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Fosfomycin calcium and trimethoprim capsule used for gastrointestinal diseases

A technology of calcium trimethoprim and gastrointestinal diseases, applied in the field of compound preparations, can solve the problems of fast action, short course of treatment, low gastrointestinal absorption rate of oral fosfomycin, etc., and achieve good antibacterial effect and good sustained release The effect of action

Inactive Publication Date: 2017-03-15
重庆希尔安药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The author thinks that the possible factors are as follows: ①Because the gastrointestinal absorption rate of oral fosfomycin is not high and the blood concentration is low, it is generally only suitable for simple lower urinary tract and intestinal infections, so sodium salt injections are usually given intravenously for other infections
② At present, some clinicians are related to patients’ irrational drug habits, and believe that intravenous injection of drugs has a fast effect and a short course of treatment, so it is easy to rush to choose fosfomycin sodium for injection in the process of clinical treatment of acute infection
It is clearly pointed out in the "Guiding Principles for the Clinical Application of Antibacterial Drugs" that aminoglycoside antibiotics and quinolones should be used with caution in children, because aminoglycosides have obvious ototoxicity and nephrotoxicity, and quinolones may have adverse effects on bone development. influences! Coupled with the increasing number of clinical drug-resistant strains, the selection of anti-infective drugs for children is becoming more and more difficult

Method used

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  • Fosfomycin calcium and trimethoprim capsule used for gastrointestinal diseases
  • Fosfomycin calcium and trimethoprim capsule used for gastrointestinal diseases
  • Fosfomycin calcium and trimethoprim capsule used for gastrointestinal diseases

Examples

Experimental program
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Effect test

Embodiment 1

[0020] 1. Sample preparation

[0021] According to the weight ratio of fosfomycin calcium, trimethoprim and glycyrrhizic acid is 8:3:1 to take raw materials as prescription 1, according to the weight ratio of fosfomycin calcium, trimethoprim and glycyrrhizic acid is 30:5: 3 Weigh the raw materials as prescription 2, and weigh the raw materials as prescription 3 according to the weight ratio of fosfomycin calcium, trimethoprim and glycyrrhizic acid as 5:5:3. According to the weight ratio of sodium carboxymethyl cellulose, stearic acid and sodium bicarbonate of 8:4:1, the raw materials are weighed, mixed and pulverized, and passed through a No. 5 sieve; Sodium cellulose, stearic acid, sodium bicarbonate, calcium mycin, trimethoprim and glycyrrhizinic acid were mixed and packed into empty capsules; the packed capsules were heat treated in a constant temperature heater at 60°C for 10 minutes; The heat-treated capsules are naturally cooled to room temperature to obtain the compoun...

Embodiment 2

[0027] Example 2 Research on the in vitro bactericidal activity of Staphylococcus aureus

[0028] The test bacteria is the standard strain MSSA-ATCC29213 of Staphylococcus aureus. The minimum inhibitory concentration (MIC) was determined by the agar plate double dilution method, and the MIC of fosfomycin was determined by adding 25 μg / mL of 6-phosphate-glucose according to the requirements of CLSI.

[0029] According to the MIC test results, the antibacterial drug preparation method will be the experimental group A (the mass ratio of fosfomycin calcium, trimethoprim and glycyrrhizic acid is 8:3:1) and the experimental group B ( The mass ratio of fosfomycin calcium, trimethoprim and glycyrrhizic acid is 30:5:3), experimental group C (the mass ratio of fosfomycin calcium, trimethoprim and glycyrrhizic acid is 5:5:3) and The stock solution of the control group (the mass ratio of fosfomycin calcium and trimethoprim is 5:1) was diluted to 7 serial concentrations of 1 / 4MIC, 1 / 2MIC,...

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Abstract

The invention provides a compound fosfomycin calcium drug. The active component of the compound fosfomycin calcium drug is composed of fosfomycin calcium, trimethoprim and glycyrrhizic acid in a weight ratio of (10-30): (5-10): (3-6). The invention provides a capsule of the compound fosfomycin calcium drug, and the capsules has good slow-release effect; and the compound fosfomycin calcium drug provided by the invention has better antibacterial effect compared with commercially-available related products.

Description

technical field [0001] The invention relates to a compound preparation, in particular to a fosfomycin calcium trimethoprim capsule for gastrointestinal diseases. [0002] technical background [0003] At present, fosfomycin dosage forms that have obtained approval numbers in China include injections (fosfomycin sodium for injection) and oral preparations (fosfomycin calcium tablets, fosfomycin calcium capsules, fosfomycin calcium granules, fosfomycin calcium trimethoprim) Pyridine capsules, fosfomycin trometamol powder). Since fosfomycin calcium trimethoprim capsules and fosfomycin trometamol powder are compound preparations of fosfomycin and other drugs, the analysis of curative effect and adverse reactions is more complicated than that of fosfomycin alone, so this data will not its inclusion in the study. According to statistics, the effective rate of intravenous infusion accounts for 88.01%, but there are also many adverse reactions corresponding to 57 cases. The author...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/665A61K31/704A61P1/00A61P31/04A61K31/505
CPCA61K31/704A61K9/0002A61K9/4866A61K31/505A61K31/665A61K2300/00
Inventor 梅勇杨莉罗磊珠峰龙涛李林霞唐攀袁开超
Owner 重庆希尔安药业有限公司
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