Ceftiofur hydrochloride liposome lyophilized agent and preparation method thereof

A technology of ceftiofur hydrochloride and cephalosporin hydrochloride, applied in the directions of liposome delivery, freeze-drying delivery, pharmaceutical formulation, etc., can solve the problems of thermodynamic instability, easy leakage of drugs, limited application, etc., and achieves extended cycle time and stability. Good, good encapsulation efficiency

Active Publication Date: 2015-10-21
JIANGXI BOLAI PHARMACY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional liposomes composed of lecithin and cholesterol are thermodynamically unstable systems with poor stability in aqueous media, and the encapsulated drugs are easy to leak. The weak stability in vivo and in vitro limits their application as drug carriers.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1 A ceftiofur hydrochloride liposome lyophilizate, 100ml liposome and lyoprotectant according to the following composition ratio:

[0054] Ceftiofur Hydrochloride 3g

[0055] Lecithin 15g

[0056] Cholesterol 15g

[0057]Macrogol 2000 5g

[0058] Phosphate buffer to full volume

[0059] Lyoprotectant 3g

[0060] ① Weigh lecithin and cholesterol respectively, and dissolve them with one or both of chloroform or ether;

[0061] ② Weigh ceftiofur hydrochloride and dissolve it in methanol to make a clear solution;

[0062] ③Mix the two solutions obtained in step ① and step ②, mix evenly, place in a pear-shaped flask, and rotate under reduced pressure to form a uniform film on the inner wall of the pear-shaped flask;

[0063] ④ Dissolve polyethylene glycol 2000 in phosphate buffer solution, then pour it into a pear-shaped flask, and shake slowly until the membrane is completely washed off to obtain a liposome suspension, and put it in an ultr...

Embodiment 2

[0065] Example 2 A ceftiofur hydrochloride liposome lyophilizate, 100ml liposome and lyoprotectant according to the following composition ratio:

[0066] Ceftiofur Hydrochloride 6.5g

[0067] Lecithin 45.5g

[0068] Cholesterol 23g

[0069] Macrogol 2000 6g

[0070] Phosphate buffer to full volume

[0071] Lyoprotectant 5g

[0072] ① Weigh lecithin and cholesterol respectively, and dissolve them with one or both of chloroform or ether;

[0073] ② Weigh ceftiofur hydrochloride and dissolve it in methanol to make a clear solution;

[0074] ③Mix the two solutions obtained in step ① and step ②, mix them evenly and place them in a pear-shaped flask, and rotate and evaporate under reduced pressure until the inner wall of the pear-shaped flask forms a uniform film;

[0075] ④ Dissolve polyethylene glycol 2000 in phosphate buffer solution, then pour it into a pear-shaped flask, and shake slowly until the membrane is completely washed off to obtain a liposome suspens...

Embodiment 3

[0077] Example 3 A ceftiofur hydrochloride liposome lyophilizate, 100ml liposome and lyoprotectant according to the following composition ratio:

[0078] Ceftiofur Hydrochloride 8g

[0079] Lecithin 60g

[0080] Cholesterol 60g

[0081] Macrogol 2000 10g

[0082] Phosphate buffer to full volume

[0083] Lyoprotectant 6g

[0084] ① Weigh lecithin and cholesterol respectively, and dissolve them with one or both of chloroform or ether;

[0085] ② Weigh ceftiofur hydrochloride and dissolve it in methanol to make a clear solution;

[0086] ③Mix the two solutions obtained in step ① and step ②, mix them evenly and place them in a pear-shaped flask, and rotate and evaporate under reduced pressure until the inner wall of the pear-shaped flask forms a uniform film;

[0087] ④ Dissolve polyethylene glycol 2000 in phosphate buffer solution, then pour it into a pear-shaped flask, and shake slowly until the membrane is completely washed off to obtain a liposome suspensio...

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Abstract

The invention discloses a ceftiofur hydrochloride liposome lyophilized agent and a preparation method thereof. The ceftiofur hydrochloride liposome lyophilized agent comprises, by weight, 3-10 parts of ceftiofur hydrochloride, 15-100 parts of lecithin, 15-100 parts of cholesterols, and 4.5-13.5 parts of polyvinyl alcohol 2000. The preparation method comprises the following steps: dissolving ceftiofur hydrochloride, lecithin and cholesterols, mixing, carrying out vacuum drying, and adding a phosphate buffer solution of polyethylene glycol 2000 to prepare a liposome suspension; and adding a lyophilizing protection agent to the suspension, uniformly mixing, packaging the obtained solution to a penicillin bottle, putting the penicillin bottle provided with the solution in a lyophilizer, and drying to obtain the ceftiofur hydrochloride liposome-carried lyophilized agent. The liposome entrapment rate is good, and a result of long-term stabilization investigation of the liposome lyophilized agent shows that the stability of the liposome lyophilized agent is good; and the lyophilized agent re-dissolved in a liquid medium has the characteristics of good dispersion and stable properties. Clinic curative effect tests prove that compared with suspensions, the liposome lyophilized agent has the advantages of prolonged circulation time in an administrated body, and definite therapeutic effect on porcine respiratory diseases induced by bacterial infection.

Description

technical field [0001] The invention relates to the technical field of veterinary medicine, in particular to a ceftiofur hydrochloride liposome freeze-dried preparation and a preparation method thereof. Background technique [0002] Ceftiofur hydrochloride is a third-generation cephalosporin antibiotic for veterinary use. It has a broad antibacterial spectrum and strong antibacterial activity. It has a stable β-lactam ring and is not prone to drug resistance and cross-resistance. Negative bacteria and some anaerobic bacteria have strong antibacterial activity. Ceftiofur hydrochloride is widely used clinically to prevent and treat bacterial infectious diseases in cattle, horses, pigs and sheep. The main ceftiofur products at home and abroad include powder injection of ceftiofur sodium salt and suspension of ceftiofur hydrochloride. Due to the need for frequent injections and administration, the stress response caused by it will affect the efficacy of the drug and inhibi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/127A61K31/546A61K47/32A61P31/04
Inventor 唐进波毛娉婷肖欣戈熊俊芳
Owner JIANGXI BOLAI PHARMACY CO LTD
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