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Tetracaine hydrochloride lipidosome gel and preparation method thereof

A technology of tetracaine hydrochloride fat and tetracaine hydrochloride, which is applied in the direction of medical formula, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problem of inability to reduce the toxic and side effects of tetracaine hydrochloride, Short time and other issues, to achieve the effect of transparent and good-looking appearance, convenient drug use, and soft skin touch

Inactive Publication Date: 2009-07-08
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And common gel is compared with liposome gel, and action time is short, can not reduce the toxic and side effects of tetracaine hydrochloride

Method used

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  • Tetracaine hydrochloride lipidosome gel and preparation method thereof
  • Tetracaine hydrochloride lipidosome gel and preparation method thereof
  • Tetracaine hydrochloride lipidosome gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Weigh 260 mg of tetracaine hydrochloride, 433 mg of carbomer, 1213 mg of azone, 8663 mg of propylene glycol, 2599 mg of glycerin, 520 mg of triethanolamine, 1733 mg of soybean lecithin, and 347 mg of cholesterol. Or weigh 520 mg of tetracaine hydrochloride, 693 mg of carbomer, 1559 mg of azone, 9529 mg of propylene glycol, 3119 mg of glycerin, 866 mg of triethanolamine, 2079 mg of soybean lecithin, and 520 mg of cholesterol.

[0030] The above-mentioned soybean lecithin and cholesterol were dissolved in chloroform and placed in a 250mL pear-shaped bottle. On a rotary evaporator, the water bath was at 40°C for 20 minutes to form a film and the chloroform was removed. Hydrate with ammonium sulfate solution for 30 minutes, and pass through the membrane with an extruder at 0.8um, 0.45um, 0.22um, and 0.1um respectively. Put this blank liposome into a dialysis bag, dialyze in 500mL normal saline, 37 ℃ circulating water bath for 17h, take out the liposome after dialysis, put i...

Embodiment 2

[0032] Release test of tetracaine hydrochloride liposome and tetracaine hydrochloride aqueous solution

[0033] Put tetracaine hydrochloride liposome 5mL in the dialysis bag (tetracaine hydrochloride concentration is about 5.56mg / mL), the corresponding concentration of the prepared drug solution is 5.56mg / mL5mL and puts in the dialysis bag, respectively simultaneously in the stripping bag that 250mL distilled water is housed Timing release in the cup, speed 100r.min -1 , temperature 37°C. Take samples at 20min, 40min, 1h, 2h, 3h, 5h, 7h, 9h, 11h, 12h, 24h respectively, measure its concentration with HPLC, draw the release curve, calculate the cumulative release amount and draw, tetracaine hydrochloride liposome and The 24h cumulative release of tetracaine hydrochloride aqueous solution see figure 1 .

[0034] Depend on figure 1 It can be seen that tetracaine hydrochloride solution releases faster, and in the time of 2h, the cumulative release amount of tetracaine hydrochlo...

Embodiment 3

[0036] Comparison of drug solution and liposome cumulative release:

[0037] Franz diffusion cell was used to compare the release of drug solution and liposome. Load 0.5mL samples respectively, take samples at 0.5h, 1h, 2h, 3h, 4h, 6h, and 8h, and calculate the concentration and cumulative release, see figure 2 .

[0038] Depend on figure 2 It can be seen that the release of the drug solution is faster than that of the liposome, and the release amount is larger, which is also the reason why the drug solution fails quickly and cannot last too long. Liposome release is slow and stable.

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Abstract

The invention belongs to the technical field of medicine, and relates to pontocaine lipidosome gel and a preparation method thereof. The pontocaine gel comprises pontocaine, propping agent and other lipide ingredients, wherein, the content of the pontocaine is 0.5%-1.0%. The preparation method comprises the following steps: (1) the pontocaine and other lipide ingredients are dissolved by organic solvent, and then the organic solvent is removed for hydration, so that blank lipidosome solution is manufactured; (2) dug-loading by ammonium sulphate gradient method : after being dialyzed, the blank lipidosome is added with pontocaine aqueous solution and brooded by water bath to be made into pontocaine lipidosome; (3) carbomer is weighed and is dipped in the prepared part of the pontocaine lipidosome, sealed and placed to stay over the night, the mixture is added with the rest pontocaine lipidosome and added with other auxiliary materials at last to be stirred evenly, so that the pontocaine lipidosome gel is prepared. In the invention, the pontocaine lipidosome gel is made of pontocaine, so as to not only achieve the effect of slow release, but also reduce the toxic side effect of the medicine.

Description

Technical field: [0001] The invention relates to the field of pharmaceutical preparations, and relates to tetracaine hydrochloride liposome gel and a preparation method thereof. Background technique: [0002] Tetracaine hydrochloride is a commonly used local anesthetic with strong penetrating power and good diffusivity, and can penetrate mucous membranes. It is mainly used for mucous membrane anesthesia. toxic side effect. The products already on the market are mainly raw materials, which are clinically used and prepared solutions (often used in combination with epinephrine to prolong the drug effect time). In addition, there is tetracaine hydrochloride gel, which is not available. The listing of tetracaine hydrochloride liposome gel. Since it is necessary to prolong the drug effect time of tetracaine hydrochloride clinically, the added epinephrine can constrict the blood vessels, so it can reduce the drug absorption and prolong the action time, which brings inconvenience ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/245A61K47/32A61P23/02
Inventor 邓英杰王敏
Owner SHENYANG PHARMA UNIVERSITY
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