CN103610663B - Ubenimex capsule medicament composition and preparation method thereof - Google Patents
Ubenimex capsule medicament composition and preparation method thereof Download PDFInfo
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- CN103610663B CN103610663B CN201310664815.5A CN201310664815A CN103610663B CN 103610663 B CN103610663 B CN 103610663B CN 201310664815 A CN201310664815 A CN 201310664815A CN 103610663 B CN103610663 B CN 103610663B
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- ubenimex
- capsule
- lactose
- fatty acid
- acid ester
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- VGGGPCQERPFHOB-MCIONIFRSA-N Bestatin Chemical compound CC(C)C[C@H](C(O)=O)NC(=O)[C@@H](O)[C@H](N)CC1=CC=CC=C1 VGGGPCQERPFHOB-MCIONIFRSA-N 0.000 title claims abstract description 124
- 229950009811 ubenimex Drugs 0.000 title claims abstract description 124
- 239000002775 capsule Substances 0.000 title claims abstract description 102
- 238000002360 preparation method Methods 0.000 title claims abstract description 46
- 239000000203 mixture Substances 0.000 title claims abstract description 33
- 239000003814 drug Substances 0.000 title abstract description 3
- 239000000463 material Substances 0.000 claims abstract description 15
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 96
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 48
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 48
- 239000008101 lactose Substances 0.000 claims description 48
- 235000019359 magnesium stearate Nutrition 0.000 claims description 48
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 48
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 48
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 48
- 229930006000 Sucrose Natural products 0.000 claims description 47
- -1 Sucrose fatty acid ester Chemical class 0.000 claims description 47
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 47
- 239000000194 fatty acid Substances 0.000 claims description 47
- 229930195729 fatty acid Natural products 0.000 claims description 47
- 239000005720 sucrose Substances 0.000 claims description 47
- 238000011049 filling Methods 0.000 claims description 28
- 239000011812 mixed powder Substances 0.000 claims description 28
- 238000002156 mixing Methods 0.000 claims description 14
- 238000004519 manufacturing process Methods 0.000 abstract description 10
- 239000003795 chemical substances by application Substances 0.000 abstract description 6
- 239000000126 substance Substances 0.000 abstract description 6
- 239000011230 binding agent Substances 0.000 abstract description 4
- 230000000694 effects Effects 0.000 abstract description 2
- 238000009776 industrial production Methods 0.000 abstract 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 38
- 229960001375 lactose Drugs 0.000 description 38
- 230000000052 comparative effect Effects 0.000 description 13
- 238000012360 testing method Methods 0.000 description 8
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 6
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 4
- 239000004141 Sodium laurylsulphate Substances 0.000 description 4
- 238000004090 dissolution Methods 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 4
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 4
- 210000004881 tumor cell Anatomy 0.000 description 4
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 description 3
- 238000004132 cross linking Methods 0.000 description 3
- 238000000605 extraction Methods 0.000 description 3
- 229960000540 polacrilin potassium Drugs 0.000 description 3
- WVWZXTJUCNEUAE-UHFFFAOYSA-M potassium;1,2-bis(ethenyl)benzene;2-methylprop-2-enoate Chemical compound [K+].CC(=C)C([O-])=O.C=CC1=CC=CC=C1C=C WVWZXTJUCNEUAE-UHFFFAOYSA-M 0.000 description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- SZYSLWCAWVWFLT-UTGHZIEOSA-N [(2s,3s,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)-2-[(2r,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxolan-2-yl]methyl octadecanoate Chemical compound O([C@@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@]1(COC(=O)CCCCCCCCCCCCCCCCC)O[C@H](CO)[C@@H](O)[C@@H]1O SZYSLWCAWVWFLT-UTGHZIEOSA-N 0.000 description 2
- 239000008351 acetate buffer Substances 0.000 description 2
- 239000000872 buffer Substances 0.000 description 2
- 230000001186 cumulative effect Effects 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 102000005606 Activins Human genes 0.000 description 1
- 108010059616 Activins Proteins 0.000 description 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 1
- 241000459479 Capsula Species 0.000 description 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 description 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 206010020880 Hypertrophy Diseases 0.000 description 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 description 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 1
- 208000002454 Nasopharyngeal Carcinoma Diseases 0.000 description 1
- 206010061306 Nasopharyngeal cancer Diseases 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 239000000488 activin Substances 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 239000007963 capsule composition Substances 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 230000019522 cellular metabolic process Effects 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000036737 immune function Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000002386 leaching Methods 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 231100001224 moderate toxicity Toxicity 0.000 description 1
- 201000011216 nasopharynx carcinoma Diseases 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
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- Medicinal Preparation (AREA)
Abstract
The invention provides an ubenimex capsule medicament composition and a preparation method thereof. Compared with the prior art, the prescription and process for preparing the ubenimex capsule, which are disclosed by the invention has the advantages that auxiliary materials, such as a binder and a disintegrating agent in the prescription are not used, the prescription is simple, and the safety is greatly improved. The preparation technology is easy to operate, and very suitable for large-scale industrial production. The prepared product can be completely dissolved out within a short period of time, and good in dissolving effect, relatively low in content of related substances, and stable in quality, and has a remarkable progress in comparison with the prior art.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, be specifically related to a kind of ubenimex pharmaceutical capsules composition and method of making the same.
Background technology
Ubenimex can effectively disturb tumor cell metabolism, and inhibition tumor cell hypertrophy, makes apoptosis of tumor cells, and human activin cellular immune function, the generation of stimulating cytokine and secretion, promote generation and the propagation of Graft Versus Tumor cell.Clinically for the auxiliary treatment of anticancer chemotherapy, radiotherapy, there is obvious curative effects to acute and chronic myelocytic leukemia, lung squamous cancer, nasopharyngeal carcinoma etc.Domestic listing dosage form has Tablet and Capsula agent.
By finding ubenimex capsule commercialized product clinical trail, there is disintegrate and the problem such as drug-eluting is slow in capsule, have impact on the bioavailability of medicine to a certain extent.Chinese patent (CN103142544A) discloses a kind of Ubenimex capsule composition and preparation method thereof, and this ubenimex capsule is made up of ubenimex, lactose, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, polacrilin potassium, polyvidone, sodium lauryl sulphate, sucrose stearate and magnesium stearate.Because supplementary product kind is more, preparation technology is more complicated, and production cost is high, is unfavorable for industrialized great production.
Summary of the invention
The invention provides a kind of ubenimex pharmaceutical capsules composition and method of making the same, prescription provided by the invention and preparation method comparatively prior art are simple, are more suitable for industrialized great production, and obtained product stripping is rapid, steady quality.
The invention discloses following technical scheme:
A kind of ubenimex pharmaceutical capsules compositions, the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 10.0～30.0mg |
| Sucrose fatty acid ester | 0.8～20.0mg |
| Lactose | 35.0～125.0mg |
| Microcrystalline Cellulose | 95.0～125.0mg |
| Magnesium stearate | 0.3～3.5mg |
Further, the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 10.0～30.0mg |
| Sucrose fatty acid ester | 1.2～15.0mg |
| Lactose | 47.5～115.0mg |
| Microcrystalline Cellulose | 100.0～115.0mg |
| Magnesium stearate | 0.5～3.0mg |
Further, the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 10.0～30.0mg |
| Sucrose fatty acid ester | 1.7～13.5mg |
| Lactose | 52.5～111.9mg |
| Microcrystalline Cellulose | 105.0～111.9mg |
| Magnesium stearate | 0.8～2.7mg |
Concrete, in ubenimex pharmaceutical capsules compositions of the present invention, the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 10.0mg |
| Sucrose fatty acid ester | 1.7mg |
| Lactose | 52.5mg |
| Microcrystalline Cellulose | 105.0mg |
| Magnesium stearate | 0.8mg |
Or the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 10.0mg |
| Sucrose fatty acid ester | 1.2mg |
| Lactose | 47.5mg |
| Microcrystalline Cellulose | 100.0mg |
| Magnesium stearate | 0.5mg |
Or the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 10.0mg |
| Sucrose fatty acid ester | 0.8mg |
| Lactose | 35.0mg |
| Microcrystalline Cellulose | 95.0mg |
| Magnesium stearate | 0.3mg |
Or the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 25.0mg |
| Sucrose fatty acid ester | 5.9mg |
| Lactose | 75.5mg |
| Microcrystalline Cellulose | 108.5mg |
| Magnesium stearate | 1.6mg |
Or the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 20.0mg |
| Sucrose fatty acid ester | 7.5mg |
| Lactose | 80.0mg |
| Microcrystalline Cellulose | 110.3mg |
| Magnesium stearate | 2.2mg |
Or the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 15.0mg |
| Sucrose fatty acid ester | 10.5mg |
| Lactose | 65.0mg |
| Microcrystalline Cellulose | 99.5mg |
| Magnesium stearate | 2.5mg |
Or the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 30.0mg |
| Sucrose fatty acid ester | 15.0mg |
| Lactose | 115.0mg |
| Microcrystalline Cellulose | 115.0mg |
| Magnesium stearate | 3.0mg |
Or the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 30.0mg |
| Sucrose fatty acid ester | 13.5mg |
| Lactose | 111.9mg |
| Microcrystalline Cellulose | 111.9mg |
| Magnesium stearate | 2.7mg |
Or the ubenimex capsule of per unit preparation is made up of following component:
| Ubenimex | 30.0mg |
| Sucrose fatty acid ester | 20.0mg |
| Lactose | 125.0mg |
| Microcrystalline Cellulose | 125.0mg |
| Magnesium stearate | 3.5mg |
The present invention also provides a kind of preparation method of ubenimex pharmaceutical capsules compositions, and its preparation method comprises the following steps:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation; Finally add in material bin by magnesium stearate, mixing, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Further, in above-mentioned blend step, the time of preferred married operation is for the first time (5 ~ 35min), and preferably the time of second time married operation is (2 ~ 30min), and preferably the time of married operation is (5 ~ 35min) for the third time.
Adopt ubenimex capsule prepared by technical scheme provided by the invention, have the following advantages:
1. safety is better.Containing 9 kinds of components in prescription disclosed in prior art, comprise binding agent polyvidone, disintegrating agent cross-linking sodium carboxymethyl cellulose, polacrilin potassium, solubilizing agent sucrose stearate, sodium lauryl sulphate and binding agent polyvidone etc.And prescription of the present invention is very simple, prescription kind only has 5 kinds, eliminates the use of polyvidone, cross-linking sodium carboxymethyl cellulose, polacrilin potassium and sodium lauryl sulphate.Wherein, sodium lauryl sulphate has moderate toxicity, and long-term suction has infringement to lung.Adopt constant product quality prepared by technical solution of the present invention, safety improves greatly.
2. result of extraction is better.In technical scheme disclosed in prior art, need to add disintegrating agent and solubilizing agent just can make the stripping of product fater disintegration; And the present invention does not need to add disintegrating agent, still stripping is rapid for the product of preparation, and substantially discharge when 10min completely, in water, during 10min, dissolution just can reach 93%, and bioavailability is significantly improved, and meets clinical application demand.
3. prescription kind of the present invention is few, and preparation process is easy to operation, and production cost comparatively prior art reduces greatly, is more suitable for industrialized great production.
Detailed description of the invention
The present invention is described in detail below to adopt embodiment, but not limitation of the present invention, and the equivalent replacement of all any this areas done according to the disclosure of invention, all belongs to protection scope of the present invention.
Embodiment 1 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 10.0g |
| Sucrose fatty acid ester | 0.8g |
| Lactose | 35.0g |
| Microcrystalline Cellulose | 125.0g |
| Magnesium stearate | 0.3g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 10min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 30min; Finally add in material bin by magnesium stearate, mixing 15min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 2 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 10.0g |
| Sucrose fatty acid ester | 1.7g |
| Lactose | 52.5g |
| Microcrystalline Cellulose | 105.0g |
| Magnesium stearate | 0.8g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 5min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 20min; Finally add in material bin by magnesium stearate, mixing 5min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 3 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 10.0g |
| Sucrose fatty acid ester | 1.2g |
| Lactose | 47.5g |
| Microcrystalline Cellulose | 100.0g |
| Magnesium stearate | 0.5g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 25min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 10min; Finally add in material bin by magnesium stearate, mixing 8min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 4 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 20.0g |
| Sucrose fatty acid ester | 7.5g |
| Lactose | 80.0g |
| Microcrystalline Cellulose | 110.3g |
| Magnesium stearate | 2.2g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 20min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 6min; Finally add in material bin by magnesium stearate, mixing 12min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 5 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 25.0g |
| Sucrose fatty acid ester | 5.9g |
| Lactose | 75.5g |
| Microcrystalline Cellulose | 108.5g |
| Magnesium stearate | 1.6g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 17min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 30min; Finally add in material bin by magnesium stearate, mixing 10min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 6 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 20.0g |
| Sucrose fatty acid ester | 4.0g |
| Lactose | 70.8g |
| Microcrystalline Cellulose | 125.0g |
| Magnesium stearate | 1.2g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 6min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 15min; Finally add in material bin by magnesium stearate, mixing 30min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 7 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 30.0g |
| Sucrose fatty acid ester | 15.0g |
| Lactose | 115.0g |
| Microcrystalline Cellulose | 115.0g |
| Magnesium stearate | 3.0g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 15min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 5min; Finally add in material bin by magnesium stearate, mixing 25min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 8 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 30.0g |
| Sucrose fatty acid ester | 13.5g |
| Lactose | 111.9g |
| Microcrystalline Cellulose | 111.9g |
| Magnesium stearate | 2.7g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 5min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 20min; Finally add in material bin by magnesium stearate, mixing 5min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 9 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 30.0g |
| Sucrose fatty acid ester | 20.0g |
| Lactose | 125.0g |
| Microcrystalline Cellulose | 95.0g |
| Magnesium stearate | 3.5g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 15min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 30min; Finally add in material bin by magnesium stearate, mixing 10min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 10 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 10.0g |
| Sucrose fatty acid ester | 0.8g |
| Lactose | 35.0g |
| Microcrystalline Cellulose | 95.0g |
| Magnesium stearate | 0.3g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 20min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 2min; Finally add in material bin by magnesium stearate, mixing 30min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 11 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 15.0g |
| Sucrose fatty acid ester | 10.5g |
| Lactose | 65.0g |
| Microcrystalline Cellulose | 99.5g |
| Magnesium stearate | 2.5g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 35min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 15min; Finally add in material bin by magnesium stearate, mixing 10min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Embodiment 12 ubenimex capsule prescription: (in 1000, unit: g)
| Ubenimex | 30.0g |
| Sucrose fatty acid ester | 20.0g |
| Lactose | 125.0g |
| Microcrystalline Cellulose | 125.0g |
| Magnesium stearate | 3.5g |
Preparation technology:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation 9min; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation 12min; Finally add in material bin by magnesium stearate, mixing 35min, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
Test example 1: stripping curve contrast test
Comparative example: the sample prepared according to the method for Chinese patent CN103142544A embodiment 1.
Get the embodiment of the present invention 2,3,4,5,7,8,11 sample and each 6 of comparative example respectively, according to Chinese Pharmacopoeia version in 2010 two annex Ⅹ C dissolution methods, measure the cumulative defaultlogic of each time point, actual conditions is as follows:
Dissolution medium: water, pH1.2 sodium chloride/hydrochloride buffer, pH4.0 acetic acid/acetate buffer, pH6.8 phosphate buffer;
Rotating speed: 50 turns/min;
Respectively at 10,15,20,30min time sample, adopt high effective liquid chromatography for measuring, result is as shown in the table:
Table 1 is stripping curve comparative study result in water
Table 2 is stripping curve comparative study result in pH1.2 sodium chloride/hydrochloride buffer
Table 3 is stripping curve comparative study result in pH4.0 acetic acid/acetate buffer
Table 4 is stripping curve comparative study result in pH6.8 phosphate buffer
As can be seen from the above data, in above-mentioned 4 kinds of media, just release is complete substantially when 10min for embodiment of the present invention sample, and dissolution rate all comparatively comparative example is rapider.And in same media, the cumulative defaultlogic of embodiment of the present invention sample, apparently higher than the comparative example under identical leaching condition, illustrates that the ubenimex capsule result of extraction adopting prescription of the present invention and technique to prepare is better.
Test example 2: stability contrast test
Comparative example: the sample prepared according to the method for Chinese patent CN103142544A embodiment 1.
Get the embodiment of the present invention 2,3,4,5,7,8,11 sample and comparative example to be respectively placed in 40 DEG C, to investigate under relative humidity 75% condition, respectively at 0 month, January, February, March and June time sampling its character, content, related substance and dissolution are detected.Testing result is as shown in table 5.
Table 5 embodiment of the present invention sample and comparative example accelerated stability results contrast
Can be found out by table 5, in ubenimex capsule prepared by the embodiment of the present invention, the content of ubenimex is in 99.4% ~ 101.1% scope, the content of related substance is 0.05% ~ 0.08%, dissolution is 98% ~ 102%, all obviously be better than the regulation that 90.0% ~ 110.0% and stripping limit that ubenimex capsule content limit that Chinese Pharmacopoeia records in version for 2010 should be labelled amount are 80% of labelled amount, and in accelerated test 6 months, not there is significant change in quality; Comparative example was when accelerated test 6 months, and the content of related substance rises to 0.22% from 0.05%, increased obviously.Therefore, embodiment of the present invention sample is obviously better than comparative example in related substance index, and product quality is highly stable.
Known by above-mentioned result of the test, adopt the ubenimex capsule that prescription of the present invention and technique prepare, compared with the use eliminating the adjuvant such as binding agent, disintegrating agent in prior art prescription, prescription is simple, preparation process is easy to operation, is very applicable to industrialized great production.The product prepared can stripping be complete at short notice, and result of extraction is better, and the related substance of product is lower, and product quality is highly stable, and comparatively prior art tool has made marked progress.
Claims (10)
1. a ubenimex pharmaceutical capsules compositions, is characterized in that, the ubenimex capsule of per unit preparation is made up of following component:
。
2. ubenimex pharmaceutical capsules compositions according to claim 1, is characterized in that, the ubenimex capsule of per unit preparation is made up of following component:
。
3. ubenimex pharmaceutical capsules compositions according to claim 2, is characterized in that, the ubenimex capsule of per unit preparation is made up of following component:
。
4. ubenimex pharmaceutical capsules compositions according to claim 3, is characterized in that, the ubenimex capsule of per unit preparation is made up of following component:
。
5. ubenimex pharmaceutical capsules compositions according to claim 2, is characterized in that, the ubenimex capsule of per unit preparation is made up of following component:
。
6. ubenimex pharmaceutical capsules compositions according to claim 3, is characterized in that, the ubenimex capsule of per unit preparation is made up of following component:
。
7. ubenimex pharmaceutical capsules compositions according to claim 3, is characterized in that, the ubenimex capsule of per unit preparation is made up of following component:
。
8. ubenimex pharmaceutical capsules compositions according to claim 2, is characterized in that, the ubenimex capsule of per unit preparation is made up of following component:
。
9. ubenimex pharmaceutical capsules compositions according to claim 3, is characterized in that, the ubenimex capsule of per unit preparation is made up of following component:
。
10. the preparation method of a kind of ubenimex pharmaceutical capsules compositions according to any one of claim 1 ~ 9, it is characterized in that, this preparation method comprises the steps:
(1) mix: first the ubenimex of the microcrystalline Cellulose of recipe quantity, sucrose fatty acid ester and recipe quantity is added in mixer hopper successively, mixer performs married operation; Then lactose is added in above-mentioned mixer hopper, mixer performs married operation; Finally add in material bin by magnesium stearate, mixing, is always mixed powder;
(2) capsule-filling: ubenimex capsule is always mixed powder and add in capsule filling machine hopper, filled capsules.
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|---|---|---|---|---|
| CN100525756C (en) * | 2007-05-30 | 2009-08-12 | 深圳万乐药业有限公司 | Coated ubenimex table |
| CN101716156B (en) * | 2010-01-08 | 2011-06-22 | 成都苑东药业有限公司 | Ubenimex dispersive tablet composition |
| CN103142544B (en) * | 2013-02-28 | 2014-01-08 | 成都苑东药业有限公司 | Ubenimex capsule composition and preparation method thereof |
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Address after: 611731 Chengdu province high tech Zone, west of the source road, No. 8, No. Patentee after: Chengdu Easton Biopharmaceuticals Co.,Ltd. Address before: 611731 Chengdu province high tech Zone, west of the source road, No. 8, No. Patentee before: Chengdu Easton Pharmaceutical Co.,Ltd. |
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Denomination of invention: A drug combination of Ubenazepril capsules and its preparation method Effective date of registration: 20231130 Granted publication date: 20150506 Pledgee: Chengdu Bank Co.,Ltd. High tech Branch Pledgor: Chengdu Easton Biopharmaceuticals Co.,Ltd. Registration number: Y2023980068371 |
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