Injection doxycycline hyclate freeze-drying powder and preparation method thereof

A technology of doxycycline hydrochloride and freeze-dried powder, which is applied in the field of doxycycline hydrochloride freeze-dried powder for injection and its preparation, can solve the problems of the increase of related substances, failure to shape, low analysis and drying temperature, etc., and achieve relevant The effect of small substance content, prolonging the service life, and improving stability

Active Publication Date: 2018-01-30
JINAN KANGHE MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This patent does not control vitamin C-related substances. Although the freeze-drying curve of this patent has a long sublimation time, most of the free water can be removed, but the analytical drying temperature is low, and the drying time is too short to be conducive to the sublimation of bound water. Product moisture may be high
[0008] Chinese patent CN105078905A discloses a preparation method of doxycycline hydrochloride freeze-dried preparations. The patent test example involves a repeated pre-freezing process. After freeze-drying, the surface of the product is bubbling, with obvious shrinkage, and cannot be formed.
This repeated pre-freezing process cannot meet the characteristics of "cooling and freezing the product first, then raising the temperature to

Method used

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  • Injection doxycycline hyclate freeze-drying powder and preparation method thereof
  • Injection doxycycline hyclate freeze-drying powder and preparation method thereof
  • Injection doxycycline hyclate freeze-drying powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Prescription (1000 sticks): specification 0.1g (in C 22 h 24 N 2 o 8 count)

[0037] Element

Dosage

Doxycycline hydrochloride (in C 22 h 24 N 2 o 8 count)

100g

Vitamin C

400g

cysteine ​​hydrochloride

5g

lactose

300g

hydrochloric acid or sodium hydroxide

Appropriate amount

Water for Injection

Add to 3500ml

[0038] Preparation:

[0039] (1) Dosing: inject 2625ml of water for injection into the dosing tank, control the temperature at 20°C, add 400g of vitamin C, 5g of cysteine ​​hydrochloride, stir to dissolve; add 300g of lactose, 100g of doxycycline hydrochloride in turn, stir Make it dissolve, adjust the pH to 1.8 with sodium hydroxide or hydrochloric acid, add 0.03% (w / v) activated carbon to the liquid medicine, stir at room temperature for 15 minutes, add water for injection to 3500ml, titanium rod filter (specification: 1.0μm material : Titanium rod) filtration cycle for 5-1...

Embodiment 2

[0049] Prescription (1000 sticks): specification 0.15g (in C 22 h 24 N 2 o 8 count)

[0050]

[0051]

[0052] Preparation:

[0053] (1) Dosing: Inject 2625ml of water for injection into the dosing tank, control the temperature at 25°C, add 500g of vitamin C, 8g of cysteine ​​hydrochloride, stir to dissolve; add 350g of lactose, 150g of doxycycline hydrochloride in turn, and stir Make it dissolve, adjust the pH to 2.2 with sodium hydroxide or hydrochloric acid, add 0.03% (w / v) activated carbon to the liquid medicine, stir at room temperature for 15 minutes, add water for injection to 3500ml, and use a titanium rod filter (specification: 1.0μm material : Titanium rod) filtration cycle for 5-10 minutes for decarburization. Pass the liquid medicine through the pre-filter (specification: 0.45μm material: polyethersulfone), secondary filter (specification: 0.22μm material: polyethersulfone), terminal sterilization filter (specification: 0.22μm material) within 30 minutes...

Embodiment 3

[0058] Prescription (1000 sticks): specification 0.2g (in C 22 h 24 N 2 o 8 count)

[0059] Element

Dosage

Doxycycline hydrochloride (in C 22 h 24 N 2 o 8 count)

200g

Vitamin C

600g

cysteine ​​hydrochloride

10g

lactose

400g

hydrochloric acid or sodium hydroxide

Appropriate amount

Water for Injection

Add to 3500ml

[0060] Preparation:

[0061] (1) Dosing: Inject 2625ml of water for injection into the dosing tank, control the temperature at 30°C, add 600g of vitamin C, 10g of cysteine ​​hydrochloride, stir to dissolve; add 400g of lactose, 200g of doxycycline hydrochloride in turn, and stir Make it dissolve, adjust the pH to 3.3 with sodium hydroxide or hydrochloric acid, add 0.03% (w / v) activated carbon to the liquid medicine, stir at room temperature for 15 minutes, add water for injection to 3500ml, titanium rod filter (specification: 1.0μm material : Titanium rod) filtration cycle f...

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PUM

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Abstract

The invention relates to injection doxycycline hyclate freeze-drying powder and a preparation method thereof. The freeze-dry powder comprises active components, namely doxycycline hyclate, a stabilizer, an excipient and injection water, wherein the stabilizer is vitamin C and cysteine hydrochloride; the excipient is lactose; the weight ratio of doxycycline hyclate, vitamin C, cysteine hydrochloride to the lactose is (10-20):(40-60):(0.5-1):(30-40). A good eutectic compound is prepared from the doxycycline hyclate, the vitamin C, the cysteine hydrochloride and the lactose. According to the preparation method of the freeze-drying powder, a repeated heating and cooling mode is adopted in pre-freezing, and the analysis drying temperature is appropriately increased. By adopting the technical scheme, the freeze-drying powder is good in shape, full in appearance, loosened and porous and good in redissolubility, controllable in moisture limit and stable in quality, and the storage life of themedicine can be effectively prolonged.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a doxycycline hydrochloride freeze-dried powder for injection and a preparation method thereof. Background technique [0002] The chemical name of doxycycline hydrochloride is: 6-methyl-4-(dimethylamino)-3,5,10,12,12α-pentahydroxy-1,11-dioxo-1,4,4α,5 ,5α,6,11,12α-Octahydro-2-tetracenecarboxamide hydrochloride hemiethanol hemihydrate. The structural formula is: [0003] [0004] Doxycycline hydrochloride is a broad-spectrum semi-synthetic tetracycline antibiotic. Its antibacterial spectrum is similar to that of tetracycline, and its antibacterial effect is 10 times stronger. The medicine has strong water solubility, good absorption, wide distribution, more clinical application and good effect, and its antibacterial activity in vivo and in vitro is stronger than that of tetracycline. This product can inhibit Gram-negative bacteria, positive bacteria, spirochetes, ri...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/65A61K47/22A61K47/18A61K47/26A61P31/04
Inventor 张颖朱文霞李鹏张作平
Owner JINAN KANGHE MEDICAL TECH
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