Local used composition containing analgesic, and preparation method and use of local used composition

A technology for topical use and composition, applied in the field of pharmacy, can solve the problems of easy decomposition of ozone, limited application, low solubility, etc., and achieve the effects of easy portability, reduced toxicity and addiction, and simple preparation process

Inactive Publication Date: 2019-11-08
YICHANG HUMANWELL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] But ozone is very easy to decompose, very unstable, and can be decomposed into oxygen at normal temperature and normal pressure
And the solubility in water or organic solvents is relatively low, thus limiting its further clinical application

Method used

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  • Local used composition containing analgesic, and preparation method and use of local used composition
  • Local used composition containing analgesic, and preparation method and use of local used composition
  • Local used composition containing analgesic, and preparation method and use of local used composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment example 1

[0061] Prepare the prescription as follows: 10mg / 100g, the paste is calculated as 100g:

[0062]

[0063]

[0064] Preparation Process:

[0065] (1) Dissolve β-cyclodextrin and hydromorphone hydrochloride in water, control the pH at 6.0 to 7.5 by adding a buffer solution, and fully include β-cyclodextrin and the drug through ultrasound. The temperature is between 20 and 30°C.

[0066] (2) Add sodium sulfite to the aqueous solution of β-cyclodextrin inclusion drug.

[0067] (3) Dissolve the egg yolk lecithin and olive oil in the organic solvent ethyl acetate under stirring to obtain the oil phase, and pass through the prescription amount of ozone, add the cream base and transdermal absorbent, and put it in a water bath at 40-50°C Heating at medium temperature for 30-60 minutes;

[0068] (4) The oil phase is added to the water phase under stirring conditions, and an emulsion is prepared by using a high-speed shearing instrument, and the particle size is controlled below...

Embodiment example 2

[0073] The preparation prescription is as follows, the specification is 5mg / 100g, and the paste is calculated as 100g:

[0074]

[0075] Preparation Process:

[0076] (1) Dissolve hydroxypropyl-β-cyclodextrin and nalbuphine hydrochloride in water, control the pH at 6.0-7.5 by adding a buffer solution, and fully encapsulate the hydroxypropyl-β-cyclodextrin and the drug by ultrasonic In the process of ultrasonic inclusion, the temperature is controlled at 20-30°C.

[0077] (2) Add sodium thiosulfate to the aqueous solution of hydroxypropyl-β-cyclodextrin inclusion drug.

[0078] (3) Dissolve the poloxamer and olive oil in the organic solvent ethyl acetate under stirring to obtain the oil phase, and inject the prescribed amount of ozone, add the cream base and the transdermal absorbent, and heat the mixture at 40-50°C Heating in a water bath for 30-60 minutes;

[0079] (4) The oil phase is added to the water phase under stirring conditions, and an emulsion is prepared by us...

Embodiment example 3

[0084] Prepare the prescription as follows, the specification is 0.1mg / 100g, and the paste is calculated as 100g:

[0085]

[0086] Preparation Process:

[0087] (1) Dissolve hydroxyethyl-β-cyclodextrin and sufentanil citrate in water, control the pH at 6.0-7.5 by adding buffer solution, and make hydroxyethyl-β-cyclodextrin and The drug is fully included, and the temperature is controlled at 20-30°C during the ultrasonic inclusion process.

[0088] (2) Add propyl gallate to the aqueous solution of hydroxyethyl-β-cyclodextrin inclusion drug.

[0089] (3) Dissolve the egg yolk lecithin and olive oil in the organic solvent ethyl acetate under stirring to obtain the oil phase, and pass through the prescription amount of ozone, add the cream base and transdermal absorbent, and put it in a water bath at 40-50°C Heating at medium temperature for 30-60 minutes;

[0090] (4) Adding the oil phase to the water phase under stirring conditions, using a high-speed shearing instrument ...

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Abstract

The invention discloses a local used medicine composition containing analgesic. The local used medicine composition is fundamentally prepared from the following components: opioid agents, ozone and acceptable local used medicine composition ingredients in pharmacy. According to the local used medicine composition, medicine packaging efficiency is improved, and up to more than 90%, the phenomenon of initial burst release of medicine is effectively reduced, the medicine releasing rate is stable and lasting, and a slow release period can be 2-3 days. The medicine composition is easy to smear, carrying is convenient, and compliance of a patient is improved; and a preparation method is simple, the condition is mild, the preparation process is simple, parameters can be controlled, production efficiency is high, continuous and large-scale production can be realized, the requirement of the storage condition is low, and the medicine composition is easy to package, transport and store.

Description

technical field [0001] The present invention relates to but not limited to pharmaceutical technology, especially but not limited to topical composition containing analgesic and its preparation method and application. Background technique [0002] Opioids are the most effective weapon in medical pain management. In 1952, morphine was approved by the US Food and Drug Administration (FDA); in 1982, pethidine was launched; in 1984, fentanyl was launched; from 1986 to 1996, sufentanil, alfentanil, and remifentanil were successively launched , providing a good choice for perioperative clinical anesthesia and analgesia. [0003] Current studies suggest that there are four major opioid receptors in the human body, including μ receptor (MOR), kappa receptor (KOR), delta receptor (DOR), and FQ receptor (ORL1). The function of the FQ receptor has not yet been elucidated. Clinically, opioids are usually classified according to the interaction between opioids and opioid receptors, whi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K33/00A61K45/06A61K47/10A61K47/69A61P25/04A61P17/04A61P17/00A61P33/14
CPCA61K9/06A61K9/0014A61K33/00A61K45/06A61K47/10A61K47/6951A61P25/04A61P17/04A61P17/00A61P33/14
Inventor 李莉娥李杰杜文涛安健雄汤和清郭建锋廖娇金芬田峦鸢吕金良李禹琼汪淼
Owner YICHANG HUMANWELL PHARMA
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