CN105147629B - A kind of sharp ketone tablet of isobutyl and preparation method - Google Patents
A kind of sharp ketone tablet of isobutyl and preparation method Download PDFInfo
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- CN105147629B CN105147629B CN201510613457.4A CN201510613457A CN105147629B CN 105147629 B CN105147629 B CN 105147629B CN 201510613457 A CN201510613457 A CN 201510613457A CN 105147629 B CN105147629 B CN 105147629B
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- isobutyl
- ketone
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Abstract
The present invention provides the tablet and preparation method of a kind of sharp ketone of isobutyl, mainly it is made up of the sharp ketone of isobutyl, malt flour and other pharmaceutically acceptable auxiliary materials, present invention addition malt flour in the sharp ketone of isobutyl causes the bioavilability of the sharp ketone of isobutyl to improve 30%, reach 60%, and the addition of malt flour greatly strengthen the drug effect of the sharp ketone of isobutyl.
Description
Technical field
The present invention discloses a kind of tablet of the sharp ketone of isobutyl, while additionally providing its preparation method, belongs to pharmaceutical preparation
Production technical field.
Background technology
The sharp ketone of isobutyl of the present invention is a kind of Paliperidone derivative, with Paliperidone（Trade name Invega）Phase
Than isobutyl profit ketone has good bioavilability and biological half-life longer in vivo, is used as anti-schizophrenia of new generation
Disease drug, the new product that its tablet will have very strong competitiveness as mental illness therapy field.At present for the sharp ketone piece of isobutyl
The preparation of agent, mainly isobutyl profit ketone and pharmaceutic adjuvant direct tablet compressing, although compared with Paliperidone tablet, its bioavilability
All significantly improved with biological half-life, but its bioavilability also only has 40% or so, continues to improve biological profit by additive
Expenditure is very necessary.
The content of the invention
The sharp ketone tablet of a kind of isobutyl that the present invention is provided, by adding additive, further improves the biological utilisation of formulation
Degree.And after malt flour is added as additive, isobutyl profit ketone drug effect is significantly improved.
Present invention also offers a kind of preparation method of the sharp ketone tablet of isobutyl, technique is simple, it is adaptable to industrialized production.
The sharp ketone tablet of a kind of isobutyl of the present invention, it is characterised in that mainly by following raw materials by weight portion than making
Into：
Isobutyl profit ketone：1st, malt flour 1-10, other pharmaceutically acceptable auxiliary materials.
A kind of preparation method of the sharp ketone tablet of isobutyl of the present invention, comprises the following steps：
Weigh the sharp ketone of isobutyl in proportion uniformly to mix with malt flour, pharmaceutically acceptable auxiliary material, using direct tablet compressing work
Skill compacting is formed；Option should meet《2010 editions Chinese Pharmacopoeias》Under tablet formulation.Pharmaceutically acceptable auxiliary material be filler,
Disintegrant, lubricant.
Described filler is microcrystalline cellulose, lactose, mannitol, starch and dextrin；
Described disintegrant is sodium carboxymethyl starch, Ac-Di-Sol, PVPP and low-substituted hydroxypropyl
Base cellulose；
Described lubricant is magnesium stearate, talcum powder and silica.
Described filler is lactose；
Described disintegrant is PVPP；
Described lubricant is magnesium stearate.
The positive effect of the present invention is：The present invention provides the tablet and preparation method of a kind of sharp ketone of isobutyl, mainly by
What isobutyl profit ketone, malt flour and other pharmaceutically acceptable auxiliary materials were made, present invention addition malt flour in the sharp ketone of isobutyl makes
The bioavilability for obtaining the sharp ketone of isobutyl improves 30%, has reached 60%, and the addition of malt flour greatly strengthen the sharp ketone of isobutyl
Drug effect.
Brief description of the drawings：
Fig. 1 is the tablet Drug-time curve of embodiment 1；
Fig. 2 is the tablet pharmacodynamics curve of embodiment 1；
Fig. 3 is the tablet Drug-time curve of embodiment 2；
Fig. 4 is the tablet pharmacodynamics curve of embodiment 2；
Fig. 5 is the tablet Drug-time curve of embodiment 3；
Fig. 6 is the tablet pharmacodynamics curve of embodiment 3；
Fig. 7 is the tablet Drug-time curve of embodiment 4；
Fig. 8 is the tablet pharmacodynamics curve of embodiment 4；
Fig. 9 is the tablet Drug-time curve of embodiment 5；
Figure 10 is the tablet pharmacodynamics curve of embodiment 5；
Figure 11 is the tablet Drug-time curve of embodiment 6；
Figure 12 is the tablet pharmacodynamics curve of embodiment 6.
Embodiment
The present invention specific implementation method, by following embodiment for example, but protection scope of the present invention do not limit to
In this.
Embodiment 1
Prescription：Isobutyl founds ketone 1.0g, malt flour 10g, microcrystalline cellulose 73.5g, sodium cellulose glycolate 15g, talcum powder
1g, altogether into 500.
Isobutyl is weighed according to prescription and founds ketone, malt flour, microcrystalline cellulose, sodium cellulose glycolate, talcum powder, uses three-dimensional
Mixed instrument mixing 10min, that is, reach well mixed state；By the mixture prepared in proportion, with the tabletting that pressure is 15 tons
Machine carries out tabletting, sealing preserve after tabletting sterilizing.Drug-time curve is shown in Fig. 1；Pharmacodynamics curve is shown in Fig. 2.
Embodiment 2
Prescription：Isobutyl founds ketone 1.5g, malt flour 6g, lactose 76.5g, PVPP 15g, magnesium stearate 1g, altogether into 500
Piece.
Isobutyl, which is weighed, according to prescription founds ketone, malt flour, lactose, PVPP, magnesium stearate, it is mixed using three-dimensional hybrid instrument
10min is closed, that is, reaches well mixed state；By the mixture prepared in proportion, pressed with pressure for 15 tons of tablet press machine
Piece, sealing preserve after tabletting sterilizing.Drug-time curve is shown in Fig. 3；Pharmacodynamics curve is shown in Fig. 4.
Embodiment 3
Prescription：Isobutyl founds ketone 1.0g, malt flour 1g, lactose 76.5g, PVPP 15g, magnesium stearate 1g, altogether into 500
Piece.
Isobutyl, which is weighed, according to prescription founds ketone, malt flour, lactose, PVPP, magnesium stearate, it is mixed using three-dimensional hybrid instrument
10min is closed, that is, reaches well mixed state；By the mixture prepared in proportion, pressed with pressure for 15 tons of tablet press machine
Piece, sealing preserve after tabletting sterilizing.Drug-time curve is shown in Fig. 5；Pharmacodynamics curve is shown in Fig. 6.
Embodiment 4
Prescription：Isobutyl founds ketone 1.0g, malt flour 7g, microcrystalline cellulose 75g, sodium cellulose glycolate 10g, talcum powder 1g,
Altogether into 500.
Isobutyl is weighed according to prescription and founds ketone, malt flour, microcrystalline cellulose, sodium cellulose glycolate, talcum powder, uses three-dimensional
Mixed instrument mixing 10min, that is, reach well mixed state；By the mixture prepared in proportion, with the tabletting that pressure is 10 tons
Machine carries out tabletting, sealing preserve after tabletting sterilizing.Drug-time curve is shown in Fig. 7；Pharmacodynamics curve is shown in Fig. 8.
Embodiment 5
Prescription：Isobutyl founds ketone 1.0g, malt flour 2g, lactose 76.5g, sodium cellulose glycolate 10g, talcum powder 1g, altogether into
500.
Isobutyl is weighed according to prescription and founds ketone, malt flour, lactose, sodium cellulose glycolate, talcum powder, uses three-dimensional hybrid instrument
10min is mixed, that is, reaches well mixed state；By the mixture prepared in proportion, carried out with pressure for 10 tons of tablet press machine
Tabletting, sealing preserve after tabletting sterilizing.Drug-time curve is shown in Fig. 9；Pharmacodynamics curve is shown in Figure 10.
Embodiment 6
Prescription：Isobutyl founds ketone 1.0g, malt flour 3g, lactose 80g, sodium cellulose glycolate 15g, magnesium stearate 1g, altogether into
500.
Isobutyl is weighed according to prescription and founds ketone, malt flour, lactose, sodium cellulose glycolate, magnesium stearate, uses three-dimensional hybrid
Instrument mixing 10min, that is, reach well mixed state；By the mixture prepared in proportion, entered with pressure for 10 tons of tablet press machine
Row tabletting, sealing preserve after tabletting sterilizing.Drug-time curve is shown in Figure 11；Pharmacodynamics curve is shown in Figure 12.
Show that Tablets bioavilability ratio does not add the tablet of malt flour to have bright by pharmacokinetics and pharmacodynamic experiment
It is aobvious to improve, more than 60% is can reach, as shown in 1 ~ Figure 12 of accompanying drawing.
The present invention provides the tablet and preparation method of a kind of sharp ketone of isobutyl, mainly by the sharp ketone of isobutyl, malt flour and other
What pharmaceutically acceptable auxiliary material was made, present invention addition malt flour in the sharp ketone of isobutyl causes the bioavilability of the sharp ketone of isobutyl
30% is improved, 60% has been reached, and the addition of malt flour greatly strengthen the drug effect of the sharp ketone of isobutyl.
Claims (2)
1. a kind of sharp ketone tablet of isobutyl, it is characterised in that mainly by following raw materials by weight portion than being made：
Isobutyl profit ketone 1, malt flour 1-10, other pharmaceutically acceptable auxiliary materials.
2. a kind of preparation method of the sharp ketone tablet of isobutyl as described in claims 1, comprises the following steps：
Weigh the sharp ketone of isobutyl in proportion uniformly to mix with malt flour and pharmaceutically acceptable auxiliary material, using direct tablet compressing technique pressure
System is formed；
Pharmaceutically acceptable auxiliary material is filler, disintegrant, lubricant；
Described filler is microcrystalline cellulose, lactose, mannitol, starch and dextrin；
Described disintegrant is that sodium carboxymethyl starch, Ac-Di-Sol, PVPP and low substituted hydroxy-propyl are fine
Dimension element；
Described lubricant is magnesium stearate, talcum powder and silica.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510613457.4A CN105147629B (en) | 2015-09-24 | 2015-09-24 | A kind of sharp ketone tablet of isobutyl and preparation method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510613457.4A CN105147629B (en) | 2015-09-24 | 2015-09-24 | A kind of sharp ketone tablet of isobutyl and preparation method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105147629A CN105147629A (en) | 2015-12-16 |
| CN105147629B true CN105147629B (en) | 2017-08-25 |
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| CN201510613457.4A Active CN105147629B (en) | 2015-09-24 | 2015-09-24 | A kind of sharp ketone tablet of isobutyl and preparation method |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1684670A (en) * | 2002-07-29 | 2005-10-19 | 阿尔扎公司 | Methods and dosage forms for controlled delivery of paliperidone |
| CN1840109A (en) * | 2006-01-12 | 2006-10-04 | 岳顺疆 | Chewing tablet of malt and preparation method thereof |
| CN102058517A (en) * | 2010-12-31 | 2011-05-18 | 泰州万全医药科技有限公司 | Paliperidone slow release formulation and preparation method thereof |
-
2015
- 2015-09-24 CN CN201510613457.4A patent/CN105147629B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1684670A (en) * | 2002-07-29 | 2005-10-19 | 阿尔扎公司 | Methods and dosage forms for controlled delivery of paliperidone |
| CN1840109A (en) * | 2006-01-12 | 2006-10-04 | 岳顺疆 | Chewing tablet of malt and preparation method thereof |
| CN102058517A (en) * | 2010-12-31 | 2011-05-18 | 泰州万全医药科技有限公司 | Paliperidone slow release formulation and preparation method thereof |
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| Publication number | Publication date |
|---|---|
| CN105147629A (en) | 2015-12-16 |
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