CN102000038A - Vinpocetine dispersible tablet and preparation method thereof - Google Patents

Vinpocetine dispersible tablet and preparation method thereof Download PDF

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Publication number
CN102000038A
CN102000038A CN 201010551167 CN201010551167A CN102000038A CN 102000038 A CN102000038 A CN 102000038A CN 201010551167 CN201010551167 CN 201010551167 CN 201010551167 A CN201010551167 A CN 201010551167A CN 102000038 A CN102000038 A CN 102000038A
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Prior art keywords
vinpocetine
dispersible tablet
parts
essence
cross
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CN 201010551167
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Chinese (zh)
Inventor
高志亮
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HENAN RUNHONG PHARMACEUTICAL CO Ltd
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HENAN RUNHONG PHARMACEUTICAL CO Ltd
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Priority to CN 201010551167 priority Critical patent/CN102000038A/en
Publication of CN102000038A publication Critical patent/CN102000038A/en
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Abstract

The present invention discloses a vinpocetine dispersible tablet and preparation method thereof, wherein the vinpocetine dispersible tablet comprises the following constituents according part by weight: 3-20 parts of vinpocetine, 18-52.5 parts of fillers, 20-58 parts of disintegrating agents, 1.5-4.5 parts of bonds, 10-30 parts of flavouring agents and 0.5-2 parts of lubricants. The vinpocetine dispersible tablet of the present invention has the advantages of fast dispersity, good dissolution, greatly improved flavour, smooth appearance and good compressibility. The vinpocetine dispersible tablet is used for improving the dissolution and dispersity of pharmaceuticals; the preparation method of the present invention adopts a method that vinpocetine and mannitol are crushed together, so to prevent vinpocetine from generating static electricity, as well as to improve the dissolution of vinpocetine.

Description

Vinpocetine dispersible tablet and preparation method thereof
Technical field
The present invention relates to the vinpocetine dispersible tablet, also relate to a kind of preparation method of this dispersible tablet simultaneously.
Background technology
Vinpocetine (Vinpocetine) is a kind of natural drug that obtains from Herba Catharanthi Rosei, belongs to indoles alkaloid, and is fat-soluble strong, is insoluble in water, has selectivity expansion cerebral vessels, initiatively improves pharmacological actions such as glucose metabolism, neuroprotective unit.Vinpocetine is usually used in treating disturbance of cerebral circulation diseases such as cerebral arteriosclerosis, ischemic cerebrovascular, hemorrhagic apoplexy sequela, transient ischemic attack, is used for the treatment of symptom that circulatory disturbance brings out etc.In addition, vinpocetine also is used for the treatment of acute and chronic ophthalmic diseases, the sensory nerve hearing impairment that multiple reason causes.
Vinpocetine is succeeded in developing by Hungary Gedeon Richter company at first, and the chemosynthesis process is open.The vinpocetine conventional tablet of present listing, 5 parts of specifications, now existing Duo Jia pharmaceutical factory produces.But because puckery, bitter, the common tablet taste bad will of vinpocetine, dispersion is bad; Vinpocetine plays static easily when pulverizing, and is the slightly water-soluble chemical compound, and dissolution is poor.
Summary of the invention
The object of the present invention is to provide a kind of vinpocetine dispersible tablet.
A kind of vinpocetine dispersible tablet comprises the component of following weight portion: vinpocetine 3-20 part, filler 18-52.5 part, disintegrating agent 20-58 part, binding agent 1.5-4.5 part, correctives 10-30 part, lubricant 0.5-2 part.
Filler is conventional medicinal filler lactose, pregelatinized Starch, dextrin, microcrystalline Cellulose, medical cane sugar, medicinal fructose, preferably microcrystalline cellulose.
The kind of disintegrating agent and consumption are most important to disintegrate, the result of extraction of dispersible tablet, and disintegrating agent commonly used has crospolyvinylpyrrolidone, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, Sodium Hydroxymethyl Stalcs, hyprolose etc.The present invention designs different prescriptions, one or more in the preferred polyvinylpolypyrrolidone of process test of many times, cross-linking sodium carboxymethyl cellulose, the hyprolose.
Binding agent be in polyvidone, hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose, methylcellulose, the starch slurry any or several, preferred hydroxypropyl emthylcellulose.
Lubricant is Pulvis Talci, magnesium stearate, micropowder silica gel, polyethylene glycols etc., preferred magnesium stearate.
Correctives is selected from Aspartane, mannitol, citric acid, Herba Menthae essence, flavoring banana essence, green apple essence, strawberry essence, orange flavor, one or any several combination in preferably citric acid, mannitol, Aspartane, the Herba Menthae essence.
In order to improve the stripping of medicine, can also add surfactant such as sodium lauryl sulphate etc.In addition, the vinpocetine dispersible tablet can also comprise other suitable adjuvant or additives.
Another object of the present invention provides a kind of preparation method of vinpocetine dispersible tablet.
Be used to improve drug dissolution, dispersibility, the preparation method that the present invention determines has adopted the method for pulverizing altogether with mannitol when pulverizing.Avoid vinpocetine to play static on the one hand, can improve the stripping of vinpocetine on the other hand.In the Recipe screening process, find in addition, add hyprolose after granulation is finished and not only can accelerate disintegrate, also can improve the compressibility of tablet, increase the hardness of tablet, therefore adopt the mode that adds hyprolose after granulating.Concrete steps are:
(1) with vinpocetine and mannitol mix homogeneously, pulverize, cross 100 mesh sieves, standby, get the material I;
(2) get polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, Aspartane, hyprolose, essence, lubricant and cross 60 mesh sieves respectively, standby; Filler, citric acid are crossed 80 mesh sieves respectively, and be standby;
(3) with material I and filler, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, citric acid, Aspartane, place mixer, mix homogeneously, the material II;
(4) take by weighing binding agent, add in a certain amount of water, fully stirring and dissolving;
(5) the material II is added binding agent, granulate;
(6) wet granular places air dry oven or ebullated dryer drying;
(7) behind the particle drying with 24 mesh sieve granulate;
(8) dried granule is placed mixer, after adding adds hyprolose, essence mix homogeneously, add lubricant at last, mix homogeneously;
(9) measure granule content, determine that sheet is heavy, tabletting.
The specific embodiment
The present invention is further elaborated by following examples, but the present invention is not limited to this.
Embodiment 1
The vinpocetine dispersible tablet of present embodiment comprises the component of following parts by weight: 5 parts of vinpocetines, 33 parts of pregelatinized Starch, 20 parts of polyvinylpolypyrrolidone, 22 parts of cross-linking sodium carboxymethyl celluloses, 9 parts of citric acid, 9 parts in mannitol, 6 parts of Aspartane, 4 parts of methylcellulose, 8 parts of hyprolose, 3 parts of Fructus Citri Limoniae essence, 1 part of magnesium stearate.
Prepare according to following step:
(1) vinpocetine and mannitol is even by the mixed in the prescription, pulverize, cross 100 mesh sieves, standby, get the material I;
(2) polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, Aspartane, hyprolose, Fructus Citri Limoniae essence, the magnesium stearate of getting in the prescription crossed 60 mesh sieves respectively, and be standby; Pregelatinized Starch, citric acid are crossed 80 mesh sieves respectively, and be standby;
(3) with pregelatinized Starch, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, citric acid, the Aspartane of material I and formula ratio, place wet mixing pelletizer, mix homogeneously gets the material II;
(4) take by weighing the methylcellulose of formula ratio, add in the entry, abundant stirring and dissolving is as binding agent;
(5) open wet mixing pelletizer, add binding agent, granulate;
(6) wet granular places air dry oven or ebullated dryer drying;
(7) behind the particle drying with 24 mesh sieve granulate;
(8) dried granule is placed mixer, behind the hyprolose of adding formula ratio, the Fructus Citri Limoniae essence mix homogeneously, add magnesium stearate at last, mix homogeneously;
(9) measure granule content, determine that sheet is heavy, with the stamping of diameter Ф 7mm scrobicula.
Embodiment 2
The vinpocetine dispersible tablet of present embodiment comprises the component of following parts by weight: 5 parts of vinpocetines, 28 parts of microcrystalline Cellulose, 20 parts of polyvinylpolypyrrolidone, 26 parts of cross-linking sodium carboxymethyl celluloses, 10 parts of citric acid, 8 parts in mannitol, 6 parts of Aspartane, 3 parts of hydroxypropyl emthylcelluloses, 9 parts of hyprolose, 3 parts in Herba Menthae essence, 2 parts of magnesium stearate.
Prepare according to following step:
(1) vinpocetine and mannitol is even by the mixed in the prescription, pulverize, cross 100 mesh sieves, standby, get the material I;
(2) polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, Aspartane, hyprolose, Herba Menthae essence, the magnesium stearate of getting in the prescription crossed 60 mesh sieves respectively, and be standby; Microcrystalline Cellulose, citric acid are crossed 80 mesh sieves respectively, and be standby;
(3) with microcrystalline Cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, citric acid, the Aspartane of material I and formula ratio, place wet mixing pelletizer, mix homogeneously gets the material II;
(4) take by weighing the hydroxypropyl emthylcellulose of formula ratio, add in the entry, abundant stirring and dissolving is as binding agent;
(5) open wet mixing pelletizer, add binding agent, granulate;
(6) wet granular places air dry oven or ebullated dryer drying;
(7) behind the particle drying with 24 mesh sieve granulate;
(8) dried granule is placed mixer, behind the hyprolose of adding formula ratio, the Herba Menthae essence mix homogeneously, add magnesium stearate at last, mix homogeneously;
(9) measure granule content, determine that sheet is heavy, with the stamping of diameter Ф 7mm scrobicula.
Embodiment 3
The vinpocetine dispersible tablet of present embodiment comprises the component of following parts by weight: 5 parts of vinpocetines, 25 parts of lactose, 15 parts of polyvinylpolypyrrolidone, 30 parts of cross-linking sodium carboxymethyl celluloses, 10 parts of citric acid, 8 parts in mannitol, 8 parts of Aspartane, 3.5 parts of hydroxypropyl emthylcelluloses, 12 parts of hyprolose, 2.5 parts of strawberry essences, 1 part of Pulvis Talci.
Prepare according to following step:
(1) vinpocetine and mannitol is even by the mixed in the prescription, pulverize, cross 100 mesh sieves, standby, get the material I;
(2) polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, Aspartane, hyprolose, strawberry essence, the Pulvis Talci of getting in the prescription crossed 60 mesh sieves respectively, and be standby; Lactose, citric acid are crossed 80 mesh sieves respectively, and be standby;
(3) with lactose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, citric acid, the Aspartane of material I and formula ratio, place wet mixing pelletizer, mix homogeneously gets the material II;
(4) take by weighing the hydroxypropyl emthylcellulose of formula ratio, add in the entry, abundant stirring and dissolving is as binding agent;
(5) open wet mixing pelletizer, add binding agent, granulate;
(6) wet granular places air dry oven or ebullated dryer drying;
(7) behind the particle drying with 24 mesh sieve granulate;
(8) dried granule is placed mixer, behind the hyprolose of adding formula ratio, the strawberry essence mix homogeneously, add Pulvis Talci at last, mix homogeneously;
(9) measure granule content, determine that sheet is heavy, with the stamping of diameter Ф 7mm scrobicula.
Embodiment 4
The vinpocetine dispersible tablet of present embodiment comprises the component of following parts by weight: 5 parts of vinpocetines, 26 parts of microcrystalline Cellulose, 21 parts of polyvinylpolypyrrolidone, 28 parts of cross-linking sodium carboxymethyl celluloses, 13 parts of citric acid, 11 parts in mannitol, 4 parts of Aspartane, 1.5 parts of sodium carboxymethyl cellulose, 7 parts of hyprolose, 2 parts in green apple essence, 1.5 parts of micropowder silica gels.
Prepare according to following step:
(1) vinpocetine and mannitol is even by the mixed in the prescription, pulverize, cross 100 mesh sieves, standby, get the material I;
(2) 60 mesh sieves are crossed in polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, Aspartane, hyprolose, green apple essence, the micropowder silica gel of getting in the prescription respectively, and are standby; Microcrystalline Cellulose, citric acid are crossed 80 mesh sieves respectively, and be standby;
(3) with microcrystalline Cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, citric acid, the Aspartane of material I and formula ratio, place wet mixing pelletizer, mix homogeneously gets the material II;
(4) take by weighing the sodium carboxymethyl cellulose of formula ratio, add in the entry, abundant stirring and dissolving is as binding agent;
(5) open wet mixing pelletizer, add binding agent, granulate;
(6) wet granular places air dry oven or ebullated dryer drying;
(7) behind the particle drying with 24 mesh sieve granulate;
(8) dried granule is placed mixer, behind the hyprolose of adding formula ratio, the green apple essence mix homogeneously, add micropowder silica gel at last, mix homogeneously;
(9) measure granule content, determine that sheet is heavy, with the stamping of diameter Ф 7mm scrobicula.

Claims (9)

1. a vinpocetine dispersible tablet is characterized in that, it comprises the component of following weight portion: vinpocetine 3-20 part, filler 18-52.5 part, disintegrating agent 20-58 part, binding agent 1.5-4.5 part, correctives 10-30 part, lubricant 0.5-2 part.
2. according to the vinpocetine dispersible tablet described in the claim 1, it is characterized in that described disintegrating agent is a polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, a kind of or several combination arbitrarily in the hydroxypropyl cellulose.
3. according to the vinpocetine dispersible tablet described in the claim 2, it is characterized in that described disintegrating agent is a polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, the combination of hyprolose.
4. according to the vinpocetine dispersible tablet described in the claim 1, it is characterized in that, described correctives is an Aspartane, mannitol, a kind of or several combination arbitrarily in citric acid, Herba Menthae essence, flavoring banana essence, orange flavor, strawberry essence, the green apple essence.
5. according to the vinpocetine dispersible tablet described in the claim 4, it is characterized in that described correctives is an Aspartane, mannitol, the combination of citric acid, Herba Menthae essence.
6. according to the vinpocetine dispersible tablet described in the claim 1, it is characterized in that described filler is selected from a kind of or several combination arbitrarily in lactose, pregelatinized Starch, dextrin, microcrystalline Cellulose, medical cane sugar, the medicinal fructose.
7. according to the vinpocetine dispersible tablet described in the claim 1, it is characterized in that described binding agent is selected from a kind of or several combination arbitrarily in polyvidone, hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose, methylcellulose, the starch slurry.
8. according to the vinpocetine dispersible tablet described in the claim 1, it is characterized in that described lubricant is selected from a kind of or several combination arbitrarily of magnesium stearate, Pulvis Talci, micropowder silica gel, Polyethylene Glycol apoplexy due to endogenous wind.
9. the preparation method of a vinpocetine dispersible tablet is characterized in that, comprises following steps:
(1) with vinpocetine and mannitol mix homogeneously, pulverize, cross 100 mesh sieves, get the material I, standby;
(2) get polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, Aspartane, hyprolose, essence, lubricant and cross 60 mesh sieves respectively, standby; Filler, citric acid are crossed 80 mesh sieves respectively, and be standby;
(3) with material I and filler, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, citric acid, Aspartane, place the mixer-granulator mix homogeneously, the material II;
(4) take by weighing binding agent, add in the entry and dissolve;
(5) the material II adds binding agent, granulates, and is dry back with 24 mesh sieve granulate;
(6) dried granule is placed mixer, after adding adds hyprolose, essence mix homogeneously, add lubricant at last, mix homogeneously;
(7) measure granule content, determine that sheet is heavy, tabletting.
CN 201010551167 2010-11-19 2010-11-19 Vinpocetine dispersible tablet and preparation method thereof Pending CN102000038A (en)

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Application Number Priority Date Filing Date Title
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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1060024A (en) * 1991-10-31 1992-04-08 东北制药总厂 The preparation method of apovincamine acid ethyl ester

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1060024A (en) * 1991-10-31 1992-04-08 东北制药总厂 The preparation method of apovincamine acid ethyl ester

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
《中华医药杂志》 20060131 唐开智等 长春西汀分散片溶出度测定 第82-83页 1-9 第6卷, 第1期 2 *

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Application publication date: 20110406