Hydrobromic acid lappaconitine solid lipid nano particle and preparation method thereof

A technology of urbinine hydrobromide and solid lipid nanotechnology, which is applied in the direction of pharmaceutical formulas, medical preparations with no active ingredients, and medical preparations containing active ingredients, etc. Problems such as solid lipid nanoparticles and drug loading limit the wide application of solid lipid nanoparticles, and low drug loading of solid lipid nanoparticles to improve bioavailability, reduce drug dosage and side effects, and have good analgesic effects Effect

Active Publication Date: 2010-03-03
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, the preparation of solid lipid nanoparticles requires the use of organic solvents, which can easily cause residual organic solvents, resulting in certain toxicity
In addition, the drug loading of solid lipid nanoparticles is low. So far, the drug loading of solid lipid nanoparticles is generally only 1% to 5%. The low drug loading limits the wide application of solid lipid nanoparticles.
And also do not see the report that there is homogenine hydrobromide solid lipid nanoparticle in the prior art

Method used

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  • Hydrobromic acid lappaconitine solid lipid nano particle and preparation method thereof
  • Hydrobromic acid lappaconitine solid lipid nano particle and preparation method thereof
  • Hydrobromic acid lappaconitine solid lipid nano particle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The percentage in the prescription is the weight percentage that this component accounts for in the whole prescription, and the following examples are the same.

[0051] Prescription: Hovenine Hydrobromide 200mg

[0052] Glyceryl monostearate 2.5g

[0053] Poloxamer 188 1.5g

[0054] Tween-80 1.5g

[0055] water 50mL

[0056] Preparation of homogenate hydrobromide solid lipid nanoparticles:

[0057] Step 1: After mixing Poloxamer 188 and Tween-80 in a beaker, add an appropriate amount of distilled water to ultrasonically disperse until completely dissolved to form an aqueous phase; fully mix urine hydrobromide and glyceryl monostearate Mix and melt to form the oil phase;

[0058] Step 2: Heat the water phase and the oil phase to 75°C respectively, and add the water phase to the oil phase dropwise under stirring conditions to make colostrum;

[0059] Step 3: Homogenize colostrum high pressure milk to obtain a transparent suspension with ligh...

Embodiment 2

[0063] Prescription: Hovenine Hydrobromide 320mg

[0064] Palmitic acid 1g

[0065] Poloxamer 407 3.5g

[0066] water 50mL

[0067] Preparation of homogenate hydrobromide solid lipid nanoparticles:

[0068] Step 1: Put Poloxamer 407 in a beaker, add an appropriate amount of distilled water to ultrasonically disperse until completely dissolved, and form a water phase; fully mix and melt homogenin hydrobromide and palmitic acid to form an oil phase;

[0069] Step 2: Heat the water phase and the oil phase to 85°C respectively, and add the water phase to the oil phase dropwise under stirring conditions to make colostrum;

[0070] Step 3: Homogenize colostrum high pressure milk to obtain a transparent suspension with light blue opalescence;

[0071] Step 4: placing the translucent suspension at 0-4° C., cooling and solidifying to form an aqueous dispersion of solid lipid nanoparticles.

[0072] Detection: the average particle size of the solid lipid nanoparti...

Embodiment 3

[0074] Prescription: Hovenine Hydrobromide 500mg

[0075] Glyceryl Behenate 1.5g

[0076] Poloxamer 188 0.5g

[0077] Egg yolk phospholipids 2g

[0078] water 50mL

[0079] Preparation of homogenate hydrobromide solid lipid nanoparticles:

[0080] Step 1: Put Poloxamer 188 in a beaker, add an appropriate amount of distilled water to ultrasonically disperse until completely dissolved, and form a water phase; fully mix and melt homogenin hydrobromide, glyceryl behenate, and egg yolk phospholipids to form an oil Mutually;

[0081] Step 2: Heat the water phase and the oil phase to 65°C respectively, and add the water phase to the oil phase dropwise under stirring conditions to make colostrum;

[0082] Step 3: Homogenize colostrum high pressure milk to obtain a transparent suspension with light blue opalescence;

[0083] Step 4: placing the translucent suspension at 0-4° C., cooling and solidifying to form an aqueous dispersion of solid lipid nanoparti...

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Abstract

The invention provides a hydrobromic acid lappaconitine solid lipid nano particle and a preparation method thereof. The hydrobromic acid lappaconitine solid lipid nano particle is prepared from the following components, by weight percent: 0.1-1% of hydrobromic acid lappaconitine, 1-8% of lipid material, 0-5% of phospholipid, 0.5-10% of emulsifying agent and the balance water. The preparation method comprises the following steps: mixing the emulsifying agent and the water fully and evenly and preparing a water phase; mixing the hydrobromic acid lappaconitine, the lipid material and the phospholipid fully, melting and preparing an oil phase; heating the water phase and the oil phase respectively to 65-85 DEG C, adding the water phase into the oil phase under a stirring condition and preparing primary emulsion; emulsifying the primary emulsion at high pressure evenly and obtaining suspensoid liquid; and putting the suspensoid liquid under a condition of 0-4 DEG C, cooling, solidifying andpreparing the hydrobromic acid lappaconitine solid lipid nano particle. The invention adopts a high-pressure even emulsification method to prepare the hydrobromic acid lappaconitine solid lipid nanoparticle, does not need to use an organic solvent and is suitable for large industrialized production.

Description

technical field [0001] The invention relates to a kind of homogenin hydrobromide solid lipid nanoparticles and a preparation method thereof, belonging to the technical field of pharmacy. Background technique [0002] Lappaconite Hydrobromide, C 32 h 44 N 2 o 8 ·HBr·H 2 O) is the alkali hydrobromide of Rabaaconitum, an active ingredient extracted from the root of the ranunculaceae plant Aconitum aconitum. . Mainly by blocking the voltage-dependent sodium ion channel, inhibiting nerve conduction, inhibiting the reuptake of norepinephrine by the presynaptic membrane, increasing the norepinephrine between the synapses, thereby inhibiting the afferent fiber substance P released to exert an analgesic effect. Its analgesic strength is 7 times that of aminopyrine, and its analgesic effect is equivalent to that of peperidine, but it lasts for a long time. It is an excellent non-addictive analgesic, has no teratogenic mutagenic effect, and will not cause Accumulation of poison...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/19A61K31/439A61K47/12A61K47/14A61K47/24A61K47/34A61P25/04A61K47/10A61K47/26
Inventor 林华庆张蜀邓红陈桐楷李园余楚钦
Owner GUANGDONG PHARMA UNIV
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