Preparation method and application of magnolol-carboxyl terminal polyamide controlled release formulation

A technology of terminated polyamide and magnolol, which is applied in the field of oral medical materials, can solve the problems of easy oxidation of phenolic hydroxyl groups, variability of preparation storage, and insoluble drugs in water, etc., to prolong the release time, improve solubility, and effect strong effect

Inactive Publication Date: 2018-05-08
SICHUAN UNIV
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Problems solved by technology

[0002] Magnolol is the main active ingredient of the traditional Chinese medicine Magnolia Bark. The study found that Magnolol has central nervous system inhibition, anti-inflammatory, anti-ulcer, anti-tumor, antibacterial and other pharmacological effects. Actinomyces viscosus, Lactobacillus, Streptococcus sanguis, Actinomyces naeseri and other oral caries-related bacteria have a strong inhibitory effect, especially the effect on Streptococcus mutans, the minimum inhibitory concentration can reach 15.7μg / mL , and can inhibit the formation of Streptococcus mutans biofilm and reduce the already formed biofilm, its action concentration and effect are superior to other traditional Chinese medicines; compared with traditional antibiotics, magnolol has no drug resistance and has a strong effect on bacteria ; Although magnolol has superior antibacterial activity, two defects have limited its clinical application; the first, the phenolic hydroxyl group of magnolol is easily oxidized, and the preparation is easily denatured, which is not conducive to popularization; the second , the drug is hardly soluble in water, therefore, in view of the above problems, the present invention provides a preparation method that can improve the solubility of the drug and ensure the stability of the drug

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  • Preparation method and application of magnolol-carboxyl terminal polyamide controlled release formulation
  • Preparation method and application of magnolol-carboxyl terminal polyamide controlled release formulation
  • Preparation method and application of magnolol-carboxyl terminal polyamide controlled release formulation

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preparation example Construction

[0032] A preparation method of magnolol-carboxyl-terminated polyamide slow-release agent, comprising the following steps:

[0033] (1) Using the mixed solvent method, mix dimethyl sulfoxide and double distilled water at a volume ratio of 1:7 to obtain a mixed solution;

[0034] (2) Add 10 mL of the mixed solution obtained in step (1) into a 15 mL centrifuge tube, add 60 mg of carboxy-terminal polyamide at a ratio of 6 mg / mL, and add 20 mg of magnolol at a ratio of 2.0 mg / mL;

[0035] (3) The solution obtained in step (2) was ultrasonically oscillated, that is, after the centrifuge tube was closed, the centrifuge tube was ultrasonically oscillated at 37°C for 1 hour, then a stirrer was placed in the centrifuge tube, and after closure, it was placed in a constant temperature mixer at 37°C and stirred at 200rpm for 72 hours;

[0036] (4) Add 8 mL of water to precipitate the excess drug, centrifuge at 3000 rpm for 10 min to remove the precipitate, and freeze-dry the supernatant to...

Embodiment 1

[0039] Differential scanning calorimetry DSC detection was carried out, and the samples to be tested were divided into four groups: carboxy-terminal polyamide (PAMAM-COOH), magnolol (M), a mixture of magnolol and carboxy-terminal polyamide (M+ PAMAM- COOH) and M-PAMAM-COOH.

[0040] The specific process is as follows: Weigh 5 mg of each group of samples, put them into aluminum sample dishes and seal them, and perform DSC detection; the detection conditions are: gas pressure 0.06Mpa~0.1Mpa, gas flow rate 20mL / min~40mL / min, scan the samples , scan the sample at a heating rate of 10°C / min, the scanning range is 50°C~300°C, and the scanning results are analyzed and processed by Pyris Manager software; figure 1 As shown, it can be seen from the figure: PAMAM-COOH has no peak in the scanning temperature range, indicating that there is no endothermic or exothermic in PAMAM-COOH in this temperature range; the literature suggests that the DSC spectrum of magnolol is around 103°C The e...

Embodiment 2

[0042] 1H NMR detection was carried out, and the samples to be tested were divided into three groups: carboxy-terminal polyamide (PAMAM-COOH), magnolol (M) and M-PAMAM-COOH;

[0043] The specific process is as follows: each group of samples weighed 5 mg respectively, and the weighed samples were dissolved in 0.6 mL of heavy water (D 2 O), M was dissolved in deuterated dimethyl sulfoxide (DMSO-d 6 ); then add the liquid into the NMR tube, put the NMR tube into the NMR spectrometer, select 1 H detects the sample to obtain a nuclear magnetic spectrum, and uses MestReNova software to analyze and process the spectrum; figure 2 It can be seen from the figure that: figure 2 The middle is the nuclear magnetic resonance spectrum of each group of samples, A is the nuclear magnetic spectrum of magnolol, and the solvent is D 2 O, D appears at 4.86ppm in the figure 2 The solvent peak of O, the peak of magnolol appears at 3.25ppm, and no peak appears at other positions; B is the NMR s...

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Abstract

The invention discloses a preparation method and application of a magnolol-carboxyl terminal polyamide controlled release formulation. The preparation method comprises the following steps: mixing dimethyl sulfoxide and double distilled water according to a volume ratio of 1:7 so as to obtain a mixed solution; taking the mixed solution, adding carboxyl terminal polyamide according to a ratio of 6mg/mL, and adding magnolol according to a ratio of 2.0mg/mL; performing ultrasonic oscillation, and fully stirring; adding water and centrifuging to remove the precipitate, and freeze-drying the supernatant, thereby obtaining the needed magnolol-carboxyl terminal polyamide controlled release formulation, namely M-PAMAM-COOH. The preparation method disclosed by the invention is simple in operation and high in feasibility; the prepared M-PAMAM-COOH overcomes the application defects of the magnolol, and the high polymer material PAMAM-COOH is combined with a drug, so that an excellent effect of thedrug can be achieved, the drug release time is prolonged, clinical application is facilitated, and the prepared M-PAMAM-COOH has an effect of inhibiting streptococcus mutans and bio-membranes and canbe used for prevention and treatment of dental caries.

Description

technical field [0001] The invention relates to the field of oral medical materials, in particular to a preparation method and application of a magnolol-carboxyl-terminated polyamide slow-release agent. Background technique [0002] Magnolol is the main active ingredient of the traditional Chinese medicine Magnolia Bark. The study found that Magnolol has central nervous system inhibition, anti-inflammatory, anti-ulcer, anti-tumor, antibacterial and other pharmacological effects. Actinomyces viscosus, Lactobacillus, Streptococcus sanguis, Actinomyces naeseri and other oral caries-related bacteria have a strong inhibitory effect, especially the effect on Streptococcus mutans, the minimum inhibitory concentration can reach 15.7μg / mL , and can inhibit the formation of Streptococcus mutans biofilm and reduce the already formed biofilm, its action concentration and effect are superior to other traditional Chinese medicines; compared with traditional antibiotics, magnolol has no dr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/59A61K31/05A61P1/02A61P31/02
CPCA61K31/05
Inventor 李继遥张敏杨熙周学东李建树向臻婷廖琳
Owner SICHUAN UNIV
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