Preparation method for triamcinolone acetonide acetate ultradeformable nanometer lipid vesicle spraying agent and application to target hypertrophic scars

A technology of triamcinolone acetonide acetate and nano-lipids, which is applied in aerosol delivery, medical preparations containing active ingredients, and pharmaceutical formulas. There are no reports on the preparation of vesicle sprays, etc., and the therapeutic effect is remarkable and the effect is long-lasting.

Inactive Publication Date: 2014-12-03
SHANGHAI SEVENTH PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The preparation of triamcinolone acetonide acetate flexible nano-lipid vesicles has been reported abroad, but the preparation of triamcinolone acetonide acetate

Method used

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  • Preparation method for triamcinolone acetonide acetate ultradeformable nanometer lipid vesicle spraying agent and application to target hypertrophic scars
  • Preparation method for triamcinolone acetonide acetate ultradeformable nanometer lipid vesicle spraying agent and application to target hypertrophic scars
  • Preparation method for triamcinolone acetonide acetate ultradeformable nanometer lipid vesicle spraying agent and application to target hypertrophic scars

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0024] Example 1 Screening of phospholipid ratio of triamcinolone acetonide acetate flexible nanolipid vesicle spray

[0025] Prescription group distribution ratio (w / w / %) and dosage:

[0026]

[0027] The distribution ratio of the two prescriptions (w / w / %) and dosage:

[0028]

[0029]

[0030] The three-group distribution ratio (w / w / %) and dosage of prescription:

[0031]

[0032] Preparation

[0033] Quantitatively weigh the phospholipids and triamcinolone acetonide in the above recipes into an eggplant-shaped bottle, add 30ml of a mixed solvent of chloroform-methanol (1∶1, v / v), in a constant temperature water bath at 37°C, and evaporate the organic solvent under reduced pressure with a water pump , A uniform lipid-like film is formed on the inner wall of the bottle, and nitrogen is injected. Adding the aqueous solution of sodium cholate with the prescribed content and rotating the membrane for 2 hours to obtain a suspension of flexible nanolipid vesicles. Under the condition of...

Example Embodiment

[0043] Example 2 Screening of sodium cholate ratio of triamcinolone acetonide acetate flexible nanolipid vesicle spray

[0044] Prescription group distribution ratio (w / w / %) and dosage:

[0045]

[0046] The distribution ratio of the two prescription groups (w / w / %) and dosage:

[0047]

[0048] Distribution ratio of the three prescriptions (w / w / %) and dosage:

[0049]

[0050]

[0051] Preparation

[0052] Quantitatively weigh the phospholipids and triamcinolone acetonide in the above recipes into an eggplant-shaped flask, add 30 ml of a mixed solvent of chloroform-methanol (1∶1, v / v), in a constant temperature water bath at 37°C, and evaporate the organic solvent under reduced pressure by a water pump , A uniform lipid-like film is formed on the inner wall of the bottle, and nitrogen is injected. Adding the aqueous solution of sodium cholate with the prescribed content and rotating the membrane for 2 hours to obtain a suspension of flexible nanolipid vesicles. Under the condition o...

Example Embodiment

[0065] Example 3 Drug release experiment on isolated scar skin

[0066] Skin preparation

[0067] Selected patients with hypertrophic scars with a disease course of more than 1 year, relatively smooth local scars, no ulceration, an area of ​​3cm×3cm or more, requiring surgical resection, and informed consent before surgery. After the scar skin is removed by surgery, the subcutaneous fat is removed, rinsed with saline, and stored at -20°C for later use.

[0068] Penetration experiment

[0069] The modified Franz diffusion cell is used to fix the skin between the supply tank and the receiving tank, the stratum corneum faces the supply tank, and the effective penetration area is 0.952cm 2 . The supply pool was put into prescription one to prepare 0.1% triamcinolone acetonide acetate flexible nanolipid vesicle spray, 0.1% triamcinolone acetonide acetate nanolipid vesicles, 0.1% triamcinolone acetonide solution, and commercially available triamcinolone acetonide milk Each ointment is 0...

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Abstract

The invention discloses a preparation method for a triamcinolone acetonide acetate ultradeformable nanometer lipid vesicle spraying agent and application to target hypertrophic scars. The triamcinolone acetonide acetate ultradeformable nanometer lipid vesicle spraying agent is composed of the following compositions in percent by weight: 0.05%- 0.5% of triamcinolone acetonide acetate, 0.5%- 10% of phosphatide, and 0.2%- 50% of a softener. The prepared triamcinolone acetonide acetate ultradeformable nanometer lipid vesicle spraying agent has the average particle size of 50-500 nm. By optimizing the above ratio, the medicine can be relatively highly concentrated at a scar skin nidus area, and the composition ratio comprises, in percent by weight, 0.1% of triamcinolone acetonide, 4% of phosphatide, and 0.77% of sodium cholate. The prepared triamcinolone acetonide acetate ultradeformable nanometer lipid vesicle spraying agent solves many problems caused by multi-point injection in scar and triamcinolone acetonide external application, and is substantial in the hypertrophic-scar targeting effect.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, and relates to a preparation method of triamcinolone acetonide acetate flexible nano-lipid vesicle spray and its application in targeting hypertrophic scars. Background technique [0002] The pathological features of hypertrophic scars are the excessive proliferation of epidermal and dermal fibroblasts, and the massive deposition of collagen, which is difficult to be absorbed or remodeled by the body, causing long-term physical and mental torture and pain to patients. At present, local administration of scars, including multi-point injections into scars and external application of triamcinolone acetonide, is the main non-surgical therapy. However, multi-point injection in the scar has disadvantages such as unbearable pain, inaccurate dosage, and uneven drug diffusion; while external application of highly lipophilic triamcinolone acetonide does not have an excellent transdermal...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K31/58A61P17/02
Inventor 张立超张娟娟时扣荣吴志宏顾伟鹰
Owner SHANGHAI SEVENTH PEOPLES HOSPITAL
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