CN101305988A - Compound alendronate sodium vitamine D3 orally disintegrating tablets and preparation method thereof - Google Patents
Compound alendronate sodium vitamine D3 orally disintegrating tablets and preparation method thereof Download PDFInfo
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- CN101305988A CN101305988A CNA2007100993419A CN200710099341A CN101305988A CN 101305988 A CN101305988 A CN 101305988A CN A2007100993419 A CNA2007100993419 A CN A2007100993419A CN 200710099341 A CN200710099341 A CN 200710099341A CN 101305988 A CN101305988 A CN 101305988A
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Abstract
The invention relates to compound alendronate sodium vitamin D3 orally-disintegrating tablets used for preventing and treating stmenopausal osteoporosis and a preparation method thereof, aims to provide a novel preparation, i.e. the compound alendronate sodium vitamin D3 orally-disintegrating tablets to patients and medical workers; wherein, the compound alendronate sodium vitamin D3 orally-disintegrating tablets have fast absorption and high bioavailability, need no water when in administration, have little intestinal residue and insignificant side effects, and avoid the first-pass effect in liver sausage. Alendronate sodium vitamin D3 is used as a raw material, auxiliary materials are added in, and the alendronate sodium vitamin D3 orally-disintegrating tablets are prepared according to the technical means.
Description
Technical field
The present invention relates to medicine of a kind of taking convenience and preparation method thereof, particularly be preparation method and the application thereof that is used to prevent and treat the alendronate sodium vitamine D 3 orally disintegrating tablets of postmenopausal osteoporosis.
Background technology
Alendronate sodium is similar to estrogen to the effect of gain of bone, is better than calcitonin, and significantly bone density improving reduces the fracture incidence rate, and oral effective, effect is lasting, has good tolerability and higher safety.The danger that there is not the increase thrombosis that has when using estrogen in this medicine and causes breast cancer incidence to increase, do not exist first generation medicine etidronate disodium to take continuously yet and can cause the bone mineralising to suppress, causing halisteretic side effect, is the osteoporosis control medicine that present international clinical boundary has higher rating.With the common compound preparation of vitamin D in April, 2005 by drugs approved by FDA, name is that Fosamax Plus D is the osteoporosis therapeutic drug compound of Merck ﹠ Co., Inc.'s listing, (Fosamax Fosamax) with the 2800IU vitamin D3, only need be taken once weekly to contain the 70mg Alendronate sodium.
Oral cavity disintegration tablet is a kind of new pharmaceutical dosage forms, English " Orally disintegrating tables " by name.Be that a kind of water that do not need in the oral cavity can disintegrate or dissolved tablet.It can be in the oral cavity rapidly disintegrate, no grittiness, good mouthfeel, swallow easily, to the oral mucosa nonirritant.The distinguishing feature of this dosage form: 1. absorption is fast, bioavailability is high; 2. instructions of taking does not need water, makes things convenient for part crowd medication, as the patient's medication under old man, child, dysphagia or the special environment; 3. intestinal is residual few, few side effects; 4. avoid the first pass effect of liver sausage.
By retrieval, do not see the pertinent literature and the patent report of relevant oral disintegration tablet of prulifloxacin.
Summary of the invention
The purpose of this invention is to provide a kind of disintegrate fast, absorb rapidly, can effectively improve the bioavailability and the blood drug level of prulifloxacin, improve alendronate sodium vitamine D 3 orally disintegrating tablets of alendronate sodium vitamin D 3 stink, taking convenience, few side effects and preparation method thereof simultaneously.
Alendronate sodium vitamine D 3 orally disintegrating tablets of the present invention also contains adjuvant except principal agent.Adjuvant is any available adjuvant that is fit to make oral cavity disintegration tablet, and they can comprise filler, disintegrating agent, effervescent, correctives or odor mask, binding agent, lubricant etc.
Because oral cavity disintegration tablet requires disintegrate rapidly in the oral cavity, good mouthfeel, to the oral mucosa nonirritant.Therefore the selection to supplementary product kind and performance thereof is the key of preparation oral cavity disintegration tablet.
The present invention is through selecting, found the pharmaceutic adjuvant of suitable alendronate sodium vitamine D 3 orally disintegrating tablets, wherein filler selects to be used for increasing the weight and volume of oral cavity disintegration tablet, so that the molding of preparation and divided dose, filler preferably is selected from one or more the mixture in lactose, microcrystalline Cellulose, sucrose, fructose, mannitol, pregelatinized Starch, sorbitol, the xylitol etc. among the present invention.
The kind of disintegrating agent and the selection of consumption are for can this preparation disintegrate be most important fully at the appointed time.Disintegrating agent of the present invention one of is selected to comprise in low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, corn starch, pregelatinized Starch, carboxymethylcellulose calcium, the carboxymethyl starch sodium or wherein several mixture.
In oral cavity disintegration tablet, can add an amount of effervescent, help the disintegrate of tablet, and an amount of acid can also be regulated taste.Acid source is selected from one or more the mixture in citric acid, tartaric acid, four caproic acids, lysine, the arginine in the effervescent that the present invention selects, or alkali source is selected from one or more mixture wherein such as sodium bicarbonate, sodium carbonate, potassium carbonate, potassium bicarbonate.
When the percentage by weight of principal agent in preparation is higher, owing to bitterness may occur, therefore can select to add an amount of odor mask so that the patient accepts and takes, odor mask of the present invention comprises one or more the mixture in acrylic resin copolymer, Magnesiumaluminumsilicate, gelatin, melon glue, arabic gum, xanthan gum, paraffin, the Brazil wax.
The correctives that the present invention uses one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, Mentholum, aspartame, stevioside, the acesulfame-K or wherein several mixture.
The adding of binding agent and lubricant is for the ease of the preparation of preparation and molding.Binding agent is selected from one or more the mixture in syrup, starch slurry, carboxymethylcellulose sodium solution, HPMC solution, the povidone solution.Lubricant is selected from one or more the mixture in micropowder silica gel, magnesium stearate, PEG6000, the Pulvis Talci.
Oral cavity disintegration tablet of the present invention can be by freeze-drying or direct powder compression or granulating tabletting process preparation.
Adopt freeze-drying to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, correctives and odor mask (if necessary), prulifloxacin can be mixed with various adjuvants, add the suitable quantity of water dilution, behind the mix homogeneously, place suitable sheet shape mould, lyophilization, being shaped to the material lyophilizing gets final product.
Adopt direct powder compression to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, effervescent, lubricant, correctives and odor mask (if necessary), and behind prulifloxacin and various adjuvant mix homogeneously, direct powder compression gets final product.
Adopt granulating tabletting process to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, binding agent, lubricant, correctives and odor mask (if necessary) with prulifloxacin and partial supplementary material mix homogeneously, add binding agent system soft material, granulate, dry, granulate, add the disintegrating agent and the lubricant of surplus, behind the mix homogeneously, tabletting gets final product.
Adopt granulating tabletting process to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, effervescent, binding agent, lubricant, correctives and odor mask (if necessary), the main method step is: acid source in the effervescent and alkali source can be separated granulation, or acid source mixed with alkali source, employing contains the dehydrated alcohol binding agent granulates, dry, granulate, the disintegrating agent and the lubricant of adding surplus, behind the mix homogeneously, tabletting gets final product.
The specific embodiment
Come alendronate sodium vitamin D 3 cavity disintegrating tablet of the present invention done further specifying by following example, but be not limited in following example.
Embodiment 1
Prescription:
Preparation method:
Alendronate sodium vitamin D 3 is added in the Eudragit L30D suspension, add suitable quantity of water, after stirring, add polyvinylpolypyrrolidone, mannitol, flavoring orange essence, the limit edged stirs, and behind the one-tenth suspension, is poured in the suitable mould, lyophilization, press seal, packing.
Embodiment 2
Prescription:
Preparation method:
With the alendronate sodium vitamin D 3, pregelatinized Starch, mannitol, lactose of all crossing 80 mesh sieves according to the equivalent method mix homogeneously that progressively increases, other gets protein sugar, flavoring pineapple essence mixes with above mixture, add the micropowder silica gel mix homogeneously, direct powder compression gets final product.
Claims (8)
1. an alendronate sodium vitamine D 3 orally disintegrating tablets contains alendronate sodium vitamin D 3 active component and the excipient substance that is fit to make oral cavity disintegration tablet, and pharmaceutically suitable carrier and the about 400mg of about 25mg-are contained in every preparation unit.
2. the described oral cavity disintegration tablet of claim 1 is characterized in that, the described excipient substance that is fit to make oral cavity disintegration tablet comprises one or more in filler, disintegrating agent, effervescent, correctives, odor mask, binding agent or the lubricant etc.
3. the described oral cavity disintegration tablet of claim 2 is characterized in that described filler is selected from one or more the mixture in lactose, microcrystalline Cellulose, sucrose, fructose, mannitol, pregelatinized Starch, sorbitol, the xylitol.Described disintegrating agent is selected from a kind of or wherein several mixture in low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, corn starch, pregelatinized Starch, carboxymethylcellulose calcium, the carboxymethyl starch sodium.Acid source is selected from one or more the mixture in citric acid, tartaric acid, four caproic acids, lysine, the arginine in the described effervescent, and alkali source is selected from one or more mixture wherein such as sodium bicarbonate, sodium carbonate, potassium carbonate, potassium bicarbonate.Described odor mask is selected from one or more the described binding agent of mixture in acrylic resin copolymer, Magnesiumaluminumsilicate, gelatin, melon glue, arabic gum, xanthan gum, paraffin, the Brazil wax and is selected from one or more mixture in syrup, starch slurry, carboxymethylcellulose sodium solution, HPMC solution, the povidone solution; Described lubricant is selected from that one or more the described correctives of mixture in micropowder silica gel, magnesium stearate, PEG6000, the Pulvis Talci one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, aspartame, stevioside, the acesulfame-K or wherein several mixture.
4. the preparation method of the oral cavity disintegration tablet of claim 1 is characterized in that, adopts the preparation of freeze-drying or direct powder compression or granulating tabletting process.
5. the preparation method of the described oral cavity disintegration tablet of claim 6, wherein the preparation process of freeze-drying is: alendronate sodium vitamin D 3 and filler, disintegrating agent, correctives and odor mask are added the suitable quantity of water dilution, behind the mix homogeneously, place suitable sheet shape mould, lyophilization is shaped to the material lyophilizing.
6. the preparation method of the described oral cavity disintegration tablet of claim 6, wherein the direct powder compression preparation process is: behind prulifloxacin and filler, disintegrating agent, effervescent, lubricant, correctives and odor mask mix homogeneously, direct powder compression.
7. the preparation method of the described oral cavity disintegration tablet of claim 6, wherein the granulating tabletting process preparation process is: with alendronate sodium vitamin D 3 and partially filled dose, disintegrating agent, correctives and odor mask, add binding agent system soft material, granulate, dry, granulate, the disintegrating agent and the lubricant that add surplus, behind the mix homogeneously, tabletting.
8. the described preparation method of claim 9, it is characterized in that, the step that wherein adds effervescent is, acid source in the effervescent and alkali source are separated granulation, or acid source is mixed with alkali source, adopt to contain the granulation of dehydrated alcohol binding agent, dry, granulate, the disintegrating agent and the lubricant that add surplus, behind the mix homogeneously, tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007100993419A CN101305988A (en) | 2007-05-17 | 2007-05-17 | Compound alendronate sodium vitamine D3 orally disintegrating tablets and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007100993419A CN101305988A (en) | 2007-05-17 | 2007-05-17 | Compound alendronate sodium vitamine D3 orally disintegrating tablets and preparation method thereof |
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| CN101305988A true CN101305988A (en) | 2008-11-19 |
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| CNA2007100993419A Pending CN101305988A (en) | 2007-05-17 | 2007-05-17 | Compound alendronate sodium vitamine D3 orally disintegrating tablets and preparation method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102210697A (en) * | 2010-04-02 | 2011-10-12 | 秦引林 | Medicine composition for treating metabolic bone diseases |
| CN105193827A (en) * | 2015-10-08 | 2015-12-30 | 北京康力基生物科技有限公司 | Quickly disintegrated calcium vitamin D tablet and preparation method thereof |
| CN105287392A (en) * | 2015-10-09 | 2016-02-03 | 北京万全德众医药生物技术有限公司 | Alendronate sodium effervescent granules |
-
2007
- 2007-05-17 CN CNA2007100993419A patent/CN101305988A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102210697A (en) * | 2010-04-02 | 2011-10-12 | 秦引林 | Medicine composition for treating metabolic bone diseases |
| CN102210697B (en) * | 2010-04-02 | 2013-05-22 | 秦引林 | Medicine composition for treating metabolic bone diseases |
| CN105193827A (en) * | 2015-10-08 | 2015-12-30 | 北京康力基生物科技有限公司 | Quickly disintegrated calcium vitamin D tablet and preparation method thereof |
| CN105193827B (en) * | 2015-10-08 | 2019-01-08 | 北京康力基生物科技有限公司 | It can quickly disintegrated calcium dimension D tablet and preparation method thereof |
| CN105287392A (en) * | 2015-10-09 | 2016-02-03 | 北京万全德众医药生物技术有限公司 | Alendronate sodium effervescent granules |
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Open date: 20081119 |