CN105287392A - Alendronate sodium effervescent granules - Google Patents
Alendronate sodium effervescent granules Download PDFInfo
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- CN105287392A CN105287392A CN201510647560.0A CN201510647560A CN105287392A CN 105287392 A CN105287392 A CN 105287392A CN 201510647560 A CN201510647560 A CN 201510647560A CN 105287392 A CN105287392 A CN 105287392A
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- alendronate sodium
- sodium
- effervescent
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Abstract
The invention discloses alendronate sodium effervescent granules, and belongs to the field of a pharmaceutical preparation. Specifically, the alendronate sodium effervescent granules consist of alendronate sodium, a filling agent, effervescing agents, a binding agent and a flavoring agent. The effervescent granules disclosed by the invention are prepared by respectively pelletizing sodium hydrogen carbonate and tartaric acid, which serve as the effervescing agents, with other materials, and mixing the two obtained granules. The alendronate sodium effervescent granules are simple in preparation process, relatively low in cost and suitable for industrial production, and the prepared alendronate sodium effervescent granules are good in effervescing and dispersing effects and appropriate in taste.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition for the treatment of osteoporosis or control and to cause because of osteoporosis fracturing, be specifically related to a kind of effervescent granule containing Alendronate sodium, belong to field of pharmaceutical preparations.
Background technology
Osteoporosis is a kind of cachectic ostealis, and because a variety of causes causes osseous tissue amount to reduce, bone fine structure changes, and causes the increase of bone fragility easily to be fractured, mostly occurs old people and postmenopausal women.Alendronate sodium (AlendronateSodium) belongs to third generation diphosphonates bone resorption inhibitor, is used for the treatment of osteoporosis clinically or prevents and treats to cause fracture because of osteoporosis, evident in efficacy.
Alendronate sodium is for bone resorption position, particularly the site of action of osteoclast has stronger affinity, can be combined with osteoclast, suppress it active, and while reduction osteoclast activity, osteoblastic activity is not affected, effectively can reduce Bone tumour, make bone formation exceed bone resorption, thus bone amount is increased, reach treatment osteoporosis, alleviate clinical symptoms, the object of prevention fracture.
Alendronate sodium is developed by Mo Shadong pharmaceutical Co. Ltd, and commodity are called Fosamax
?, this medicine, went on the market at more than 50 state approvals successively from November, 1993 since Italian Initial Public Offering is used for the treatment of osteoporosis.The alendronate sodium formulation of domestic and international listing is mainly tablet, the patient taking this medicine mostly is mid-aged population, may there is dysphagia in some patients, what tablet can reduce patient takes compliance, and the Alendronate sodium effervescent granule that this provides can effective head it off.
Effervescent granule take effervescent as the novel instant granular of disintegrating agent, drop in water and can produce a large amount of bubbles, and dissolve within a short period of time, compared with plain particles agent, have instant, do not need to stir can be evenly distributed, the feature of good palatability, be particularly suitable for old people and the patient of solid preparation can not be swallowed.
Summary of the invention
The object of the present invention is to provide one can dissolve rapidly in water, and can be uniformly distributed, the Alendronate sodium effervescent granule of sour and sweet palatability.
The component that Alendronate sodium effervescent granule of the present invention comprises has: (1) effective ingredient Alendronate sodium; (2) filler; (3) effervescent; (4) adhesive; (5) correctives
Described Alendronate sodium weight ratio is 0.01 ~ 5%, is preferably 0.01 ~ 2%.
Described filler is one or more in glucose, sucrose, lactose, xylitol, modified starch, microcrystalline Cellulose, maltodextrin, mannitol, sorbitol, is preferably lactose; Its weight ratio is 5 ~ 90%, is preferably 20 ~ 80%.
Described effervescent is made up of acid foaming agent and alkaline foaming agent:
Described acid foaming agent is one or more in citric acid, tartaric acid, malic acid, fumaric acid, adipic acid, succinic acid, is preferably tartaric acid; Its weight ratio is 5 ~ 25%, is preferably 10 ~ 20%;
Described alkaline foaming agent is one or more in sodium carbonate and sodium bicarbonate, is preferably sodium bicarbonate; Its weight ratio, for being 5 ~ 25%, is preferably 10 ~ 20%;
Described adhesive is one or more in ethylmethylcellulose, methylcellulose, maltodextrin, starch, hydroxyethylmethyl-cellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, is preferably hydroxypropyl methylcellulose; Its weight ratio is 2 ~ 30%; Be preferably 5 ~ 25%.
Described correctives is one or more in aspartame, saccharin sodium, acesulfame potassium, sucralose, is preferably acesulfame potassium; Its weight ratio is 0.1 ~ 10%; Be preferably 0.5 ~ 5%.
Alendronate sodium effervescent granule is prepared by all or part of of above-claimed cpd.
Effervescent granule containing Alendronate sodium disclosed by the invention, its preparation method comprises the following steps:
(1) by equal for all supplementary materials grinding particle size to 60-120 order, for subsequent use;
(2) Alendronate sodium after pulverizing and acid foaming agent is taken in proportion, and the filler of recipe quantity half, adhesive and correctives, mix homogeneously in wet granulator, adds purified water and makes soft material, granulation, drying, granulate;
(3) the alkaline foaming agent after pulverizing is taken in proportion, and remaining filler, adhesive and correctives, mix homogeneously in wet granulator, adds purified water and makes soft material, granulation, drying, granulate;
(4) by dried particles mix homogeneously in three-dimensional mixer of above-mentioned (2) and (3), subpackage.
Specific embodiments
Be below specific embodiments of the invention, technical scheme of the present invention is described further, but protection scope of the present invention is not limited to these embodiments.Every do not deviate from the present invention's design change or equivalent substituting include within protection scope of the present invention.
embodiment 1:the screening of acid foaming agent
In the selection of effervescent, sodium bicarbonate is as alkaline foaming agent, and consumption is few, and gas production is large, and the present invention adopts sodium bicarbonate as alkaline foaming agent.And the selection of acid foaming agent not only affects effervescent dispersion effect, also affect preparation mouthfeel, therefore acid foaming agent is screened.Adopt different types of acid foaming agent to granulate, obtain granule with the alkaline foaming agent of employing and be mixed into sample, investigate its dispersion effect and mouthfeel.Specific experiment and the results are shown in following table:
Note: mouthfeel is investigated in item, and "-" mouthfeel is very poor, and "-" mouthfeel is poor, " ± " mouthfeel is general, and "+" mouthfeel is better, and " ++ " mouthfeel is fine.
From investigation result, above-mentioned several organic acid all can be used as acid foaming agent of the present invention, the result of comprehensive dispersion effect and mouthfeel, and acid foaming agent of the present invention is more preferably tartaric acid.
embodiment 2:the preparation of Alendronate sodium effervescent granule
Prescription forms:
| Title | Weight ratio/% |
| Alendronate sodium | 0.5 |
| Lactose | 75 |
| Sodium bicarbonate | 10 |
| Tartaric acid | 8 |
| Hydroxypropyl methylcellulose | 5 |
| Acesulfame potassium | 1.5 |
Preparation technology:
(1) by equal for all supplementary materials grinding particle size to 80-120 order, for subsequent use;
(2) Alendronate sodium after pulverizing and tartaric acid is taken in proportion, and the lactose of recipe quantity half, hydroxypropyl methylcellulose and acesulfame potassium, mix homogeneously in wet granulator, adds purified water and makes soft material, granulation, drying, granulate;
(3) sodium bicarbonate after pulverizing is taken in proportion, and remaining lactose, hydroxypropyl methylcellulose and acesulfame potassium, mix homogeneously in wet granulator, adds purified water and makes soft material, granulation, drying, granulate;
(4) by dried particles mix homogeneously in three-dimensional mixer of above-mentioned (2) and (3), subpackage.
embodiment 3:the preparation of Alendronate sodium effervescent granule
Prescription forms:
| Title | Weight ratio/% |
| Alendronate sodium | 0.5 |
| Xylitol | 50 |
| Maltodextrin | 20.5 |
| Sodium bicarbonate | 12 |
| Malic acid | 10 |
| Starch | 6 |
| Aspartame | 1 |
Preparation technology:
(1) by equal for all supplementary materials grinding particle size to 80-120 order, for subsequent use;
(2) Alendronate sodium after pulverizing and malic acid is taken in proportion, and the xylitol of recipe quantity half, maltodextrin, starch and aspartame, mix homogeneously in wet granulator, adds purified water and makes soft material, granulation, drying, granulate;
(3) sodium bicarbonate after pulverizing is taken in proportion, and remaining xylitol, maltodextrin, starch and aspartame, mix homogeneously in wet granulator, adds purified water and makes soft material, granulation, drying, granulate;
(4) by dried particles mix homogeneously in three-dimensional mixer of above-mentioned (2) and (3), subpackage.
embodiment 4:the preparation of Alendronate sodium effervescent granule
Prescription forms:
| Title | Weight ratio/% |
| Alendronate sodium | 0.5 |
| Sucrose | 77.5 |
| Sodium carbonate | 6 |
| Citric acid | 7 |
| Hydroxypropyl cellulose | 7 |
| Saccharin sodium | 2 |
Preparation technology:
(1) by equal for all supplementary materials grinding particle size to 80-120 order, for subsequent use;
(2) Alendronate sodium after pulverizing and citric acid is taken in proportion, and the sucrose of recipe quantity half, hydroxypropyl cellulose and saccharin sodium, mix homogeneously in wet granulator, adds purified water and makes soft material, granulation, drying, granulate;
(3) sodium carbonate after pulverizing is taken in proportion, and remaining sucrose, hydroxypropyl cellulose and saccharin sodium, mix homogeneously in wet granulator, adds purified water and makes soft material, granulation, drying, granulate;
(4) by dried particles mix homogeneously in three-dimensional mixer of above-mentioned (2) and (3), subpackage.
Alendronate sodium effervescent granule melting checks
Inspection method: Example 2-4 Alendronate sodium effervescent granule 6 bags respectively, puts respectively in the beaker filling 200mL water (water temperature 15 ~ 25 DEG C), observes it and dissolve situation.
Criterion: should produce rapidly gas and form effervescent shape, within 5 minutes, endoparticle all should be dispersed or dissolved in water completely.
Result: each embodiment sample all conforms with the regulations.
Claims (8)
1. an Alendronate sodium effervescent granule, is characterized in that: containing as the Alendronate sodium of effective ingredient, filler, effervescent, adhesive and correctives.
2. Alendronate sodium effervescent granule according to claim 1, is characterized in that: described Alendronate sodium weight ratio is 0.01 ~ 5%, is preferably 0.01 ~ 2%.
3. Alendronate sodium effervescent granule according to claim 1, it is characterized in that: described filler is one or more in glucose, sucrose, lactose, xylitol, modified starch, microcrystalline Cellulose, maltodextrin, mannitol, sorbitol, be preferably lactose; Its weight ratio is 5 ~ 90%, is preferably 20 ~ 80%.
4. Alendronate sodium effervescent granule according to claim 1, is characterized in that: described effervescent is made up of acid foaming agent and alkaline foaming agent.
5. effervescent according to claim 4, is characterized in that: described acid foaming agent is one or more in citric acid, tartaric acid, malic acid, fumaric acid, adipic acid, succinic acid, is preferably tartaric acid; Its weight ratio is 5 ~ 25%, is preferably 10 ~ 20%.
6. effervescent according to claim 4, is characterized in that: described alkaline foaming agent is one or more in sodium carbonate and sodium bicarbonate, is preferably sodium bicarbonate; Its weight ratio is 5 ~ 25%, is preferably 10 ~ 20%.
7. Alendronate sodium effervescent granule according to claim 1, it is characterized in that: described adhesive is one or more in ethylmethylcellulose, methylcellulose, maltodextrin, starch, hydroxyethylmethyl-cellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, be preferably hydroxypropyl methylcellulose; Its weight ratio is 2 ~ 30%; Be preferably 5 ~ 25%.
8. Alendronate sodium effervescent granule according to claim 1, is characterized in that: described correctives is one or more in aspartame, saccharin sodium, acesulfame potassium, sucralose, is preferably acesulfame potassium; Its weight ratio is 0.1 ~ 10%; Be preferably 0.5 ~ 5%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510647560.0A CN105287392A (en) | 2015-10-09 | 2015-10-09 | Alendronate sodium effervescent granules |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510647560.0A CN105287392A (en) | 2015-10-09 | 2015-10-09 | Alendronate sodium effervescent granules |
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| CN105287392A true CN105287392A (en) | 2016-02-03 |
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| CN201510647560.0A Pending CN105287392A (en) | 2015-10-09 | 2015-10-09 | Alendronate sodium effervescent granules |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101305988A (en) * | 2007-05-17 | 2008-11-19 | 北京利乐生制药科技有限公司 | Compound alendronate sodium vitamine D3 orally disintegrating tablets and preparation method thereof |
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2015
- 2015-10-09 CN CN201510647560.0A patent/CN105287392A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101305988A (en) * | 2007-05-17 | 2008-11-19 | 北京利乐生制药科技有限公司 | Compound alendronate sodium vitamine D3 orally disintegrating tablets and preparation method thereof |
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Application publication date: 20160203 |
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