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Clarithromycin liposome microsphere injection and its prepn. method

A technology of clarithromycin and lipid microspheres, applied in the field of medicine, can solve problems such as impossible preparation, and achieve the effects of reducing toxicity and irritation, providing drug efficacy and increasing drug loading

Inactive Publication Date: 2007-04-18
刘玉辉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen from the above that it is impossible and impossible to prepare clarithromycin emulsion or clarithromycin lipid microsphere injection from this patent

Method used

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  • Clarithromycin liposome microsphere injection and its prepn. method
  • Clarithromycin liposome microsphere injection and its prepn. method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: a clarithromycin lipid microsphere injection, which comprises the following components:

[0041] Castor Oil for Injection 10g

[0042] Clarithromycin 0.5g

[0043] Lecithin 3g

[0044] Glycerin 2.5g

[0045] Caproic acid 0.6g

[0046] Water for injection 100ml

[0047] Its preparation method is as follows:

[0048] 1) Dissolve 0.5g of clarithromycin in 0.6g of caproic acid, mix with 10g of castor oil for injection to form an oil phase, stir magnetically and heat to 60°C;

[0049] 2) Disperse 3g of lecithin and 2.5g of glycerin in 80ml of water for injection, magnetically stir to disperse evenly, and heat to 60°C as the water phase;

[0050] 3) Add the oil phase to the water phase under magnetic stirring, and continue stirring for 10 minutes after the addition to obtain colostrum;

[0051] 4) Homogenizing the prepared colostrum at 30,000 rpm for 10 minutes, repeating it 3 times to obtain a milky white emulsion;

[0052] 5) add remaining 20ml water f...

Embodiment 2

[0053] Embodiment 2: a clarithromycin lipid microsphere injection, which comprises the following components:

[0054] Corn oil for injection 33g

[0055] Clarithromycin 0.7g

[0056] Soy Lecithin 0.3g

[0057] Glycerin 8.8g

[0058] Oleic acid 3g

[0059] Water for injection 64ml

[0060] Its preparation method is as follows:

[0061] 1) Dissolve 0.7g of clarithromycin in 3g of oleic acid, then mix with 33g of corn oil for injection to form an oil phase, magnetically stir and heat to 50°C;

[0062] 2) Disperse 0.3g soybean lecithin and 8.8g glycerin in 50ml water for injection, stir magnetically to disperse evenly, and heat to 50°C as the water phase;

[0063] 3) Add the oil phase to the water phase under magnetic stirring, and continue stirring for 15 minutes after the addition to obtain colostrum;

[0064] 4) Homogenizing the prepared colostrum at 20,000 rpm for 15 minutes, repeating it 3 times to obtain a milky white emulsion;

[0065] 5) add remaining 14ml water fo...

Embodiment 3

[0066] Embodiment 3: a clarithromycin lipid microsphere injection, which comprises the following components:

[0067] C7-C9 Fatty Acid Triglycerides 10g

[0068] Clarithromycin 1g

[0069] Tween 80 3g

[0070] Glycerin 5g

[0071] Pelargonic acid 2g

[0072] Water for injection 79ml

[0073] Its preparation method is as follows:

[0074] 1) Dissolve 1 g of clarithromycin in 2 g of nonanoic acid, then mix it with 10 g of C7-C9 fatty acid triglyceride to form an oil phase, magnetically stir and heat to 80°C;

[0075] 2) Disperse 3g of Tween 80 and 5g of glycerin in 60ml of water for injection, stir magnetically to disperse evenly, and heat to 80°C as the water phase;

[0076] 3) Add the oil phase to the water phase under magnetic stirring, and continue stirring for 12 minutes after the addition to obtain colostrum;

[0077] 4) Homogenizing the prepared colostrum at 20,000 rpm for 15 minutes, repeating it 3 times to obtain a milky white emulsion;

[0078] 5) add remaining...

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Abstract

A lipide microball type injection of clarithromycin with high stability and low toxin is prepared from the oil for injection, clarithromycin, surfactant, glycerin, oil-phase solubilizer, metallic chelating agent, and the water for injection. Its preparing process is also disclosed.

Description

field of invention [0001] The invention relates to the technical field of medicine, in particular the invention relates to a lipid microsphere injection of clarithromycin and a preparation method thereof. Background of the invention [0002] The chemical name of clarithromycin (Clarithromycin, CAM) is 6-O-methylerythromycin, which is the third-generation derivative of macrolides, as shown in the following chemical structure formula. Since in C 6 A methoxy group (-OCH 3 ), so clarithromycin is more acid stable than erythromycin. [0003] [0004] Clarithromycin is widely used clinically in the treatment of infectious and non-infectious diseases such as Helicobacter pylori infection, bacterial infection of respiratory tract and skin soft tissue, biofilm disease, anti-tuberculosis, mycobacterium infection, Pseudomonas aeruginosa biofilm Infection, sexually transmitted diseases, anti-tumor, treatment of sick thyroid syndrome, arteriosclerosis, reduction of serum coagulatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K9/127A61K9/16A61P31/04A61P31/06A61P11/00A61P35/00
Inventor 刘玉辉谢瑞钢
Owner 刘玉辉
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