Local anesthetic phospholipid-mixed solvent-oil sustained-release drug delivery system and preparation method thereof

A technology for local anesthetics and drug delivery system, applied in the field of pharmacy, can solve the problems of difficult absorption and low bioavailability, and achieve the effects of stable drug release concentration, reduced administration times and improved safety.

Active Publication Date: 2018-11-06
XIAN LIBANG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Phospholipid complex is a new type of drug delivery system discovered by Bombardelli. Many drug active ingredients are difficult to absorb and have low bioavailability due to their phy...

Method used

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  • Local anesthetic phospholipid-mixed solvent-oil sustained-release drug delivery system and preparation method thereof
  • Local anesthetic phospholipid-mixed solvent-oil sustained-release drug delivery system and preparation method thereof
  • Local anesthetic phospholipid-mixed solvent-oil sustained-release drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0159] prescription:

[0160]

[0161] Preparation process: Take the prescribed amount of ethanol and benzyl alcohol, add 0.01g of ropivacaine, stir to make it fully dissolved, then add the prescribed amount of benzyl benzoate, mix well to obtain a drug solution; then add the prescribed amount of vitamin E acetate, stir to make it fully dissolved; then add the prescribed amount of egg yolk lecithin PC-98T, ultrasonically, to fully dissolve; then slowly add soybean oil to the drug solution to 10ml, and ultrasonically mix; Miscellaneous, sterilized, divided into vials, sealed, and packaged after passing the light inspection.

Embodiment 2

[0163] prescription:

[0164]

[0165]

[0166] Preparation process: Take the prescribed amount of ethanol and benzyl alcohol, put 0.8g of ropivacaine into it, stir to make it fully dissolve, then add the prescribed amount of benzyl benzoate, mix well to obtain a drug solution; then add the prescribed amount of vitamin E acetate, stir to make it fully dissolved; then add the prescribed amount of egg yolk lecithin PC-98T, ultrasonically, to fully dissolve; then slowly add soybean oil to the drug solution to 10ml, and ultrasonically mix; Miscellaneous, sterilized, divided into vials, sealed, and packaged after passing the light inspection.

Embodiment 3

[0168] prescription:

[0169]

[0170] Preparation process: take the prescribed amount of ethanol, throw 0.3g of ropivacaine, stir to make it fully dissolve, add the prescribed amount of benzyl benzoate, mix well, and obtain a drug solution; then add the prescribed amount of vitamin E acetate, Stir to make it fully dissolved; then add the prescribed amount of egg yolk lecithin PC-98T, and ultrasonically dissolve it; then slowly add soybean oil to the drug solution to 10ml, and ultrasonically mix; remove impurities and bacteria by membrane filtration , sub-packed into vials, sealed, and packaged after passing the light inspection.

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PUM

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Abstract

The invention relates to a local anesthetic sustained-release preparation with phospholipid-mixed solvent-oil as a carrier, and a preparation method thereof. The sustained-release preparation is prepared from local anesthetic as an active ingredient and a mixture of phospholipid-mixed solvent-oil as a sustained-release drug delivery system, and selectively is prepared from an antioxidant, whereinthe local anesthetic is selected from one of bupivacaine or ropivacaine free base or a mixture thereof; the mixed solvent is a mixture of benzyl benzoate and one or two of benzyl alcohol, ethanol; theantioxidant is vitamin E acetate, lipoic acid and the like; in the phospholipid-mixed solvent-oil mixture, the content of phospholipid does not exceed 50%, the content of benzyl benzoate does not exceed 10%, and the rest is oil.

Description

field of invention [0001] The invention belongs to the field of pharmacy, and mainly relates to a local anesthetic slow-release drug delivery system and a preparation method using phospholipid-miscible solvent-oil as a carrier. Background of the invention [0002] Pain is a complex physiological and psychological activity, which includes two components, one is the pain sensation caused by noxious stimuli acting on the body, and the other is the individual's pain response to noxious stimuli, accompanied by complex psychological activities. . The International Association for the Study of Pain (IASP) defines pain as: Pain is an unpleasant sensation and actual or potential tissue damage caused by emotional experience; or a description of this damage. Pain is an unpleasant physiological experience that widely occurs in the course of various diseases. Pain not only brings discomfort to the patient's body, but also has varying degrees of impact on the mental, psychological, and ...

Claims

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Application Information

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IPC IPC(8): A61K47/24A61K47/44A61K47/14A61K47/10A61K47/22A61K31/445A61P23/02A61P29/00A61P17/12
CPCA61K31/445A61K47/10A61K47/14A61K47/22A61K47/24A61K47/44A61P17/12A61P23/02A61P29/00A61K2300/00
Inventor 卢伍党梁娜陈涛董建平
Owner XIAN LIBANG PHARMA TECH
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