CN1235598C - Process for preparing buccal lozenge contg. compound sede-iodine - Google Patents
Process for preparing buccal lozenge contg. compound sede-iodine Download PDFInfo
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- CN1235598C CN1235598C CN 03149507 CN03149507A CN1235598C CN 1235598 C CN1235598 C CN 1235598C CN 03149507 CN03149507 CN 03149507 CN 03149507 A CN03149507 A CN 03149507A CN 1235598 C CN1235598 C CN 1235598C
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Abstract
The name of the present invention is the preparing method for compound cydiodine buccal tablets. The present invention relates to medicine for treating diseases in the field of buccal cavities and throats. Iodine has a nonselective killing function to all bacteria, fungi and viruses, and can be called a broad-spectrum sterilizing disinfectant with high efficiency. But because the physicochemical property of iodine is unstable, and iodine has intense stimulation and stinks to mucosae, the clinical application of iodine in the treatment of diseases of buccal cavities and throats is limited. An inclusion compound of host molecules and guest molecules with the proportion of 1:1 of beta-cyclodextrin-iodine is directly formed from beta-cyclodextrin and iodine in an optimum technological condition by the present invention so as to become molecule state iodine, namely the cydiodine. In addition, the cydiodine is used as main medicine which is matched with materials of sucrose, citric acid, menthol, etc. so that the compound cydiodine buccal tablets is prepared. The cydiodine and the compound cydiodine buccal tablets prepared by the novel method have the advantages of stable physicochemical property and preparation performance, good mouth feel, easy bulk production and broad-spectrum disinfecting performance with high efficiency, and is an ideal excellent preparation for treating diseases of buccal cavities and throats.
Description
Technical field
The present invention relates to a kind of outstanding medicine---preparation method of compound xidi iodine sucked tablet for the treatment of oral cavity, laryngopharyngeal diseases at present clinically.
Background technology
Oral disease (oral ulcer, stomatitis, gingivitis, periodontitis, pericoronitis etc.), bottleneck throat disease (acute and chronic pharyngitis, tonsillitis etc.) are the department of stomatology, hals,Nasen und Ohrenheilkunde common clinical and frequently-occurring disease.Iodine (I
2) as existing more than the 100 year history of disinfectant, it all has or not optionally killing action to antibacterial, fungus, virus, can be rated as the broad-spectrum high efficacy antibacterial.But because the physics of iodine itself, the poor stability of chemical property, stink is big, and is big to the zest of skin and oral cavity, pharyngolaryngeal mucosa, therefore, limited iodine application clinically.It is " iodine lozenge " that past is used maximum a kind of general formulations clinically, but prove through clinical use widely and a large amount of experimentatioies, " iodine lozenge " do not solve the stability of formulation problem, not only the iodine consumption is few in the preparation, because the unstability of its preparation, in preparation, content of iodine is atomic, and this medicine is to play a role with the iodide ion form, thereby bactericidal action is atomic, even do not have bactericidal action substantially.Therefore, the new drug formulation of research and development iodine is subjected to the attention of Chinese scholars always.
From twentieth century seventies, research worker is utilized the molecular dispersion technology both at home and abroad, and (β-Cyclodextrin is called for short β-CYD) as carrier, make β-CYD and I to select beta-schardinger dextrin-
2Form clathrate (β-CYD-I
2), become numerator iodine---cydiodine (β-Cyclodextrin Inclusion Compound of Iodine is called for short Cydiodine---cydiodine).This I
2Clathrate (cydiodine) not only physics, chemical property are stable, and do not have I
2Stink and zest, can be used as disinfectant, antiseptic, deodorizer, collut, dentifrice etc., also can be used as the medicine of human, enlarged I
2Range of application.
1976, Japan Patent Japan.Kokai 76 88625 (1976); 76 101123 (1976); 76 101124 (1976) have reported beta-schardinger dextrin--iodine clathrate (β-CYD-I respectively
2, cydiodine) preparation method and purposes.The preparation method of the cydiodine of these patents is: 12g I
2, 8gKI adds water 200ml, makes I
2After the dissolving, add 50g β-CYD, stir, behind 50-80 ℃ of heating 2-3hrs, placed one day, produce coffee-like β-CYD-I
2The clathrate precipitation is filtered, washed several times with water, and drying gets pulverous β-CYD-I
2Clathrate.This β-CYD-I
2Clathrate is mainly used in the antiseptic of food, and disinfectant, agent of deodorising and sterilizing.Nineteen eighty-three, Japan Patent Jpn.Kokai Tokkyo Koho JP83 152808 (1983) uses above-mentioned similar methods to prepare β-CYD-I
2, be prepared into antimicrobial collut, dentifrice with it.China Poison ﹠ Medicine Inst. of Military Medicial Sciences Academy has applied for the patent of " preparation method of compound xidi iodine sucked tablet " August 16 nineteen ninety, and invests patent right March 31 nineteen ninety-five.This patent prepares cydiodine (β-CYD-I
2) method and the Japan Patent method relatively, be consistent substantially, but, be prepared into the treatment oral cavity of human, " compound xidi iodine sucked tablet " (cydiodine) of laryngopharyngeal diseases cydiodine and other supplementary product compatibilities.This patent prepares β-CYD-I
2Method be: 12g KI adds 18g I again with behind the 40ml water dissolution
2, make iodine liquid; 75g β-CYD adds water 300ml, 60-90 ℃ of dissolving; The iodine drop is gone in β-CYD aqueous solution, and 60-90 ℃ is stirred 2hrs, and after room temperature left standstill, filtration, washing, 60-70 ℃ drying got β-CYD-I
2, yield 90%.
To the analysis of above-mentioned patent documentation as can be seen, these patents prepare cydiodine (β-CYD-I
2) method be consistent basically, all be with KI and I
2In water, at first form the complex (I of iodine
- 3), and then with β-CYD enclose, actual that form is β-CYD-I
- 3Clathrate.This inclusion method can be referred to as β-CYD and I
2Indirect enclose.The KI that contains a great deal of in this clathrate.These KI are necessary as food additive (antiseptic), and KI exists in other purposes (disinfectant, antiseptic, deodorizer, collut, dentifrice), stablize I except rising
2Effect outside, do not have other essential meanings, but do not influence the essence purposes of these medicaments yet.As the medicine of human, KI has drug action, and the use of KI and the existence in medicine are always not useful to human body; As main active ingredient I
2, when playing therapeutical effect, I
2Molecule has become iodide ion (I
-); The use of KI is particularly used in as OTC Class B medicine at Dobell, makes human body will absorb more potassium ion (K
+) and iodide ion (I
-), therefore, in Dobell, use more KI, may be to do harm rather than good to human body.
Summary of the invention
The present invention relates to the preparation method of cydiodine, do not use KI, but be dissolved in β-CYD in the water or in the Diluted Alcohol, make β-CYD aqueous solution or β-CYD Diluted Alcohol solution; With I
2Be dissolved in the ethanol, make iodine tincture; Iodine tincture is splashed in β-CYD solution,, be chilled to below the room temperature, filter at 60-70 ℃ of inclusion reaction 2-hrs, washing, 60-70 ℃ of drying gets coffee-like β-CYD-I
2(cydiodine).The cydiodine of this method preparation, 60 ℃ and 80 ℃ of constant temperature were deposited 10 days, and its outward appearance and content have no significant change, and the cydiodine of this method preparation be described, and its physics, chemical property are stablized.The present invention prepares the method for cydiodine, does not use KI, but in certain solvent, with the direct enclose I of β-CYD
2, this inclusion method can be referred to as β-CYD and I
2Direct enclose.β-the CYD-I of indirect enclose preparation
- 3β-CYD-I with direct enclose preparation
2, action effect is consistent, all is with numerator iodine, performance iodine is to the broad-spectrum high efficacy bactericidal action of antibacterial, fungus, virus.
The cydiodine of the present invention's method preparation is as the compound xidi iodine sucked tablet of principal agent preparation, bactericidal action is strong, satisfactory for result, and cydiodine stable performance, in use keep playing a role with the iodine molecule form, solve the stability problem of Operand well, possessed the condition of medication in the buccal tablet prescription fully.For bringing into play the effect of cydiodine better,, be prepared into compound xidi iodine sucked tablet with cydiodine and suitable material compatibility.The ratio of each component is in this compound recipe buccal tablet:
(1). cydiodine 0.2-9.0%
1. iodine (I
2) 1.0-20.0%
2. beta-schardinger dextrin-80.0-99.0%
(2). sucrose 85.0-99.0%
(3). Mentholum 0.1-1.0%
(4). citric acid 0.4-3.5%
(5). magnesium stearate 0.4-2.5%
(6). sodium carboxymethyl cellulose 0.0-3.0%
(7). hypromellose 0.0-3.0%
In this compound recipe buccal tablet prescription,, can use two kinds simultaneously singly with any for sodium carboxymethyl cellulose and two kinds of adjuvants of hypromellose, can also two kinds all need not, all can decide according to the hardness requirement of tablet.In general, buccal tablet hardness is the bigger the better, because the time of sucking is long more, the time of performance drug action is just lasting more, and medicine more can be given full play to therapeutic effect.
The preparation technology of the compound xidi iodine sucked tablet that the present invention proposes, be iodine to be dissolved in to make iodine tincture in the ethanol earlier, join in β-CYD aqueous solution or the dilute alcohol solution, under the certain reaction condition, be prepared into the solid cydiodine, pulverized 120 mesh sieves, standby behind the mensuration content.Then, after taking by weighing cydiodine by recipe quantity again and crossing sucrose (and sodium carboxymethyl cellulose or hydroxyl first third cellulose singly add a kind ofly, or both add entirely, or both the do not add entirely) mixing of 80 mesh sieves, 1. water makes soft material.With an amount of 95% ethanol or dehydrated alcohol with Mentholum, citric acid dissolving after, join equably soft material 1. in, make soft material 2..2. soft material granulates through 20 mesh sieves, and 60-70 ℃ of drying adds the magnesium stearate mixing, granulate, and tabletting is promptly made compound xidi iodine sucked tablet.
Prove that through experimentation the prepared compound xidi iodine sucked tablet of the present invention has the following advantages:
1. cydiodine is to be scattered in equably in the preparation with iodine molecule attitude form in this buccal tablet, has improved the dispersion of iodine, has improved dissolution, has strengthened the stability of the physicochemical properties of iodine, and effect duration reached more than 2 years.
2. this buccal tablet is to play a role with the iodine molecule form, thereby improves and guaranteed that iodine is to the broad-spectrum high efficacy fungicidal effectiveness of antibacterial, fungus, virus in this compound recipe troche.
3. of many uses.Not only be used for the treatment of oral diseases such as oral ulcer, stomatitis, gingivitis, periodontitis, pericoronitis, can also be used for the treatment of laryngopharyngeal diseasess such as acute and chronic pharyngitis, tonsillitis.This two classes disease all there is definite and good curative effect.
4. this buccal tablet mouthfeel is good, nonirritant, and no stink, the patient takes like a shot.
The specific embodiment
The preparation of embodiment one cydiodine
1. get iodine 10.0g and be dissolved in 95% ethanol or the dehydrated alcohol, make iodine tincture.
2. get beta-schardinger dextrin-100g, add 20% ethanol 300ml, be heated to 65 ℃ of dissolvings, make beta-schardinger dextrin-solution.
3. the iodine drop is gone in the beta-schardinger dextrin-solution, 65-70 ℃ of stirring reaction 2hrs, reduce to room temperature after, put refrigerator overnight, sucking filtration, water, Diluted Alcohol wash successively, drain, and coffee-like solid in 60-70 ℃ of drying, is crossed 120 mesh sieves, weigh, and survey behind the content standby.Weight yield 95.0-97.0%, iodine yield 90.0-95.0%.
The preparation of embodiment two compound xidi iodine sucked tablets
1. material is handled: sucrose is crossed 80 mesh sieves, and sodium carboxymethyl cellulose, hypromellose, cydiodine raw material are crossed 120 mesh sieves respectively.
2. get Mentholum 2.1g, citric acid 4.3g, add an amount of 95% ethanol, 1. stirring and dissolving makes solution.
3. get cydiodine 19.0g, sucrose 435g, sodium carboxymethyl cellulose 4.5g (or hypromellose 4.5g, or the two is all got, or the two is not all got), adopt the high speed material mixer, fully mixing, add water make in right amount soft material 1. after, add solution equably 1. again, make moistening soft material 2..2. soft material is granulated through 20 mesh sieves, after the 60-70 ℃ of drying, add magnesium stearate 4.5g, mix homogeneously, granulate is measured granule content, and tabletting promptly makes compound xidi iodine sucked tablet.Specification 1.5mg; The heavy 0.45-0.48g of sheet; The thick 3.5-3.7mm of sheet.
Claims (6)
1. the preparation method of a compound xidi iodine sucked tablet is characterized in that: comprise the following steps: to be prepared into beta-schardinger dextrin-solution in the water-soluble or Diluted Alcohol of beta-schardinger dextrin-; Iodine is dissolved in the 50-100% alcohol makes iodine tincture; Iodine tincture is joined in the beta-schardinger dextrin-solution, at 50-80 ℃ of inclusion reaction 0.5-4.0hrs, crystallisation by cooling, sucking filtration, 60-70 ℃ of dry 2hrs, the molecular state cydiodine of stable in properties; Be equipped with sucrose, citric acid, Mentholum and magnesium stearate and be prepared into compound xidi iodine sucked tablet.
2. the preparation method of a compound xidi iodine sucked tablet is characterized in that: comprise the following steps: to be prepared into beta-schardinger dextrin-solution in the water-soluble or Diluted Alcohol of beta-schardinger dextrin-; Iodine is dissolved in the 50-100% ethanol makes iodine tincture; Iodine tincture is joined in the beta-schardinger dextrin-solution, at 50-80 ℃ of inclusion reaction 0.5-4.0hrs, crystallisation by cooling, sucking filtration, 60-70 ℃ of dry 2hrs, the molecular state cydiodine of stable in properties; Be equipped with sucrose, citric acid, Mentholum, sodium carboxymethyl cellulose, hypromellose and magnesium stearate and be prepared into compound xidi iodine sucked tablet.
3. the preparation method of compound xidi iodine sucked tablet according to claim 2, it is characterized in that: the weight proportion of each component is:
(1) cydiodine 0.2～9.0%
1. iodine (I
2) 1.0～20.0%
2. beta-schardinger dextrin-80.0～99.0%
(2) sucrose 85.0～99.0%
(3) Mentholum 0.1～1.0%
(4) citric acid 0.4～3.5%
(5) magnesium stearate 0.4～2.5%
(6) sodium carboxymethyl cellulose 0.0～3.0%
(7) hypromellose 0.0～3.0%, and to satisfy the each component sum be 100%.
4. the preparation method of compound xidi iodine sucked tablet according to claim 3, it is characterized in that: the preparation process of compound xidi iodine sucked tablet is with behind load weighted cydiodine, cane sugar powder and sodium carboxymethyl cellulose and/or the hypromellose mixing, make soft material 1. with the water that accounts for the heavy total amount 1.5-8.5% of sheet earlier, 2. the alcoholic solution of reuse Mentholum and citric acid makes soft material, granulate, drying is with the magnesium stearate mixing, granulate, tabletting.
5. the preparation method of compound xidi iodine sucked tablet according to claim 1 and 2, it is characterized in that: described beta-schardinger dextrin-solution is the dilute alcohol solution of aqueous solution or 0-50% alcohol.
6. the preparation method of compound xidi iodine sucked tablet as claimed in claim 5, it is characterized in that: beta-schardinger dextrin-solution wherein is saturated solution or unsaturated solution; Iodine tincture is saturated solution or unsaturated solution.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03149507 CN1235598C (en) | 2003-07-14 | 2003-07-14 | Process for preparing buccal lozenge contg. compound sede-iodine |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03149507 CN1235598C (en) | 2003-07-14 | 2003-07-14 | Process for preparing buccal lozenge contg. compound sede-iodine |
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| Publication Number | Publication Date |
|---|---|
| CN1513475A CN1513475A (en) | 2004-07-21 |
| CN1235598C true CN1235598C (en) | 2006-01-11 |
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|---|---|---|---|
| CN 03149507 Expired - Fee Related CN1235598C (en) | 2003-07-14 | 2003-07-14 | Process for preparing buccal lozenge contg. compound sede-iodine |
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| CN100591358C (en) * | 2008-02-01 | 2010-02-24 | 山东省农业科学院家禽研究所 | Method for preparing highly water-soluble cydiodine |
| CN103393717B (en) * | 2013-07-23 | 2015-04-22 | 何元龙 | Method for preparing high-water-solubility cydiodine with low cost |
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Granted publication date: 20060111 Termination date: 20120714 |