CN1565477A - Iodine microsphere clathrate compound and its preparation method and uses - Google Patents
Iodine microsphere clathrate compound and its preparation method and uses Download PDFInfo
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- CN1565477A CN1565477A CN 03149243 CN03149243A CN1565477A CN 1565477 A CN1565477 A CN 1565477A CN 03149243 CN03149243 CN 03149243 CN 03149243 A CN03149243 A CN 03149243A CN 1565477 A CN1565477 A CN 1565477A
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- 229910052740 iodine Inorganic materials 0.000 title claims abstract description 120
- 239000011630 iodine Substances 0.000 title claims abstract description 120
- 238000002360 preparation method Methods 0.000 title claims abstract description 27
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 title claims abstract 26
- 150000001875 compounds Chemical class 0.000 title description 2
- 239000004005 microsphere Substances 0.000 title 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 claims abstract description 109
- 238000000034 method Methods 0.000 claims abstract description 12
- 210000000214 mouth Anatomy 0.000 claims abstract description 3
- 239000000243 solution Substances 0.000 claims description 32
- NLKNQRATVPKPDG-UHFFFAOYSA-M potassium iodide Chemical compound [K+].[I-] NLKNQRATVPKPDG-UHFFFAOYSA-M 0.000 claims description 27
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 23
- 239000007787 solid Substances 0.000 claims description 22
- XMBWDFGMSWQBCA-UHFFFAOYSA-M iodide Chemical compound [I-] XMBWDFGMSWQBCA-UHFFFAOYSA-M 0.000 claims description 21
- 229940006461 iodide ion Drugs 0.000 claims description 21
- 238000005303 weighing Methods 0.000 claims description 20
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 15
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 15
- 239000007788 liquid Substances 0.000 claims description 15
- 239000002904 solvent Substances 0.000 claims description 14
- 239000008187 granular material Substances 0.000 claims description 11
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 9
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 9
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 9
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 9
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 9
- FVAUCKIRQBBSSJ-UHFFFAOYSA-M sodium iodide Chemical compound [Na+].[I-] FVAUCKIRQBBSSJ-UHFFFAOYSA-M 0.000 claims description 9
- 238000001035 drying Methods 0.000 claims description 8
- 238000003756 stirring Methods 0.000 claims description 8
- 239000003826 tablet Substances 0.000 claims description 7
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 claims description 7
- 239000006189 buccal tablet Substances 0.000 claims description 4
- 229940046011 buccal tablet Drugs 0.000 claims description 4
- 235000013305 food Nutrition 0.000 claims description 4
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 claims description 4
- HSZCZNFXUDYRKD-UHFFFAOYSA-M lithium iodide Chemical compound [Li+].[I-] HSZCZNFXUDYRKD-UHFFFAOYSA-M 0.000 claims description 4
- 238000005498 polishing Methods 0.000 claims description 4
- UAYWVJHJZHQCIE-UHFFFAOYSA-L zinc iodide Chemical compound I[Zn]I UAYWVJHJZHQCIE-UHFFFAOYSA-L 0.000 claims description 4
- 239000012046 mixed solvent Substances 0.000 claims description 3
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims description 3
- 235000009518 sodium iodide Nutrition 0.000 claims description 3
- XZXYQEHISUMZAT-UHFFFAOYSA-N 2-[(2-hydroxy-5-methylphenyl)methyl]-4-methylphenol Chemical compound CC1=CC=C(O)C(CC=2C(=CC=C(C)C=2)O)=C1 XZXYQEHISUMZAT-UHFFFAOYSA-N 0.000 claims description 2
- UNMYWSMUMWPJLR-UHFFFAOYSA-L Calcium iodide Chemical compound [Ca+2].[I-].[I-] UNMYWSMUMWPJLR-UHFFFAOYSA-L 0.000 claims description 2
- DKNPRRRKHAEUMW-UHFFFAOYSA-N Iodine aqueous Chemical compound [K+].I[I-]I DKNPRRRKHAEUMW-UHFFFAOYSA-N 0.000 claims description 2
- 229940107816 ammonium iodide Drugs 0.000 claims description 2
- 229940046413 calcium iodide Drugs 0.000 claims description 2
- 229910001640 calcium iodide Inorganic materials 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims description 2
- 239000000084 colloidal system Substances 0.000 claims description 2
- 150000002497 iodine compounds Chemical class 0.000 claims description 2
- 239000000865 liniment Substances 0.000 claims description 2
- 229940040145 liniment Drugs 0.000 claims description 2
- 239000004570 mortar (masonry) Substances 0.000 claims description 2
- 239000006188 syrup Substances 0.000 claims description 2
- 235000020357 syrup Nutrition 0.000 claims description 2
- 239000002966 varnish Substances 0.000 claims description 2
- 201000007100 Pharyngitis Diseases 0.000 abstract description 3
- 201000001245 periodontitis Diseases 0.000 abstract description 2
- -1 methyl hydroxypropyl-beta-cyclodextrin Chemical compound 0.000 abstract 2
- 208000025865 Ulcer Diseases 0.000 abstract 1
- 231100000397 ulcer Toxicity 0.000 abstract 1
- 210000004877 mucosa Anatomy 0.000 description 7
- 230000035943 smell Effects 0.000 description 7
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 6
- 239000000843 powder Substances 0.000 description 6
- 230000001954 sterilising effect Effects 0.000 description 6
- 238000004659 sterilization and disinfection Methods 0.000 description 6
- 229960004756 ethanol Drugs 0.000 description 5
- 230000000737 periodic effect Effects 0.000 description 5
- 239000012153 distilled water Substances 0.000 description 4
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 3
- 229930195725 Mannitol Natural products 0.000 description 3
- 229930006000 Sucrose Natural products 0.000 description 3
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 3
- 230000002159 abnormal effect Effects 0.000 description 3
- 235000019359 magnesium stearate Nutrition 0.000 description 3
- 239000000594 mannitol Substances 0.000 description 3
- 235000010355 mannitol Nutrition 0.000 description 3
- 239000011812 mixed powder Substances 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 239000005720 sucrose Substances 0.000 description 3
- 229920000858 Cyclodextrin Polymers 0.000 description 2
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
- 230000000844 anti-bacterial effect Effects 0.000 description 2
- 238000005352 clarification Methods 0.000 description 2
- 238000004821 distillation Methods 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- NOOLISFMXDJSKH-UHFFFAOYSA-N p-menthan-3-ol Chemical compound CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 2
- 235000011837 pasties Nutrition 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 2
- 241000233866 Fungi Species 0.000 description 1
- 206010067997 Iodine deficiency Diseases 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 208000016150 acute pharyngitis Diseases 0.000 description 1
- 230000002421 anti-septic effect Effects 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000019884 chronic gingivitis Diseases 0.000 description 1
- 238000010668 complexation reaction Methods 0.000 description 1
- 239000006184 cosolvent Substances 0.000 description 1
- 230000009849 deactivation Effects 0.000 description 1
- 229960000935 dehydrated alcohol Drugs 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 208000007565 gingivitis Diseases 0.000 description 1
- 235000006479 iodine deficiency Nutrition 0.000 description 1
- 239000008297 liquid dosage form Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000011259 mixed solution Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 231100000017 mucous membrane irritation Toxicity 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000010409 thin film Substances 0.000 description 1
- 206010044008 tonsillitis Diseases 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention relates to a hepu iodine for treating faucitis, oral cavity ulcer, periodontitis, chronic pharyngitis, process for preparation and use thereof, which comprises methyl hydroxypropyl-beta-cyclodextrin, iodine, and iodine ions by the the molecular proportion ratio is 1:1 - 10:1 - 100.
Description
Technical field
The present invention relates to a kind of Preparation Method And Use of Grain General Iodine that is used for the treatment of diseases such as chronic pharyngolaryngitis, stomatocace, chronic gingivitis, periodontitis, acute and chronic pharyngitis, tonsillitis, iodine deficiency.
Background technology
Iodine is of long duration as antiseptic sterilization agent, and the iodine solution of high concentration all has stronger deactivation to various antibacterials, fungus, virus.But because iodine has extremely strong abnormal smells from the patient, bigger when being directly used in mucosa delivery to the zest of mucosa, cause patient's compliance relatively poor.And the dissolubility of iodine in water is relatively poor, often needs take off iodine with ethanol after using iodine tincture sterilization skin clinically, thereby also gives to use clinically and bring some inconvenience.
Iodine very easily distils during room temperature, and the iodine distillation is accelerated more than 40 ℃ the time, brings many problems for the suitability for industrialized production of Operand.Therefore, when ensureing the iodine active function, carrying periodic dissolubility, covering its bad smell, reduce its zest for mucosa, improve iodine is to perplex technical barrier of related personnel for a long time to the stability of temperature.
At present commercially available Operand or employing add potassium iodide as cosolvent, by carrying periodic dissolubility with the potassium iodide complexation.Or adopt adding glycerol, ethanol, plant wet goods organic solvent to improve the dissolubility of iodine in oil.Or adopt beta-schardinger dextrin-that iodine molecule is carried out the bad smell that enclose (cydiodine) is covered iodine.
The prepared Operand of method all exists shortcoming in one aspect above adopting.Add that glycerol, ethanol, plant wet goods organic solvent can be carried periodic dissolubility but the abnormal smells from the patient that is difficult to cover iodine can not be eliminated its zest to mucosa although form soluble complexes or adopt by potassium iodide and iodine.The Operand that adopts above-mentioned several method to prepare also is difficult to avoid the distillation of iodine, brings difficulty for packing, storage, the transportation of these Operands.Can effectively cover the foreign odor of iodine, reduce the zest of iodine though adopt Chinese patent 90106682.6 usefulness beta-schardinger dextrin-s that iodine molecule is carried out enclose, put forward periodic stability, can not significantly improve the dissolubility of iodine in water mucosa.Have data to show that the sterilization speed of iodine and the concentration of its formation solution present certain relation: 1% iodine tincture can kill 90% antibacterial in 90 seconds, and 5% iodine tincture only needs 60 seconds, and 7% iodine tincture then only needs 15 seconds.And adopt the clathrate process of beta-schardinger dextrin-to iodine, and the full solution concentration of closing of iodine is less than 0.2%, and its sterilization usually needs a few minutes to arrive dozens of minutes.
Summary of the invention
Thereby the object of the invention is to develop a kind of abnormal smells from the patient that can cover iodine, reduce iodine to the zest of mucosa, put forward periodic stability and can increase substantially the Operand that contains that the dissolubility of iodine in water shortens its sterilization time, the i.e. general iodine of standing grain simultaneously again.
The present invention adopts a kind of novel pharmaceutic adjuvant: HP-, utilize the focus method of the research of pharmaceutics in recent years: cyclodextrin inclusion method.Make formed complex of iodine and iodide ion and HP-molecule form a kind of microencapsulated form clathrate.
The technical problem to be solved in the present invention provides Preparation Method And Use of Grain General Iodine, thereby by HP-iodine and the formed complex of iodide ion is carried out the hydroxypropyl-beta-cyclodextrin inclusion of enclose preparation iodine and iodide ion complex and utilize this clathrate to prepare a series of Related products.
The general iodine of standing grain contains iodine, iodide ion, HP-, and wherein the molecule mol ratio of iodine and iodide ion, HP-is 1: 1～10: 1～100.
Iodide ion comprises: sodium iodide, potassium iodide, ammonium iodide, lithium iodide, zinc iodide, calcium iodide etc. contain the iodide ion in the iodine compound, wherein preferred potassium iodide.
The preparation method of the general iodine of standing grain is as follows:
The solvent method:
Take by weighing HP-and be dissolved in right amount in the suitable solvent, make concentration range at 1～75% solution; Take by weighing iodine and iodide are an amount of, form complex solution with a small amount of suitable solvent dissolving, this solution is mixed, stirs with HP-solution, promptly get the hydroxypropyl-beta-cyclodextrin inclusion of iodine and iodide ion complex, promptly get the general iodine of liquid standing grain, the general iodine drying of liquid standing grain can be got the general iodine of solid, shaped standing grain.
Polishing:
Get HP-and place colloid mill, mortar or grinder in right amount, add an amount of solvent and stir, make into pastel; Molecule mol ratio according to iodine, iodide ion, HP-, take by weighing iodine and iodide in above-mentioned pastel, ground 1～4 hour, get uniform pastel, promptly get the hydroxypropyl-beta-cyclodextrin inclusion of the complex of iodine and iodide ion, be the general iodine of pasty state standing grain, the general iodine drying of pasty state standing grain can be got the general iodine of solid standing grain.
In above-mentioned solvent method and polishing, described suitable solvent can be water, ethanol, methanol, propanol, isopropyl alcohol, ethylene glycol, propylene glycol, glycerol, acetone, also can be arbitrarily two or more mixed solvent, wherein preferred water.
In above-mentioned solvent method and polishing, the clathrate solid that described drying means can use rotating thin film evaporation, drying under reduced pressure, constant pressure and dry, spray drying, lyophilization and other methods to obtain.
The general iodine liquid of standing grain can be directly used in liquid preparations such as preparing oral liquid, syrup, varnish, liniment or contain iodine food; The general iodine solid of standing grain can be processed into solid preparations such as tablet, capsule, granule, buccal tablet, solution sheet, oral cavity adhesion tablet or contain iodine food.
The invention has the beneficial effects as follows by HP-iodine and the formed complex of iodide ion are carried out enclose, the formed complex of iodine and iodide ion is embedded in the tubular structure of HP-molecule becomes the general iodine of standing grain, thereby improve the dissolubility of iodine in water, solved the problem that the iodine water solublity is low, zest big and the iodine solution sterilization time of low concentration is long.By the HP-molecule to the enclose of iodine and iodide ion complex the physical behavior of iodine is changed, dissolubility increases, bad smell disappears, stability strengthens, mucous membrane irritation reduces.Make iodine be applied to solid, liquid dosage form with the form of clathrate.
HP-is the less water solublity pharmaceutic adjuvant of a kind of toxicity, be suitable for making multiple liquid preparation and solid preparation with the general iodine of the standing grain of its preparation, the enclose by HP-makes the general iodine of standing grain have good water solubility, bland characteristics.
In the time of 25 ℃, the general iodine of the standing grain that adopts HP-to make after measured, the dissolubility in the water are greater than 8.9g/100ml, and its dissolubility is much larger than the Operand-cydiodine (0.2g/100ml) with cyclodextrin inclusion compound.Owing to improved water solublity, the solid preparation of using the general iodine preparation of standing grain has also that disintegrate is fast, stripping good, curative effect characteristics rapidly, is more conducive to clinical practice.The general iodine of prepared standing grain is compared with iodine, the bad smell of iodine is covered, iodine to the zest of mucosa be lowered, the stability of iodine is improved, the dissolubility of iodine in water also obtained increasing substantially.Realized purpose of the present invention.
The specific embodiment
The preferred version of general iodine of standing grain and preparation method thereof is to contain iodine, potassium iodide, HP-.
The preferred solvent method of preparation method:
It is soluble in water in right amount to take by weighing HP-, makes the solution of concentration range at 1-75%; Take by weighing iodine and potassium iodide is an amount of, form complex solution, this solution is mixed, stirs with HP-solution, promptly get the hydroxypropyl-beta-cyclodextrin inclusion of iodine and iodide ion complex, i.e. the general iodine of standing grain with the low amounts of water dissolving.The general iodine solution drying of the standing grain of gained (40-90 ℃) is got the general iodine solid of standing grain.
For technical scheme of the present invention is described better, the spy provides following examples, but the present invention is not limited to this.
Embodiment 1: prepare the general iodine of a kind of liquid standing grain
(1) take by weighing the 7g HP-, be dissolved in the 100ml distilled water, stirring makes it all be dissolved to the solution clarification;
(2) take by weighing potassium iodide 1.8g, make it dissolving, get solution A with a small amount of distilled water.Take by weighing iodine 1.2g and in solution A, grind and make it all form solution, and this solution is poured in the above-mentioned HP-solution;
(3) mixed liquor stirred 10 minutes, observed solution to clear, promptly got the general iodine of a kind of liquid standing grain.
Embodiment 2: prepare the general iodine of a kind of solid standing grain
(1), (2), (3) are with embodiment 1;
(4) the general iodine of liquid standing grain is concentrated, drying under reduced pressure promptly gets the general iodine of a kind of solid standing grain.
Embodiment 3: prepare the general iodine of another kind of liquid standing grain
(1) take by weighing the 7g HP-, be dissolved in the 100ml distilled water, stirring makes it all be dissolved to the solution clarification;
(2) take by weighing sodium iodide 1.2g, make it dissolving, get solution A with a small amount of distilled water.Take by weighing iodine 1.2g and in solution A, grind and make it all form solution, and this solution is poured in the above-mentioned HP-solution;
(3) mixed solution was stirred 10 minutes, observe solution to clear, the general iodine of another kind of liquid standing grain.
Embodiment 4: prepare the general iodine of another kind of solid standing grain
(1) (2) (3) are with embodiment 3;
(4) the general iodine of liquid standing grain among the embodiment (3) is concentrated, drying under reduced pressure promptly gets the general iodine of another kind of solid standing grain.
Embodiment 5: the general iodine buccal tablet of standing grain preparation method
Obtain the general iodine of solid standing grain by embodiment 2.It is standby that the general iodine of solid standing grain of gained was pulverized 100 mesh sieves.Take by weighing Mentholum 2.5g in beaker, dissolve with dehydrated alcohol 30ml.The ethanol solution of gained Mentholum had been sprayed in the mixed-powder that the 160g sucrose of crossing 80 mesh sieves and 160g mannitol and 20g citric acid formed with spray gun, and fully mixing is dried in 60～90 ℃ of baking ovens, dried powder A.Get the general iodine 10g of standing grain, other gets mixed-powder A300g, adds entry 20ml behind the mix homogeneously and granulates with 20 mesh sieves, and made granule is dried in 60～90 ℃ of baking ovens, behind the 24 mesh sieve granulate, sneaked into the 2g magnesium stearate and get powder B.Adjust tablet machine with powder B tabletting, promptly get the general iodine buccal tablet of standing grain.
Embodiment 6: the general iodine solution piece preparation method of standing grain
Take by weighing the general iodine of standing grain and obtain the general iodine of solid standing grain by embodiment 2.It is standby that the general iodine of solid standing grain of gained was pulverized 100 mesh standard sieves.In 150g sucrose and 150g mannitol, the 30g sodium carboxymethyl cellulose mixed-powder, fully mixing is got the general iodine 10g of standing grain, and adds entry 20ml after the above-mentioned powder mixes and granulates with 20 mesh sieves, behind oven dry, 24 mesh sieve granulate in 60～90 ℃ of baking ovens of made granule, sneak into the 2g magnesium stearate.Adjust the tablet machine tabletting, promptly get the general iodine solution sheet of standing grain.
Embodiment 7: the preparation method of the general iodine sheet of a kind of standing grain
Obtain the general iodine of solid standing grain by embodiment 2.It is standby that the general iodine of solid standing grain of gained was pulverized 100 mesh standard sieves.Take by weighing sucrose 120g, the mannitol 120g, citric acid 50g, the sodium bicarbonate 15g that cross 80 mesh sieves, take by weighing the general iodine 10g of standing grain, fully mixing adds entry 20ml and granulates with 20 mesh sieves, made granule is dried in 60～90 ℃ of baking ovens, behind the 24 mesh sieve granulate, sneaked into the 2g magnesium stearate and get powder B.Adjust tablet machine with powder B tabletting, promptly get the general iodine sheet of standing grain.
Claims (9)
1, the general iodine of a kind of standing grain is characterized in that being made up of iodine, iodide ion, HP-, and the molecule mol ratio is 1: 1～10: 1～100.
2, the general iodine of standing grain according to claim 1, it is characterized in that iodide ion comprises: sodium iodide, potassium iodide, ammonium iodide, lithium iodide, zinc iodide, calcium iodide etc. contain the iodide ion in the iodine compound.
3, the general iodine of standing grain according to claim 1 and 2, its preferred version is to contain iodine, potassium iodide, HP-.
4, the preparation method of the general iodine of a kind of standing grain is characterized in that the solvent method: take by weighing HP-and be dissolved in right amount in the suitable solvent, make concentration range at 1～75% solution; Take by weighing iodine and iodide are an amount of, form complex solution, this solution is mixed, stirs with HP-solution, promptly get the hydroxypropyl-beta-cyclodextrin inclusion of iodine and iodide ion complex, i.e. the general iodine of standing grain with a small amount of suitable solvent dissolving.
5, according to the general iodine preparation method of the described standing grain of claim 4, it is characterized in that suitable solvent comprises: water, ethanol, methanol, propanol, isopropyl alcohol, ethylene glycol, propylene glycol, glycerol, acetone, also can be arbitrarily two or more mixed solvent, wherein preferred water.
6, according to claim 4 or the general iodine preparation method of 5 described standing grain, the preferred for preparation method is that to take by weighing HP-soluble in water in right amount, makes the solution of concentration range at 1-75%; Take by weighing iodine and potassium iodide is an amount of, form complex solution, this solution is mixed, stirs with HP-solution, promptly get the hydroxypropyl-beta-cyclodextrin inclusion of iodine and iodide ion complex, i.e. the general iodine of standing grain with the low amounts of water dissolving; The general iodine solution drying of the standing grain of gained (40-90 ℃) is got the general iodine solid of standing grain.
7, the preparation method of the general iodine of a kind of standing grain is characterized in that polishing: get HP-and place colloid mill, mortar or grinder in right amount, add suitable solvent and stir, make into pastel; Molecule mol ratio according to iodine and iodide ion, HP-takes by weighing iodine and iodide in above-mentioned pastel, ground 1～4 hour, uniform pastel, promptly get the hydroxypropyl-beta-cyclodextrin inclusion of iodine and iodide ion complex, i.e. the general iodine of standing grain.
8, according to the general iodine preparation method of the described standing grain of claim 7, it is characterized in that suitable solvent comprises: water, ethanol, methanol, propanol, isopropyl alcohol, ethylene glycol, propylene glycol, glycerol, acetone also can be two or more mixed solvents arbitrarily.
9, the purposes of the general iodine of standing grain is characterized in that: the general iodine of liquid standing grain can be directly used in liquid preparations such as preparing oral liquid, syrup, varnish, liniment or contain iodine food; The general iodine of solid standing grain can be processed into solid preparations such as tablet, capsule, granule, buccal tablet, solution sheet, oral cavity adhesion tablet or contain iodine food.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03149243 CN1283259C (en) | 2003-06-20 | 2003-06-20 | Iodine microsphere clathrate compound and its preparation method and uses |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03149243 CN1283259C (en) | 2003-06-20 | 2003-06-20 | Iodine microsphere clathrate compound and its preparation method and uses |
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| CN1565477A true CN1565477A (en) | 2005-01-19 |
| CN1283259C CN1283259C (en) | 2006-11-08 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107137371A (en) * | 2017-06-27 | 2017-09-08 | 石家庄学院 | A kind of double layer adhesive sheet for treating canker sore |
| CN107517963A (en) * | 2017-08-31 | 2017-12-29 | 山东省农业科学院家禽研究所 | A kind of high stability BETA Cyclodextrin Inclusion Compound of Iodine powder and its preparation, application method |
-
2003
- 2003-06-20 CN CN 03149243 patent/CN1283259C/en not_active Expired - Lifetime
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107137371A (en) * | 2017-06-27 | 2017-09-08 | 石家庄学院 | A kind of double layer adhesive sheet for treating canker sore |
| CN107517963A (en) * | 2017-08-31 | 2017-12-29 | 山东省农业科学院家禽研究所 | A kind of high stability BETA Cyclodextrin Inclusion Compound of Iodine powder and its preparation, application method |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1283259C (en) | 2006-11-08 |
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