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Micronizing solid external application local anesthetic and preparation method thereof

A technology of local anesthetics and solids, which is applied in the direction of anesthetics, medical preparations of non-active ingredients, powder delivery, etc., and can solve the problems of slow onset of action, large dosage, patient tolerance, and convenience of use.

Inactive Publication Date: 2008-06-04
TIANJIN PHARMA GROUP CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, sprays and creams of local anesthetics have come out, but due to the general dosage of local anesthetic sprays and creams, they are generally more than 10 mg / time; the onset of effect is slow, and the general onset time is about 1 hours (see compound lidocaine cream instructions), the patient's tolerance and convenience of use will be affected

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Dissolve 10 grams of lidocaine, 200 grams of soybean lecithin, and 1,500 grams of stearic acid in acetone to form an organic phase, add 10 grams of poloxamer, 40 grams of laurocapram, and 5 grams of propylene glycol into water to form an aqueous phase. Both the organic phase and the aqueous phase are heated to 75 degrees, and the two phases are quickly mixed under stirring to form a transparent system. The transparent system is removed under reduced pressure to remove the organic solvent and then concentrated, and then diluted in water at 5 degrees to form micronized drugs. combination.

[0028] The average particle size is 287nm, and the transdermal absorption rate is 6.9±1.1μg·cm -2 min -1 , The pain suppression rate reached 70% in 1 minute, and the highest peak reached 94%.

Embodiment 2

[0030]Dissolve 10 grams of tetracaine, 100 grams of lecithin, and 1,500 grams of triolein in dioxane to form an organic phase. Mix 10 grams of Tween 80, 40 grams of dimethyl sulfoxide, and glycerol Add 2 grams into water to form the water phase, heat both the organic phase and the water phase to 85 degrees, mix the two phases quickly under stirring, and form a transparent system, remove the transparent system under reduced pressure, remove the organic solvent, concentrate again, and then dilute to 0 degree of water to form a micronized pharmaceutical composition.

[0031] The average particle size is 225nm, and the transdermal absorption rate is 7.2±0.8μg·cm -2 min -1 , The pain suppression rate reached 65% in 1 minute, and the highest peak reached 96%.

Embodiment 3

[0033] Dissolve 10 grams of prilocaine, 500 grams of egg yolk phospholipids, and 2000 grams of Precirol ATO 5 (mainly composed of stearic acid and palmitic acid, mp 60°C) in tetrahydrofuran to form an organic phase, and add 200 grams of poloxamer to water Constitute the water phase, the organic phase and the water phase are heated to 65 degrees, and the two phases are quickly mixed under stirring to form a transparent system. The transparent system is removed under reduced pressure to remove the organic solvent and then concentrated again, and then diluted in water at 10 degrees. A micronized pharmaceutical composition is formed.

[0034] The average particle size is 421nm, and the transdermal absorption rate is 3.9±2.1μg·cm -2 ·Min -1 , The pain suppression rate reaches 35% in 1 minute, and the highest peak reaches 80%.

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Abstract

The invention relates to a medicine compound, in particular to a micro-powder local anesthesia medicine compound and a preparation method of the medicine compound; the medicine compound consists of solid local anesthesia medicines which has the average granule-diameter of being less than 50Mum and medical subsidiary substance, with the optimized average granule-diameter which is less than 1000nm. The medicine compound is characterized in that absorbing effect of the local anesthesia medicine is better; the used medicine dose is less and reaction time is quick.

Description

technical field [0001] The invention relates to a pharmaceutical composition, in particular to a micropowder local anesthetic drug combination and a preparation method thereof. Background technique [0002] Jenning Gysler A, Schafer-Korting M et al. (Eur J Pharm Biopharm, 2000, 49(3):211-218) and Sivaramakrishnan R, Nakamura C, Mehnert W et al. (J Controlled Release, 2004, 97(3): 493-502) all introduced that solid lipid nanoparticles (SLN) refers to the use of natural or synthetic high-melting solid lipids as carriers to adsorb and encapsulate drugs in lipid cores to make particles with a particle size of 50 ~1000nm solid colloidal particles are a new type of nano drug delivery system that has developed rapidly in recent years. When SLN is administered topically to the skin, it is easy to adhere to the skin to form a thin film, which can reduce the loss of water on the skin surface through occlusion properties, and at the same time increase the penetration rate of the drug ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/166A61K31/167A61K31/245A61K31/40A61K31/445A61K31/46A61K31/47A61K31/473A61K47/24A61P23/00
Inventor 孙亮张其婉李金禄李静陈立营
Owner TIANJIN PHARMA GROUP CORP
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