Cefuroxime axetil oral liquid and preparation method thereof

A technology for oral nitroxide axetil and cefuroxime axetil, which is applied in the field of antibiotic drugs, can solve the problems of affecting the efficacy of preparations, low dissolution rate, uneven particle size, etc., and achieves improved bioavailability and onset time, mixing High uniformity and uniform particle size effect

Active Publication Date: 2010-11-24
HAINAN RIZHONGTIAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The oral preparation obtained in this way has the disadvantages of uneven particle size and poor material mixing effect, which ultimately affects the drug efficacy of the preparation.
[0004] In addition, the existing cefuroxime axetil capsules have the disadvantage that the dissolution rate is generally low. As stipulated in the 2005 edition of "Chinese Pharmacopoeia", the dissolution rate limit of cefuroxime axetil capsules is 60% of the labeled amount in 15 minutes and 60% in 45 minutes. 75% of the labeled amount
The main reason is that cefuroxime axetil is insoluble in water, once in contact with water, it will coalesce into agglomerates, resulting in reduced dissolution rate and reduced absorption in the gastrointestinal tract, affecting the curative effect

Method used

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  • Cefuroxime axetil oral liquid and preparation method thereof
  • Cefuroxime axetil oral liquid and preparation method thereof
  • Cefuroxime axetil oral liquid and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Cefuroxime axetil capsules

[0028] Cefuroxime axetil capsules, including the following ingredients and their weight:

[0029] Cefuroxime axetil 310g (equivalent to C 16 H 16 N 4 O 8 S 250.0g)

[0030] Talc 70.0g

[0031] PVPP 30.0g

[0032] 2wt% HPMC aqueous solution 200g

[0033] After mixing the above-mentioned API and talc, pass through an 80 mesh sieve, mix with PVPP, pass through a 60 mesh sieve, add 2% hydroxypropyl methylcellulose (HPMC) aqueous solution, granulate at 30 mesh, dry at 60 degrees, 24 mesh Sieve whole granules, fill capsules (0 # Capsules), a total of 1000 capsules are made, each capsule is 0.25gC 16 H 16 N 4 O 8 S.

[0034] Using the conventional dissolution test method, the dissolution rate of cefuroxime axetil capsules was 87% in 15 minutes and 95% in 45 minutes.

Embodiment 2

[0035] Example 2 Cefuroxime axetil tablets

[0036] Cefuroxime axetil tablets, including the following weights of various ingredients:

[0037] Cefuroxime axetil 280g

[0038] Talc 50.0g

[0039] PVPP 15.0g

[0040] 5wt% HPMC aqueous solution 150g

[0041] After mixing the above-mentioned crude drug and talc, pass through an 80 mesh sieve, mix with PVPP, pass through a 60 mesh sieve, add 2% hydroxypropyl methylcellulose (HPMC) aqueous solution, granulate at 30 mesh, dry at 60 degrees, 24 mesh Sieve and granulate, and then obtain 1000 cefuroxime axetil tablets according to the conventional tableting method.

[0042] Using conventional dissolution testing methods, the dissolution rate of cefuroxime axetil tablets reached 85% in 15 minutes and 93% in 45 minutes.

Embodiment 3

[0043] Example 3 Cefuroxime axetil dispersible tablet

[0044] Cefuroxime axetil tablets, including the following weights of various ingredients:

[0045] Cefuroxime axetil 350g

[0046] Talc 100.0g

[0047] PVPP 50.0g

[0048] 3wt% HPMC aqueous solution 180g

[0049] After mixing the above-mentioned crude drug and talc, pass through an 80 mesh sieve, mix with PVPP, pass through a 60 mesh sieve, add 2% hydroxypropyl methylcellulose (HPMC) aqueous solution, granulate at 30 mesh, dry at 60 degrees, 24 mesh Sieve and granulate, and make 1,000 cefuroxime axetil dispersible tablets according to conventional methods.

[0050] Using the conventional dissolution test method, the dissolution rate of cefuroxime axetil dispersible tablets was 84% ​​in 15 minutes and 94% in 45 minutes.

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Abstract

The invention discloses a cefuroxime axetil oral liquid, comprising the following components in parts by weight: 280-350 parts of cefuroxime axetil, 50-100 parts of talcum powders, 10-50 parts of cross-linked polyvinylpyrrolidone and 3-4 parts of hydroxypropyl methyl cellulose. The invention also discloses a preparation method of the oral liquid. The cefuroxime axetil oral liquid of the inventionhas good stability; and in addition, the dissolution within 15 minutes is higher than 80% of that of labeled amount and the dissolution within 45 minutes is higher than 90% of that of the labeled amount.

Description

technical field [0001] The invention relates to the technical field of antibiotic medicines, in particular to oral cefuroxime axetil and a preparation method thereof. Background technique [0002] Cefuroxime axetil is a second-generation cephalosporin antibiotic. After oral absorption through the gastrointestinal tract, it is rapidly hydrolyzed into cefuroxime under the action of esterase to exert an antibacterial effect. It is safe, efficient and resistant to enzymes. Because cephalosporin has a special bitter taste, as an oral preparation, it brings adverse reactions to patients, such as difficulty in swallowing, gastrointestinal discomfort, etc., so its dosage form needs to be improved. [0003] At present, oral preparations of cefuroxime axetil mainly include tablets, dispersible tablets, dry suspensions and capsules, which basically adopt a dry granulation process: the main drug and various auxiliary materials are directly stirred and mixed, and then formed by extrusion...

Claims

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Application Information

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IPC IPC(8): A61K31/546A61K47/38A61P31/04
Inventor 张光春庄太能舒军罗乐郭荣芳陈治锦
Owner HAINAN RIZHONGTIAN PHARMA
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