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Ofloxacin molecular inclusion nanometer preparation and preparation method thereof

A technology of ofloxacin and nano preparations, which is applied in the field of medicine, can solve the problems of reduced curative effect, reduced intestinal absorption, and reduced bioavailability, and achieves the effects of simple preparation process, small stimulating effect, and fast drug absorption

Inactive Publication Date: 2012-09-19
商丘天华生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But ofloxacin has some problems in practical application, ①ofloxacin has poor water solubility, reduced intestinal absorption, and reduced bioavailability; ②bitter taste, poor palatability, and large gastrointestinal irritation, resulting in Feed intake of animals is small, and the utilization rate of conventional preparations is 3~52%; ③The stability is poor, and the curative effect is reduced after the light changes color
Due to the existence of the above problems, the therapeutic effect of ofloxacin is reduced
In order to enhance the therapeutic effect, it is usually necessary to increase the dosage, but because the palatability has not been fundamentally improved, the feed intake of animals cannot be increased, and the curative effect is still very poor
Also lead to a large amount of drug waste and damage to the ecological environment

Method used

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  • Ofloxacin molecular inclusion nanometer preparation and preparation method thereof
  • Ofloxacin molecular inclusion nanometer preparation and preparation method thereof
  • Ofloxacin molecular inclusion nanometer preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] (1) The molecular inclusion nano-preparation of ofloxacin is mainly made of the following raw materials in parts by weight:

[0028] Ofloxacin 0.5 parts by weight,

[0029] 5 parts by weight of β-cyclodextrin,

[0030] 0.05 parts by weight of acetic acid,

[0031] 0.5 parts by weight of hydroxypropyl methylcellulose.

[0032] (2) Method for preparing ofloxacin molecular inclusion nano-preparation:

[0033] Dissolve 0.5 parts by weight ofloxacin in distilled water containing 0.05 parts by weight of acetic acid; add 5 parts by weight of β-cyclodextrin to the ofloxacin solution under 100KHz ultrasonic conditions in a water bath at 40°C for 10 minutes Minutes; Stir and sonicate for 25 minutes under 45KHz ultrasonic conditions in a 40°C water bath; Stir and sonicate for 15 minutes under 28KHz ultrasonic conditions in a 40°C water bath; then mechanically grind for 20 minutes. After adding 0.5 parts by weight of hydroxypropylmethylcellulose, continue to grind for 20 minute...

Embodiment 2

[0035] (1) The molecular inclusion nano-preparation of ofloxacin is mainly made of the following raw materials in parts by weight:

[0036] 1 part by weight ofloxacin,

[0037] 7 parts by weight of β-cyclodextrin,

[0038] 0.05 parts by weight of acetic acid,

[0039] 1.95 parts by weight of hydroxypropyl methylcellulose.

[0040] (2) Method for preparing ofloxacin molecular inclusion nano-preparation:

[0041] Dissolve 1 part by weight ofloxacin in distilled water containing 0.05 parts by weight of acetic acid; add 7 parts by weight of β-cyclodextrin to the ofloxacin solution under 100KHz ultrasonic conditions in a water bath at 40°C, and ultrasonic time for 10 Minutes; Stir and sonicate for 20 minutes under 45KHz ultrasonic conditions in a 40°C water bath; Stir and sonicate for 15 minutes under 28KHz ultrasonic conditions in a 40°C water bath; then mechanically grind for 25 minutes. After adding 1.95 parts by weight of hydroxypropylmethylcellulose, continue to grind for ...

Embodiment 3

[0043] (1) The molecular inclusion nano-preparation of ofloxacin is mainly made of the following raw materials in parts by weight:

[0044] Ofloxacin 2 parts by weight,

[0045] Hydroxypropyl-β-cyclodextrin 6 parts by weight,

[0046] 0.1 parts by weight of methanesulfonic acid,

[0047] 1.9 parts by weight of hydroxypropyl methylcellulose.

[0048] (2) Method for preparing ofloxacin molecular inclusion nano-preparation:

[0049] Dissolve 2 parts by weight ofloxacin in distilled water containing 0.1 part by weight of methanesulfonic acid; add 6 parts by weight of hydroxypropyl-β-cyclodextrin to ofloxacin under 100KHz ultrasonic conditions in a water bath at 40°C In the solution, ultrasonic time was 20 minutes; stirred and sonicated for 30 minutes under 45KHz ultrasonic conditions in a 40°C water bath; stirred and sonicated for 25 minutes under 28KHz ultrasonic conditions in a 40°C water bath; then mechanically ground for 30 minutes. After adding 1.9 parts by weight of hydr...

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Abstract

The invention relates to an ofloxacin molecular inclusion nanometer preparation and a preparation method thereof, belonging to the technical field of medicines. The main raw materials of the molecular inclusion nanometer preparation are cyclodextrin, solubilizer, polymer materials, ofloxacin and the like. The preparation method comprises the steps of: adding the cyclodextrin after dissolving the ofloxacin in a solution containing the solubilizer and preparing a molecular inclusion compound through a gradient ultrasonic grinding method; then adding the polymer materials for grinding; and drying and smashing to obtain the ofloxacin molecular inclusion nanometer preparation. The average particle size of the molecular inclusion nanometer preparation is 252.3 nm; and the drug content is 1%-25%. The preparation method, disclosed by the invention, has the advantages of being simple in a preparation process, high in drug carrying amount and stability, controllable in quality, suitable for industrial production and the like. The ofloxacin molecular inclusion nanometer preparation prepared by the method has the advantages of efficiently improving stability of the drug and dissolution degree as well as dissolution speed of the drug in a gastrointestinal tract, improving a drug absorption rate, realizing rapid and efficient effects, masking bitter taste of the drug, reducing drug irradiation and improving drug palatability and drug availability.

Description

technical field [0001] The invention relates to a fluoroquinolone antibacterial drug, in particular to an ofloxacin molecular inclusion nano preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Ofloxacin (Ofloxacin) is a synthetic, highly effective and broad-spectrum antibacterial fluoroquinolone drug. Ofloxacin has a strong effect on Gram-positive bacteria (including methicillin-resistant Staphylococcus aureus) and Gram-negative bacteria (including Pseudomonas aeruginosa). Anaerobic bacteria and Mycobacterium tuberculosis also have some activity. Ofloxacin is a bactericide that inhibits DNA synthesis and replication by acting on the A subunit of bacterial DNA helicase, leading to bacterial death. The drug has no cross-resistance with other antibacterial drugs, and is widely used in the prevention and treatment of bacterial diseases in livestock and poultry with remarkable curative effect. But ofloxacin ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/19A61K47/40A61K31/5383A61P31/04
Inventor 赵永星朱冬雪杜向党陈五常袁之润
Owner 商丘天华生物科技有限公司
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