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Composition for improving absorbance of aminoglycoside drug

An aminoglycoside and composition technology, which is applied in the field of compositions for improving the absorption of aminoglycosides, can solve problems such as low oral absorption, and achieve the effects of low toxicity and side effects, stable quality, and a wide range of applicable drugs.

Active Publication Date: 2011-08-10
RINGPU TIANJIN BIOLOGICAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the problem of low oral absorption of aminoglycosides, the present invention provides a composition for improving the absorption of aminoglycosides through the determination of oral absorption promotion, cytotoxicity research, and observation of toxic and side effects of experimental animals. The composition is composed of 0.1-5% (W / W) absorption enhancer, 5-20% (W / W) aminoglycoside drugs and auxiliary materials

Method used

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  • Composition for improving absorbance of aminoglycoside drug
  • Composition for improving absorbance of aminoglycoside drug
  • Composition for improving absorbance of aminoglycoside drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Embodiment 1: A kind of composition that improves oral absorption of gentamicin sulfate

[0015] Party:

[0016]

[0017] Preparation method:

[0018] Anhydrous glucose is used to mix sodium caprate and sodium glycocholate in an equal volume gradient for 6 times, and then mix all the raw and auxiliary materials, and after fully mixing uniformly, a pharmaceutical composition of powder is obtained.

Embodiment 2

[0019] Embodiment 2: A kind of composition granule that improves kanamycin sulfate oral absorption

[0020]

[0021] Carry out the preparation of granule according to following process:

[0022] (1) Weigh sodium caprate, sodium laurate, and sodium taurocholate, and dilute with starch for 3 times respectively, mix and fully stir to obtain three kinds of mixtures;

[0023] (2) Mix the above three mixtures with the remaining starch, anhydrous glucose and kanamycin sulfate in a mixer for 30 minutes to obtain mixture B;

[0024] (3) Weigh PVP and dissolve it in ethanol, mix evenly to obtain mixture C;

[0025] (4) Slowly pour mixture C into mixture B, granulate with a 14-mesh sieve when dry and wet, and granulate with a 16-mesh sieve after the granules are dried to obtain a drug absorption rate of kanamycin sulfate composition particles.

Embodiment 3

[0026] Embodiment 3: Investigation of the absorption-promoting effect of the composition

[0027] Give the product of embodiment 1 to 60 days old piglets of 20 fasting states, 4mg / kg body weight (calculated as gentamicin), drinking water throws something and feeds, and this is test group; Mycin soluble powder (5%), 4mg / kg body weight (calculated as gentamicin), fed with drinking water. Determination of blood drug concentration at different times, the results are shown in the attached figure 1 shown, from the attached figure 1 It can be concluded that after adding the absorption enhancer, the absorption of gentamicin sulfate can be detected from 1 hour after administration, and reaches the peak value after 3 hours of administration, which is more than 2 times higher than that of the control drug. The pharmacokinetic parameters of the two drugs were calculated according to the blood drug concentrations, and the average values ​​are shown in Table 1 below.

[0028] The pharmac...

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Abstract

The invention provides a composition for improving the absorbance of aminoglycoside drug, which has greatly-improved absorbance in organisms and exhibits effective pharmacological action. The composition contains 0.1 to 5% absorption enhancer, which is one or more of medium chain sodium aliphatate salt and cholic acid salts; 5 to 20% of aminoglycoside drug, and the balance of pharmaceutically acceptable auxiliaries. Oral administration of the aminoglycoside drug results in quite little absorption of the aminoglycoside drug, and clinical oral drug is used only as the drug for enteric infection. According to the invention, as the absorption enhancer is added, the applicable scope of the aminoglycoside drug is widened, and oral administration can reach the purpose of treating general infection.

Description

technical field [0001] The invention relates to a composition for improving the absorption of aminoglycoside drugs. The composition can effectively exhibit pharmacological effects in a living body through oral administration. Background technique [0002] Aminoglycoside antibiotics are glycoside antibiotics formed by linking aminosugar and aminocyclic alcohol through oxygen bridges. Aminoglycoside drugs can be divided into three categories according to their sources: the first category is obtained from the culture filtrate of Streptomyces, such as streptomycin, dihydrostreptomycin, neomycin, paromomycin, and redunomycin , Kanamycin, Kanamycin B, Tobramycin, Ribomycin, etc. The second class of antibiotics produced by Micromonospora, such as gentamicin, sisomycin, spectinomycin, abramycin, small nomicin. The third category is semi-synthetic aminoglycoside drugs, such as Qingda-minornomycin, dibekacin, amikacin, netilmicin, etc. [0003] A common feature of aminoglycoside an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/12A61K47/28A61K31/7036A61P31/04
Inventor 刘桂兰刘爱玲夏雪林
Owner RINGPU TIANJIN BIOLOGICAL PHARMA
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