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Andrographolide nano crystal intermediate, preparation method and applications thereof

A technology of andrographolide and nanocrystals, which is applied in the direction of pharmaceutical formulations, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problem of adding a large amount of carrier materials or toxic solvents, poor stability of liquid preparations, The problem of low bioavailability of the preparation can be solved, and the effect of prolonging the adhesion time and residence time, enhancing the adhesion and improving the bioavailability of the drug can be achieved.

Inactive Publication Date: 2015-10-21
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some people also prepared it into cyclodextrin inclusion compound. Although it overcomes the problem of low solubility of insoluble drugs, the metabolism of cyclodextrin inclusion compound in vivo is slow, has serious kidney toxicity, and the cost is high (CN 102343096A)
It is also reported in literature that andrographolide is made into solid lipid nanoparticles (CN 102716080A); made into solid dispersion (CN 101433522A); made into nanoemulsion (CN1931130A); made into lipid microspheres (CN 1686108A); The method of grinding suspension (CN 102614133A) is used to improve the stripping and absorption of andrographolide, but a large amount of carrier material needs to be added, the preparation process is complicated, and the drug loading is low, the stability is poor, the effect is not ideal, and there is no product Successfully developed and listed
[0005] The methods involved in the above documents and patents have improved the in vivo absorption of andrographolide to a certain extent, but there are still many problems, such as the bioavailability of the preparation is still low, the stability of the liquid preparation is poor, and a large amount of carrier materials are added during the preparation process. Or toxic solvents, complex preparation process, high cost, etc.

Method used

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  • Andrographolide nano crystal intermediate, preparation method and applications thereof
  • Andrographolide nano crystal intermediate, preparation method and applications thereof
  • Andrographolide nano crystal intermediate, preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: the preparation of different average particle size ranges (500nm, 600nm, 700nm, 800nm, 900nm) andrographolide nanocrystal suspension

[0037] Weigh 0.15g of polyvinylpyrrolidone-K30 (stabilizer Ⅰ) and add 100ml of water to dissolve, mix well, then add 0.15g of D-alpha-tocopheryl succinate polyethylene glycol (stabilizer Ⅱ) and mix well, Obtain stabilizer solution; Then, the andrographolide of 0.5g is dispersed in stabilizer solution, shear through high-speed shear emulsification method, and rotating speed is: 13000rpm, and shearing time is 5min; The primary particle diameter that makes is 45 μ m Suspension; then the above primary suspension is subjected to high-pressure homogenization, the homogenization temperature is controlled at 10°C, and nanocrystal suspensions of different particle size ranges are prepared according to the following homogenization process:

[0038] Homogenization process ①: First, homogenize 5 times at 200bar, 400bar, 600bar, 800bar,...

Embodiment 2

[0043] Example 2: Determination of Saturation Solubility of Andrographolide Nanocrystal Suspensions with Different Particle Sizes

[0044] Dissolution was determined by the paddle method, using 900 mL of pH 7.4 phosphate buffer solution as the dissolution medium, and the speed was 100 r min -1 , the temperature of the water bath is 37 ° C, and the average particle diameter prepared in the above example 1 is 10ml each of 500nm, 600nm, 700nm, 800nm, and 900nm, and the suspension is placed in the dissolution cup for 0.5min and 1min. 1.5min, 4min, 6min, 10min, 20min, 1mL of samples were taken after 30min, filtered through a 0.22μm microporous membrane, and determined by HPLC. According to the standard curve of andrographolide, A=29593C(R 2 =0.9994), linear range 0.0456~0.0912mg / ml, calculate its dissolution rate, its content is shown in Table 1, and the dissolution rate and time relationship curve of andrographolide nanocrystal suspension in different particle size ranges are show...

Embodiment 3

[0049] Embodiment 3: the preparation of andrographolide nano crystal intermediate powder

[0050] Experimental method: Get the nanocrystal suspension sample that the average particle diameter that makes according to the experimental method of embodiment 1 is 500nm, add 1.0g lactose (stabilizer III) to disperse and dissolve, then adopt spray drying rapid solidification technology, spray drying hot air temperature The temperature is 120° C., the air outlet temperature is 60° C., and the peristaltic speed of the pump is 5 ml / min. After drying and solidification, the andrographolide nanocrystal intermediate powder is obtained.

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Abstract

The invention belongs to the field of medicinal preparation, and relates to an andrographolide nano crystal intermediate and a preparation method thereof. The provided andrographolide nano crystal intermediate can be immediately dispersed into a nano state after being contacted with water; the solubility, dissolving-out speed, and bioavailability of andrographolide are prominently improved; the intermediate can be made into different dosage forms containing the nano crystal intermediate; the intermediate can be disintegrated into nano crystals after being contacted with water; the drug stability is enhanced, and the drug function is reinforced. The preparation technology is simple, no toxic solvent is used, the cost is low, and the technology can be easily industrialized, and thus has a good application prospect.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an andrographolide nanocrystal intermediate and a preparation method thereof. Background technique [0002] Andrographolide has special curative effects on many infectious diseases. It is clinically used as the first choice for antiviral drugs and is called "natural antibiotic". It has antibacterial, anti-inflammatory, antiviral, antipyretic, immune function and antitumor effects Synthesis, release and inflammatory activity of prostaglandins, mainly used for bacillary dysentery, viral pneumonia, viral upper respiratory tract infection, acute tonsillitis, etc. However, andrographolide has poor water solubility (69 μg / ml at 22°C) and poor stability (easy to ring-open, dehydrate, isomerize, etc. at pH>12), and the oil-water partition coefficient (LogP) at neutral pH is 2.013, low bioavailability (oral bioavailability 0.98%) (Wei Cunfang. Pharmacokinetic study...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/365A61K47/34A61K47/38A61K47/26A61P31/04A61P1/12A61P11/00A61P31/12A61P11/04A61K47/22A61K47/32
CPCY02A50/30
Inventor 岳鹏飞杨明但济修郑琴伍振峰胡鹏翼王雅琪
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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