CN104546782A - Lipoate enteric-coated micro-pill preparation and preparation method thereof - Google Patents
Lipoate enteric-coated micro-pill preparation and preparation method thereof Download PDFInfo
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- CN104546782A CN104546782A CN201410596121.7A CN201410596121A CN104546782A CN 104546782 A CN104546782 A CN 104546782A CN 201410596121 A CN201410596121 A CN 201410596121A CN 104546782 A CN104546782 A CN 104546782A
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Abstract
The invention relates to the field of pharmaceutical preparations, and particularly relates to a lipoate preparation and a preparation method thereof. A lipoate enteric-coated micro-pill preparation disclosed by the invention is prepared into various dosage forms from enteric-coated micro-pills, and the preparation is characterized in that each enteric-coated micro-pill contains a pharmacologically active pill core, an isolated coating layer and an enteric coating layer. Due to the adoption of unique auxiliary material and a unique preparation process, in the process of taking the preparation disclosed by the invention, a series of disadvantages such as stimulation to upper respiratory tracts and stomachs existing in original dosage forms of lipoic acids are overcome; and in the process of preparing, no shortcoming such as sticking exists.
Description
Technical field
The present invention relates to field of medicine preparations, particularly relate to a kind of thioctic acid enteric coated pellets formulation and preparation method thereof.
Background technology
Thioctic acid (alpha lipoic acid) is that one is present in mitochondrial enzyme, and similar vitamin, can eliminate acceleration
The aging free radical with causing a disease.Thioctic acid enters cell in vivo after intestinal absorption, has fat-soluble and water miscible characteristic concurrently, therefore can go everywhere without any hindrance here at whole body, arrive any one cell area, provides human body comprehensive usefulness, is the fat-soluble and water miscible universal antioxidant of tool.
Thioctic acid is mainly used in the removing toxic substances etc. of hepatic insufficiency, subacute necrotizing encephalopathy and heavy metal poisoning as traditional drug; In Europe, thioctic acid injection is uniquely identified and the medicine of the multiple Micro-circutation syndrome for the treatment of diabetes that gone on the market; U.S. FDA goes on the market in approval thioctic acid in 1997 as health food; Thioctic acid is classified as food additive in 2004 by Japan, can be used as health product application.In China, in November, 2009, national new edition medical insurance catalogue has included α ?thioctic acid injection first for regulating blood glucose medical insurance Class B medicine.
Current thioctic acid oral dosage form mainly contains tablet and capsule.Thioctic acid fusing point is 60 ~ 62 DEG C, after it mixes with adjuvant, easily forms eutectic phenomenon, causes being difficult to batch production in tableting processes or capsule filling process because of sticking.Meanwhile, due to the distinctive physicochemical property of thioctic acid, make patient take the rear side effect occurring upper respiratory tract, gastrointestinal stimulation, this side effect is painful for patient, causes this medicine clinical compliance undesirable.
Present invention employs unique adjuvant and preparation technology, make the present invention take in process the series of malpractice overcoming the original dosage form of thioctic acid and exist, as to upper respiratory tract, gastrointestinal stimulation etc.; There is not the shortcomings such as sticking in preparation process simultaneously.
Summary of the invention
The object of the present invention is to provide a kind of good patient compliance to be applicable to the thioctic acid pellet preparations of suitability for industrialized production simultaneously.
Another object of the present invention is to the preparation method that a kind of thioctic acid pellet preparations is provided.
The present invention is by after thioctic acid and the wiring solution-forming such as binding agent, solubilizing agent, adopts fluid bed, above-mentioned solution is sprayed onto celphere surface, forms pharmaceutically active ball core; Then carry out sealing coat coating to containing pill core, finally enteric layer coating is carried out to ball core obtained above.
For solving Problems existing in background technology, the present invention adopts following technical scheme:
A kind of thioctic acid enteric coated pellets formulation, described pellet preparations is the various dosage forms be prepared from by micropill, and described micropill is enteric coated micropill, and this micropill is made up of the active ball core of drug containing, isolation coat layer and enteric coat layer.
The active ball core of described drug containing comprises thioctic acid, celphere, binding agent, solubilizing agent.
One or more mixing in the cane sugar type celphere of described celphere to be diameter be 0.8 ~ 1.2mm, silicon dioxide celphere, microcrystalline Cellulose celphere.
Described binding agent is hypromellose K100 LV; Described solubilizing agent is tween 80.
Enteric coating material in described enteric coat layer is polyacrylic resin
, polyacrylic resin
, Methacrylic Acid Copolymer Type A, Methacrylic Acid Copolymer Type B, one or more mixing in Lac.
Plasticizer in described enteric coat layer is one or more mixing in triethyl citrate, diethyl phthalate, SA dibutyl ester.
Described pellet preparations can be prepared into capsule, tablet or granule.
The invention also discloses a kind of preparation method of thioctic acid enteric coated pellets formulation, described preparation method comprises:
getting 0.8 ~ 1.2mm celphere puts in multi-functional granulating coated machine, by thioctic acid, binding agent, solubilizing agent and water wiring solution-forming, this solution side is sprayed medicine, prepares pharmaceutically active ball core.It is dry that side spray medicine-feeding terminates top spray, stops dry, take out during pharmaceutically active ball core moisture 4 ~ 6%.
the above-mentioned ball core prepared is put in multi-functional granulating coated machine, sprays coating with at the bottom of isolation coat liquid, stop during weightening finish 8% ~ 16%.Test
After to filter out suitable micropill for subsequent use.
the ball core prepared is placed in multi-functional granulating coated machine, sprays coating with at the bottom of enteric coat layer, stop during weightening finish 20% ~ 40%.
gained micropill is prepared into various preparation.
Due to the distinctive technique of the present invention and prescription, make its release Mechanisms become multilamellar semipermeable membrane coated systems, micropill of the present invention is not dissolved at gastric, thus stimulation can not be caused to upper respiratory tract and stomach, and ensure the sustained release of medicine in intestinal.
Detailed description of the invention
Below in conjunction with embodiment, the present invention will be further described.
Embodiment 1: the present embodiment is prepared 1000g thioctic acid enteric coated micropill and adopted following formula:
Thioctic acid 150g, microcrystalline Cellulose ball core 500g, hypromellose K100LV 20g, tween 80 15g, 295F type Opadry coating powder 90g, enteric coating material 225g.(polyacrylic resin
200g, triethyl citrate 20g, Pulvis Talci 5g)
Preparation technology: take 30g hypromellose K100 LV, 15g tween 80 and be dissolved in water, add 150g thioctic acid, 40 DEG C of stirring in water bath are to dissolving completely, and after filtering with 80 eye mesh screens, obtained solution is for subsequent use; Get 0.8 ~ 1.2mm microcrystalline Cellulose ball core to put in multi-functional granulating coated machine, spray medicine by above-mentioned solution side, prepare plain ball.Multi-functional granulating coated machine parameter: rotary speed 150 ~ 300rpm, inlet temperature 45 ~ 55 DEG C, temperature of charge 25 ~ 32 DEG C, air-introduced machine frequency 15 ~ 25Hz, feed flow rotating speed 5 ~ 25rpm, sprays 0. 10 ~ 0.25Mpa; Plain ball moisture is controlled 5 ~ 15% in preparation process.It is dry that side spray medicine-feeding terminates top spray, stops dry, take out during plain ball moisture 4 ~ 6%.Top spray drying parameter: inlet temperature 50-55 DEG C, air-introduced machine frequency 15-25Hz, filters out 40 ~ 60 order number element balls, for subsequent use.
Bag contagion gown: take 80g 295 type Opadry coating powder and be dispersed in suitable quantity of water, the above-mentioned plain ball prepared is put in multi-functional granulating coated machine, sprays coating the end of with.Multi-functional granulating coated machine parameter: inlet temperature 40 ~ 55 DEG C, temperature of charge 26 ~ 32 DEG C, air-introduced machine frequency 8 ~ 20Hz, feed flow rotating speed 5 ~ 25rpm, sprays 0.14 ~ 0.25Mpa.30 ~ 50 order number micropills are filtered out after test.
Enteric coated: by polyacrylic resin
, triethyl citrate, Pulvis Talci be proportionally made into the enteric coating powder of 225g, it is dissolved by ethanol in proper amount, the above-mentioned micropill ball prepared is put in multi-functional granulating coated machine, sprays coating the end of with.Multi-functional granulating coated machine parameter: inlet temperature 40 ~ 55 DEG C, temperature of charge 27 ~ 32 DEG C, air-introduced machine frequency 10 ~ 18Hz, feed flow rotating speed 3 ~ 15rpm, sprays 0.16 ~ 0.28Mpa.
The micropill obtained is overlapped the thioctic acid enteric coated capsule of capsule shells.
Embodiment 2: the present embodiment provides a kind of thioctic acid micro-pill type tablet, is obtained by thioctic acid enteric coated micropill tabletting.
The preparation of micropill is identical with embodiment 1, and adds 7% polyvinylpolypyrrolidone, 25% microcrystalline Cellulose, and 40% lactose and 1.2% magnesium stearate tabletting obtain.
Embodiment 3: the present embodiment is prepared 1000g thioctic acid enteric coated micropill and adopted following formula:
Thioctic acid 45g, microcrystalline Cellulose ball core 300g, sucrose ball core 300g, hypromellose K100LV 10g, tween 80 15g, 295F type Opadry coating powder 55g, enteric coating material 275g(Methacrylic Acid Copolymer Type B 244g, diethyl phthalate 24.4g, Pulvis Talci 6.6g)
Preparation technology is identical with embodiment 1.The micropill obtained is prepared into granule.
Embodiment 4: the present embodiment is prepared 1000g thioctic acid enteric coated micropill and adopted following formula:
Thioctic acid 240g, silicon dioxide ball core 400g, hypromellose K100LV 64g, tween 80 14g, 295F type Opadry coating powder 114g, enteric coating material 168g(Lac 150g, diethyl phthalate 10g, SA dibutyl ester 5g, Pulvis Talci 3g)
Preparation technology is identical with embodiment 1.The micropill obtained is prepared into capsule.
Claims (5)
1. a thioctic acid enteric coated pellets formulation, described enteric coated pellets formulation is prepared into various dosage form by enteric coated micropill, it is characterized in that enteric coated micropill comprises pharmaceutically active ball core, isolation coat layer and enteric coat layer;
The composition weight proportion of its pharmaceutical active ball core is:
Thioctic acid 15 ~ 30 parts
Celphere 50 ~ 200 parts
Binding agent 2 ~ 8 parts
Solubilizing agent 0.5 ~ 5 part
Wherein isolation coat layer is prepared from by isolation coat powder, and wherein, contagion gown layer increases weight as 8% ~ 16% with pharmaceutically active ball core weighing scale;
Wherein enteric coat layer increases weight as 20% ~ 40% with ball core weighing scale after bag contagion gown; The weight proportion of its composition is:
Enteric coating material, 8 parts,
Plasticizer, 0.8 part,
Pulvis Talci 0.2 part,
Described thioctic acid pellet preparations adopts following preparation method to obtain:
getting 0.8 ~ 1.2mm celphere puts in multi-functional granulating coated machine, by thioctic acid, binding agent, solubilizing agent and water wiring solution-forming, this solution side is sprayed medicine, prepares plain ball; It is dry that side spray medicine-feeding terminates top spray, stops dry, take out during plain ball moisture 4 ~ 6%;
the above-mentioned ball core prepared is put in multi-functional granulating coated machine, sprays coating with at the bottom of isolation coat liquid, stop during weightening finish 8% ~ 16%; Suitable micropill is filtered out for subsequent use after test;
the ball core prepared is placed in multi-functional granulating coated machine, sprays coating with at the bottom of enteric coat layer, stop during weightening finish 20% ~ 40%;
gained micropill is prepared into various preparation.
2. thioctic acid enteric coated pellets formulation according to claim 1, wherein, one or more mixing in the cane sugar type celphere of described celphere to be diameter be 0.8 ~ 1.2mm, silicon dioxide celphere, microcrystalline Cellulose celphere.
3. thioctic acid enteric coated pellets formulation according to claim 1, wherein, described binding agent is hypromellose K100 LV; Described solubilizing agent is tween 80, and described isolation coat powder is 295F type Opadry coating powder.
4. thioctic acid enteric coated pellets formulation according to claim 1, wherein, the enteric coating material in enteric coat layer is polyacrylic resin
, polyacrylic resin
, Methacrylic Acid Copolymer Type A, Methacrylic Acid Copolymer Type B, one or more mixing in Lac; Plasticizer is one or more mixing in triethyl citrate, diethyl phthalate, SA dibutyl ester.
5. a kind of thioctic acid enteric coated pellets formulation according to claim 1, is characterized in that described pellet preparations is prepared into capsule, tablet or granule.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410596121.7A CN104546782A (en) | 2014-10-30 | 2014-10-30 | Lipoate enteric-coated micro-pill preparation and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410596121.7A CN104546782A (en) | 2014-10-30 | 2014-10-30 | Lipoate enteric-coated micro-pill preparation and preparation method thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105687142A (en) * | 2016-03-15 | 2016-06-22 | 重庆康刻尔制药有限公司 | Lipoic acid capsule and preparation method thereof |
| EP3366291A1 (en) | 2017-02-22 | 2018-08-29 | Montero Gida Sanayi Ve Ticaret A.S. | Solid oral pharmaceutical compositions comprising alpha lipoic acid and water-soluble vitamins |
| EP3970722A1 (en) | 2020-09-21 | 2022-03-23 | Sanovel Ilac Sanayi ve Ticaret A.S. | A pharmaceutical bilayer tablet comprising alpha lipoic acid and at least one b vitamin |
| EP4061369A4 (en) * | 2019-11-19 | 2024-04-10 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | A pharmaceutical form comprising acidic substance |
-
2014
- 2014-10-30 CN CN201410596121.7A patent/CN104546782A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105687142A (en) * | 2016-03-15 | 2016-06-22 | 重庆康刻尔制药有限公司 | Lipoic acid capsule and preparation method thereof |
| CN105687142B (en) * | 2016-03-15 | 2019-03-22 | 重庆康刻尔制药有限公司 | A kind of lipoic acid capsule and preparation method thereof |
| EP3366291A1 (en) | 2017-02-22 | 2018-08-29 | Montero Gida Sanayi Ve Ticaret A.S. | Solid oral pharmaceutical compositions comprising alpha lipoic acid and water-soluble vitamins |
| WO2018153914A1 (en) | 2017-02-22 | 2018-08-30 | Montero Gida Sanayi Ve Ticaret A.S. | Solid oral pharmaceutical compositions comprising alpha lipoic acid and water-soluble vitamins |
| EP4061369A4 (en) * | 2019-11-19 | 2024-04-10 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | A pharmaceutical form comprising acidic substance |
| EP3970722A1 (en) | 2020-09-21 | 2022-03-23 | Sanovel Ilac Sanayi ve Ticaret A.S. | A pharmaceutical bilayer tablet comprising alpha lipoic acid and at least one b vitamin |
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Application publication date: 20150429 |