Topical pharmaceutical composition containing water-insoluble analgesic and preparation method and application thereof

A water-insoluble, composition-based technology, applied in the field of pharmacy, can solve the problems of easy decomposition of ozone, limited application, and low solubility, and achieve the effects of easy portability, enhanced analgesic effect, and simple preparation process

Inactive Publication Date: 2019-11-22
YICHANG HUMANWELL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] 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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  • Topical pharmaceutical composition containing water-insoluble analgesic and preparation method and application thereof
  • Topical pharmaceutical composition containing water-insoluble analgesic and preparation method and application thereof
  • Topical pharmaceutical composition containing water-insoluble analgesic and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment example 1

[0048] Implementation case 1 prepares the prescription as follows (the specification of flurbiprofen axetil is 10mg / 100g, and the ointment is calculated in 100g):

[0049]

[0050]

[0051] Preparation Process:

[0052] (1) Dissolve flurbiprofen axetil, PLGA-PEG-NHS and olive oil in the organic solvent ethyl acetate under stirring to obtain the oil phase, and pass through the prescription amount of ozone, and heat in a water bath at 40-50°C 30~60min;

[0053] (2) By adding buffer solution (NaH 2 PO 4 ---Na 2 HPO 4 ) controlling the pH of the aqueous phase containing a certain proportion of egg yolk lecithin at 6.7 to 7.7;

[0054] (3) Adding the oil phase to the water phase under stirring conditions, using a high-speed shearing instrument to prepare an emulsion, and controlling its particle size below 120nm;

[0055] (4) Under stirring, the emulsion is then fed into the ultrafine particle preparation system (UPPS) at a constant speed by a peristaltic pump under sti...

Embodiment example 2

[0059] Prepare the prescription as follows (the specification of propofol is 100mg / 100g, and the ointment is calculated as 100g):

[0060]

[0061] Preparation Process:

[0062] (1) Dissolve propofol, mPEG2000-b-PLGA1000 and camellia oil in the organic solvent ethyl acetate under stirring to obtain the oil phase, and inject the prescribed amount of ozone, and heat in a water bath at 40-50°C for 30- 60min;

[0063] (2), by adding buffer solution (NaH 2 PO 4 ---Na 2 HPO 4 ) controlling the pH of the aqueous phase containing a certain proportion of egg yolk lecithin at 6.7 to 7.7;

[0064] (3) The oil phase is added to the water phase under stirring conditions, and an emulsion is prepared by using a cell disruptor, and the particle size is controlled below 120nm;

[0065] (4) Under stirring, the emulsion is fed into the ultrafine particle preparation system (UPPS) at a constant speed by a peristaltic pump, and ethyl acetate is removed under negative pressure vacuum condi...

Embodiment example 3

[0069] Prepare the prescription as follows (the specification of flurbiprofen axetil is 20mg / 100g, and the ointment is calculated in 100g):

[0070]

[0071] Preparation Process:

[0072] (1) Dissolve flurbiprofen axetil, mPEG-PLGA-NHS, and soybean oil in the organic solvent ethyl acetate under stirring to obtain the oil phase, and pass through the prescribed amount of ozone, and heat in a water bath at 40-50°C 30~60min;

[0073] (2) By adding buffer solution (NaH 2 PO 4 ---Na 2 HPO 4 ) controlling the pH of the aqueous phase containing a certain proportion of poloxamer at 6.7 to 7.7;

[0074] (3) Add the oil phase to the water phase under stirring conditions, and prepare an emulsion by using a high-speed shearing instrument, and control its particle size below 120nm;

[0075] (4) Under stirring, the emulsion is then fed into the ultrafine particle preparation system (UPPS) at a constant speed by a peristaltic pump under stirring, and ethyl acetate is removed under ne...

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Abstract

The invention discloses a topical pharmaceutical composition containing a water-insoluble analgesic and a preparation method and application thereof. The topical composition includes a water-insolubleanalgesic drug and ozone. The water-insoluble analgesic drug is flurbiprofen axetil or propofol. The weight ratio of the water-insoluble analgesic drug to ozone is (10-100): (6-15). The drug encapsulation rate is improved and can reach 90% and above, which effectively reduces burst release of the drug. The drug release rate is stable and durable, and the sustained release period can reach 2 to 3days. The pharmaceutical composition is easy to apply and convenient to carry, and patient compliance is improved. The preparation method is simple, the conditions are mild, the preparation process issimple, parameters are controllable, reproducibility is good, production efficiency is high, and continuous large-scale production can be achieved. The pharmaceutical composition has low requirementson storage conditions and 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 water-insoluble analgesic, its preparation method and application. Background technique [0002] Flurbiprofen axetil (Flurbiprofen Axetil) is a prodrug of flurbiprofen, a non-steroidal targeted analgesic. The pharmacological effect is to reduce the synthesis of prostaglandins by inhibiting cyclooxygenase (COX) in the spinal cord and the periphery, and reduce the hyperalgesic state caused by surgical trauma. It can be used for pain relief after surgery and various cancers. Flurbiprofen axetil is insoluble in water, so it needs to be prepared as a liquid emulsion suitable for intravenous administration. Flurbiprofen axetil prepared into fat emulsion has a rapid onset of action and a long duration, and it is not easy to cause adverse reactions such as gastric mucosal damage. The advantage is that it has no central ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/00A61K9/06A61P17/00A61P17/02A61P17/04A61P29/00A61K31/222A61K31/05
CPCA61K9/0014A61K9/06A61K31/05A61K31/222A61K33/00A61K47/44A61P17/00A61P17/02A61P17/04A61P29/00A61K2300/00
Inventor 李莉娥安健雄汤和清郭建锋廖娇金芬田峦鸢吕金良李禹琼李杰杜文涛汪淼
Owner YICHANG HUMANWELL PHARMA
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