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Phospholipid-miscible solvent-oil sustained-release drug delivery system composition and preparation method of local anesthetic

A technology of local anesthetics and sustained-release preparations, applied in the field of pharmacy, can solve the problems of difficult absorption and low bioavailability

Active Publication Date: 2021-08-31
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 physical and chemical properties, which limits their clinical application. However, after forming a complex with phospholipids, they can show Pharmacological activity different from parent drug

Method used

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  • Phospholipid-miscible solvent-oil sustained-release drug delivery system composition and preparation method of local anesthetic
  • Phospholipid-miscible solvent-oil sustained-release drug delivery system composition and preparation method of local anesthetic
  • Phospholipid-miscible solvent-oil sustained-release drug delivery system composition and preparation method of local anesthetic

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0162] prescription:

[0163]

[0164] 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

[0166] prescription:

[0167]

[0168]

[0169] 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

[0171] prescription:

[0172]

[0173] 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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Abstract

The present invention relates to a local anesthetic sustained-release preparation and preparation method using phospholipid-miscible solvent-oil as a carrier. The sustained-release preparation includes: a local anesthetic as an active ingredient, and a phospholipid-as a sustained-release drug delivery system. The mixture of miscible solvent-oil, and optionally can also include antioxidant; Wherein, described local anesthetic is selected from: one of bupivacaine or ropivacaine free base or the mixture of both; Described The miscible solvent is a mixture of benzyl benzoate, benzyl alcohol, ethanol or both; the antioxidant is vitamin E acetate and lipoic acid etc.; in the mixture of phospholipid-miscible solvent-oil, the phospholipid content is no more 50%, benzyl benzoate content is not less than 10%, and the rest is oil.

Description

[0001] field of invention [0002] 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. [0003] Background of the invention [0004] 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, psyc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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