CN101032507B - Bacteria resisting medicine of erythrocin nanometer-emulsion and the preparing method - Google Patents
Bacteria resisting medicine of erythrocin nanometer-emulsion and the preparing method Download PDFInfo
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- CN101032507B CN101032507B CN2007100176418A CN200710017641A CN101032507B CN 101032507 B CN101032507 B CN 101032507B CN 2007100176418 A CN2007100176418 A CN 2007100176418A CN 200710017641 A CN200710017641 A CN 200710017641A CN 101032507 B CN101032507 B CN 101032507B
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- erythromycin
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- erythrocin
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Abstract
The nanometer antibacterial erythromycin medicine consists of erythromycin in 0.5-1.5 wt% and nanometer emulsion matrix in 98.5-99.5 wt%. It is yellowish transparent liquid, and has medicine granularity of 1-100 nm, low viscosity, high stability, fast absorption, targeted medicine release, high bioavailability, less toxic side effect and other features. The medicine may be attached well onto bacteria and permeated into bacteria to disturb their metabolism and to reach bacteriostasis and bactericidal effect. It is used mainly for treating serious infection caused by penicillin resisting staphylococcus aureus and hemolytic streptococcus as well as chicken's chronic respiratory tract disease, malignant rhinitis, etc. The medicine has simple preparation process, less toxicity and high safety.
Description
Technical field
The invention belongs to field of medicaments, relate to a kind of novel form of antibacterials, particularly a kind of bacteria resisting medicine of erythrocin nanometer-emulsion and preparation method thereof.
Background technology
Erythromycin is macrolide antibiotics, is mainly used to the drug resistance staphylococcus aureus, and the caused severe infections of Hemolytic streptococcus is as pneumonia, septicemia, endometritis, mastitis etc.; To the caused chronic respiratory tract disease of mycoplasma, the Mycoplasma pneumonia also has better curative effect.It not only is used for the people doctor, also has broad application prospects on veterinary clinic.But the conventional dosage forms of erythromycin is for oral administration easily by stomach acids destroy, also has a great deal of to be inactivated in liver, causes taking dose big, and the half-life is short and take frequent and characteristics such as digestive tract reaction is obvious in the body.Though continue to bring out out many erythromycin derivatives in recent years to overcome these shortcomings, difference in various degree all arranged at aspects such as drug effect and side effect and prices.Therefore, how to seek a kind of suitable dosage form and become a current urgent problem with the drug effect of bringing into play erythromycin more fully.
Summary of the invention
At the shortcomings and deficiencies of above-mentioned prior art, the object of the present invention is to provide that a kind of viscosity is low, good stability, dispersibility is strong, toxic and side effects is low bacteria resisting medicine of erythrocin nanometer-emulsion.
The technical scheme that realizes the foregoing invention purpose is a kind of bacteria resisting medicine of erythrocin nanometer-emulsion, and it is to be made by following raw materials by weight percent:
Erythromycin 0.5%～1.5%
Nano-emulsion substrate 98.5%～99.5%
Described nano-emulsion substrate is to be made by following weight percentages:
Surfactants/cosurfactants 20.0%～40.0%
Oil phase 2.2%～10.0%
Distilled water 49.0%～78.3%
The selected surfactant of the present invention is Tween80.
The selected cosurfactant of the present invention is a dehydrated alcohol.
The selected oil of the present invention is ethyl acetate.
The mass ratio of selected surfactant of the present invention and cosurfactant is km=2: 1～4: 1, and their sums are 9: 1～8: 2 with the mass ratio of oil.
Another object of the present invention provides the preparation method of above-mentioned bacteria resisting medicine of erythrocin nanometer-emulsion, specifically comprises the following steps:
1) it is standby to take by weighing erythromycin crude drug, surfactant, cosurfactant, oil, distilled water etc.;
2) elder generation adds surfactant after the erythromycin crude drug is dissolved in dehydrated alcohol fully, again with the oil phase stirring and evenly mixing; Slowly drip water then, constantly stir in the time of dropping, the system until forming homogeneous transparent promptly gets bacteria resisting medicine of erythrocin nanometer-emulsion.
Transmission electron microscope is observed down, and the drop of bacteria resisting medicine of erythrocin nanometer-emulsion is spherical in shape, and is evenly distributed, favorable dispersibility.
Measure through particle size analyzer, the particle diameter of bacteria resisting medicine of erythrocin nanometer-emulsion is 1nm～100nm.
Bacteria resisting medicine of erythrocin nanometer-emulsion of the present invention also can add other components and be prepared into new compound nanometer emulsion preparation.
A further object of the invention is protected exactly based on erythromycin nano-emulsion of the present invention, adds other components and is prepared into new compound nanometer emulsion preparation and application thereof.
It has characteristics such as viscosity is low, good stability, dispersibility is strong, absorption is rapid, targeting drug release, and can improve bioavailability of medicament, reduction toxic and side effects.
It also has the characteristics that surface tension is low, wellability is good, thus medicine well is attached on the antibacterial, and penetrate into its metabolism of internal interference of antibacterial and bring into play antibacterial or bactericidal action.
Whether bacteria resisting medicine of erythrocin nanometer-emulsion stability is measured, and sample is carried out high speed centrifugation and carries out reserved sample observing and see its stability under-4 ℃, room temperature, 60 ℃ of conditions, have layering and crystallization to separate out.
1. the high speed centrifugation test is to the influence of nano-emulsion stability
Get the bacteria resisting medicine of erythrocin nanometer-emulsion liquid that makes in right amount in centrifuge tube, sealing orifice is put in the high speed centrifuge, carries out centrifugal with the rotating speed of 12000r/min, still keep clear through the centrifugal nanoemulsions of 20min, the show mycin is not separated out and the profit lamination.
2. reserved sample observing experiment
Get the part bacteria resisting medicine of erythrocin nanometer-emulsion, be sub-packed in several vials, placing respectively after the sealing keeps sample under refrigerator-4 ℃, 25 ℃, 60 ℃ conditions of room temperature investigates 60d, observes every the 5d sampling.The result shows that this nano-emulsion all keeps the outward appearance of clear under three kinds of temperature conditions, and breakdown of emulsion, layering and crystallization are not separated out.
This drug system is the liquid of faint yellow clear, does not have crystallization to separate out low temperature-4 ℃ long-term down a placement, does not also have muddy phenomenon under 60 ℃ of hot conditionss, as seen is a kind of stable pharmaceutical dosage form; And preparation method is simple, energy consumption is low, toxicity is little, safe, do not need special installation to can be used for producing in enormous quantities, be used for clinical treating disease.
Below further set forth the in-vitro antibacterial effect of particle diameter and the uniform distribution situation and the medicine of the present invention of medicine of the present invention by testing example.
Test example 1
Medicine of the present invention carries out microscopic pattern with transmission electron microscope to be observed, and the result shows and sees that Fig. 1, Fig. 1 are erythromycin nano-emulsion electromicroscopic photographs, shows erythromycin nanometer emulsion droplet, spherical in shape and be evenly distributed, favorable dispersibility, particle diameter is all less than 100nm; Erythromycin nano-emulsion electromicroscopic photograph, spherical in shape and be evenly distributed, favorable dispersibility, particle diameter Fig. 2) also is erythromycin nano-emulsion electromicroscopic photograph all less than 100nm, the nano-emulsion drop is spherical, and be evenly distributed, favorable dispersibility.Fig. 3 uses the particle size analyzer measurement result, shows that bacteria resisting medicine of erythrocin nanometer-emulsion emulsion droplet mean diameter is 6.00nm.
Test example 2
The in-vitro antibacterial result of the test of medicine of the present invention
With erythromycin enteric-coated tablet, Roxithromycin sheet is contrast, and bacteria resisting medicine of erythrocin nanometer-emulsion of the present invention is as described below to the antibacterial efficacy of staphylococcus aureus, Hemolytic streptococcus.
The visible bacteria resisting medicine of erythrocin nanometer-emulsion of extracorporeal bacteria inhibitor test equals the Roxithromycin sheet to MIC, the MBC of staphylococcus aureus less than erythromycin enteric-coated tablet, show that the external bacteriostasis of bacteria resisting medicine of erythrocin nanometer-emulsion is better than erythromycin enteric-coated tablet; Streptococcic MIC, MBC then are respectively 0.0625 and 0.125mg/mL, significantly are lower than erythromycin enteric-coated tablet and Roxithromycin sheet, this shows that its fungistatic effect is better than erythromycin enteric-coated tablet and Roxithromycin sheet.The results are shown in Table 4:
Table 4 minimal bactericidal concentration (MBC) and minimum inhibitory concentration (MIC) (unit: ug/mL)
Following method is further set forth the preparation of medicine of the present invention.
1) it is standby to take by weighing erythromycin crude drug, dehydrated alcohol, ethyl acetate, water etc. by following examples prescription;
2) elder generation adds Tween80 after the erythromycin crude drug is dissolved in dehydrated alcohol fully, again with the ethyl acetate stirring and evenly mixing; Slowly drip water then, constantly stir in the time of dropping, the system until forming homogeneous transparent promptly gets bacteria resisting medicine of erythrocin nanometer-emulsion of the present invention.
Embodiment 1 compounding pharmaceutical concentration is 0.5% erythromycin nano-emulsion
Erythromycin 0.5g
Dehydrated alcohol 5.0g
Tween 80 15.0g
Ethyl acetate 2.2g
Distilled water 78.3g
Embodiment 2 compounding pharmaceutical concentration are 0.5% erythromycin nano-emulsion
Erythromycin 0.5g
Dehydrated alcohol 5.0g
Tween 80 15.0g
Ethyl acetate 5.0g
Distilled water 74.5g
Embodiment 3 compounding pharmaceutical concentration are 1% erythromycin nano-emulsion
Erythromycin 0.5g
Dehydrated alcohol 5.0g
Tween 80 15.0g
Ethyl acetate 2.2g
Distilled water 27.3g
Embodiment 4 compounding pharmaceutical concentration are 1% erythromycin nano-emulsion
Erythromycin 0.5g
Dehydrated alcohol 5.0g
Ethyl acetate 5.0g
Distilled water 24.5g
Embodiment 5 compounding pharmaceutical concentration are 1.2% erythromycin nano-emulsion
Erythromycin 0.5g
Dehydrated alcohol 5.0g
Ethyl acetate 1.4g
Distilled water 27.3g
Embodiment 6 compounding pharmaceutical concentration are 1.2% erythromycin nano-emulsion
Erythromycin 0.5g
Dehydrated alcohol 5.0g
Ethyl acetate 2.0g
Distilled water 26.7g
Embodiment 7 compounding pharmaceutical concentration are 1.5% erythromycin nano-emulsion
Erythromycin 0.5g
Dehydrated alcohol 5.0g
Ethyl acetate 1.4g
Distilled water 19.0g
Embodiment 8 compounding pharmaceutical concentration are 1.5% erythromycin nano-emulsion
Erythromycin 0.5g
Dehydrated alcohol 5.0g
Ethyl acetate 2.0g
Distilled water 19.0g
Claims (2)
1. a bacteria resisting medicine of erythrocin nanometer-emulsion is characterized in that, the particle diameter of this nano-emulsion preparation is made up of following weight percentages between 1～100nm:
Erythromycin 0.5%～1.5%
Nano-emulsion substrate 98.5%～99.5%
Described nano-emulsion substrate is to be made by following weight percentages:
Surfactants/cosurfactants 20.0%～40.0%
Oil phase 2.2%～10.0%
Distilled water 49.0%～78.3%
Described surfactant is Tween80;
Described cosurfactant is a dehydrated alcohol;
Described oil is ethyl acetate;
The surfactant in the described nano-emulsion substrate and the mass ratio of cosurfactant are 2: 1～4: 1.
2. bacteria resisting medicine of erythrocin nanometer-emulsion according to claim 1 is characterized in that, surfactant in the described nano-emulsion substrate and cosurfactant sum are 9: 1～8: 2 with the mass ratio of oil.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2007100176418A CN101032507B (en) | 2007-04-06 | 2007-04-06 | Bacteria resisting medicine of erythrocin nanometer-emulsion and the preparing method |
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| CN101032507B true CN101032507B (en) | 2010-09-29 |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102283806A (en) * | 2011-08-25 | 2011-12-21 | 西北农林科技大学 | Roxithromycin nanoemulsion antibacterial drug and preparation method thereof |
| CN103830726A (en) * | 2012-11-23 | 2014-06-04 | 魏维 | Antimicrobial organic nanometer composition and preparation method thereof |
| CN103735503B (en) * | 2013-12-06 | 2016-06-08 | 鼎正动物药业（天津）有限公司 | A kind of erythromycin thiocyanate emulsion and preparation method thereof |
| CN106511982A (en) * | 2016-12-06 | 2017-03-22 | 郑州郑先医药科技有限公司 | Western medicine composition for treating enteritis and preparation method thereof |
Citations (7)
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| CN1433314A (en) * | 1999-12-30 | 2003-07-30 | 密执安州立大学董事会 | Antimicrobial compositions and methods of use |
| CN1872058A (en) * | 2005-05-31 | 2006-12-06 | 华北制药集团新药研究开发有限责任公司 | Medication composition of containing macrolides |
| CN1931131A (en) * | 2006-09-18 | 2007-03-21 | 西北农林科技大学 | Oil-in-water type nanometer peonol emulsion oral liquid and its prepn process |
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| CN1931130A (en) * | 2006-09-18 | 2007-03-21 | 西北农林科技大学 | Nanometer emulsion oral liquid of andrographolide and its prepn process |
| CN1931232A (en) * | 2006-09-21 | 2007-03-21 | 西北农林科技大学 | Oil-in-water nanometer perilla seed oil emulsion oral liquid and its prepn process |
| CN1931163A (en) * | 2006-09-20 | 2007-03-21 | 西北农林科技大学 | Nanometer clotrimazole emulsion medicine and its prepn process |
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- 2007-04-06 CN CN2007100176418A patent/CN101032507B/en not_active Expired - Fee Related
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1433314A (en) * | 1999-12-30 | 2003-07-30 | 密执安州立大学董事会 | Antimicrobial compositions and methods of use |
| CN1872058A (en) * | 2005-05-31 | 2006-12-06 | 华北制药集团新药研究开发有限责任公司 | Medication composition of containing macrolides |
| CN1931131A (en) * | 2006-09-18 | 2007-03-21 | 西北农林科技大学 | Oil-in-water type nanometer peonol emulsion oral liquid and its prepn process |
| CN1931130A (en) * | 2006-09-18 | 2007-03-21 | 西北农林科技大学 | Nanometer emulsion oral liquid of andrographolide and its prepn process |
| CN1931163A (en) * | 2006-09-20 | 2007-03-21 | 西北农林科技大学 | Nanometer clotrimazole emulsion medicine and its prepn process |
| CN1931293A (en) * | 2006-09-21 | 2007-03-21 | 西北农林科技大学 | Oil-in-water type nanometer grassleaved sweetflag oil emulsion oral liquid and its prepn process |
| CN1931232A (en) * | 2006-09-21 | 2007-03-21 | 西北农林科技大学 | Oil-in-water nanometer perilla seed oil emulsion oral liquid and its prepn process |
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