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Medicinal use of paeonol and its derivatives

A derivative, the technology of paeonol, applied in the field of medicine, can solve the problems of easy volatility, poor water solubility, and low melting point, and achieve good medicinal prospects, rich sources of raw materials, and strong pharmacological effects

Inactive Publication Date: 2015-09-30
张筱梅
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The compound has the characteristics of low melting point [mp(51+1)℃], volatile and poor water solubility

Method used

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  • Medicinal use of paeonol and its derivatives
  • Medicinal use of paeonol and its derivatives
  • Medicinal use of paeonol and its derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation of Paeonol Sodium Sulfonate Eye Drops: Prepare different concentrations of Paeonol Sodium Sulfonate Eye Drops according to the conventional method for preparing eye drops. The eye drops are based on Paeonol Sodium Sulfonate. active ingredient. In the preparation process, in addition to conventionally adding co-solvents, osmotic pressure regulators, antioxidants, preservatives, and pH regulators, auxiliary materials such as borneol, peppermint, and sodium hyaluronate or methylcellulose or Viscous excipients such as hydroxypropylmethylcellulose. Its purpose is to increase the concentration of the drug in the eye tissue, increase its bioavailability, enhance the curative effect and reduce adverse reactions.

[0034] The above co-solvent refers to: at least one selected from cyclodextrin, polypropylene polymer, polyvinyl alcohol, polyvinylpyrrolidone, p-aminobenzoic acid, polysorbate, or at least one of their mixtures A sort of. The osmotic pressure regulator...

Embodiment 2

[0040] Preparation of paeonol eye ointment: Paeonol eye ointment with different concentrations was prepared according to the conventional method for preparing eye ointment, and the eye ointment uses paeonol as its main active ingredient. In the preparation process, different pastes such as lanolin, yellow petrolatum, liquid paraffin, or their mixtures can be selected, and auxiliary materials such as borneol, mint, and cyclodextrin can also be optionally added. Its purpose is to increase the concentration of the drug in the eye tissue, increase its bioavailability, enhance the curative effect and reduce adverse reactions.

[0041] Concrete example: the configuration of 1% paeonol eye ointment. In 1000 grams of paeonol eye ointment, 10 grams of paeonol and 5 grams of borneol are contained, and the rest is an eye ointment base composed of yellow vaseline, lanolin and liquid paraffin.

[0042] The ratio of each component of the above eye ointment base is: yellow petrolatum: lanol...

Embodiment 3

[0046] Research on the therapeutic effect of the present invention on active immune conjunctivitis induced by ovalbumin.

[0047] 1. Test material

[0048] The sodium paeonol xanthate of the present invention is used to prepare 0.05%, 0.1%, 0.5%, 1% eye drops; the paeonol of the present invention is used to prepare 0.25%, 0.5%, 2.0% ophthalmic ointment. Sodium chromylate eye drops were used as the positive control group.

[0049] 2. Test method

[0050] (1) Modeling method

[0051] 50 SD rats, weighing 100g-120g, half male and half male. Using the animal model method of "active allergic conjunctivitis induced by ovalbumin" reported in open literature, rats are made as a rat model of immune (also known as allergic) conjunctivitis.

[0052] (2) Test groups

[0053] 50 rats that have been made into immune conjunctivitis animal models are randomly divided into 10 groups, with 5 animals (10 eyes) in each group: model control group 1 (vehicle group of paeonol xanthate eye drops...

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Abstract

The invention relates to new application of paeonol and derivatives thereof in the pharmacy field. The animal experiment research shows that paeonol and derivatives thereof can obviously relieve or eliminate the inflammatory reaction of the local tissue of the eye with immunologic conjunctivitis, obviously reduce the infiltration of acidophilic cells and the degranulation of mast cells in the conjunctiva tissue, obviously relieve the inflammatory reaction of the anterior segment of the eye with uveitis, reduce the infiltration of inflammatory cells in the vitreous body and retinal tissue, effectively control the non-infectious immune inflammation of the dry eye, and obviously relieve the inflammatory reaction of the animal model eye with chronic conjunctivitis; and the clinical experiment research shows that the paeonol can be used for effectively treating eye diseases such as sclerotitis and the like. The invention provides a medicament for treating eye diseases, which has the advantages of exact curative effect and wide source and is safe and convenient; and the medicament can be combined with one or more pharmaceutically acceptable carriers or excipients to be prepared into a pharmaceutical composition or preparation of the paeonol and derivatives thereof.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the new medical application of paeonol and its derivatives, in particular to the application of paeonol and its derivatives in the preparation of medicines for treating and preventing eye diseases. Background technique [0002] Existing literature has disclosed compound paeonol and some derivatives thereof, and the structural formula of paeonol is [0003] [0004] The chemical formula is: 2-hydroxy-4-methoxyacetophenone, the molecular formula is C 9 h 10 o 3 , the relative molecular mass is 166.18. English name: Paeonolum. Alias: paeoniflorol, paeonol. The compound has the characteristics of low melting point [mp(51+1)°C], easy volatility and poor water solubility. [0005] Paeonol sodium sulfonate, one of its main derivatives, is obtained after sulfonation of paeonol. Its chemical structure is sodium 2-methoxy-4-hydroxy-5-acetylbenzenesulfonate. Sexuality has been si...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/185A61K31/12A61P27/02A61P27/14
Inventor 张筱梅
Owner 张筱梅
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