CN106539765A - A kind of Abiraterone Acetate Tablets and preparation method thereof - Google Patents
A kind of Abiraterone Acetate Tablets and preparation method thereof Download PDFInfo
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- CN106539765A CN106539765A CN201510596145.7A CN201510596145A CN106539765A CN 106539765 A CN106539765 A CN 106539765A CN 201510596145 A CN201510596145 A CN 201510596145A CN 106539765 A CN106539765 A CN 106539765A
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- abiraterone acetate
- solid dispersion
- copolyvidone
- weight portion
- abiraterone
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Abstract
The invention discloses a kind of Abiraterone Acetate Tablets and preparation method thereof, the tablet is made up of Abiraterone acetate solid dispersion and pharmaceutic adjuvant, and wherein Abiraterone acetate solid dispersion is obtained by Abiraterone acetate and Copolyvidone.On the one hand Abiraterone Acetate Tablets of the present invention can reduce medicine irritation, improve patient's Compliance, improve absorption rate, make medicine be preferably extensive patients service；On the other hand Abiraterone Acetate Tablets are caused safely and effectively, it is quality controllable.
Description
Technical field
The present invention relates to pharmaceutical technology field, and in particular to a kind of Abiraterone Acetate Tablets and preparation method thereof.
Background technology
Abiraterone acetate, Abiraterone
Acetate, chemical name：（3β）-17-（3- pyridines）Androstane -5,16- diene -3- base acetates, are a kind of oral 17 α-hydroxylase/C17,20- lyase inhibitors, androgen levels are reduced by suppressing the key enzyme-CYP450c17 in androgen synthesis, and the androgen to testis and other positions of body has inhibitory action.
201210451393.9 disclose a kind of stable Abiraterone acetate oral solid drug composition, and said composition includes Abiraterone acetate, citrate and pharmaceutic adjuvant, overcome the degradation problem during Abiraterone acetate storage.
201280045417 disclose solid dispersion composition, improve dissolubility and dissolution rate.
201310099497 disclose a kind of stable Abiraterone Acetate Tablets agent, and which does not contain micropowder silica gel, obtained tablet have stable, preparation process is simple, it is controllable the characteristics of.
By the research to prior art, it has been found that a kind of new Abiraterone acetate pharmaceutical composition, said composition can preferably improve the dissolubility and dissolution rate of Abiraterone acetate,, and safely and effectively, quality controllable requirement, preparation technology is easy and efficient, and product yield is high.
The content of the invention
Present invention is primarily targeted at providing a kind of new Abiraterone Acetate Tablets agent.
The purpose of the present invention is achieved in the following ways：
A kind of Abiraterone Acetate Tablets, is characterized in that the tablet includes Abiraterone acetate solid dispersion and pharmaceutic adjuvant, and wherein Abiraterone acetate solid dispersion is made up of Abiraterone acetate and Copolyvidone.
Wherein in Abiraterone acetate solid dispersion, the weight ratio of Abiraterone acetate and Copolyvidone is 1: 2-3, preferably 1:2.
The tablet contains 30～60 weight portion of Abiraterone acetate solid dispersion, 10～30 weight portion of diluent, 0.5～2 weight portion of 3～10 weight portion of disintegrating agent and lubricant.
Described diluent is mixed with any ratio for one or more in Mannitol, Microcrystalline Cellulose and Lactose, and preferred diluent is Lactose, Microcrystalline Cellulose.Described disintegrating agent is that one or more of copolymerzation with cross-linking dimension ketone, hydroxypropylcellulose and Croscarmellose Sodium are mixed with any ratio.Described lubricant is magnesium stearate, one or two in silicon dioxide with any than mixing.
Preferably following components composition of the invention：Abiraterone acetate solid dispersion 30-50 weight portions, 10 weight portion of Microcrystalline Cellulose, 10 weight portion of Lactose, 3～5 weight portion of disintegrating agent, 0.5～2 weight portion of lubricant, wherein, Abiraterone acetate solid dispersion is made up of Abiraterone acetate and Copolyvidone, and weight ratio is 1: 2.
The preparation method of above-mentioned Abiraterone Acetate Tablets specifically includes following steps：
The preparation of a, Abiraterone acetate solid dispersion：Abiraterone acetate, Copolyvidone are taken for 1: 2-3 by weight, Copolyvidone is completely dissolved, 80 DEG C are heated to while stirring, Abiraterone acetate is added, is stirred to after being completely dissolved, continue to stir and be cooled to 0～-10 DEG C, 15～20 hours are placed into crisp shape breakable object, crush, cross 60～80 mesh sieves, obtain Abiraterone acetate solid dispersion；B, 10～30 weight portion of diluent, 0.5～2 weight portion of 3～10 weight portion of disintegrating agent and lubricant are weighed, mixed homogeneously with 10～20 parts by weight acetic acid abiraterone solid dispersion；
The direct powder compression of c, mix homogeneously, obtains final product Abiraterone Acetate Tablets.
In said method, the weight ratio preferably 1: 2 of Abiraterone acetate and Copolyvidone in Abiraterone acetate solid dispersion.
Above-mentioned Copolyvidone is applied in product of the present invention, it is possible to decrease zest, increase dissolution rate.Percentage composition of the present invention is weight percentage, and material therefor is commercially available.
Abiraterone acetate is made into solid dispersion in technical solution of the present invention, on the one hand single dose Abiraterone acetate and diluent, correctivess, disintegrating agent and mix lubricant instead of with solid dispersion system, make it easy to mix homogeneously, when avoiding tabletting, caused product content is unstable by wall absorption for Abiraterone acetate, while so that direct compression efficiently, easy is achieved.
And, when Abiraterone acetate-Copolyvidone solid dispersion is cooled down rapidly upon dissolution, as during low temperature, dielectric viscosity is very big, hardening time short, it is extremely difficult that medicine forms core crystalline substance, therefore solute Abiraterone acetate ultimately forms amorphous state so that the dissolution rate of medicine is greatly improved than ordinary tablet, absorb quick and complete in the gastrointestinal tract, being capable of quick acting, it is ensured that the curative effect of medicine.
Just in the thinking and solid dispersion system of the present invention, substance classes and consumption grope process below, are briefly described.
The screening test of substance classes has been carried out first, 5 kinds of high molecular polymers be have selected through primary dcreening operation,, succinic acid hydroxypropylmethylcellulose acetate methylcellulose, Polyethylene Glycol, Copolyvidone, ethyl cellulose, polyvinyl alcohol, according to the solid dispersion preparation process of embodiment 2, by its respectively with Abiraterone acetate and be prepared into solid dispersion, investigate dynamic viscosity（m㎡/s）, and solid dispersion pulverize and sieve after (60 mesh sieve) heap density（g/mL）, angle of repose（°）Deng the key parameter related to direct compression technique.Experimental result summary is shown in Table 1.
Substance classes screening (the unit of 1 solid dispersion of table：Weight portion)
As a result such as following table：
By above-mentioned experiment, it is optimal carrier preferably to go out Copolyvidone.Solid dispersion viscosity degradation made by Copolyvidone, heap appropriate density, angle of repose is added to be less than 30 °, powder flowbility is good.The optimal combination ingredient of consumption and this case below to Copolyvidone, manufactures experimently multiple schemes.
The consumption the selection result of Copolyvidone（Unit：Weight portion）
In sum, the consumption of Copolyvidone could obtain optimal effect only in the case where consumption is moderate（Scheme 1）.
Specific embodiment：
By the embodiment of invention now given below, present disclosure is expanded on further, but the present invention is not limited by embodiment.
Embodiment 1 (formulation and technology of solid dispersion technology is not used)
Prescription (weight portion)：
Abiraterone acetate 10
Copolyvidone 20
Lactose 10
Microcrystalline Cellulose 10
Croscarmellose Sodium 5
0.8 preparation technology of magnesium stearate：
1) Abiraterone acetate, Copolyvidone, Lactose, Microcrystalline Cellulose, Croscarmellose Sodium and the magnesium stearate of recipe quantity, are weighed, is sieved, mix homogeneously；
2), tabletting, obtains final product Abiraterone Acetate Tablets.
Embodiment 2
Prescription (weight portion)：
Abiraterone acetate 10
Copolyvidone 20
Lactose 10
Microcrystalline Cellulose 20
Croscarmellose Sodium 5
0.8 preparation technology of magnesium stearate：
1）, Abiraterone acetate solid dispersion preparation：Abiraterone acetate, Copolyvidone are taken for 1: 2 by weight, Copolyvidone is completely dissolved, 80 DEG C are heated to while stirring, Abiraterone acetate is added, is stirred to after being completely dissolved, continue to stir and be cooled to 0～-10 DEG C, 15 hours are placed into crisp shape breakable object, crush, cross 60～80 mesh sieves, obtain Abiraterone acetate solid dispersion；2) Microcrystalline Cellulose, Lactose, Croscarmellose Sodium and the magnesium stearate of recipe quantity, are weighed, is mixed homogeneously with Abiraterone acetate solid dispersion；
3), tabletting, obtains final product Abiraterone Acetate Tablets.
Embodiment 3
Prescription (weight portion)：
Abiraterone acetate 10
Copolyvidone 25
Lactose 15
Microcrystalline Cellulose 15
Hydroxypropylcellulose 10
Magnesium stearate 0.8
Preparation technology：
1）, Abiraterone acetate solid dispersion preparation：Abiraterone acetate, Copolyvidone are taken for 1: 2.5 by weight, Copolyvidone is completely dissolved, 80 DEG C are heated to while stirring, Abiraterone acetate is added, is stirred to after being completely dissolved, continue to stir and be cooled to 0～-10 DEG C, 20 hours are placed into crisp shape breakable object, crush, cross 60～80 mesh sieves, obtain Abiraterone acetate solid dispersion；
2) Microcrystalline Cellulose, Lactose, hydroxypropylcellulose and the magnesium stearate of recipe quantity, are weighed, is mixed homogeneously with Abiraterone acetate solid dispersion；
3), tabletting, obtains final product Abiraterone Acetate Tablets.
Embodiment 4
Prescription (weight portion)：
Abiraterone acetate 10
Copolyvidone 30
Lactose 10
Microcrystalline Cellulose 10
Hydroxypropylcellulose 10
Magnesium stearate 0.8
Preparation technology：
1）, Abiraterone acetate solid dispersion preparation：Abiraterone acetate, Copolyvidone are taken for 1: 3 by weight, Copolyvidone is completely dissolved, 80 DEG C are heated to while stirring, Abiraterone acetate is added, is stirred to after being completely dissolved, continue to stir and be cooled to 0～-10 DEG C, 20 hours are placed into crisp shape breakable object, crush, cross 60～80 mesh sieves, obtain Abiraterone acetate solid dispersion；
2) Microcrystalline Cellulose, Lactose, hydroxypropylcellulose and the magnesium stearate of recipe quantity, are weighed, is mixed homogeneously with Abiraterone acetate solid dispersion；
3), tabletting, obtains final product Abiraterone Acetate Tablets.
Embodiment 5
Beneficial effects of the present invention are illustrated by several embodiment formulation and technologies are prepared with the quality index of sample.
The formulation and technology of embodiment 1-4 is chosen, and sample, and investigation quality is prepared according to pilot-scale.Inspection target is：Character, content, relevant material, dissolution, uniformity of dosage units, dispersing uniformity, tablet weight variation, product yield, investigation the results are shown in Table 3.3 each embodiment of table prepares the quality investigation result of sample
In sum, using the formulation and technology of technical scheme embodiment 2-4, smoothly efficiently, product yield is high, good quality for production process.
Claims (8)
1. a kind of Abiraterone Acetate Tablets, is characterized in that the tablet includes Abiraterone acetate solid dispersion and pharmaceutic adjuvant, and wherein Abiraterone acetate solid dispersion is made up of Abiraterone acetate and Copolyvidone.
2. Abiraterone Acetate Tablets according to claim 1, it is characterised in that the weight ratio of Abiraterone acetate and Copolyvidone is 1: 2-3 in Abiraterone acetate solid dispersion.
3. Abiraterone Acetate Tablets according to claim 1, it is characterised in that 30～60 weight portion of Abiraterone acetate solid dispersion, 10～30 weight portion of diluent, 0.5～2 weight portion of 3～10 weight portion of disintegrating agent and lubricant.
4. Abiraterone Acetate Tablets according to claim 3, is characterized in that the weight ratio of Abiraterone acetate and Copolyvidone in described Abiraterone acetate solid dispersion is 1: 2.
5. Abiraterone Acetate Tablets according to claim 3, is characterized in that described diluent for one or more in Mannitol, Microcrystalline Cellulose and Lactose with any than mixing.
6. Abiraterone Acetate Tablets according to claim 3, it is characterized in that described disintegrating agent be copolymerzation with cross-linking tie up ketone, hydroxypropylcellulose and Croscarmellose Sodium one or more with any than mixing.
7. Abiraterone Acetate Tablets according to claim 3, it is characterized in that described lubricant be magnesium stearate, one or two in silicon dioxide with any than mixing.
8. the preparation method of the Abiraterone Acetate Tablets described in a kind of claim 1, it is characterised in that the method comprises the steps：The preparation of a, Abiraterone acetate solid dispersion：Abiraterone acetate, Copolyvidone are taken for 1: 2-3 by weight, Copolyvidone is completely dissolved, 80 DEG C are heated to while stirring, Abiraterone acetate is added, is stirred to after being completely dissolved, continue to stir and be cooled to 0～-10 DEG C, 15～20 hours are placed into crisp shape breakable object, crush, cross 60～80 mesh sieves, obtain Abiraterone acetate solid dispersion；B, 10～30 weight portion of diluent, 0.5～2 weight portion of 3～10 weight portion of disintegrating agent and lubricant are weighed, mixed homogeneously with 10～20 parts by weight acetic acid abiraterone solid dispersion；The direct powder compression of c, mix homogeneously, obtains final product Abiraterone Acetate Tablets.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109125276A (en) * | 2017-06-19 | 2019-01-04 | 齐鲁制药有限公司 | A kind of pharmaceutical composition and preparation method thereof of Abiraterone acetate tablet |
| WO2019042247A1 (en) * | 2017-08-28 | 2019-03-07 | 江苏恒瑞医药股份有限公司 | Pharmaceutical composition of cyp17 inhibitor and preparation method therefor |
| WO2019208725A1 (en) * | 2018-04-25 | 2019-10-31 | 富士フイルム株式会社 | Pharmaceutical composition, and method for producing pharmaceutical composition |
| CN113384532A (en) * | 2020-03-14 | 2021-09-14 | 鲁南制药集团股份有限公司 | CYP17 inhibitor solid dispersion and preparation method thereof |
| WO2021184611A1 (en) * | 2020-03-14 | 2021-09-23 | 山东新时代药业有限公司 | Tablet of steroid cyp17 inhibitor solid dispersion and preparation method therefor |
-
2015
- 2015-09-18 CN CN201510596145.7A patent/CN106539765A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109125276A (en) * | 2017-06-19 | 2019-01-04 | 齐鲁制药有限公司 | A kind of pharmaceutical composition and preparation method thereof of Abiraterone acetate tablet |
| WO2019042247A1 (en) * | 2017-08-28 | 2019-03-07 | 江苏恒瑞医药股份有限公司 | Pharmaceutical composition of cyp17 inhibitor and preparation method therefor |
| WO2019208725A1 (en) * | 2018-04-25 | 2019-10-31 | 富士フイルム株式会社 | Pharmaceutical composition, and method for producing pharmaceutical composition |
| CN113384532A (en) * | 2020-03-14 | 2021-09-14 | 鲁南制药集团股份有限公司 | CYP17 inhibitor solid dispersion and preparation method thereof |
| WO2021184611A1 (en) * | 2020-03-14 | 2021-09-23 | 山东新时代药业有限公司 | Tablet of steroid cyp17 inhibitor solid dispersion and preparation method therefor |
| CN113384532B (en) * | 2020-03-14 | 2024-03-29 | 鲁南制药集团股份有限公司 | CYP17 inhibitor solid dispersion and preparation method thereof |
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Application publication date: 20170329 |
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