CN105012252A - Preparation method of mangiferin aglycon dispersible tablet and application of mangiferin aglycon dispersible tablet - Google Patents
Preparation method of mangiferin aglycon dispersible tablet and application of mangiferin aglycon dispersible tablet Download PDFInfo
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- CN105012252A CN105012252A CN201410165163.5A CN201410165163A CN105012252A CN 105012252 A CN105012252 A CN 105012252A CN 201410165163 A CN201410165163 A CN 201410165163A CN 105012252 A CN105012252 A CN 105012252A
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Abstract
The invention relates to the field of medicines, and provides a preparation method of a mangiferin aglycon dispersible tablet and an application of the mangiferin aglycon dispersible tablet. The following components: 0.2%-70% of mangiferin aglycon, 0.2%-20% of an adhesive, 5%-80% of a filling agent, 0.2%-20% of a disintegrant, 0.2%-20% of a swelling auxiliary material, 0-8% of a surfactant and 0.1%-10% of a flow aid are pressed to prepare the mangiferin aglycon dispersible tablet. The mangiferin aglycon dispersible tablet has the characteristics of beautiful appearance and high bioavailability, and is mainly used for treating hyperuricemia hyperuricuria, gout, hyperglycemia, a cough, a malignant tumor and virus infection on clinic; and the preparation method provided by the invention has the advantages of being simple in process, low in production cost, and easy to produce on a large scale, and has a good industrialized application prospect.
Description
Technical field
The present invention relates to field of medicaments, being specifically related to can a kind of mango aglycone dispersible tablet preparation method and application thereof.
Background technology
Mango aglycone extracts in plant, the natural polyphenol compounds obtained after abstraction and purification, and its structural formula is:
Mango aglycone is chimonin Mangiferin body active metabolite, is a kind of active substance after the main active chimonin desaccharide unit of Anacardiaceae plant Fructus Mangifera Indicae Mangifera indica leaf.
In 60 ~ seventies of 20th century, scholar's primary study both domestic and external various sources of chimonin, from leaf, fruit, the bark of almond Mangiferaperisciformis, in the various plants such as the Gnidia involucrata (thymelaeceae trees) of liliaceous plant Rhizoma Anemarrhenae Anemarrhena asphodeloids, Plants of Polypodiaceae Herba Pyrrosiae Calvatae Foliaum Pyrrosiae and Switzerland, extract chimonin.
Chimonin has another name called Mengiferin, mangiferin, mangiferin; English mangiferin by name, has another name called chinonin; Alpizarine; 1,3,6,7-tetrahydroxyxanthone; 2-beta-D-glucopyranosyl-1,3,6,7-tetrahydroxy-9H-xanthen-9-one; Molecular formula CisHisOu, molecular weight 422.34; For light lark acicular crystal (50% ethanol), fusing point 267-272 DEG C (decomposition), optical rotation+43.3 ° (c=0.9, than pyridine) ,+32 ° (ethanol).
Chimonin was both not dissolved in water, was also not dissolved in the non-polar solven such as petroleum ether, chloroform; Be slightly soluble in the medium polar solvents such as methanol, ethanol, acetonitrile, ethyl acetate, butyl acetate, n-octyl alcohol; Be soluble in pyridine, glycerol, 50% dioxane aqueous solution, hot Diluted Alcohol aqueous solution (40-70%), the strong acid aqueous solution of pH < 2 and pH) strong alkali aqueous solution of 10.
Mango aglycone is the active metabolite of chimonin, has antioxidation, suppresses the multiple pharmacological effect such as PTP1B activity, blood sugar lowering, antitumor, uric acid resisting and gout, cause the attention of numerous medicine scholar and chemist.Research in recent years finds, the pharmacologically active of mango aglycone is stronger than chimonin.Medical biotechnology National Key Laboratory of Nanjing University shouts on acid potassium salt inducing mouse generation hyperuricemia model at oxygen, research finds that chimonin significantly lowers the expression of heavy absorption and transport body (mURAT1) of hyperuricemia mouse kidney urate and glucose transporter 9 (mGLUT9) mRNA and albumen, and raising kidney organic anion transporter 1 (mOAT1) expression, this grinds the prompting that makes internal disorder or usurp: Fructus Mangifera Indicae Seedling heavily can absorb by suppressing kidney uric acid and increase uric acid secretion and promote that hyperuricemia mice urate excretion is to reduce its serum uric acid level.The research such as the Li Ling of unming Medical College finds that Fructus Mangifera Indicae Seedling to be made an uproar purine oxidase inhibitor as a kind of Huang of favour quinones, shows low toxicity, efficiently feature when treating gout disease.In addition, the Wu Qiu industry seminar of The 2nd Army Medical College has carried out gout activity research to the bitter unit of Fructus Mangifera Indicae, finds that Fructus Mangifera Indicae Seedling unit also has good gout active.Chimonin and aglycon thereof are as a kind of lead compound of novel treatment gout disease, both can by the generation suppressing the oxidasic activity of yellow purine to reduce uric acid, can act on again the excretion that the heavy absorption and transport body 9 (mGLUT9) of kidney urate promotes uric acid, be the newtype drug of the promising treatment gout of a class.
Dispersible tablet (dispersible tablets), also known as water dispersion tablet (water dispersible tablets), refers to that meeting water disintegrate can form the tablet of even stickiness suspension rapidly.Along with the development of medical industry, the dispersible tablet of chemicals is loaded into pharmacopoeia of each country, and " British Pharmacopoeia " starts to record 3 kinds of dispersible tablets such as aspirin for 1980, and " the People's Republic of China's pharmacopeia " 2000 years versions start to record dispersible tablet.2005 editions " the People's Republic of China's pharmacopeia " specifies, dispersible tablet requires in the 100ml water of (20 ± 1) DEG C, jolting 3min, should all disintegrates by No. two sieves, relative and general formulation, substantially increases the bioavailability of medicine like this.Dispersible tablet can add aqueous dispersion deutostoma clothes, also dispersible tablet can be contained in mouth and suck clothes or swallow, and is particularly suitable for patient that is old, young and difficulty of swallowing.It combines the advantage of tablet and liquid preparation, and overcome both deficiencies, this novel form not only taking convenience, and absorption is fast, bioavailability is high, untoward reaction is little, and the production technology of dispersible tablet and equipment are without particular/special requirement, be a kind of novel troche with DEVELOPMENT PROSPECT, developed rapidly in recent years.
Mango aglycone is owing to being insoluble in water, bioavailability is lower, therefore on peroral dosage form is selected, larger limitation is received, mango aglycone is made dispersible tablet and can effectively improve its water solublity, thus improve its bioavailability, therefore mango aglycone has been made dispersible tablet by this, has the advantage that conventional tablet is incomparable.
Summary of the invention
The present invention is directed to mango aglycone dissolubility low, the defect that bioavailability is low, provide a kind of preparation method and clinical practice thereof of dispersible tablet of mango aglycone.Mango aglycone dispersible tablet of the present invention can increase the dissolubility of mango aglycone effectively, improves its bioavailability, thus plays its treatment ventilation better, reduces the drug effect of uric acid.
In order to realize goal of the invention above, the invention provides following technical scheme:
A kind of mango aglycone dispersible tablet, its component is: mango aglycone 0.2%-70%, binding agent 0.2-20%, filler 5-80%, disintegrating agent 0.2-20%, swelling type adjuvant 0.2-20%, surfactant 0-8%, fluidizer 0.1-10%, mango aglycone dispersible tablet made by tabletting.Include following three kinds of methods and step:
The first preparation method:
Step 1: sieved respectively by raw material, claims appropriate binding agent, filler, disintegrating agent, swelling type adjuvant, surfactant;
Step 2: add mango aglycone mixing;
Step 3: after adding the mixing of appropriate fluidizer, namely direct compression obtains invents the mango aglycone dispersible tablet described in saying.
The second preparation method:
Step 1: sieved respectively by raw material, claims appropriate binding agent, filler, disintegrating agent, swelling type adjuvant, surfactant;
Step 2: add mango aglycone mixing;
Step 3: after adding wetting agent, prepares soft material, prepares granule, dry, granulate;
Step 4: after adding appropriate disintegrating agent and fluidizer mixing, namely tabletting obtains invents the mango aglycone dispersible tablet described in saying.
The third preparation method:
Step 1: sieved respectively by raw material, claims appropriate binding agent, filler, disintegrating agent, swelling type adjuvant, surfactant;
Step 2: add mango aglycone mixing;
Step 3: take fluid bed one-step method granule;
Step 4: after adding appropriate disintegrating agent and fluidizer mixing, namely tabletting obtains invents the mango aglycone dispersible tablet described in saying.
Mango aglycone dispersible tablet of the present invention and preparation method thereof tool has the following advantages:
(1), after mango aglycone and specific fast disintegrating agent and excellent excipient combine in proportion, dispersing uniformity is good, improves bioavailability.
(2) mango aglycone dispersible tablet of the present invention disintegrate can form homogeneous dispersion rapidly in water, is conducive to the disintegrate stripping of medicine, promotes the absorption of medicine.
(3) mango aglycone dispersible tablet taking convenience of the present invention, can swallow, chew, containing sucking or taking with after aqueous dispersion.
(4) preparation method technique of the present invention is simple, low production cost, easy large-scale production.
Detailed description of the invention
The invention discloses mango aglycone dispersible tablet and preparation method thereof, those skilled in the art can use for reference content of the present invention, and suitable improving technique parameter realizes.Special needs to be pointed out is, all similar replacements and change are all easily accomplish those skilled in the art, and they are also considered as comprising in the present invention.Method of the present invention and application are described by embodiment, and related personnel also can not depart from content of the present invention, under the prerequisite of spirit and scope, changes described methods and applications or changes, realize and apply the technology of the present invention.
The following example is intended to citing further and describes the present invention, but is not any restriction to scope.
Embodiment 1
Mango aglycone dispersible tablet: 1000,
Supplementary material is crossed 100 mesh sieves respectively, takes lactose, microcrystalline Cellulose, crospolyvinylpyrrolidone, polyvidone mixing by recipe quantity; Add mango aglycone mixing again; Add magnesium stearate respectively again, micropowder silica gel mixes, and tabletting, obtains mango aglycone dispersible tablet of the present invention.
The present invention is yellowish color chips, and carry out uniformity of dosage units and stripping experiment according to the rules, uniformity of dosage units all conforms with the regulations, and reaches pharmacopoeial requirements.
Embodiment 2
Mango aglycone dispersible tablet: 1000
Supplementary material is crossed 100 mesh sieves respectively, mango aglycone, lactose, mannitol, crospolyvinylpyrrolidone is taken respectively by recipe quantity, after mixing, add 95% ethanol and make wetting agent, 20 orders are granulated sub, wet granular is dry under 50-80 DEG C of condition, 20 mesh sieve granulate, add crospolyvinylpyrrolidone, magnesium stearate, tabletting after micropowder silica gel, mixing, obtains mango aglycone dispersible tablet of the present invention.
This product is yellowish color chips, carries out the experiment of uniformity of dosage units, dissolution and assay according to the rules, all reaches pharmacopoeial requirements.
Embodiment 3
Mango aglycone dispersible tablet: 1000
Supplementary material is crossed 100 mesh sieves respectively, after taking mango aglycone, lactose, mannitol, crospolyvinylpyrrolidone mixing by recipe quantity, soft material is prepared as wetting agent with 70% ethanol, 20 mesh sieves are granulated, wet granular is dry under 50-80 DEG C of condition, with 20 mesh sieve granulate, after adding crospolyvinylpyrrolidone, magnesium stearate, micropowder silica gel mix homogeneously, tabletting, obtains mango aglycone dispersible tablet of the present invention.
This product is yellowish color chips, carries out the experiment of uniformity of dosage units, dissolution and assay according to the rules, all reaches pharmacopoeial requirements.
Embodiment 4
Uric acid resisting is verified: male mice in kunming, random packet, is respectively Normal group, model control group, mango aglycone dosage group (high, medium and low), positive drug control group (allopurinol).Every day is gavage (ig) respectively, and the time is 7 days.Normal group and model control group gavage give normal saline.After 5th day administration 1h, often organize and go up metabolic cage respectively, within the 6th day, collect 24h urine, after the 7th day administration 1h, eyeball of mouse rear vein beard gets blood.Urine and serum are placed in 4 DEG C of preservations respectively, for Biochemical Indexes.Result shows: compare with Normal group, model control group mice serum uric acid level significantly increases, and shows the success of hyperuricemia animal model modeling.Compare with model control group, each dosage group of mango aglycone (50,100 and 200mg/kg) and allopurinol group (5mg/kg) all can effectively reduce animal pattern serum uric acid level.Increase with dosage, the uric acid resisting effect of mango aglycone has enhancing trend, the results are shown in Table 1.
Table 1 mango aglycone is on the impact of metabolic arthritis mice biochemical indicator
Claims (10)
1. a mango aglycone dispersible tablet, its component is: mango aglycone 0.2%-70%, binding agent 0.2-20%, filler 5-80%, disintegrating agent 0.2-20%, swelling type adjuvant 0.2-20%, surfactant 0-8%, fluidizer 0.1-10%, tabletting obtains mango aglycone dispersible tablet.
2. binding agent as claimed in claim 1, is characterized in that, it comprises one in polyvinylpyrrolidone and hydroxypropyl emthylcellulose or two kinds.
3. filler as claimed in claim 1, it is characterized in that it comprises lactose, microcrystalline Cellulose, calcium sulfate (dihydrate), one or more in calcium hydrogen phosphate, sorbitol, mannitol, maltodextrin, pregelatinized Starch, starch and dextrin.
4. disintegrating agent as claimed in claim 1, it is characterized in that it comprises in crospolyvinylpyrrolidone, low replacement carboxy-propyl cellulose, cross-linking sodium carboxymethyl cellulose and carboxymethyl starch sodium one or more.
5. swelling type adjuvant as claimed in claim 1, it is characterized in that it comprises in guar gum, XANTHAN GUM, xanthan gum, pectin, alginate, glucosan, pregelatinized Starch, polysaccharide and carboxymethylcellulose calcium, hydroxypropyl emthylcellulose, hydroxypropyl cellulose one or more.
6. surfactant as claimed in claim 1, is characterized in that it to comprise in Tween 80, sodium lauryl sulphate, cetab and stearyl alcohol sulphonic acid ester one or more.
7. fluidizer as claimed in claim 1, it is characterized in that it comprises in magnesium stearate (calcium), Pulvis Talci, micropowder silica gel, Polyethylene Glycol one or more.
8. tabletting as claimed in claim 1, is characterized in that it can be direct compression of full-powder, tabletting or add wetting agent, the one after granule processed in tabletting three kinds of methods after one-step palletizing.
9. wetting agent according to claim 8, is characterized in that it is concentration range alcoholic solution or aqueous solution composition.
10. alcoholic solution according to claim 9, is characterized in that it be concentration range is 5-95% alcoholic solution.
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1462618A (en) * | 2003-05-30 | 2003-12-24 | 李红洁 | Fibrauretine in dosage form of decentralization tablet |
| CN102807548A (en) * | 2011-05-30 | 2012-12-05 | 昆明制药集团股份有限公司 | Norathyriol crystal I and preparation method thereof |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1462618A (en) * | 2003-05-30 | 2003-12-24 | 李红洁 | Fibrauretine in dosage form of decentralization tablet |
| CN102807548A (en) * | 2011-05-30 | 2012-12-05 | 昆明制药集团股份有限公司 | Norathyriol crystal I and preparation method thereof |
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Address after: 510000 No. 40 Guanghanyu Street, Baogang, Haizhu District, Guangzhou City, Guangdong Province Applicant after: Guangdong Pharmaceutical University Address before: 510006 No. 280 East Ring Road, Guangzhou City University, Guangdong Applicant before: Guangdong Pharmaceutical University |
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Application publication date: 20151104 |