Long-acting compound doxycycline injection

A technology for doxycycline and injection, which is applied in the field of long-acting compound doxycycline injection and its preparation, can solve the problems of livestock and poultry stress, large tissue irritation, reduced drug efficacy and the like, and achieves improved therapeutic effect , the effect of relieving body surface symptoms and reducing the mortality rate

Inactive Publication Date: 2012-05-16
TIANJIN RINGPU BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, most of the doxycycline preparations on the market are injections and oral preparations, but the injections are all single preparations or compound preparations composed of two or more antibiotics. Oral preparations can effectively alleviate the problem of large tissue irritation, but the drug's efficacy is often reduced due to the chelation of metal ions such as calcium and magnesium in the intestinal tract during oral administration. Oral absorption and availability, reducing efficacy
Considering the above-mentioned shortcomings of the current doxycycline long-acting injection and the important role of anti-inflammatory drugs in clinical applications, and

Method used

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  • Long-acting compound doxycycline injection
  • Long-acting compound doxycycline injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Recipe dosage

[0022] Doxycycline hydrochloride 3000g (calculated as doxycycline)

[0023] α-Asarone 100g

[0024] Glycerin Formal 5L

[0025] Polyethylene glycol 400 1L

[0026] Hydroxypropyl beta-cyclodextrin 1000g

[0027] Magnesium chloride 1000g

[0028] Calcium chloride 100g

[0029] Sodium formaldehyde sulfoxylate 10g

[0030] Appropriate amount of ethanolamine

[0031] Add water for injection to 10L

[0032] Preparation:

[0033] A. Measure 4001L of polyethylene glycol, 2.5L of glycerin formal, and 0.8L of water for injection, mix well, add 1000g of magnesium chloride, 100g of calcium chloride, 10g of antioxidant, stir well, and make it solution 1;

[0034] B. Add doxycycline hydrochloride to solution 1, and heat up to 45-65°C while stirring. After the dissolution is complete, stop heating, cool to room temperature, and doxycycline solution;

[0035] C. Measure 2.5L of glycerin formal and 1L of water for injection, add 100g of α-asarone and 1000g of h...

Embodiment 2

[0039] Recipe dosage

[0040] Doxycycline 2000g (calculated as doxycycline)

[0041] α-Asarone 65g

[0042] Glycerin Formal 4L

[0043] Polyethylene glycol 200 1.5L

[0044]Glucosyl β-cyclodextrin 800g

[0045] Magnesium Oxide 170g

[0046] Calcium chloride 60g

[0047] Sodium sulfite 5g

[0048] Appropriate amount of ethanolamine

[0049] Add water for injection to 10L

[0050] Preparation:

[0051] A. Measure 1.5L of polyethylene glycol, 2L of glycerin formal, and 0.8L of water for injection, mix well, add 170g of magnesium oxide, 60g of calcium chloride, and 6g of antioxidant, stir well, and make it solution 1;

[0052] B. Add 2000 g of doxycycline (the content is based on doxycycline) in solution 1, and heat up to 45-65°C while stirring. After the dissolution is complete, stop heating, cool to room temperature, and doxycycline solution ;

[0053] C. Measure 2L of glycerol formal and 1L of water for injection, add 65g of α-asarone and 800g of glucosyl β-cyclodext...

Embodiment 3

[0057] Recipe dosage

[0058] Doxycycline hydrochloride 1000g (calculated as doxycycline)

[0059] α-Asarone 30g

[0060] Glycerin Formal 2L

[0061] Polyethylene glycol 600 0.7L

[0062] Methyl β-cyclodextrin 100g

[0063] Magnesium oxide 80g

[0064] Calcium chloride 30g

[0065] Sodium formaldehyde sulfoxylate 1g

[0066] Appropriate amount of ethanolamine

[0067] Add water for injection to 10L

[0068] Preparation:

[0069] A. Measure 6000.7L of polyethylene glycol, 1L of glycerin formal, and 0.8L of water for injection, mix well, add 80g of magnesium oxide, 30g of calcium chloride, 1g of antioxidant, stir well, and use it as solution 1;

[0070] B. Add 1000 g of doxycycline hydrochloride (the content is based on doxycycline) in solution 1, and heat up to 45-65 ° C while stirring. After the dissolution is complete, stop heating and cool to room temperature. solution;

[0071] C. Measure 1L of glycerol formal and 1L of water for injection, add 30g of α-asarone a...

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PUM

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Abstract

The invention discloses a long-acting copound doxycycline injection and a preparation process thereof. The injection comprises the following components in percentage by weight in volume: 5 to 30 percent of doxycycline, 0.2 to 1 percent of alpha-asarone, 0.5 to 10 percent of magnesium compound complexing agent, 0.1 to 1 percent of calcium copound complexing agent, 1 to 10 percent of inclusion material, 0.01 to 0.1 percent of antioxidant, and the balance of injection solvent which comprises glycerolformal, polyethylene glycol and injection water. In the composition disclosed by the invention, the alpha-asarone has effects of relieving cough and asthma and resisting infection, and can be used for effectively improving the situation of livestock bodies and reducing the death rate when being compounded with doxycycline.

Description

technical field [0001] The invention belongs to the field of veterinary drug preparations, in particular to a long-acting compound doxycycline injection 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 , with a molecular weight of 444.4. 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 hydroc...

Claims

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Application Information

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IPC IPC(8): A61K31/65A61K31/09A61K9/08A61K47/02A61P31/04
Inventor 魏德宝夏雪林刘桂兰聂丽娜刘爱玲
Owner TIANJIN RINGPU BIO TECH
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