Minocycline hydrochloride microballoons and preparation method and application in pharmacy thereof

A technology of minocycline hydrochloride and microspheres, which is applied in the directions of active ingredients of tetracycline, drug combination, digestive system, etc. It can solve the problems of heavy burden on patients and high listing price, and achieve lower listing price, reduce patient burden, and reduce costs Effect

Inactive Publication Date: 2008-10-22
NORTHWESTERN POLYTECHNICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the current minocycline hydrochloride sustained-release preparations are complet

Method used

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  • Minocycline hydrochloride microballoons and preparation method and application in pharmacy thereof
  • Minocycline hydrochloride microballoons and preparation method and application in pharmacy thereof
  • Minocycline hydrochloride microballoons and preparation method and application in pharmacy thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Take 3 mL of 40% polylactic acid (PLA) solution, add 0.3 g of minocycline hydrochloride, and continue heating to dissolve it. Transfer the above polylactic acid solution to a flask, add 60mL of liquid paraffin preheated to 50°C and an appropriate amount of Span 65 and Tween 80, stir and emulsify at a constant temperature for 35 minutes, quickly cool it to 0°C-5°C, add vanillin Use 1mol / L sodium hydroxide to adjust the pH value to 8-9, stir in an ice-water bath for 4 hours, pour off the paraffin on the surface after it is fully solidified, filter it with suction, and wash it with acetone for 2-3 times until there is no vanillin smell , to obtain a yellow powdery solid. Take 1.0g of methylcellulose, add appropriate amount of purified water to fully swell, take another appropriate amount of purified water, dissolve propylene glycol and glycerin, and mix with the above methylcellulose solution evenly, add sodium hydroxide solution while stirring to make it into a gel Gel b...

Embodiment 2

[0028] Take 3 mL of 35% polylactic acid (PLA) solution, add 0.2 g of minocycline hydrochloride, and continue heating to dissolve it. Transfer the above polylactic acid solution to a flask, add 50mL of preheated peanut oil and an appropriate amount of Span 65 and Tween 80, stir and emulsify at a constant temperature for 30 minutes, then quickly cool it to 0°C-5°C, add 18mL of paraformaldehyde solution, Adjust the pH value to 8-9 with 1mol / L sodium hydroxide, stir in an ice-water bath for 4 hours, pour off the peanut oil on the surface after it is fully solidified, filter with suction, wash with acetone for 2-3 times until there is no paraformaldehyde smell, and obtain Yellow powdery solid.

Embodiment 3

[0030] Take 3 mL of 30% gelatin solution, add 0.2 g of minocycline hydrochloride, and continue heating to dissolve it. Transfer the above gelatin solution to a flask, add 45mL of preheated soybean oil and an appropriate amount of Span 80, stir and emulsify at a constant temperature for 30 minutes, then quickly cool it to 0°C-5°C, add 15mL of formaldehyde, and use 1mol / L hydrogen Adjust the pH value to 8-9 with sodium oxide, stir in an ice-water bath for 4 hours, pour off the surface soybean oil after it is fully solidified, filter with suction, wash with acetone 2-3 times until there is no formaldehyde smell, and obtain a yellow powdery solid.

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Abstract

The invention relates to a minocycline hydrochloride microsphere, a preparation method thereof and the application thereof in medicine preparation; the invention is technically characterized in that the components comprise minocycline hydrochloride drug, biodegradable polymer material, emulsifier and chemical cross-linking reagent; the weight percentage of the components is 10 percent to 20 percent (W/W) of minocycline hydrochloride, 15 percent to 40 percent (W/W) of biodegradable polymer material; the ratio between biodegradable polymer material and chemical cross-linking reagent is 1g : 5mL to 1g : 20mL; the volume ratio between aqueous phase and fat phase is 1 : 10 to 1 : 20 (V/V). The minocycline hydrochloride microsphere and the related preparation thereof (such as jellies) prepared by the invention not only has the remarkable advantages of avoiding the toxic and side effects resulted from systemic antibiotics use, being able to reach the depth of periodontal pocket, sustained-release of the medicine at the bottom (one dose can result in continuous release for 7 days), etc., but also greatly reduces the marketing price owing to the cost reduction resulted from totally using home-made excipients, which is beneficial for reducing the patient burden.

Description

technical field [0001] The invention relates to a minocycline hydrochloride microsphere, a preparation method thereof and an application in pharmacy, and provides a new type of therapeutic drug suitable for local sustained-release administration of periodontitis. Background technique [0002] Periodontitis is a common bacterial infectious disease in the Department of Stomatology. The application of antibiotics has become an important means of periodontitis treatment. Minocycline is a new type of semi-synthetic tetracycline, which has the characteristics of broad antibacterial spectrum, strong antibacterial activity, high efficiency, long-term effect, easy penetration, and high sensitivity to various pathogenic bacteria of periodontitis. It is regarded as the drug of choice for the treatment of periodontal disease. [0003] In a physiological pH environment, minocycline has the strongest fat solubility among tetracyclines, and it is easier to diffuse into various body fluids...

Claims

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Application Information

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IPC IPC(8): A61K31/65A61K9/16A61K47/34A61K47/36A61K47/38A61K47/42A61P1/02
Inventor 高迎春王晓娟王荣陈涛于洋
Owner NORTHWESTERN POLYTECHNICAL UNIV
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