inner aqueous phase and slowly drop it into 5ml of the organic phase in step 1, mix and emulsify, and ultrasonicate for 5 minutes to form water-in-oil (W / O) colostrum, which is observed as a milky white translucent viscous liquid;

[0031] 4. Prepare a solution containing 3% glucose, 0.2% Span 20, and arginine with a molar concentration of 40mmol / L as the external water phase, and inject 25mL of the external water phase into the prepared W / O colostrum, Emulsified and ultrasonicated for 5 minutes to obtain a wat...

Embodiment 2

[0036] 1. Weigh 80 μmol of hydrogenated soybean lecithin, 50 μmol of dioleoylphosphatidylcholine (DOPC), 200 μmol of dipalmitoylphosphatidylglycerol (DPPG), 120 μmol of cholesterol (CH), and 10 μmol of triolein (To), Place in a volumetric flask, add ether: chloroform (volume ratio 1:1) 5ml to make it completely dissolved, and become the organic phase;

[0037] 2. Prepare 5ml of tramadol hydrochloride solution with a molar concentration of 10mmol / L to form the inner aqueous phase;

[0038] 3. Take 5ml of the above-mentioned internal water phase and slowly drop it into 5ml of the organic phase in step 1, mix and emulsify, and ultrasonicate for 10 minutes to form water-in-oil (W / O) colostrum, which is observed as a milky white translucent viscous liquid;

[0039] 4. Prepare the solution containing 0.9% sodium chloride, 0.01% Tween 80, and the arginine with a molar concentration of 50mmol / L as the external water phase, and inject the external water phase into the colostrum of the ...

Embodiment 3

[0044] 1. Weigh 30 μmol of lecithin, 80 μmol of dioleoylphosphatidylethanolamine, 50 μmol of dipalmitoylphosphatidylglycerol, 10 μmol of phosphatidylglycerol, 30 μmol of cholesterol, 12 μmol of triolein, 10 μmol of phosphatidylserine, and 10 μmol of phosphatidic acid, Put it in a volumetric flask, add 5ml of chloroform to dissolve it completely, and become the organic phase.

[0045] 2. Prepare 5ml of tramadol hydrochloride solution with a concentration of 500mmol / L as the inner water phase.

[0046] 3. Take 5ml of the inner aqueous phase and slowly drop it into 5ml of the organic phase in step 1, mix and emulsify, and ultrasonicate for 5 minutes to form water-in-oil (W / O) colostrum, which is observed as a milky white translucent viscous liquid;

[0047] 4. Prepare 3% mannitol, 0.1% polyvinyl alcohol, L-lysine solution with a molar concentration of 20mmol / L as the external water phase, and inject 25mL of external water into the prepared W / O colostrum phase, emulsified and ult...

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Abstract

The invention discloses a tramadol multivesicular liposome and a preparation method thereof. The preparation method comprises the following steps of: 1, dissolving phospholipids, cholesterol and neutral lipids into organic solvents to obtain a mixture which serves as an organic phase; 2, preparing 10 to 500mmol/L tramadol solution which serves as an internal water phase; 3, adding the internal water phase with the same volume as that of an organic phase into the organic phase, and mixing and emulsifying the mixture to obtain water-in-oil primary emulsion; 4, preparing an external water phase containing amino acid and osmotic modulators and/or surfactants, and adding the external water phase of which the volume is 2 to 10 times that of the water-in-oil primary emulsion into the water-in-oil primary emulsion, stirring the mixture to form oil-in-water type double emulsion; 5, adding the emulsion into the solution of the amino acid, introducing nitrogen or carbon dioxide into the mixed solution to remove the organic solvent from the emulsion to obtain suspension; 6, dissolving the suspension into the solution of amino acid, centrifuging and taking lower liposome suspension to obtain the tramadol multivesicular liposome. The prepared tramadol multivesicular liposome has the advantages of higher encapsulation efficiency, good slow release effect, and longer analgesic effect.

Description

Technical field: [0001] The invention relates to a sustained-release liposome injection preparation of tramadol and a preparation method thereof, in particular to a tramadol multivesicle liposome and a preparation method thereof. Background technique: [0002] Tramadol is a central opioid analgesic with two different mechanisms of action that complement each other: it has a weak affinity for μ receptors, which is about 1 / 6000 of that of morphine; Inhibits the reuptake of norepinephrine and serotonin in the pathway. Its O-desmethyl metabolite (M1) also has analgesic effect, and its affinity for μ receptor is 200 times that of the parent body. The analgesic intensity of tramadol is equivalent to 1 / 5 of morphine at the same dose, and a single dose Oral administration of tramadol 37.5 mg, the plasma concentration reached its peak after 1.8 hours, and the peak plasma concentrations of D- and L-tramadol hydrochloride were 64.3 ng / ml and 55.5 ng / ml, respectively. Currently, opioi...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/135A61K47/28A61K47/14A61K47/22A61K47/24A61K47/18A61P25/04
Inventor 何盛江刘实张明明
Owner NANJING HAILING TRADITIONAL CHINESE MEDICINE RES CO LTD
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