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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 nano-lipid vesicle spray has not been reported
In addition, there is no report on the use of triamcinolone acetonide acetate nano-lipid vesicles for scar skin targeting

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

Embodiment 1

[0024] Example 1 Phospholipid ratio screening of triamcinolone acetonide acetate flexible nano lipid vesicle spray

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

[0026]

[0027] Prescription two groups distribution ratio (w / w / %) and dosage:

[0028]

[0029]

[0030] Distribution ratio (w / w / %) and dosage of the three prescriptions:

[0031]

[0032] Preparation

[0033] Quantitatively weigh the phospholipids and triamcinolone acetonide in the above prescriptions into an eggplant-shaped bottle, add 30ml of chloroform-methanol (1:1, v / v) mixed solvent, place in a constant temperature water bath at 37°C, and evaporate the organic solvent under reduced pressure with a water pump , Form a uniform lipid-like film on the inner wall of the bottle, and inject nitrogen gas. Add an aqueous solution of sodium cholate in the prescribed amount, and wash the membrane with rotation for 2 hours to obtain a flexible nano-lipid vesicle suspension. Under th...

Embodiment 2

[0043] Example 2 Sodium cholate ratio screening of triamcinolone acetonide acetate flexible nano lipid vesicle spray

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

[0045]

[0046] Prescription two groups distribution ratio (w / w / %) and dosage:

[0047]

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

[0049]

[0050]

[0051] Preparation

[0052] Quantitatively weigh the phospholipids and triamcinolone acetonide in the above prescriptions into an eggplant-shaped bottle, add 30ml of chloroform-methanol (1:1, v / v) mixed solvent, place in a constant temperature water bath at 37°C, and evaporate the organic solvent under reduced pressure with a water pump , Form a uniform lipid-like film on the inner wall of the bottle, and inject nitrogen gas. Add an aqueous solution of sodium cholate in the prescribed amount, and wash the membrane with rotation for 2 hours to obtain a flexible nano-lipid vesicle suspension. Under ...

Embodiment 3

[0065] Embodiment 3 Ex vivo scar skin drug release experiment

[0066] skin preparation

[0067] Patients with hypertrophic scars with a course of more than 1 year, relatively flat local scars, no ulceration, an area of ​​more than 3 cm × 3 cm, and requiring surgical resection were selected, and informed consent was given before surgery. After removing the scarred skin, the subcutaneous fat was removed, rinsed with normal saline, and stored at -20°C for later use.

[0068] Penetration test

[0069] Using the improved Franz diffusion cell, the skin is fixed between the supply pool and the receiving pool, the stratum corneum faces the supply pool, and the effective penetration area is 0.952cm 2 . The supply pools were put into prescription one to prepare 0.1% triamcinolone acetonide acetate flexible nano-lipid vesicle spray, 0.1% triamcinolone acetonide acetate nano-lipid vesicles, 0.1% triamcinolone acetonide solution, commercially available triamcinolone acetonide milk ...

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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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