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A kind of roxithromycin-loaded nanostructure lipid carrier gel and preparation method thereof

A nano-structured lipid and roxithromycin-loaded technology, which is applied in liposome delivery, pharmaceutical formula, liquid delivery, etc., can solve the problems of short residence time and unfavorable conditions, and achieve increased local concentration, delayed evaporation, and increased viscosity. Adjunctive effect

Active Publication Date: 2019-04-05
QIQIHAR MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the drug easily penetrates the skin and enters the blood circulation, the local residence time is short. For roxithromycin, which is time-dependent, it is not conducive to the efficacy of the drug.

Method used

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  • A kind of roxithromycin-loaded nanostructure lipid carrier gel and preparation method thereof
  • A kind of roxithromycin-loaded nanostructure lipid carrier gel and preparation method thereof
  • A kind of roxithromycin-loaded nanostructure lipid carrier gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] ① Roxithromycin nanostructured lipid carrier

[0065] Accurately weigh 1 mg of roxithromycin, 75 mg of glyceryl distearate, 45 mg of caprylic / capric glycerides, and 67 mg of soybean lecithin, dissolve them in 1 mL of ethanol, melt them in a water bath at 75 °C, and use them as the oil phase; Each 80 mg of Tween 80 and F18 was dissolved in 20 mL of water as the water phase. Under magnetic stirring in a constant temperature water bath, slowly add the oil phase to the water phase at a rate of 0.2 mL / min. After all the addition is complete, continue to stir for 30 min, transfer while hot, and ultrasonicate the probe for 90 s at 20% ultrasonic power. Quickly transferred to an ice-water bath to solidify for 20 minutes, and filtered through a 0.22 μm microporous membrane to obtain a roxithromycin nanostructured lipid carrier.

[0066] ② Roxithromycin-loaded nanostructured lipid carrier gel

[0067] Prepare and take by weighing 4g of roxithromycin-loaded nanostructured lipid ...

Embodiment 2

[0069] ① Roxithromycin nanostructured lipid carrier

[0070] Precisely weigh 4 mg of roxithromycin, 45 mg of glyceryl distearate, 30 mg of caprylic / capric macrogol glycerides, and 67 mg of soybean lecithin, dissolve them in 3 mL of ethanol, and melt in a water bath at 75 °C to form an oil phase ; Precisely weigh 38 mg each of Tween 80 and F68, and dissolve them in 10 mL of water to form an aqueous phase. Under magnetic stirring in a constant temperature water bath, slowly add the oil phase to the water phase at a rate of 0.2mL / min. After all the addition is complete, continue to stir for 30 min, quickly transfer to an ice-water bath to solidify for 30 min, and pass through a 0.22 μm microporous filter. Membrane filtration, the roxithromycin nanostructure lipid carrier is prepared.

[0071] ② Roxithromycin-loaded nanostructured lipid carrier gel

[0072] Preparation Weigh 5.5g of roxithromycin-loaded nanostructured lipid carrier freeze-dried powder, dissolve it in 7mL of wate...

Embodiment 3

[0074] ① Roxithromycin nanostructured lipid carrier

[0075] Accurately weigh 7mg of roxithromycin, 60mg of glyceryl monostearate, 60mg of medium-chain triglycerides, and 67mg of soybean lecithin, dissolve them in 5mL of ethanol, melt in a water bath at 75°C, and form an oil phase; Each 150mg of Tween 80 and HS15 is dissolved in the prescribed amount of water to form an aqueous phase. Under magnetic stirring in a constant temperature water bath, slowly add the oil phase to the water phase at a rate of 0.2mL / min. After all the addition is complete, continue to stir for 30 min, quickly transfer to an ice-water bath to solidify for 10 min, and pass through a 0.22 μm microporous filter. Membrane filtration, the roxithromycin nanostructure lipid carrier is prepared.

[0076] ② Roxithromycin-loaded nanostructured lipid carrier gel

[0077] Prepare and take by weighing 7g of roxithromycin-loaded nanostructured lipid carrier freeze-dried powder, dissolve with 7mL water to obtain the...

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Abstract

The invention discloses a roxithromycin-loaded nanostructure lipid carrier gel and a preparation method thereof, and belongs to the technical field of new medicines. The roxithromycin-loaded nanostructure lipid carrier gel is prepared by two parts: 1, a roxithromycin-loaded nanostructure lipid carrier, which is prepared from the following components by weight: 1-7mg of roxithromycin, 45-75mg of a solid lipid material, 30-60mg of a liquid lipid material, 45-300mg of an emulsifier and 5-25mL of water; and 2, the roxithromycin-loaded nanostructure lipid carrier gel, which is prepared from the following components by weight: 4-7g of roxithromycin-loaded nanostructure lipid carrier freeze-dried powder, 0.01-0.01g of gel substrate, 1.0-3.0g of a humectant, 0.001-0.003g of a preservative, 0.004-0.02g of a pH modifier and 5-15g of water; the roxithromycin, the solid lipid material, the liquid lipid material ethanol, 45-300mg of emulsifier and 10-20mL of water are heated to 50-80 DEG C; and the prepared roxithromycin-loaded nanostructure lipid carrier freeze-dried powder is added to the gel substrate and are fully stirred to obtain the roxithromycin-loaded nanostructure lipid carrier gel.

Description

technical field [0001] The invention relates to a roxithromycin-loaded nanostructure lipid carrier gel and a preparation method thereof, belonging to the technical field of new drugs. Background technique [0002] Roxithromycin (ROXYTHROMYCIN, referred to as ROX), also known as Roxithromycin, is a new generation of macrolide antibiotics. Its antibacterial mechanism is to inhibit bacterial protein synthesis. The drug of choice, external use can be used to treat purulent skin diseases such as impetigo, small area burns, infection of ulcer surfaces, acne vulgaris, folliculitis, etc. [0003] Studies have found that roxithromycin is a time-dependent antibiotic, and its antibacterial efficacy is directly proportional to the contact time between the drug and bacteria. Because roxithromycin has a suitable oil-water partition coefficient, the skin has good permeability, and it is easy to enter the blood circulation, causing nausea. Gastrointestinal adverse reactions such as vomitin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K31/7048A61P31/04A61P17/02A61P17/10A61P17/00
CPCA61K9/0014A61K9/06A61K9/127A61K31/7048A61K47/24
Inventor 韩翠艳金珊珊马晓星隋小宇刘畅袁橙潘虹黄海涛李瑶
Owner QIQIHAR MEDICAL UNIVERSITY
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