CN104721165B - A kind of risedronate sodium is coated tablet composition and preparation method thereof - Google Patents
A kind of risedronate sodium is coated tablet composition and preparation method thereof Download PDFInfo
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- CN104721165B CN104721165B CN201510133271.9A CN201510133271A CN104721165B CN 104721165 B CN104721165 B CN 104721165B CN 201510133271 A CN201510133271 A CN 201510133271A CN 104721165 B CN104721165 B CN 104721165B
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- risedronate sodium
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Abstract
It is coated tablet composition and preparation method thereof the invention provides a kind of risedronate sodium.Risedronate sodium coating tablet of the invention contains the auxiliary materials such as shitosan, Hydroxypropyl methylcellulose, polyethylene glycol, microcrystalline cellulose, has the advantages that relevant content of material is low, side effect of digestive tract is few, drug safety is high.
Description
Technical field
The present invention relates to technical field of medicine, and in particular to a kind of risedronate sodium is coated tablet composition and its preparation
Method.
Background technology
Risedronate sodium (Risedronate Sodium) chemistry is entitled：2- (3- pyridine radicals) -1- hydroxyl ethane -1,1- is double
Two times of semihydrates of phosphonic acids mono-sodium salt, molecular formula C7H10NO7P2Na·2.5H2O, structural formula is as follows：
Risedronate sodium is third generation bisphosphonate compound, belongs to pyridine radicals diphosphonate, by U.S. Proctor
And Gamble Pharmacertical companies develop, and in December, 1998 lists in US and European.
Risedronate sodium has definite treatment and prevention effect to the osteoporosis of postmenopausal women.But, it is existing
The research of risedronate sodium solid pharmaceutical preparation it is more rare, and there is many defects.For example, profit plug phosphine disclosed in CN101601661A
Sour sodium tablet, although use direct compression method, has some superiority, but still exist relevant at aspects such as production technology, costs
Content of material is higher, the low defect of drug safety；For another example, the risedronate sodium piece of listing has stronger to digestion stage property at present
Excitant, taken at least 30 minutes before the meal orthostatic positions, although it is required that a large amount of clear water (200ml) take, and after the tablet has been ingested
30 minutes domestic demands keep standing or sit up straight posture, but still may cause dysphagia, esophagitis, gastric ulcer, stomachache, diarrhoea,
Various side effect of digestive tract such as constipation.
Therefore, the relevant content of material of risedronate sodium piece how is reduced, side effect of digestive tract is reduced, is improved medication peace
Full property etc. is as this area technical problem in the urgent need to address.
The content of the invention
It is an object of the invention to provide a kind of about content of material is low, side effect of digestive tract is few, drug safety is high
Residronate sodium tablet product.By numerous studies, the invention provides a kind of risedronate sodium coating tablet, by piece sandwich layer and bag
Clothing layer composition, wherein described piece sandwich layer includes：
Wherein described coatings are made up of (a) Opadry stomach dissolution type film-coating pre-mixing agent and (b) purified water or ethanol, its
In the weight ratio of (a) and (b) be 0.5-1.2：10, the weightening of the coatings is the 2-4% of label layer weight.
As optimal technical scheme, wherein label layer also includes disintegrant and/or glidant, wherein the disintegrant
It is preferred that PVPP, its content is 1-50 weight portions, and the preferred silica of glidant, content is 1-20 weights
Amount part.
Specifically, the invention provides following risedronate sodium coating tablet：
(1) a kind of risedronate sodium coating tablet, is made up of piece sandwich layer and coatings, wherein described piece sandwich layer composition is：
Wherein described coatings are made up of (a) Opadry stomach dissolution type film-coating pre-mixing agent and (b) purified water or ethanol, its
In the weight ratio of (a) and (b) be 1：10, the weightening of the coatings is the 2% of label layer weight.
(2) a kind of risedronate sodium coating tablet, is made up of piece sandwich layer and coatings, wherein described piece sandwich layer composition is：
Wherein described coatings are made up of (a) Opadry stomach dissolution type film-coating pre-mixing agent and (b) purified water or ethanol, its
In the weight ratio of (a) and (b) be 1：20, the weightening of the coatings is the 3% of label layer weight.
(3) a kind of risedronate sodium coating tablet, is made up of piece sandwich layer and coatings, wherein described piece sandwich layer composition is：
Wherein described coatings are made up of (a) Opadry stomach dissolution type film-coating pre-mixing agent and (b) purified water or ethanol, its
In the weight ratio of (a) and (b) be 1.2：10, the weightening of the coatings is the 4% of label layer weight.
(4) a kind of risedronate sodium coating tablet, is made up of piece sandwich layer and coatings, wherein described piece sandwich layer composition is：
Wherein described coatings are made up of (a) Opadry stomach dissolution type film-coating pre-mixing agent and (b) purified water or ethanol, its
In the weight ratio of (a) and (b) be 1：10, the weightening of the coatings is the 4% of label layer weight.
The invention further relates to the preparation method of the risedronate sodium coating tablet：According to prescription, risedronate sodium, hydroxypropyl are taken
Methylcellulose, polyethylene glycol, are dissolved in the water, and are spray dried to be coated powder, add other auxiliary materials such as shitosan, mix, pressure
Piece, is coated, and obtains final product.
By adopting the above-described technical solution, the present invention achieves following beneficial effect：With prior art
(CN101601661A) compare, the relevant content of material of risedronate sodium coating tablet of the invention is substantially reduced, drug safety
Significantly improve.In addition, risedronate sodium coating tablet of the invention forms triple protection to alimentary canal mucous membrane：(1) it is outermost
Film-coating is protected；(2) shitosan is covered in alimentary canal mucous membrane surface after forming gel, forms protective layer；(3) powder is coated in stomach
Gradually discharged again after interior dispersion, reduce conventional tablet and concentrate the release shortcoming big to gastric irritation.Accordingly, those skilled in the art
It is contemplated that risedronate sodium coating tablet of the invention can effectively reduce the side effect of digestive tract such as esophagitis, gastric ulcer
Incidence.
Depending on the dosage of risedronate sodium coating tablet of the present invention is needed according to the judgement of clinician, for example, day agent
Amount can be 5mg.
Specific embodiment
Specific embodiment of the invention is only further to carry out illustrative explanation to the present invention, is not necessarily to be construed as to this
Any limitation of invention.
Raw and auxiliary material used is purchased in market in embodiment.
The risedronate sodium coating tablet of the invention of embodiment 1 (5mg/ pieces)
Prescription：
Piece sandwich layer：
Coatings：
Opadry stomach dissolution type film-coating pre-mixing agent 3g,
Purified water 30g.
Preparation method：
Take the risedronate sodium of recipe quantity, Hydroxypropyl methylcellulose, polyethylene glycol to be dissolved in the water, be spray dried to coating powder
End, adds other auxiliary materials such as the shitosan of recipe quantity, mixes, compressing tablet, and (weightening of coatings is label layer weight to coating
2%), obtain final product.
The risedronate sodium coating tablet of the invention of embodiment 2 (35mg/ pieces)
Prescription：
Piece sandwich layer：
Coatings：
Opadry stomach dissolution type film-coating pre-mixing agent 6g,
85% ethanol 120g.
Preparation method：
Take the risedronate sodium of recipe quantity, Hydroxypropyl methylcellulose, polyethylene glycol to be dissolved in the water, be spray dried to coating powder
End, adds other auxiliary materials such as the shitosan of recipe quantity, mixes, compressing tablet, and (weightening of coatings is label layer weight to coating
3%), obtain final product.
The risedronate sodium coating tablet of the invention of embodiment 3 (70mg/ pieces)
Prescription：
Piece sandwich layer：
Coatings：
Opadry stomach dissolution type film-coating pre-mixing agent 12g,
Purified water 100g.
Preparation method：
Take the risedronate sodium of recipe quantity, Hydroxypropyl methylcellulose, polyethylene glycol to be dissolved in the water, be spray dried to coating powder
End, adds other auxiliary materials such as the shitosan of recipe quantity, mixes, compressing tablet, and (weightening of coatings is label layer weight to coating
4%), obtain final product.
The risedronate sodium coating tablet of the invention of embodiment 4 (150mg/ pieces)
Prescription：
Piece sandwich layer：
Coatings：
Opadry stomach dissolution type film-coating pre-mixing agent 20g,
Absolute ethyl alcohol 200g,
Preparation method：
Take the risedronate sodium of recipe quantity, Hydroxypropyl methylcellulose, polyethylene glycol to be dissolved in the water, be spray dried to coating powder
End, adds other auxiliary materials such as the shitosan of recipe quantity, mixes, compressing tablet, and (weightening of coatings is label layer weight to coating
4%), obtain final product.
The stability study of experimental example risedronate sodium piece
According to《Chinese Pharmacopoeia》Two relevant regulations of version in 2010, under conditions of 25 DEG C/60%RH, investigate embodiment 1
Risedronate sodium piece (reference examples) prepared by~4 risedronate sodium coating tablets for preparing and CN101601661A embodiments 1
Steadiness, relevant material (%) testing result such as following table, the detection method about material (%) is as follows：
The fine powder for weighing this product is appropriate (being approximately equivalent to risedronate sodium 50mg), puts in 25ml measuring bottles, is dissolved in water and dilute
Release to scale, shake up, filter, take subsequent filtrate as need testing solution.Precision measures need testing solution in right amount, and dilute with water is made
Solution containing the μ g of risedronate sodium 2 in per 1ml, as contrast solution.According to high performance liquid chromatography (Chinese Pharmacopoeia version two in 2010
The D of portion's annex V) determine, it is filler with octadecylsilane chemically bonded silica；16.15g phosphoric acid hydrogen (is weighed with phosphate buffer
Dipotassium and 0.46g disodium ethylene diamine tetraacetates, the 400ml that adds water dissolvings, pH is to 7.5 ± 0.1 for regulation, is diluted with water to 480ml, plus
Enter methyl alcohol 20ml, be well mixed, filtration, ultrasound) it is mobile phase, flow velocity is 1.0ml/min, Detection wavelength 263nm.Precision is measured
The μ l of above-mentioned need testing solution 10, inject liquid chromatograph, record chromatogram.It is (auxiliary if any impurity peaks in need testing solution chromatogram
Material peak and less than 0.05% chromatographic peak are disregarded), by Self-control method with calculated by peak area.
| Sample time | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Reference examples |
| 0 month | 0.08 | 0.08 | 0.07 | 0.08 | 0.30 |
| 3 months | 0.08 | 0.10 | 0.07 | 0.08 | 0.31 |
| 6 months | 0.08 | 0.10 | 0.08 | 0.09 | 0.33 |
| 9 months | 0.10 | 0.11 | 0.08 | 0.11 | 0.41 |
| 12 months | 0.10 | 0.11 | 0.09 | 0.11 | 0.54 |
| 18 months | 0.10 | 0.11 | 0.09 | 0.12 | 0.62 |
| 24 months | 0.11 | 0.11 | 0.09 | 0.12 | 0.68 |
Claims (5)
1. a kind of risedronate sodium coating tablet, is made up of piece sandwich layer and coatings, wherein described piece sandwich layer includes：
Wherein described coatings are made up of (a) Opadry stomach dissolution type film-coating pre-mixing agent and (b) purified water or ethanol, wherein
A () is 1-2: 10 with the weight ratio of (b), the weightening of the coatings is the 2-4% of label layer weight.
2. risedronate sodium coating tablet according to claim 1, is made up of piece sandwich layer and coatings, wherein described label
Layer is constituted：
Wherein described coatings are made up of (a) Opadry stomach dissolution type film-coating pre-mixing agent and (b) purified water or ethanol, wherein
A () is 1 with the weight ratio of (b)：10, the weightening of the coatings is the 2% of label layer weight.
3. risedronate sodium coating tablet according to claim 1, is made up of piece sandwich layer and coatings, wherein described label
Layer is constituted：
Wherein described coatings are made up of (a) Opadry stomach dissolution type film-coating pre-mixing agent and (b) purified water or ethanol, wherein
A () is 3 with the weight ratio of (b)：20, the weightening of the coatings is the 3% of label layer weight.
4. risedronate sodium coating tablet according to claim 1, is made up of piece sandwich layer and coatings, wherein described label
Layer is constituted：
Wherein described coatings are made up of (a) Opadry stomach dissolution type film-coating pre-mixing agent and (b) purified water or ethanol, wherein
A () is 1.2 with the weight ratio of (b)：10, the weightening of the coatings is the 4% of label layer weight.
5. risedronate sodium coating tablet according to claim 1, is made up of piece sandwich layer and coatings, wherein described label
Layer is constituted：
Wherein described coatings are made up of (a) Opadry stomach dissolution type film-coating pre-mixing agent and (b) purified water or ethanol, wherein
A () is 1 with the weight ratio of (b)：10, the weightening of the coatings is the 4% of label layer weight.
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| CN201510133271.9A CN104721165B (en) | 2015-03-25 | 2015-03-25 | A kind of risedronate sodium is coated tablet composition and preparation method thereof |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008040993A1 (en) * | 2006-10-07 | 2008-04-10 | Pliva Hrvatska D.O.O. | Pharmaceutical formulation of risedronate |
| CN101601661A (en) * | 2009-07-08 | 2009-12-16 | 昆明积大制药有限公司 | A kind of risedronic acid sodium tablet and preparation method thereof |
| CN102885759A (en) * | 2011-07-20 | 2013-01-23 | 杭州赛利药物研究所有限公司 | Risedronate sodium sustained-release preparation and preparation method thereof |
| CN103784405A (en) * | 2012-11-02 | 2014-05-14 | 沈阳药科大学 | A preparation for improving oral bioavailability of risedronate sodium and a preparing method thereof |
-
2015
- 2015-03-25 CN CN201510133271.9A patent/CN104721165B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008040993A1 (en) * | 2006-10-07 | 2008-04-10 | Pliva Hrvatska D.O.O. | Pharmaceutical formulation of risedronate |
| CN101601661A (en) * | 2009-07-08 | 2009-12-16 | 昆明积大制药有限公司 | A kind of risedronic acid sodium tablet and preparation method thereof |
| CN102885759A (en) * | 2011-07-20 | 2013-01-23 | 杭州赛利药物研究所有限公司 | Risedronate sodium sustained-release preparation and preparation method thereof |
| CN103784405A (en) * | 2012-11-02 | 2014-05-14 | 沈阳药科大学 | A preparation for improving oral bioavailability of risedronate sodium and a preparing method thereof |
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| CN104721165A (en) | 2015-06-24 |
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Address after: 051500 Haixing Road, Zhaoxian County Industrial Park, Shijiazhuang, Hebei Patentee after: HEBEI RENHE YIKANG PHARMACEUTICAL CO., LTD. Address before: 053411 Hengshui City, Hebei, Wuyi County, Qing Liang store town Patentee before: HEBEI RENHE YIKANG PHARMACEUTICAL CO., LTD. |
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