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Medicinal composition for treating periodontitis and method for preparing sustained-release microsphere by using same

A technology of sustained-release microspheres and compositions, which is applied in the directions of drug combination, digestive system, bulk delivery, etc., to achieve the effects of good encapsulation efficiency and good in vitro sustained-release performance

Inactive Publication Date: 2014-09-10
THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Ornidazole and pefloxacin are routine clinical drugs for treating periodontitis. However, how to combine ornidazole and pefloxacin to produce a significant synergistic effect in the treatment of periodontitis, this type of research less; in addition, there is currently no technical introduction for the preparation of sustained-release microsphere capsules by pefloxacin and ornidazole based on the double-emulsion solvent evaporation method

Method used

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  • Medicinal composition for treating periodontitis and method for preparing sustained-release microsphere by using same
  • Medicinal composition for treating periodontitis and method for preparing sustained-release microsphere by using same
  • Medicinal composition for treating periodontitis and method for preparing sustained-release microsphere by using same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The preparation of the internal aqueous phase of embodiment 1 sustained-release microspheres

[0039] The pefloxacin is dissolved in an aqueous medium to prepare a pefloxacin aqueous solution, and the pefloxacin aqueous solution is an internal water phase. Because the physical and chemical properties of pefloxacin determine its high solubility in water, when preparing the inner water phase, any dosage of pefloxacin within the solubility range can be made into the inner water phase.

Embodiment 2

[0040] The preparation of the oil phase of embodiment 2 sustained-release microspheres

[0041] Take ornidazole and the polylactic acid-glycolic acid copolymer fully dissolved in an organic solvent, as the oil phase, the organic solvent is a mixture of dichloromethane, dichloromethane and ethanol, dichloromethane and ether solution, a mixed solution of dichloromethane and ethyl acetate, any of the above four.

[0042] (1) Selection of organic solvents

[0043] In the prior art, dichloromethane is used as a single organic solvent to dissolve polymeric materials and water-insoluble drugs. The volatilization process of the organic solvent has a great influence on the encapsulation efficiency of the drug. If the volatilization is too fast, the pore structure on the surface of the microsphere will increase, which will affect the drug release performance of the microsphere, and part of the drug will enter with the rapid volatilization of the organic substance. The external water p...

Embodiment 3

[0069] The preparation of the colostrum of embodiment 3 slow-release microspheres

[0070] The internal water phase and the oil phase are emulsified to obtain colostrum. Ultrasonic emulsification is performed on the inner water phase and the oil phase at a volume ratio of 1:5-10 under ice bath conditions. The internal aqueous phase can be obtained by the method in Example 1, or by other methods. The oil phase can be obtained by the method in Example 2, or by other methods.

[0071] (1) Selection of preparation equipment

[0072] 1 container type

[0073] The containers for preparing microspheres were selected in turn: beaker, flask, and Erlenmeyer flask. The influence of different containers on the sphericity of microspheres was investigated under a light microscope. The preparation status of different containers is shown in Table 5. Therefore, therefore, a beaker is preferred as a container for the preparation of microspheres in the examples.

[0074] Table 5 Evaluation...

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Abstract

The invention belongs to the field of medicinal preparation, and particularly relates to a preparation technology of a periodontitis medicine by mixing ornidazole and pefloxacin. The technology comprises the following steps of: dissolving pefloxacin and an aqueous medium to obtain an inner aqueous phase; completely dissolving ornidazole and polylactic acid-glycollic acid copolymer in organic solvent to obtain an oil phase; emulsifying the inner aqueous phase and the oil phase to obtain primary emulsion; adding polyvinyl alcohol solution into the primary emulsion, and sufficiently stirring to obtain multiple emulsion; and volatilizing the organic solvent to obtain the sustained-release microsphere for treating periodontitis. The sustained-release microsphere has good fluidity, pelletizing property, particle size distribution, encapsulation rate and in-vitro sustained-release performance, and is suitable for local injection for periodontium; the carrier material, medicines and related auxiliary components in the dosage form are not toxic to cells at the concentration; the sustained-release microsphere realizes an obvious bacteriostatic effect on the major pathogenic bacteria of periodontitis within 20 days; and the medicinal preparation provided by the invention has certain advantages in treatment of chronic periodontitis.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a preparation process of periodontitis medicine prepared by mixing ornidazole and pefloxacin. Background technique [0002] Double emulsion solvent evaporation method is often used to prepare polylactic-co-glycolic acid (PLGA) sustained-release microspheres. This method consists of three main phase layers: internal water phase (W1), oil phase (O) and External aqueous phase (W2). Usually, the easily soluble drug is placed in the inner water phase, the insoluble drug and carrier polymer are placed in the oil phase (organic solvent), the oil phase and the inner water phase are homogenized to form colostrum, and then the colostrum is transferred to the outer water phase (generally choose PVA solution), homogenize to obtain double emulsion (W1 / O / W2). Stir the double emulsion under certain conditions to volatilize the organic solvent, and the carrier polymer gradually solid...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K9/16A61K47/34A61P1/02A61K31/4164
Inventor 刘鲁川刘锐邓蔓菁
Owner THE THIRD AFFILIATED HOSPITAL OF THIRD MILITARY MEDICAL UNIV OF PLA
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