CN104069121A - Topiramate slow release composition and preparation process thereof - Google Patents
Topiramate slow release composition and preparation process thereof Download PDFInfo
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- CN104069121A CN104069121A CN201410250057.7A CN201410250057A CN104069121A CN 104069121 A CN104069121 A CN 104069121A CN 201410250057 A CN201410250057 A CN 201410250057A CN 104069121 A CN104069121 A CN 104069121A
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- topiramate
- slow releasing
- releasing composition
- slow release
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Abstract
The invention provides a topiramate slow release composition, comprising the following components in parts by mass: 65-85 parts of raw material medicine, 10-30 parts of slow release material, 5-20 parts of porogenic agent, 10-20 parts of lubricant and 1-3 parts of plasticizer. The invention further discloses a process of preparing the topiramate slow release composition. A powder coating process is adopted in the preparation method to cover the raw material medicine slow release material at one time to prepare the slow release composition. The slow release composition can be made into capsules, tablets, granules, suspensions and emulsions. The slow release composition and the preparation process thereof provided in the invention are used for simplifying the production process and reducing the production cost.
Description
Technical field
The present invention relates to medicine preparation field, refer to especially a kind of topiramate slow releasing composition and preparation technology thereof.
Background technology
Topiramate is a kind of wide spectrum Newer antiepileptic, has multiple antiepileptic mechanism of action, all effective to each pyknolepsy, and the single therapy of partial seizure, constitutional Generalized seizure, Secondary cases Generalized seizure and interpolation treatment are all had to obvious curative effects.But its treatment window is very narrow, and blood concentration fluctuation can produce a lot of side effect, therefore for improving patient compliance and clinical administration, need, be made generally in slow releasing preparation.
In present slow releasing preparation, as all announced the preparation technology of topiramate slow releasing composition in Chinese invention patent CN1988889, CN102824302A, CN102579367A and PCT application international publication number WO2008/061226A2, but above-mentioned patent is all specially after making pastille micropill, adopt again slow-release material coating, make film controlling type slow releasing preparation, production process is loaded down with trivial details, has improved production cost, has increased the difficulty of quality control.
Summary of the invention
The present invention proposes a kind of topiramate slow releasing composition and preparation technology thereof, do not need to make after pastille micropill coating again, can a step make slow releasing composition.
Technical scheme of the present invention is achieved in that
Topiramate slow releasing composition and a preparation technology thereof, comprise the component of following parts by weight: topiramate 65-85 part, slow-release material 10-30 part, porogen 5-20 part, lubricant 10-20 part, plasticizer 1-3 part.
Further, described slow-release material is a kind or 2 kinds of mixing in propylene resin or ethyl cellulose.
Further, described porogen is a kind or any mixture in hypromellose, Polyethylene Glycol or polyvidone.
Further, described lubricant is a kind or any mixture in Pulvis Talci, magnesium stearate or silicon dioxide.
Further, described plasticizer is a kind or 2 kinds of mixing in triethyl citrate or dibutyl sebacate.
The technique of a kind of topiramate slow releasing composition that preparation is described, comprising:
(1) slow-release material is made into by formula ratio the solution that mass fraction is 10-30%, and solvent for use is the ethanol of concentration 70-90%;
(5) add porogen, lubricant and the plasticizer of formula ratio to be made into coating solution;
(6) by formula ratio raw materials weighing medicine medicine, put in powder coating machine, with coating solution, carry out powder coating;
(7) coating complete after 30-50 ℃ of dry 8-14h, obtain described topiramate slow releasing composition.
Further, described topiramate slow releasing composition is for the preparation of capsule, tablet, granule, suspensoid, Emulsion.
Beneficial effect of the present invention:
Topiramate is the material that a kind of level is slightly soluble in water, and under room temperature, in water, dissolubility is 9.8mg/mL.Prepare in slow releasing agent process, pastille micropill is first made in many employings, then makes slow-release micro-pill with slow-release material coating.Preparation process is at least carried out twice being dried, and technique is loaded down with trivial details, and quality control difficulty is large.And topiramate slow releasing composition and preparation technology thereof that the present invention proposes utilize topiramate extremely low feature of dissolubility in water, adopt the method for powder coating, once complete crude drug slow-release material coated, make slow releasing composition.Described slow releasing composition can add relevant auxiliary materials to make capsule, tablet, granule, suspensoid, Emulsion etc.Slow releasing composition and preparation technology thereof that the present invention proposes, carry out coating after not needing to make pastille micropill again, simplified production technology, reduced production cost, is convenient to carry out quality control.
The specific embodiment
Below in conjunction with the embodiment of the present invention, the technical scheme in the present invention is clearly and completely described, obviously, described embodiment is only the present invention's part embodiment, rather than whole embodiment.Embodiment based in the present invention, those of ordinary skills, not making the every other embodiment obtaining under creative work prerequisite, belong to the scope of protection of the invention.
Embodiment 1
A topiramate slow releasing composition, comprises the component of following parts by weight: topiramate 650g, propylene resin 100g, hypromellose 50g, Pulvis Talci 100g, triethyl citrate 10g.
The preparation technology of described topiramate composition is:
(1) by formula ratio, taking 100g propylene resin, to be made into mass fraction be 10% solution, and solvent for use is 70% ethanol;
(2) above-mentioned alcoholic solution adds 50g hypromellose, 100g Pulvis Talci, 10g triethyl citrate to be made into coating solution;
(3) take 650g topiramate and put in powder coating machine, with above-mentioned coating solution, carry out powder coating;
(4) coating complete after 30 ℃ of dry 8h, obtain described topiramate slow releasing composition.
Embodiment 2
A topiramate slow releasing composition, comprises the component of following parts by weight: ethyl cellulose 300g, hydroxyl Macrogol 200 g, magnesium stearate 200g, dibutyl sebacate 30g, topiramate 850g.
The preparation technology of described topiramate composition is:
(1) taking 300g ethyl cellulose, to be made into mass fraction be 30% solution, the ethanol that solvent for use is 90%;
(2) above-mentioned alcoholic solution adds 200g Polyethylene Glycol, 200g magnesium stearate, 30g dibutyl sebacate to be made into coating solution;
(3) take 850g topiramate and put in powder coating machine, with above-mentioned coating solution, carry out powder coating;
(4) coating complete after 50 ℃ of dry 14h, obtain described topiramate slow releasing composition.
Embodiment 3
A topiramate slow releasing composition, comprises the component of following parts by weight: ethyl cellulose 200g, hydroxyl polyvidone 130g, silica 1 50g, triethyl citrate 20g, topiramate 750g.
The preparation technology of described topiramate composition is:
(1) taking 200g propylene resin, to be made into mass fraction be 20% solution, the ethanol that solvent for use is 80%;
(2) above-mentioned alcoholic solution adds 130g polyvidone, 150g silicon dioxide and 20g triethyl citrate to be made into coating solution;
(3) take 750g crude drug and put in powder coating machine, with above-mentioned coating solution, carry out powder coating;
(4) coating complete after 40 ℃ of dry 11h, obtain described topiramate slow releasing composition.
Embodiment 4
A topiramate slow releasing composition, comprises the component of following mass fraction: propylene resin 100g, polyvidone 130g, silica 1 50g, dibutyl sebacate 10g, topiramate 650g.
The preparation technology of described topiramate composition is:
(1) taking propylene resin 100g, to be made into mass fraction be 20% solution, the ethanol that solvent for use is 90%;
(2) above-mentioned alcoholic solution adds hydroxyl polyvidone 130g, silica 1 50g and 10g dibutyl sebacate to be made into coating solution;
(3) take 650g topiramate and put in powder coating machine, with above-mentioned coating solution, carry out powder coating;
(4) coating complete after 50 ℃ of dry 11h, obtain described topiramate slow releasing composition.
Embodiment 5
A topiramate slow releasing composition, comprises the component of following mass fraction: propylene resin 200g, Macrogol 200 g, silica 1 00g, triethyl citrate 20g, topiramate 750g.
The preparation technology of described topiramate composition is:
(1) taking 200g propylene resin, to be made into mass fraction be 10% solution, the ethanol that solvent for use is 80%;
(2) above-mentioned alcoholic solution adds 200g Polyethylene Glycol, 100g silicon dioxide, 20g triethyl citrate to be made into coating solution;
(3) take 750g crude drug and put in powder coating machine, with above-mentioned coating solution, carry out powder coating;
(4) coating complete after 30 ℃ of dry 14h, obtain described topiramate slow releasing composition.
Embodiment 6
A topiramate slow releasing composition, comprises the component of following mass fraction: propylene resin 300g, hypromellose 50g, silicon dioxide 200g, dibutyl sebacate 30g, topiramate 850g.
The preparation technology of described topiramate composition is:
(1) taking 300g propylene resin, to be made into mass fraction be 30% solution, and solvent for use is 70% ethanol;
(2) above-mentioned alcoholic solution adds 50g hypromellose, 200g silicon dioxide and 30g dibutyl sebacate to be made into coating solution;
(3) take 850g topiramate and put in powder coating machine, with above-mentioned coating solution, carry out powder coating;
(4) coating complete after 40 ℃ of dry 8h, obtain described topiramate slow releasing composition.
The topiramate slow releasing composition of above-described embodiment gained can be used for preparing capsule, tablet, granule, suspensoid, Emulsion etc.
In above-described embodiment, slow-release material is replaceable is the propylene resin of equivalent and the mixture of ethyl cellulose, and the ratio of the two is not done requirement; Porogen is replaceable is the mixture of any 2 kinds or 3 kinds in hypromellose, Polyethylene Glycol and the polyvidone of equivalent, and its ratio is not done requirement; Lubricant is replaceable is the mixture of any 2 kinds or 3 kinds of Pulvis Talci, magnesium stearate and the silicon dioxide of equivalent, and its ratio is not done requirement; Plasticizer is replaceable is the triethyl citrate of equivalent and the mixture of dibutyl sebacate, and its ratio is not done requirement.Topiramate slow releasing capsule vitro release of the present invention is investigated
Adopt dissolution test system according to Chinese Pharmacopoeia (2010 editions) release first method, to measure the variation of 6 prepared slow releasing capsule vitro releases of embodiment of the present invention, with commercially available topiramate slow releasing capsule (7) (U.S. Vivus, Inc., specification 46mg/ grain) be contrast, its result is as table 1.
Described in calculating respectively according to table 1, the slow releasing capsule dissolution curve of each embodiment gained and the similar factors of commercially available topiramate slow releasing capsule release curve are followed successively by: 88,83,81,89,92,93.Similar factors is all greater than 50, shows that the prepared Toby's ester of the present invention slow releasing capsule is consistent with the vitro release characteristic of commercially available topiramate slow releasing capsule.
The comparison of table 1 the present invention obtained topiramate slow releasing capsule vitro release and commercially available sample
The variation of blood drug level in vivo of the prepared topiramate slow releasing capsule of the present invention
Respectively with commercially available topiramate slow releasing capsule (U.S. Vivus, specification 46mg/ grain) and topiramate quick-release capsules (U.S. Vivus, Inc. Inc.,, specification 46mg/ grain) be contrast, investigate the variation of blood drug level in vivo of the prepared topiramate slow releasing capsule of the embodiment of the present invention.
Choose at random epileptic 77 people, divide and do 8 groups, every group of each 5 people of men and women, give respectively topiramate slow releasing capsule, commercially available topiramate slow releasing capsule (7) and the commercially available topiramate quick-release capsules (8) of 6 embodiment gained of 50mg the present invention, after taking medicine, gather blood plasma, application high performance liquid chromatography (HPLC) is measured topiramate blood drug level in blood plasma, the results are shown in Table 2.
The variation of blood drug level in the obtained topiramate slow releasing capsule of table 2 the present invention body
As can be seen from Table 2, after the prepared topiramate slow releasing capsule of 6 embodiment of the present invention is taken, its blood drug level is basically identical with commercially available topiramate slow releasing capsule (7) variation characteristic over time, illustrate that the prepared topiramate slow releasing capsule of 6 embodiment of the present invention has slow releasing function, reached the object of controlling drug release rate, stabilised blood concentration.And commercially available topiramate quick-release capsules (8) takes rear 2h blood drug level and rises rapidly, at 4h, reach peak, blood drug level amplitude of variation is larger; And the prepared topiramate slow releasing capsule of 6 embodiment of the present invention is taken blood drug level in rear 24h and is not occurred compared with macrorelief, present variation tendency stably, show that topiramate slow releasing composition of the present invention can effectively control the rate of release of medicine in vivo, make within blood drug level remains on a metastable scope, reached the effect of slow release, controlled release.
The foregoing is only preferred embodiment of the present invention, in order to limit the present invention, within the spirit and principles in the present invention not all, any modification of doing, be equal to replacement, improvement etc., within all should being included in protection scope of the present invention.
Claims (7)
1. a topiramate slow releasing composition, is characterized in that, comprises the component of following parts by weight: topiramate 65-85 part, slow-release material 10-30 part, porogen 5-20 part, lubricant 10-20 part, plasticizer 1-3 part.
2. a kind of topiramate slow releasing composition as claimed in claim 1, is characterized in that: described slow-release material is a kind or 2 kinds of mixing in propylene resin or ethyl cellulose.
3. a kind of topiramate slow releasing composition as claimed in claim 1, is characterized in that: described porogen is a kind or any mixture in hypromellose, Polyethylene Glycol or polyvidone.
4. a kind of topiramate slow releasing composition as claimed in claim 1, is characterized in that: described lubricant is a kind or any mixture in Pulvis Talci, magnesium stearate or silicon dioxide.
5. a kind of topiramate slow releasing composition as claimed in claim 1, is characterized in that: described plasticizer is a kind or 2 kinds of mixing in triethyl citrate or dibutyl sebacate.
6. the technique of a kind of topiramate slow releasing composition of preparation as described in claim 1 to 6 any one, is characterized in that, comprising:
(1) slow-release material is made into by formula ratio the solution that mass fraction is 10-30%, and solvent for use is the ethanol of concentration 70-90%;
(2) add porogen, lubricant and the plasticizer of formula ratio to be made into coating solution;
(3) by formula ratio raw materials weighing medicine medicine, put in powder coating machine, with coating solution, carry out powder coating;
(4) coating complete after 30-50 ℃ of dry 8-14h, obtain described topiramate slow releasing composition.
As claim 6 as described in a kind of preparation technology of topiramate slow releasing composition, it is characterized in that: described topiramate slow releasing composition is for the preparation of capsule, tablet, granule, suspensoid, Emulsion.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105326814A (en) * | 2015-10-09 | 2016-02-17 | 北京万全德众医药生物技术有限公司 | Topiramate sustained release preparation pharmaceutical composition |
| CN107998092A (en) * | 2016-10-28 | 2018-05-08 | 上海宣泰医药科技有限公司 | Medicament slow release unit, Orally disintegrating sustained release tablets comprising the medicament slow release unit and its preparation method and application |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579367A (en) * | 2012-03-23 | 2012-07-18 | 中国人民解放军军事医学科学院毒物药物研究所 | Topiramate sustained-release drug composition, method for preparing same and application of Topiramate sustained-release drug composition |
-
2014
- 2014-06-06 CN CN201410250057.7A patent/CN104069121A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102579367A (en) * | 2012-03-23 | 2012-07-18 | 中国人民解放军军事医学科学院毒物药物研究所 | Topiramate sustained-release drug composition, method for preparing same and application of Topiramate sustained-release drug composition |
Non-Patent Citations (1)
| Title |
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| 徐晨等: "粉末包衣技术在药物制剂领域的应用研究进展", 《药学进展》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105326814A (en) * | 2015-10-09 | 2016-02-17 | 北京万全德众医药生物技术有限公司 | Topiramate sustained release preparation pharmaceutical composition |
| CN107998092A (en) * | 2016-10-28 | 2018-05-08 | 上海宣泰医药科技有限公司 | Medicament slow release unit, Orally disintegrating sustained release tablets comprising the medicament slow release unit and its preparation method and application |
| CN107998092B (en) * | 2016-10-28 | 2021-01-29 | 上海宣泰医药科技股份有限公司 | Drug sustained-release unit, orally disintegrating sustained-release tablet containing drug sustained-release unit, and preparation method and application thereof |
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Effective date of registration: 20151229 Address after: 519000, Zhuhai, Guangdong hi tech Zone, Tang Wan Town, harbour Avenue, science and technology road, No. 10 main building, fifth, 512 units Applicant after: Zhuhai Tianyi Medicine Technology Development Co., Ltd. Applicant after: Zhong Shanwanhan Pharmaceutical Technology Co., Ltd Address before: 519000, Zhuhai, Guangdong hi tech Zone, Tang Wan Town, harbour Avenue, science and technology road, No. 10 main building, fifth, 512 units Applicant before: Zhuhai Tianyi Medicine Technology Development Co., Ltd. |
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Application publication date: 20141001 |