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Doxycycline hydrochloride long-acting injection

A technology of doxycycline hydrochloride and injection, which is applied to the long-acting injection of doxycycline hydrochloride and the field of preparation thereof, can solve the problem that doxycycline hydrochloride is easy to degrade, is not easy to inject, and has large tissue irritation. problem, to achieve the effect of not easy oxidative degradation, ensuring effective concentration, and stable product properties

Inactive Publication Date: 2012-05-09
TIANJIN RINGPU BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The invention provides a long-acting injection of doxycycline, which solves the disadvantages of oral administration of doxycycline hydrochloride, and solves the problem that doxycycline hydrochloride is easy to degrade in aqueous solution, is not easy to make injections, and causes tissue irritation. Disadvantages of high reliability and high cost

Method used

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  • Doxycycline hydrochloride long-acting injection
  • Doxycycline hydrochloride long-acting injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Recipe dosage

[0029] Doxycycline Hydrochloride 3000g

[0030] Glycerin Formal 5L

[0031] Polyethylene glycol 400 1L

[0032] N-Methylpyrrolidone 1L

[0033] Magnesium chloride 1000g

[0034] Calcium chloride 100g

[0035] Sodium formaldehyde sulfoxylate 4g

[0036] Appropriate amount of ethanolamine

[0037] Add water for injection to 10L

[0038] Preparation:

[0039] A, take each component by prescription quantity, standby;

[0040] B. Mix 5L glycerin formal, 1L polyethylene glycol 400, 1L N-methylpyrrolidone, and 1L water for injection, and heat to 40-60°C;

[0041] C, under stirring state, add sodium formaldehyde sulfoxylate, magnesium chloride, calcium chloride successively;

[0042] D, add the doxycycline hydrochloride of prescription quantity under stirring state, stir until dissolving;

[0043] F. Take it out and cool it at room temperature, add ethanolamine, and adjust the pH value to 8.0-9.0;

[0044] G. Add water for injection to 10L, and final...

Embodiment 2

[0046] Recipe dosage

[0047] Doxycycline Hydrochloride 2000g

[0048] Glycerin Formal 4L

[0049] Polyethylene glycol 600 0.5L

[0050] N-Methylpyrrolidone 2L

[0051] Magnesium Oxide 170g

[0052] Calcium chloride 60g

[0053] Sodium sulfite 10g

[0054] Appropriate amount of ethanolamine

[0055] Add water for injection to 10L

[0056] Preparation:

[0057] A, take each component by prescription quantity, standby;

[0058] B. Mix 4L glycerin formal, 0.5L polyethylene glycol 400, 2L N-methylpyrrolidone, and 1L water for injection, and heat to 40-60°C;

[0059] C, under stirring state, add sodium sulfite, magnesium oxide, calcium chloride successively;

[0060] D, add the doxycycline hydrochloride of prescription quantity under stirring state, stir until dissolving;

[0061] F. Take it out and cool it at room temperature, add ethanolamine, and adjust the pH to 8.0-9.0;

[0062] G. Add water for injection to 10L, and finally pour the obtained solution into a steril...

Embodiment 3

[0064] Recipe dosage

[0065] Doxycycline Hydrochloride 1000g

[0066] Glycerin Formal 2L

[0067] Macrogol 400 0100g

[0068] N-Methylpyrrolidone 1L

[0069] Magnesium oxide 80g

[0070] Calcium chloride 30g

[0071] Sodium formaldehyde sulfoxylate 1g

[0072] Appropriate amount of ethanolamine

[0073] Add water for injection to 10L

[0074] Preparation:

[0075] A, take each component by prescription quantity, standby;

[0076] B. Mix 2L glycerin formal, 0.1L polyethylene glycol 400, 1L N-methylpyrrolidone, and 1L water for injection, and heat to 40-60°C;

[0077] C, under stirring state, add sodium formaldehyde sulfoxylate, magnesium oxide, calcium chloride successively;

[0078] D, add the doxycycline hydrochloride of prescription quantity under stirring state, stir until dissolving;

[0079] F. Take it out and cool it at room temperature, add ethanolamine, and adjust the pH to 8.0-9.0;

[0080] G. Add water for injection to 10L, and finally pour the obtained ...

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Abstract

The invention discloses doxycycline hydrochloride long-acting injection and a preparation method thereof. The injection comprises the following components: 5-30% (W / V) of doxycycline hydrochloride, 25-70% (V / V) of compound organic solvent, 0.01-0.1% (W / V) of oxidation inhibitor, 0.5-10% (W / V) of magnesium compound complexing agent and 0.1-1% (W / V) of calcium compound complexing agent. The preparation method comprises the following steps of: mixing the components, adopting alkali to adjust the pH value to 8.0-9.0, and adding water for injection to 100% (V / V). According to the invention, the problem that doxycycline injection is easy to oxidize and decompose can be effectively solved.

Description

technical field [0001] The invention belongs to the field of veterinary drug preparations, in particular to a long-acting injection of doxycycline hydrochloride and a preparation method thereof. Background technique [0002] Doxycycline, also known as deoxyoxytetracycline, removes an oxygen atom at the R position of the chemical structural formula of oxytetracycline, and its chemical name is 6-methyl-4-(dimethylamino)-3,5,10, 12,12a Pentahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydro-2-tetracenecarboxamide, the molecular formula is: C 22 h 24 N 2 o 8 , the molecular weight is 512.93. The core of polycyclic tetracene carboxamide is the necessary structure for antibacterial effect. Due to the different substituents of R1, R2, and R3 at the 5, 6, and 7 positions, they exhibit different antibacterial activities. The order of antibacterial activity is minocycline > Doxycycline > Metacycline > Chlortetracycline > Tetracycline > Oxytetracycline. Doxycycline ...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/65A61K47/34A61K47/04A61P31/00
Inventor 魏德宝夏雪林刘爱玲刘桂兰
Owner TIANJIN RINGPU BIO TECH
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