Nano-scale solid-state lipid drug delivery system and preparation method thereof

A drug-carrying system and solid lipid technology, applied in the field of chemical industry, can solve the problem that there is no report on the drug-carrying system of 4-n-n-butylresorcinol, etc.

Inactive Publication Date: 2016-12-21
上海格兰化妆品有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there is no report about the drug delivery system embedded in 4-n-butylresorcinol

Method used

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  • Nano-scale solid-state lipid drug delivery system and preparation method thereof
  • Nano-scale solid-state lipid drug delivery system and preparation method thereof
  • Nano-scale solid-state lipid drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] 1) According to the preparation method involved in the summary of the invention, the following method

[0075] 1) Turn on the cooling water of the high-pressure homogenizer, turn on the heater of the high-pressure homogenizer to heat to 85°C; start the high-pressure homogenizer, and keep the circulation to keep the temperature of the pipeline in the machine at 85°C; weigh all the medicines separately, and put Liquid lipids, solid lipids and active drugs are mixed and heated to 85°C to obtain an oil phase;

[0076] 2) Mixing water, surfactant, polyol and phospholipid and heating at constant temperature to 85°C to obtain the water phase;

[0077] 3) Add the oil phase in step 1) to the water phase in step 2), and keep the temperature at 85°C to obtain a mixed phase;

[0078] 4) Put the mixed phase in step 3) into a high-pressure homogenizer for pre-emulsification at a speed of 8000 rpm for 180 seconds to form a mixed phase emulsion and obtain a sample;

[0079] 5) Feed t...

Embodiment 2

[0084] Preparation method is identical with embodiment 1,

[0085] The liquid lipid is 10% macadamia oil, the solid lipid is 10% beeswax, the active drug is 4-n-butylresorcinol 3%, the surfactant is Tween 80, 2% The polyhydric alcohol is pentylene glycol, the 0.5% phospholipid is lecithin, and the rest is water, and the above fractions all refer to mass fractions. Get Q2.

[0086] For particle size measurement, see row Q2 in Table 4, see Table 5Q2 for interface potential, see 0.7% of Q2 in Table 6 for crystallinity, and 91.94% of Q2 in Table 7 for embedding degree.

Embodiment 3

[0088] Preparation method is identical with embodiment 1,

[0089] Among them, the liquid lipid is 12% Hawaiian soybean oil, and the solid lipid is 8% ATO 888, 3% active drug is 4-n-butylresorcinol, 12% surfactant is Poloxamer 188, 2% polyol is pentylene glycol, 0.5% phospholipid is lecithin, the rest is water, and the above fractions all refer to mass fractions. Get Q3.

[0090] For particle size measurement, see row Q3 in Table 4, see Table 5Q3 for interface potential, see 14.4% of Q3 in Table 6 for crystallinity, and 91.24% of Q3 in Table 7 for embedding degree.

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Abstract

The present invention provides a nano-scale solid-state lipid drug delivery system, wherein a liquid lipid and a solid lipid are mixed as a raw material to prepare the 4-n-butylresorcinol embedded drug delivery system, and specifically the drug delivery system is the oil-in-grease and oil-in-water (O/F/W) composite nanometer lipid drug delivery system, and has characteristics of high embedding rate, high drug loading, high stability, low toxicity and good drug release. The invention further provides applications of the drug delivery system in formulas for cosmetic preparation, wherein the nano-scale solid-state lipid drug delivery system further has effects of skin whitening, dark spot removing, and freckles and melanin production inhibiting.

Description

technical field [0001] The invention belongs to the field of chemical industry, in particular to a nanoscale solid lipid drug-loading system embedding 4-n-n-butyl resorcinol. Background technique [0002] 4-n-n-butylresorcinol (1,3-Dihydroxy-4-n-butylbenzene, namely 4-n-butylresorcinol) is an effective skin lightening agent, commonly known as Kopcinol. Because Kopcinol has anti-chloasma and anti-glycation effects, so for H 2 o 2 Induced DNA damage is strongly protective. Furthermore, under the premise of basically not causing any cytotoxicity, Kopcinol has more inhibitory effect on tyrosinase activity, and can also inhibit the synthesis of tyrosinase. However, since Kopcinol absorbs ultraviolet light, its many effects (such as whitening) will be reduced due to the effect of light. In addition, high doses of 4-n-butylresorcinol can also be irritating to the skin. [0003] At present, there is no report about the drug-loading system embedded in 4-n-n-butyl resorcinol. Th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/02A61K8/34A61K8/92A61K8/37A61K8/55A61Q19/02
CPCA61K8/0245A61K8/345A61K8/347A61K8/375A61K8/553A61K8/922A61K8/927A61K2800/413A61Q19/02
Inventor 庞文心潘颀钧
Owner 上海格兰化妆品有限公司
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