CN1834087A - organic iodine complex - Google Patents
organic iodine complex Download PDFInfo
- Publication number
- CN1834087A CN1834087A CN 200510055459 CN200510055459A CN1834087A CN 1834087 A CN1834087 A CN 1834087A CN 200510055459 CN200510055459 CN 200510055459 CN 200510055459 A CN200510055459 A CN 200510055459A CN 1834087 A CN1834087 A CN 1834087A
- Authority
- CN
- China
- Prior art keywords
- acid
- iodine
- organo
- iodine complex
- complex
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 239000011630 iodine Substances 0.000 title claims abstract description 155
- 229910052740 iodine Inorganic materials 0.000 title claims abstract description 155
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 title abstract description 127
- 239000000203 mixture Substances 0.000 claims abstract description 42
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims abstract description 21
- 150000001413 amino acids Chemical class 0.000 claims abstract description 18
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical group II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 claims abstract description 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 16
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- 125000000524 functional group Chemical group 0.000 claims abstract description 6
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- 208000011580 syndromic disease Diseases 0.000 claims abstract description 5
- 206010067997 Iodine deficiency Diseases 0.000 claims abstract description 4
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Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to an organic iodine complex, wherein the coordination center of the organic iodine complex is an iodine molecule, a complexing agent is an organic compound containing functional groups, the functional groups are amino groups and/or hydroxyl groups and/or carboxyl groups, and typical representatives of the organic compounds of the hydroxyl groups are 4-methylthio-2-hydroxybutyric acid and 2-hydroxypropionic acid. The invention also relates to a composition of the organic iodine complex and application thereof in the field of pharmacy. The composition comprises as active ingredient 0.3-40% of an organic iodine complex and one or more other components selected from the group consisting of: natural amino acid iodine, solvent, surfactant, food additive, food and synthetic medicine. The composition can be used for preparing medicine for preventing and treating AIDS, prawn white syndrome, taura syndrome, grass carp hemorrhage, stomatitis, pharyngitis, vaginitis, tumor, poultry digestive tract disease, trichomoniasis, coccidiosis, human digestive tract disease or iodine deficiency disease.
Description
Technical field
The present invention relates to pharmacy field.More specifically, the present invention relates to a kind of organo-iodine complex of novelty, particularly organo-iodine complex, the invention still further relates to its composition and the application in pharmacy field thereof.
Background technology
Iodine is to comprise one of nutrient substance that human animal is essential, and the tincture of iodine uses the history in existing more than 160 year as disinfectant.Iodized oil is as diagnostic agent and the loaded Pharmacopoeia of People's Republic of China of iodine-replenishing agent (2000 editions two ones, the 961st page).Povidon iodine (being called for short PVP-I) is as the also loaded Pharmacopoeia of People's Republic of China of Cidex-7 (2000 editions two ones, the 996th page).The tincture of iodine and iodized oil stability are poor; Polyvidone in the povidon iodine is because of all having carcinogenesis to rat and mouse, so its application, especially lasting the application are greatly limited.
Chinese invention patent CN01114666.4 provides amino acid-iodine complex series, and amino acid has significantly improved the stability of iodine and the function of disinfection as the complexing agent of iodine, also is beneficial to the healing of wound simultaneously.
Life entity is the ecosystem of a complexity, and for example there is little ecology in female genital tract, and lactobacillus-fermented produces lactic acid, makes reproductive tract pH keep 4.0-4.5, and pathogenic micro-organism is difficult for breeding under this environment.Therefore, in order to keep state of health,, also need to introduce new ecological element if infective sufferer has taken place.
For overcoming the deficiencies in the prior art, the invention provides a kind of organo-iodine complex of novelty, particularly organic amino hydroxycarboxylic acid iodine complex, and composition the invention still further relates to its application in pharmacy field.
Summary of the invention
The object of the present invention is to provide a kind of new organo-iodine complex, particularly organic amino hydroxycarboxylic acid iodine complex and composition thereof.
The present invention also aims to, the application in pharmacy of described organo-iodine complex and composition thereof is provided; Said composition contains the organic iodine as activeconstituents, particularly organic amino hydroxycarboxylic acid iodine, and solvent, tensio-active agent, performance improver and auxiliary material.
Organo-iodine complex of the present invention, its coordination center are iodine molecule (I.
2), complexing agent is the organic compound that contains functional group, and functional group is amino and/or hydroxyl and/or carboxyl, and its chemical general formula is:
(R
1R
2C(R.
3)R
4)n I.
2 (I)
R wherein
1, R
2, R.
3, R
4Represent the side chain radical of iodine organic compound, R
1, R
2, R.
3, R
4Can be the same or different; The n representative is selected from the integer of 1-6.
Work as R
4When representing representation carboxy, formula (I) becomes:
(R
1R
2C(R.
3)COOH)
n I.
2 (II)
R
1, R
2, R.
3All can contain hydroxyl, and that tool typical meaning is R.
3Be hydroxyl (OH), i.e. Alpha-hydroxy organic carboxyl acid, formula (I) becomes:
(R
1R
2C(OH)COOH)
n I.
2 (III)
R
1, R
2, R.
3Can be alkane group, or aromatic hydrocarbon group.The typical case's representative that contains the hydroxyl carboxyl organic compound of alkane group is 4-methylthio group-2-hydroxybutyric acid, 2 hydroxy propanoic acid (lactic acid), hydroxy-butanedioic acid (oxysuccinic acid), tartrate, gluconic acid, tartronic acid, oxyacetic acid, 2-hydroxy-iso-butyric acid, 2-hydroxy-2-methyl propionic acid and hydroxybutyric acid etc.; The typical case's representative that contains the hydroxyl carboxyl organic compound of aromatic hydrocarbon group is 2 hydroxybenzoic acid (Whitfield's ointment), 3-cresotinic acid, 3-methoxyl group Whitfield's ointment, 5-sulphosalicylic acid, 4-hydroxyl Whitfield's ointment, 4 hydroxyisophthalic acid, 2-hydroxyl-3-naphthoic acid, hydroxyl phenylacetic acid (amygdalic acid), 6-methyl-3-sec.-propyl Whitfield's ointment (adjacent thymotic acid), agaric acid, citric acid and pyruvic acid etc.
Organic complex iodine of the present invention comprises non-natural and natural amino acid compound chelated iodine, hydroxycarboxylic acid iodine, and their composition is a kind of potent pathogenic agent agent of killing: it is kill virus, germ and protozoon simultaneously.Therefore, can be made into various anti-infective medicines, antiviral drug, antimicrobial drug, antiprotozoal drug and antitumor drug.Meanwhile, more fully little ecological protection preparation also is provided, and has become more fully ecoalimental medicine.
Can be made into antiviral.For some great difficult disease viral diseases, as acquired immune deficiency syndrome (AIDS), in this case, the preferred while is carried out administration with three kinds of approach: external application (smear, wash, gargle), (oral liquid, powder, capsule for oral administration, the cleaning digestive tube, enter blood, body fluid) and intravenous injection (killing in the blood virus in the body fluid).Safe, effective and comprehensive medicine will be provided.
Stomatitis, pharyngitis are a kind of high morbidities, mainly are to be caused by bacterium, and test proves that organic complex iodine has obvious effects to these diseases.Organic complex iodine can be made the medicine of control stomatitis, pharyngitis.
Vaginitis is the modal illness of gynaecology.Also be to cause by bacterium and trichomonad.Organic complex iodine is made irrigation, ointment, suppository etc. treats good effect is all arranged.
The pulvis of organic complex iodine can be used as the digestive tract disease disease of preventing and treating poultry, the medicine of coccidiosis.
Organic complex iodine oral liquid, organic complex iodine capsule and organic complex iodine powder can be used as the medicine of preventing and treating the human digestive tract disease.
Whole world most people are iodine deficiency, and organic complex iodine food provides the new way of supplementing iodine.
In this application, term " alkane " refers to have 1-20 carbon atom, preferred 1-8 carbon atom, the more preferably side chain of 1-6 carbon atom or the saturated hydrocarbon chain of straight chain, and this chain can be by one or more groups replacements that are selected from alkoxyl group, alkylthio and alkylamino.
Term " aromatic hydrocarbons " refers to contain the monocycle of 6-14 carbon atom or polycyclic condenses or the aromatic group of non-condensed.
Complexing agent comprises alpha-non-natural amino acid, and its general formula can be expressed as
R
5N(CH
2COOH)
2 (IV)
R wherein
5With the R in the formula (I)
1Define identical.
Typical case's representative of the complexing agent of alpha-non-natural amino acid iodine is Beta-alanine-N, N-oxalic acid, benzaminic acid-N, N-oxalic acid, ammonia oxalic acid, nitrilotriacetic acid(NTA), ammonia dipropionic acid, quadrol-N, N-oxalic acid, ethylenediamine tetraacetic acid (EDTA), ethylene diamine dipropionic acid and ethylenediamine tetrapropionic acid(EDTP) etc.
In the included organic compound of general formula (I), its complexing agent also comprises amine, and its typical case's representative is quadrol, propylene diamine, dipyridyl, thanomin, diethanolamine and trolamine etc.Can also be pyruvic acid and hydroxyquinoline etc.
Organic hydroxyl carboxyl iodine complex of the present invention by the functional component iodine of complexing, can be general iodine molecule, also can be its radio isotope.
Different and service requirements is different according to the hydroxyl organic carboxyl acid, and the hydroxyl organic carboxyl acid is generally 1-20 to the mole ratio difference of iodine molecule, preferably 1-5.
The preparation of organic hydroxyl carboxyl iodine complex of the present invention.The example that is prepared as with 4-methylthio group-2-hydroxybutyric acid iodine complex.In filling the alcoholic acid container, add 4-methylthio group-2-hydroxybutyric acid and iodine, under agitation be warming up to 45 ℃ then, continue 380min, and obtain the molten 4-methylthio group-2-hydroxybutyric acid iodine complex of alcohol.
Organic hydroxyl carboxyl bromo-complex can prepare with similar approach.
The present invention compared with prior art has following advantage: the present invention as functional group, thereby has powerful sterilization and disinfection ability with iodine molecule; Selected specific hydroxyl organic carboxyl acid has the ecological environmental protection effect as complexing agent.Thereby more help the health of organism.For example female genital tract pH keeps 4.0-4.5, is to be kept by the lactic acid that lactobacillus-fermented produces, and the lactic acid iodine complex has the dual-use function of sterilization and ecological protection concurrently.
Composition of the present invention contains the organic iodine as activeconstituents, and particularly organic amino hydroxycarboxylic acid iodine can contain amino acid iodine and solvent, tensio-active agent, performance improver and auxiliary material.This is a composition system that forms by mutual binding physics and/or chemistry.
Amino acid iodine refers to the complex compound of natural amino acid with iodine.
Solvent can be inorganic solvent and/or organic solvent, and inorganic solvent can be one or more a mixture among water, hydrochloric acid, sulfuric acid, the phosphoric acid; Organic solvent can be one or more a mixture among ethanol, ethylene glycol, glycerol, acetate, propionic acid, butyric acid, dimethyl sulfoxide (DMSO), dimethyl sulfone, the phenylcarbinol.
Tensio-active agent can be cats product, anion surfactant, zwitterionics or nonionogenic tenside and condensed phosphoric acid, phosphoric acid ester; Cats product is the quaternized thing of alkene acid amides ethyl type alkenyl imidazoline (tetrahydroglyoxaline ODD), benzethonium chloride, cationic protein peptide (QHC), octadecylamine acetate, oleic acid tri-isopropanolamine ester; Anion surfactant is alkylphenol polyoxyethylene phosphoric acid ester (D102 dispersion agent), sulfosuccinic ester 4910, PAPE (PAPE); Zwitterionics is alkylamide propyl-betaine, amino acids tetrahydroglyoxaline surface agent (FS-L), chlorination hydroxyl phosphate 12 tertiary amine ester ammoniums; Nonionogenic tenside be AEO-8, polyoxyethylene nonylphenol ether (7EO, 15EO), polyoxyethylene lauric acid ester (9EO), this dish 60, span 80, polysorbate60 and tween 80.Condensed phosphoric acid, phosphoric acid ester are tetra-sodium, three metaphosphoric acids, tripolyphosphate, trioctyl phosphate, trialkylphosphine oxide, ethylhexyl phosphoric acid and ethylhexyl phosphonic acids.
Performance improver can be among nutrient substance class, vitamins, seasoning sweetener class, the other treatment activeconstituents one or more.
The nutrient substance class is methionine(Met), Methionin, arginine, glycine; Vitamins is VITMAIN B1, Wei ShengsuB2, inositol; Inorganic salt, chelating salt are Zine Gluconate, ferrous gluconate, calcium gluconate, amino-acid zinc, amino acid copper, manganese amino acid, amino acid-ferrous, amino acid selenium; Grease, soybean phospholipid, Yelkin TTS, Sphingolipids,sialo, cholic acid wool; Dispersion agent is polyoxyethylene glycol (400); The seasonings class is ribonucleotide calcium, glycyrrhizin; The sweetener class is Oleum Cinnamomi, lemon oil, phenylcarbinol, ethyl p-hydroxybenzoate, Phenoxyethanol, borneol, spearmint oil; Performance improver also comprises functional medicine, includes, but is not limited to antipyretic and analgesic, pest-resistant medicine, antifungal drug and anti-allergy agent etc.Antipyretic and analgesic can be acetylsalicylic acid, Naproxen Base, fenbufen, preferred acetylsalicylic acid; Pest-resistant medicine is Artemisinin, metronidazole; Antifungal drug can be KETOKONAZOL, miconazole, preferred KETOKONAZOL; Anti-allergy agent is hydrocortisone (hydrocortisone), prednisone, diphenhydramine or Toldrin.
Auxiliary material is emulsifing thickener class, fruit glaze agent class and food.The emulsifing thickener class is hydroxypropylcellulose, Lalgine, chitin, casein, gelatin; Fruit glaze agent is beeswax, polyvinyl alcohol, paraffin oil or beta-cyclodextrin.Described food can be honey, white sugar, brown sugar, yolk powder, protein powder, mixed fish soluble meal, seaweed powder, sea-tangle powder.
Composition weight of the present invention is composed as follows:
Composition weight (%)
Organo-iodine complex 0.3-40
Natural amino acid iodine 0-20
Solvent 0-95
Tensio-active agent 0-30
Performance improver 0-20
Auxiliary material 80-0
Prerequisite is that each component sum is 100%.
Preparation of compositions method of the present invention comprises described organic iodine is dissolved in solvent and/or solubility promoter, and then adds above-mentioned other composition, through the system of mixing, compound, refining, homogeneous, moulding, packs subsequently and forms.
According to another aspect of the present invention, also relate to described organic iodine composition and prevent and treat application in the medicine of disease in preparation, these diseases are shrimp disease, fish hemorrhage, livestock and poultry infectious diseases, acquired immune deficiency syndrome (AIDS), stomatitis, rhinopharyngitis, vaginitis, tumour, pneumonia, digestive tract disease or iodine deficiency, also can be used as diagnostic reagent.
According to a preferred aspect of the present invention, organic iodine composition of the present invention can be made the form of sterilizing agent, said composition also contains tensio-active agent and necessary solvent except that the organic iodine that contains as active ingredient.Described tensio-active agent as mentioned above.
According to another aspect of the present invention, contain foodstuff additive in the organic iodine composition of the present invention, be used for replenishing animal body (comprising the people) desired material.
According to another aspect of the present invention, contain in the organic iodine composition of the present invention food and or synthetic drugs, be used for the treatment of some disease of animal body.These medicinal composition can be oral or medical injections.
Concrete embodiment
Adopt the following example that the present invention is further specified, but these embodiment are not used in and limit the scope of the invention.
The preparation of embodiment 1.4-methylthio group-2-hydroxybutyric acid iodine.
In the 250ml round-bottomed flask that has the stirring of heating and magnetic (down together), add ethanol 100ml, be warming up to 45 ℃ under stirring, add 4-methylthio group-2-hydroxybutyric acid 15.2g, add concentrated hydrochloric acid 2g, progressively add iodine 13.2g, stir 160min, removal of solvent under reduced pressure, products therefrom is 4-methylthio group-2-hydroxybutyric acid iodine after testing, contain iodine 13.0g, contain 4-methylthio group-2-hydroxybutyric acid 15.1g.
The preparation of embodiment 2. lactic acid iodine.
Equipment is with embodiment 1.In round-bottomed flask, add entry 105ml, stir down and be warming up to 65 ℃, add lactic acid 18g, treat dissolving fully after, progressively add iodine 25g, stir 205min, concentrated after drying, products therefrom contains iodine 23.5g through being accredited as lactic acid iodine, contains lactic acid 17.5g.
The preparation of embodiment 3.4-hydroxyl salicylic acid-iodine.
Equipment is with embodiment 1.In round-bottomed flask, add entry 135ml, be warming up to 74 ℃ under stirring, add 4-hydroxyl Whitfield's ointment 31.0g, treat dissolving fully after, add phosphatase 11 .0g, progressively add iodine 27.4g, stir 110min, cooling, leave standstill 180min, filter, separate, products therefrom after testing, contain iodine 26.0g, contain 4-hydroxyl Whitfield's ointment 30.0g.
The preparation of embodiment 4. hydroxyl phenylacetic acids (amygdalic acid) iodine.
Equipment is with embodiment 1.In round-bottomed flask, add ether 105ml, be warming up to 35 ℃ under stirring, add hydroxyl phenylacetic acid 7.5g, add sulfuric acid 0.15g, progressively add iodine 7.0g, stir 110min, filter, remove and desolvate and drying, products therefrom contains iodine 6.5g after testing, hydroxyl toluylic acid 7.1g.
The preparation of embodiment 5. ethylenediamine tetraacetic acid (EDTA) iodine.
Equipment is with embodiment 1.In round-bottomed flask, add entry 145ml, be warming up to 70 ℃ under the stirring, add ethylenediamine tetraacetic acid (EDTA) 0.5g, progressively add iodine 1.0g, stir 205min, filter, remove and desolvate and drying, products therefrom is through being accredited as ethylenediamine tetraacetic acid (EDTA) iodine.
Embodiment 6.4-methylthio group-2-hydroxybutyric acid iodine disinfectant prescription and preparation method thereof.
Prescription:
4-methylthio group-2-hydroxybutyric acid iodine (containing available iodine 35%) 50g
Glycerine 20g
Sodium Benzoate 3g
Polyoxyethylene nonylphenol ether (7EO) 150g
Phosphoric acid 30g
Distilled water 840ml
Preparation method: get 4-methylthio group-2-hydroxybutyric acid iodine and glycerine and mix post-heating, heat while stirring, stop heating during to 45 ℃, add distilled water 240ml, add Sodium Benzoate, polyoxyethylene nonylphenol ether (7EO) and 600ml distilled water successively, after stirring, cooling promptly.
The preparation of embodiment 7. lactic acid tincture of iodine agent.
Prescription:
Lactic acid iodine (containing available iodine 20%) 16g
Ethanol (95%) 550ml
Distilled water 440ml
The preparation method: extracting lactic acid iodine and ethanol successively join in the mixing vessel, stir under the room temperature, add distilled water 440ml, after fully stirring promptly.
Embodiment 8.4-methylthio group-2-hydroxybutyric acid iodine and METHIONINE AMINO-CARBOXYL IODINE COMPLEX preparation of compositions.
Prescription:
4-methylthio group-2-hydroxybutyric acid iodine (containing available iodine 35%) 3.0g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 42%) 50g
Polyoxyethylene nonylphenol ether (7EO) 150g
Trioctyl phosphate 10g
Phosphatase 11 0g
Distilled water 845ml
The preparation method: get 4-methylthio group-2-hydroxybutyric acid iodine and METHIONINE AMINO-CARBOXYL IODINE COMPLEX and join respectively in the container, add polyoxyethylene nonylphenol ether again, heat while stirring, stop heating during to 35 ℃, add distilled water 845ml at last, after stirring, cooling promptly.
The preparation of embodiment 9. lactic acid iodine and METHIONINE AMINO-CARBOXYL IODINE COMPLEX mixed solution.
Prescription:
Lactic acid iodine (containing available iodine 20%) 3.0g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 42%) 55g
Polyoxyethylene nonylphenol ether (7EO) 250g
Citric acid 6g
Distilled water 730ml
The preparation method: extracting lactic acid iodine and METHIONINE AMINO-CARBOXYL IODINE COMPLEX join respectively in the container, add entry 200ml earlier, add polyoxyethylene nonylphenol ether again, heat while stirring, and stop heating during to 40 ℃, add distilled water 530ml at last, and after stirring, cooling promptly.
The preparation of embodiment 10.4-methylthio group-2-hydroxybutyric acid iodine and METHIONINE AMINO-CARBOXYL IODINE COMPLEX tincture.
Prescription:
4-methylthio group-2-hydroxybutyric acid iodine (containing available iodine 20%) 60g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 42%) 20g
Ethanol (95%) 650ml
Distilled water 340ml
Preparation method: earlier ethanol 350ml is joined in the container, stir and join 4-methylthio group-2-hydroxybutyric acid iodine, METHIONINE AMINO-CARBOXYL IODINE COMPLEX in the mixing vessel respectively down, stir under the room temperature, and then add distilled water 340ml and remaining ethanol, after fully stirring promptly.
The preparation of embodiment 11.4-methylthio group-2-hydroxybutyric acid iodine and Diaparene.
Prescription:
4-methylthio group-2-hydroxybutyric acid iodine (containing available iodine 20%) 40g
Benzethonium chloride 10g
Ethanol (95%) 100ml
Distilled water 890ml
The preparation method: earlier water 350ml is joined in the container, stirs down 4-methylthio group-2-hydroxybutyric acid iodine, benzethonium chloride are joined respectively in the mixing vessel, stir under the room temperature, and then add ethanol and remaining distilled water, after fully stirring promptly.
The preparation of embodiment 12.4-methylthio group-2-hydroxybutyric acid iodine powder.
Prescription:
4-methylthio group-2-hydroxybutyric acid iodine (containing available iodine 20%) 40g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 42%) 5.0g
Methionin 1.0g
Protein powder 250g
Wheat bran 740g
Preparation method: earlier 4-methylthio group-2-hydroxybutyric acid iodine, METHIONINE AMINO-CARBOXYL IODINE COMPLEX and Methionin and protein powder are mixed, mix with wheat bran then, pulverize the back and cross No. five sieves promptly.
The preparation of embodiment 13. compound organic iodine liquid.
Prescription:
Lactic acid iodine (containing available iodine 20%) 30.0g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 42%) 5.0g
Lactic acid 100.0g
Distilled water 890ml
The preparation method: extracting lactic acid iodine and METHIONINE AMINO-CARBOXYL IODINE COMPLEX join respectively in the container, add entry 200ml earlier, add lactic acid again, stir, and add distilled water 690ml at last, after stirring promptly.
Embodiment 14. organic iodine particles prescription and preparation method thereof.
Prescription:
Lactic acid iodine (containing available iodine 20%) 5.0g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 45%) 10g
Acetylsalicylic acid 12g
Yelkin TTS 6g
Polyoxyethylene glycol (400) 5g
Ethanol 15g
Methylcellulose gum 9g
Icing Sugar 60g
The preparation method: extracting lactic acid iodine, METHIONINE AMINO-CARBOXYL IODINE COMPLEX and ethanol and polyoxyethylene glycol mixing join among methylcellulose gum, acetylsalicylic acid, the Icing Sugar component to pasty state again, after stirring, with No. 1 sieve series grain.40～60 ℃ of dryings, whole grain is distributed into every bag 1.0g promptly.
Embodiment 15. organic iodine capsules prescription and preparation method thereof.
Prescription:
Lactic acid iodine (containing available iodine 20%) 0.6g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 45%) 3.5g
Methionin 70g
Yelkin TTS 7g
Glycerine 5g
Magnesium Stearate 10g
Protein powder 200g
The preparation method: after extracting lactic acid iodine, METHIONINE AMINO-CARBOXYL IODINE COMPLEX and Methionin and Yelkin TTS mix, remix methylcellulose gum and Magnesium Stearate and other component, drying is pulverized, and sieves, and is promptly encapsulated.
Embodiment 16. organic iodine tablet formulations and preparation method thereof.
Prescription:
Lactic acid iodine (containing available iodine 20%) 0.5g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 43%) 15g
Methionin 30g
Tartrate 2g
Carboxymethyl cellulose 1g
Magnesium Stearate 1g
Protein powder 30g
The preparation method: extracting lactic acid iodine, METHIONINE AMINO-CARBOXYL IODINE COMPLEX and Methionin mix.It is an amount of that carboxymethyl cellulose is added water, treats to stir after its natural swelling; Get the auxiliary material except that Magnesium Stearate, add above-mentioned solution and make softwood, cross 14～16 mesh sieves and granulate, oven dry is sieved, and whole grain adds Magnesium Stearate at last and mixes, and compressing tablet promptly.
Embodiment 17. organic iodine suppositorys prescription and preparation method thereof.
Prescription:
Lactic acid iodine (containing available iodine 20%) 15g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 43%) 10g
Glycerine 150g
Poly(oxyethylene glycol) 400 40g
Macrogol 4000 80g
The preparation method: take by weighing each medicine by prescription, hot melt process prepares 50 pieces of suppositorys.
Embodiment 18. organic iodine injection formulas and preparation method thereof.
Prescription:
Lactic acid iodine (containing available iodine 20%) 0.6g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 45%) 5g
Sodium-chlor 9g
Dehydrated alcohol 5g
Water for injection 1000ml
Preparation method: get 300 waters for injection, after adding sodium-chlor stirs, slowly add lactic acid iodine and the amino acid iodine that is dissolved in dehydrated alcohol, with adding with stirring, add water for injection at last to full dose, filter, detect the qualified back embedding of pH value and content, 100 ℃ of sterilization 30min promptly.
Embodiment 19. organic iodine aerosols prescription and preparation method thereof.
Prescription:
4-methylthio group-2-hydroxybutyric acid iodine (containing available iodine 20%) 40g
Glycine iodine (containing available iodine 10%) 7g
Glycerine 50g
F
12/F
11 70g
Propylene glycol 5ml
Distilled water 1000ml
Preparation method: get amino acid iodine and glycerine and mix other solvent of back adding, stir promptly at last.
Embodiment 20. organic iodine ointment prescription and preparation method thereof.
Prescription:
4-methylthio group-2-hydroxybutyric acid iodine (containing available iodine 20%) 20g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 43%) 18g
KETOKONAZOL 10g
White vaseline 140g
Stearic acid 130g
Tween-80 30g
Glycerine 75g
Glyceryl monostearate 60g
Ethyl p-hydroxybenzoate 5g
Distilled water 500ml
Preparation method: get white vaseline, stearic acid, glyceryl monostearate and put heating in water bath and melt to 70～80 ℃, be oil phase; Other gets tween-80, glycerine, ethyl p-hydroxybenzoate and is dissolved in distilled water and is heated to 70～80 ℃, is water.During two uniform temps oil phase is slowly joined aqueous phase, be stirred to 60 ℃ matrix standby.Get METHIONINE AMINO-CARBOXYL IODINE COMPLEX and 4-methylthio group-2-hydroxybutyric acid iodine and be mixed into pasty state with an amount of glycerine, gradation adds in the above-mentioned emulsion matrix for preparing, and the limit edged stirs, to condensation promptly.
Embodiment 21. organic iodine liniments prescription and preparation method thereof.
Prescription:
4-methylthio group-2-hydroxybutyric acid iodine (containing available iodine 20%) 10g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 43%) 15g
Span 80 10g
Propionic acid 8g
Dimethyl sulfone 15ml
Phenylcarbinol 5ml
Ethanol 50ml
Distilled water 900ml
Preparation method: get organic iodine and less water, mix other solvent and auxiliary agent, stir promptly at last.
Prescription of embodiment 22. organic iodine food and preparation method thereof.
Prescription:
Lactic acid iodine (containing available iodine 20%) 2g
METHIONINE AMINO-CARBOXYL IODINE COMPLEX (containing available iodine 45%) 15g
Seaweed powder 20g
Ethanol 30ml
Wheat germ powder 880g
The preparation method: organic iodine is dissolved in edible ethanol, is heated to 45 ℃, wait to dissolve the back and add seaweed powder, drive away solvent down for 60 ℃, then with wheat germ powder uniform mixing, packing is sterilized promptly.
Biological assay
Organic complex iodine of the present invention and composition thereof are a kind of potent pathogenic agent agent of killing.Below the activity of the present composition is measured.
4-methylthio group-2-hydroxybutyric acid the iodine of embodiment 8 and the Candida albicans activity test of going out of METHIONINE AMINO-CARBOXYL IODINE COMPLEX composition
Method: 4-methylthio group-2-hydroxybutyric acid iodine and METHIONINE AMINO-CARBOXYL IODINE COMPLEX composition are diluted to the diluent of different concns with sterile distilled water; Make load sample (bacterium) sheet, bacteria containing amount 10
6The CFU/ sheet; Neutralizing agent is a 0.03mol PBS liquid, wherein contains 0.1% Yelkin TTS, 0.55 tween 80,0.5% Sulfothiorine.Behind the 4-methylthio group-2-hydroxybutyric acid iodine of different concns and METHIONINE AMINO-CARBOXYL IODINE COMPLEX composition and the bacterium sheet effect certain hour, neutralization is cultivated 48h at 35 ℃ then, does the viable bacteria enumeration.The result is as shown in table 1 below.
Table 1: the 4-methylthio group-2-hydroxybutyric acid iodine of different concns and METHIONINE AMINO-CARBOXYL IODINE COMPLEX composition contrast: 1.22 10 the oidiomycetic killing rate of white (%)
6The cfu/ sheet
| Action time (min) | 3 | 5 | 10 | |
| Available iodine amount (μ g/ml) | 170 | 100 | 100 | 100 |
| 100 | 99.5 | 100 | 100 | |
| 50 | 90.2 | 95.6 | 99.0 | |
The result shows that 4-methylthio group-2-hydroxybutyric acid iodine and METHIONINE AMINO-CARBOXYL IODINE COMPLEX composition are under the situation of 100 μ g/ml effect 5min, can kill whole Candida albicanss at available iodine.
The influenza virus that kills of the lactic acid iodine of embodiment 7 (available iodine 0.32%) is tested
Method: lactic acid iodine liquid is diluted to the diluent of different concns, 0.5ml and 0.5ml HIV-1 suspension (10 with aseptic deionized water
6TCID
50) act on 1min respectively, 5min, 10min draws 0.2ml, adds neutralizing agent (1% Sulfothiorine) 0.1ml, acts on 2min under the room temperature, adds cell nutrient solution 1ml, measures virus titer in 96 porocyte culture plates.37 ℃ of (5% CO
2) cultivated 7 days, there is index with cytopathy in observations as virus day by day.The result is as shown in table 2.
Table 2: the lactic acid iodine liquid of different concns is to the inactivating efficacy of HIV
| The test grouping | Average infection titer (the TCID of effect different time 50) | ||
| 1min | 5min | 10min | |
| The contrast of amino acid iodine group (available iodine, μ g/ml) 50 25 10 nertralizer group neutralized reaction product group disinfectant papovas | ＜1.00 2.25 4.86 - - - - | ＜1.00 ＜1.00 4.55 - - - - | ＜1.00 ＜1.00 4.00 6.60 6.38 ＜1.00 6.85 |
Illustrate:＜1.00 for not seeing cytopathy.
The result shows that amino acid iodine under the situation of effect 5min, can be killed influenza virus at available iodine 〉=12 μ g/ml, makes it inactivation.
The lactic acid iodine of embodiment 9 and METHIONINE AMINO-CARBOXYL IODINE COMPLEX mixed solution are killed the trichomonad test
Method: lactic acid iodine and METHIONINE AMINO-CARBOXYL IODINE COMPLEX mixed solution (available iodine 2.5%) are diluted to the diluent of different concns with sterile distilled water, and extension rate is respectively 250; 500; 1000; 1500; Every pipe 0.9ml is standby.Preparation Trichomonas vaginalis water liquid.Be inoculated on the trichomonad substratum, 34 ℃ of incubators were hatched 4 days.Sterilized water replaces thimerosal to compare.The result is as shown in table 3.
Table 3: the amino acid iodine liquid of different concns is to the inactivating efficacy of Trichomonas vaginalis
| Amino acid iodine liquid concentration (extension rate) | 250 | 500 | 1000 | 1500 | Contrast | |
| Action time (min) | 1 | + | + | + | + | + |
| 2 | - | + | + | + | + | |
| 5 | - | - | + | + | + | |
| 10 | - | - | + | + | + | |
| 20 | - | - | + | + | + | |
Claims (21)
1. organo-iodine complex with general formula (I):
(R
1R
2C(R.
3)R
4)
n I.
2 (I)
(R wherein
1R
2C (R.
3) R
4)
nPart is represented complexing agent, R
1, R
2, R.
3, R
4Identical or different, representation carboxy, hydroxyl or amino or contain the alkane group or the aromatic hydrocarbon group of carboxyl, hydroxyl or amido functional group respectively; The n representative is selected from the integer of 1-6, I.
2Represent coordination center.
2. the organo-iodine complex of claim 1, wherein R
4Representation carboxy.
3. the organo-iodine complex of claim 1, wherein R
1, R
2And R.
3Representation hydroxy or contain the alkane group or the aromatic hydrocarbon group of hydroxy functional group.
4. the organo-iodine complex of any one, wherein R. among the claim 1-3
3Be hydroxyl.
5. the organo-iodine complex of claim 1, wherein said complexing agent is 4-methylthio group-2-hydroxybutyric acid, 2 hydroxy propanoic acid, hydroxy-butanedioic acid, tartrate, gluconic acid, tartronic acid, oxyacetic acid, 2-hydroxy-iso-butyric acid, 2-hydroxy-2-methyl propionic acid or hydroxybutyric acid.
6. the organo-iodine complex of claim 1, wherein said complexing agent is 2 hydroxybenzoic acid, 3-cresotinic acid, 3-methoxyl group Whitfield's ointment, 5-sulphosalicylic acid, 4-hydroxyl Whitfield's ointment, 4 hydroxyisophthalic acid, 2-hydroxyl-3-naphthoic acid, hydroxyl phenylacetic acid, 6-methyl-3-sec.-propyl Whitfield's ointment, agaric acid, citric acid or pyruvic acid.
7. the organo-iodine complex of claim 1, wherein said complexing agent is the alpha-non-natural amino acid of general formula (IV):
R
5N(CH
2COOH)
2 (IV)
R wherein
5With the R in the claim 1
1Define identical.
8. the organo-iodine complex of claim 7, wherein said complexing agent is Beta-alanine-N, N-oxalic acid, benzaminic acid-N, N-oxalic acid, ammonia oxalic acid, nitrilotriacetic acid(NTA), ammonia dipropionic acid, quadrol-N, N-oxalic acid, ethylenediamine tetraacetic acid (EDTA), ethylene diamine dipropionic acid or ethylenediamine tetrapropionic acid(EDTP).
9. the organo-iodine complex of claim 1, wherein said complexing agent is an amine.
10. the organo-iodine complex of claim 9, wherein amine is quadrol, propylene diamine, dipyridyl, thanomin, diethanolamine or trolamine.
11. the organo-iodine complex of claim 1, wherein said complexing agent are pyruvic acid or hydroxyquinoline
12. I.2 the organo-iodine complex of claim 1 wherein is common iodine molecule.
13. I.2 the organo-iodine complex of claim 1 wherein is the radio isotope of iodine molecule.
14. the organo-iodine complex of claim 4, wherein the hydroxyl organic carboxyl acid is 1-20 to the mole ratio of iodine molecule.
15. the organo-iodine complex of claim 14, wherein the hydroxyl organic carboxyl acid is 1-5 to the mole ratio of iodine molecule.
16. composition, said composition contain among the claim 1-15 organo-iodine complex as activeconstituents of any one
17. the composition of claim 16, said composition also contain the performance improver performance improver.
18. the composition of claim 17, described performance improver are nutrient substance class, vitamins, seasoning sweetener class or other treatment activeconstituents.
19. the purposes of the organo-iodine complex of any one in the preparation medicine among the claim 1-15.
20. the purposes of claim 19, wherein said medicine are used for the treatment of shrimp disease, fish hemorrhage, livestock and poultry infectious diseases, acquired immune deficiency syndrome (AIDS), stomatitis, rhinopharyngitis, vaginitis, tumour, pneumonia, digestive tract disease or iodine deficiency.
21. the organo-iodine complex of any one is as the purposes of diagnostic reagent among the claim 11-15.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510055459 CN1834087A (en) | 2005-03-17 | 2005-03-17 | organic iodine complex |
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|---|---|
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Family
ID=37002005
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102526100A (en) * | 2011-01-12 | 2012-07-04 | 北京人福军威医药技术开发有限公司 | Pharmaceutical composition containing lappaconitine and iodine |
| CN105601527A (en) * | 2014-11-24 | 2016-05-25 | 天津博克尼科技发展有限公司 | Method for preparing N-dodecyl sodium alanine-iodine complex |
| CN107501078A (en) * | 2016-06-14 | 2017-12-22 | 佛山市正典生物技术有限公司 | A kind of citric acid iodo-complexes and preparation method thereof |
| CN107513014A (en) * | 2016-06-17 | 2017-12-26 | 佛山市正典生物技术有限公司 | A kind of salicylic acid-iodine complex compound, preparation method and application |
| CN111825776A (en) * | 2020-06-10 | 2020-10-27 | 青岛海大生物集团有限公司 | Preparation process and application of halogenated algal polysaccharide |
-
2005
- 2005-03-17 CN CN 200510055459 patent/CN1834087A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102526100A (en) * | 2011-01-12 | 2012-07-04 | 北京人福军威医药技术开发有限公司 | Pharmaceutical composition containing lappaconitine and iodine |
| CN102526100B (en) * | 2011-01-12 | 2013-08-21 | 北京人福军威医药技术开发有限公司 | Pharmaceutical composition containing lappaconitine and iodine |
| CN105601527A (en) * | 2014-11-24 | 2016-05-25 | 天津博克尼科技发展有限公司 | Method for preparing N-dodecyl sodium alanine-iodine complex |
| CN107501078A (en) * | 2016-06-14 | 2017-12-22 | 佛山市正典生物技术有限公司 | A kind of citric acid iodo-complexes and preparation method thereof |
| CN107513014A (en) * | 2016-06-17 | 2017-12-26 | 佛山市正典生物技术有限公司 | A kind of salicylic acid-iodine complex compound, preparation method and application |
| CN111825776A (en) * | 2020-06-10 | 2020-10-27 | 青岛海大生物集团有限公司 | Preparation process and application of halogenated algal polysaccharide |
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