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Aqueous suspension injection of cephalosporins and preparation method thereof

A technology of suspension injection and cephalosporins, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, antibacterial drugs, etc. It can solve the problems of strong tissue irritation, short expiration date and poor stability of finished products, and achieve muscle stimulation Small effect, good redispersibility and good stability

Active Publication Date: 2015-11-11
LUOYANG HUIZHONG ANIMAL MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the β-lactam ring contained in the chemical structure of cephalosporins is unstable in aqueous solution, is easily hydrolyzed or decomposed, has poor stability, and the validity period of the finished product is short, which limits its application as an aqueous injection
[0003] At present, cephalosporins in the form of injections are mostly in the form of powder injections and oily suspensions, and the oily suspensions of cephalosporins are mostly vegetable oils or mineral oils for injections, which are relatively high in viscosity, difficult to extract and inject, and oily. The solvent is highly irritating to the tissue, causing inconvenience in use; at the same time, because the cost of vegetable oil for injection or mineral oil for injection is high, resulting in high product cost
The powder injection needs to be prepared with a diluent before use, and the prepared solution must be used up within a specified short time, causing inconvenience in use

Method used

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  • Aqueous suspension injection of cephalosporins and preparation method thereof
  • Aqueous suspension injection of cephalosporins and preparation method thereof
  • Aqueous suspension injection of cephalosporins and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1 cephalosporin aqueous suspension of the present invention and preparation method thereof

[0036] Sample 1, 5% w / v cephalexin aqueous suspension and preparation method thereof

[0037]

[0038] Preparation steps:

[0039] 1) Weigh 1.0 g of sodium carboxymethyl cellulose, add it to 80 ml of water, heat slowly to about 60 ° C, stir while heating until the sodium carboxymethyl cellulose is completely dissolved, and set the volume to 100 ml to obtain 0.5% carboxymethyl cellulose Sodium cellulose solution.

[0040] 2) Weigh 10.0g of PVPK30, add a small amount of water to make a solution, add carboxymethylcellulose sodium solution 30ml, sorbitol 5.0g, sodium citrate 3.0g, poloxamer 0.5g, dihydrogen phosphate Add 0.1g of potassium, 0.01g of sodium formaldehyde sulfoxylate, 0.01g of methyl p-hydroxybenzoate, and 0.005g of methyl p-hydroxybenzoate into 50ml of water, stir to dissolve completely.

[0041] 3) Add 5.0 g of micronized cephalexin (Shijiazhuang Taih...

Embodiment 2

[0070] Embodiment 2, the appearance inspection that contains cephalosporin aqueous suspension sample

[0071] Take the aqueous suspension samples 1, 2, 3, and 4 of the present invention, observe their appearance properties, wall hanging phenomenon, measure their sedimentation volume ratio and viscosity, and evaluate the appearance quality.

[0072] For the determination method of sedimentation volume ratio and content, please refer to the second volume of "The Veterinary Pharmacopoeia of the People's Republic of China" in 2010.

[0073] Table 2, the quality inspection of the suspension sample prepared by the inventive method

[0074]

[0075] It can be seen from the table above that the appearance of aqueous suspension injection samples 1, 2, 3, and 4 is milky white liquid, and there is no wall hanging phenomenon after shaking. 99-101% of the marked amount meets the appearance quality requirements of the suspension injection.

Embodiment 3

[0076] Embodiment 3, viscosity and needle-drawing inspection

[0077] Take samples 1, 2, 3, and 4 of the aqueous suspension injection prepared by the present invention, and compare them with oily injections currently on the market, and compare the differences in viscosity and needle withdrawal.

[0078] Control 1: 5% w / v ceftiofur hydrochloride oily injection (Shu Kejian, produced by Shandong Qilu Animal Health Products Co., Ltd., batch number: 100801)

[0079] Control 2: 5% w / v ceftiofur hydrochloride oily injection (Sujieling, Upjohn Company, USA, batch number: 0A3H9,)

[0080] Viscosity measurement method: Take an appropriate amount of the test product, put it in a water bath in the container and keep the temperature at 20°C. Use a 5ml graduated straw (the diameter of the inner wall at the outlet end of the straw is 2mm) to draw 5ml of the test product, let it flow out naturally, and record the time required to flow out 5ml.

[0081] Needle-drawing property: Take an appro...

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Abstract

The invention provides an aqueous suspension injection of cephalosporin medicines, and a preparation method thereof. The aqueous suspension injection comprises the components of 5-20% W / V of a 7-aminocephalosporanic acid derivative, 10-40% W / V of an excipient, 5-25% W / V of a suspending agent, 0.1-0.6% W / V of a suspending aid, 0.1-0.5% W / V of a pH buffer, 0.1-1.0% of an addition amount of a surfactant, and balance of injection water. The 7-aminocephalosporanic acid derivative is micronized, wherein 7-aminocephalosporanic acid derivative particles with size smaller than 100mum account for no lower than 95% by volume of the total volume of the raw materials, and 7-aminocephalosporanic acid derivative particles with size smaller than 20mum and larger than 2mum account for no lower than 90% of the total volume of the raw materials. Compared with oily preparations or powdery preparations of cephalosporin medicines, the aqueous suspension injection of cephalosporin medicines provided by the invention has lower viscosity and better injection performance, such that cephalosporin medicine stability is improved. The viscosity of cephalosporin medicines is reduced, such that injection irritation is reduced.

Description

technical field [0001] The invention relates to an aqueous suspension of cephalosporins and a preparation method thereof, in particular to an aqueous suspension injection of cephalosporins and a preparation method thereof. Background technique [0002] Cephalosporins are a class of antibiotics widely used clinically, and are popular because of their strong bactericidal power, wide antibacterial spectrum, and safe use. Especially in recent years, the use of sulfonamides is limited, aminoglycosides are highly toxic, and third- and fourth-generation cephalosporins are widely used in clinics, becoming a class of antibiotics with great development prospects. However, the β-lactam ring contained in the chemical structure of cephalosporins is unstable in aqueous solution, is easily hydrolyzed or decomposed, has poor stability, and has a short validity period of the finished product, which limits its application as an aqueous injection. [0003] At present, most injections of cepha...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/545A61K31/546A61P31/04
Inventor 张许科刘兴金张晓会
Owner LUOYANG HUIZHONG ANIMAL MEDICINE
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