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A kind of rhein amide derivative nanosuspension and its preparation method and application

A technology of rhein amide and nanosuspension, which is applied in the directions of drug combination, pharmaceutical formula, medical preparation of inactive ingredients, etc., can solve the problems of poor bioavailability, low water solubility, and no in-depth research on preparations, etc. Effects of prolonged half-life, high product yield and purity, and simple and feasible preparation method

Active Publication Date: 2019-09-13
科贝源(北京)生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its low water solubility and poor bioavailability, the development and clinical application of rhein are greatly limited.
In the prior art, only the structural modification of rhein has been carried out, but there is no in-depth study of related preparations

Method used

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  • A kind of rhein amide derivative nanosuspension and its preparation method and application
  • A kind of rhein amide derivative nanosuspension and its preparation method and application
  • A kind of rhein amide derivative nanosuspension and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] The influence of embodiment 1 ultrasonic method and high-pressure homogenization method on nano-suspension

[0056] (1) Rheinyl Ileucine Nanosuspension (RH-Ile-NS)

[0057] 1) Precipitation-ultrasonic method (PU method): 50 mg of RH-Ile was weighed and dissolved in 4 mL of methanol as the oil phase for later use. Weigh 25 mg of Poloxamer 188 (Poloxamer, F68) and 25 mg of lecithin (Lecithin, LC) into a 100 mL beaker, add 40 mL of purified water, and ultrasonically dissolve as the water phase. Put the water phase in an ice-water bath, add it dropwise to the oil phase at a constant speed (1.0 mL / min) while stirring, continue stirring for 30 min after the dispersion is complete, and remove the methanol by rotary evaporation. Under the condition of 20000rpm, use a high-speed shearing machine to cut for 3min, let it stand for 10min, after defoaming, transfer it to an ultrasonic cell pulverizer, and under the condition of ultrasonic power of 315W, the probe is ultrasonicated ...

Embodiment 2

[0067] The influence of embodiment 2 homogeneous pressure on nanosuspension

[0068] Weigh 50 mg of RH-Ile and RH-Phe respectively, and dissolve them in 4 mL of methanol as the oil phase for later use. Weigh 25mg of F68 and 25mg of LC into a 100mL beaker, add 40mL of pure water, and ultrasonically dissolve it as the water phase. Put the water phase in an ice-water bath, add it dropwise to the oil phase at a constant speed while stirring, continue stirring for 30 min after the dispersion is complete, and remove the methanol by rotary evaporation. Under the condition of 20000rpm, use a high-speed shearing machine to cut for 3min, let it stand for 10min, after defoaming, transfer to a high-pressure micro-fluidizer, homogenize at 4660psi for 3 times, and then separate at 6990psi, 9320psi, 11650psi, 13980psi, 16310psi Homogenize 20 times to obtain RH-Ile-NS and RH-Phe-NS respectively. Determination of particle size and Zeta potential, the results are shown in Table 6 and Table 7. ...

Embodiment 3

[0074] The impact of embodiment 3 homogeneous times on the suspension

[0075] Weigh 50 mg of RH-Ile and RH-Phe respectively, and dissolve them in 4 mL of methanol as the oil phase for later use. Separately weigh 25mg of F68 and 25mg of LC into a 100mL beaker, add 40mL of pure water, and ultrasonically dissolve it as the water phase. Put the water phase in an ice-water bath, add it dropwise to the oil phase at a constant speed while stirring, continue stirring for 30 min after the dispersion is complete, and remove the methanol by rotary evaporation. Under the condition of 20000rpm, use a high-speed shearing machine to cut for 3min, let it stand for 10min to defoam, then transfer it to a high-pressure micro jet, homogenize for 3 times at 4660psi, then homogenize for 5 times, 10 times and 15 times under 11650psi pressure , 20 times, and 25 times to get RH-Ile-NS and RH-Phe-NS respectively. Determination of particle size and Zeta potential, the results are shown in Table 8 and...

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Abstract

The invention discloses an RH (rhein) amide derivative nanosuspension as well as a preparation method and an application thereof. The development and clinical application of RH are greatly limited due to poor water solubility and bioavailability. The preparation method, which is simpler, quick and high in yield, of the RH amide derivative nanosuspension is provided for RH amide derivatives. The method comprises steps as follows: the RH amide derivatives are dissolved in an organic solvent to serve as an oil phase; a stabilizer is dissolved in water to serve as an aqueous phase; the aqueous phase is placed in an ice-water bath, the oil phase is dropwise added with stirring, the mixture is stirred continuously for 30-40 min after complete dispersion, the organic solvent is removed through spin evaporation, the mixture is continuously sheared by a high-speed shearing machine at 20,000 rpm and left to stand, and a coarse suspension is obtained after defoaming; the RH amide derivative nanosuspension is obtained after ultrasonic method and / or high-pressure homogenization method treatment of the coarse suspension.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a rhein amide derivative nanosuspension and its preparation method and application. Background technique [0002] Rhubarb is derived from the dried roots and rhizomes of Rheum palmatum L., R. tanguticum Maxim.ex Balf. or medicinal rhubarb (Rheum officinale Baill.), a perennial herb of the family Polygonaceae. First recorded in "Shen Nong's Materia Medica", its nature and taste are bitter and cold, and it returns to the spleen, stomach, large intestine, liver, and heart meridian. Clinically, it is commonly used in the treatment of diseases such as cholecystitis, hepatitis, diabetes, nephropathy, chronic renal failure and constipation. The main pharmacological components of rhubarb are anthraquinone derivatives (about 3% to 5%) and a small amount of dianthrone derivatives. Among them, free anthraquinone is the main antibacterial component of rhubarb, and com...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/198A61K47/10A61K47/24A61P35/00
Inventor 陈立江荣景宏刘宇王欣梁啸崔庆国赵京华
Owner 科贝源(北京)生物医药科技有限公司