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Antimicrobial medicament preparation with polyanhydrides as vector and its preparing process

A technology of antimicrobial and pharmaceutical preparations, which is applied in the direction of drug combination, anti-infective drugs, pharmaceutical formulations, etc., can solve the problems of large systemic side effects, drug resistance, low selectivity, and large dosage, so as to reduce the dosage of medication and increase the dosage of drugs. Concentration, the effect of avoiding systemic side effects

Inactive Publication Date: 2007-08-08
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, at present, antimicrobial drugs are generally administered systemically, with large doses and low selectivity. When the drugs reach the lesion, the relative concentration is very low, which is easy to cause large systemic side effects and drug resistance.

Method used

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  • Antimicrobial medicament preparation with polyanhydrides as vector and its preparing process
  • Antimicrobial medicament preparation with polyanhydrides as vector and its preparing process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Polysebacic anhydride-gatifloxacin sustained release formulation.

[0028] Precisely weigh 50 mg of the gatifloxacin raw material and place it in a 100 ml volumetric flask, dissolve it with 0.1 mol / L, pH=7.4 PBS and make to volume. Precisely measure 10ml and place it in another 100ml volumetric flask, dissolve and constant volume with 0.1mol / L, pH=7.4 PBS to obtain a gatifloxacin sample solution with a concentration of 50mg / L. Use this solution for UV scanning to determine the maximum absorption wavelength is 285nm.

[0029] Take two kinds of polysebacic anhydride and gatifloxacin raw materials with weight average molecular weights of 27000 and 12000 respectively, and mix them at room temperature according to mass ratios of 90:10, 95:5, and 98:2 (see Table 1 for specific data). ), mixed in a mortar, and ground into a powder. Then move them into self-made cylindrical polytetrafluoroethylene molds (inner diameter is 14mm, inner height is 2mm), compact, heat at 90°C unde...

Embodiment 2

[0036] Polysebacic anhydride-tinidazole sustained release formulation.

[0037]Take polysebacic anhydride (weight-average molecular weight is 18000) and tinidazole crude drug respectively according to mass ratio 90: 10, 95: 5, 98: 2 mix (specific data see Table 2), put into mortar and grind into powder, Then move it into a self-made cylindrical polytetrafluoroethylene mold (with an inner diameter of 14mm and an inner height of 2mm), press it tightly, heat it at 90°C under an infrared lamp to melt it, and put it in a vacuum dryer (vacuum degree 0.09MPa) Cooling 12 hours, mold is taken off, obtains 3 kinds of drug loads and is 10%, 5%, 2% polysebacic anhydride-tinidazole round tablet (diameter is 14mm, and height is 2mm), and average piece weighs about 0.3g.

[0038] Table 2 Weighing data of polysebacic anhydride-tinidazole sustained-release preparation raw materials

[0039] weighing

quality

(g)

Mixing Ratio (Mass)

90∶10

95...

Embodiment 3

[0044] Poly[1,3-bis(p-carboxyphenoxy)propane-sebacic acid][P(CPP-SA)]-gatifloxacin sustained release formulation.

[0045] Gatifloxacin was subjected to ultraviolet scanning, and the maximum absorption wavelength was determined to be 285nm.

[0046] Weigh three kinds of poly[1,3-bis(p-carboxyphenoxy)propane-sebacic acid][P(CPP -SA)] copolymer sample and gatifloxacin bulk drug are mixed according to the mass ratio of 80:20 (see Table 3 for specific data), one is put into a mortar and ground into powder, and then it is moved into a Make a self-made mold for 10mm polytetrafluoroethylene and press it tightly. Heating at 90°C under an infrared lamp to make it melt, cooling in a vacuum desiccator (vacuum degree 0.09MPa) for 12 hours, removing the mold to obtain three kinds of poly[1,3-bis(p- Carboxyphenoxy)propane-sebacic acid][P(CPP-SA)] with a drug loading of 20% poly[1,3-bis(p-carboxyphenoxy)propane-sebacic acid][P( CPP-SA)] copolymer-gatifloxacin round drug stick (diameter 4m...

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Abstract

The invention relates to an anti-microbe drug which uses poly acid anhydride as carrier. The invention uses poly acid anhydride (as fatty group poly acid anhydride, aromatic nucleus poly acid anhydride, phosphor poly acid anhydride, polyamide poly acid anhydride, polyester poly acid anhydride or the like or their polymer) as carrier to be mixed via the drug, to be heated and fused into biological degradable slow-release agent. The inventive agent can be prepared into disc and rod shapes via mould according to the clinic demands. And the external degradation test has proved that the drug can reach zero-level release, without instant-release effect, to realize the slow-release object and confirm the safety.

Description

technical field [0001] The invention relates to an antimicrobial drug preparation with polyanhydride as a carrier and a preparation method thereof. Background technique [0002] Polyanhydrides are a new class of biodegradable synthetic polymer materials discovered by Langer et al. at the Massachusetts Institute of Technology in the early 1980s. As a controlled release agent, polyanhydride material has surface erosion degradation characteristics, and pharmaceutical preparations made of this material and various raw materials have degradation characteristics close to zero-order release. By adjusting the proportion of hydrophobic monomers that make up the polyanhydride material, the degradation rate and drug release rate of the polyanhydride can be adjusted, so that the drug can achieve zero-order release within an appropriate drug loading range, and there is no burst release effect, which avoids The possibility of a large amount of drugs entering the body fluid instantly ensu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K45/00A61P31/00
Inventor 姚军张福林王志强马慧丽王琳吕海军
Owner HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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