CN101991553B - Exemestane tablet and preparation method thereof - Google Patents
Exemestane tablet and preparation method thereof Download PDFInfo
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- CN101991553B CN101991553B CN200910075202.1A CN200910075202A CN101991553B CN 101991553 B CN101991553 B CN 101991553B CN 200910075202 A CN200910075202 A CN 200910075202A CN 101991553 B CN101991553 B CN 101991553B
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- BFYIZQONLCFLEV-DAELLWKTSA-N Aromasine Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=C)C2=C1 BFYIZQONLCFLEV-DAELLWKTSA-N 0.000 title claims abstract description 44
- 229960000255 exemestane Drugs 0.000 title claims abstract description 44
- 238000002360 preparation method Methods 0.000 title claims abstract description 26
- 239000011230 binding agent Substances 0.000 claims abstract description 21
- 238000002156 mixing Methods 0.000 claims abstract description 12
- -1 polyethylene pyrrolidone Polymers 0.000 claims description 31
- 239000008187 granular material Substances 0.000 claims description 30
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 26
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 18
- 229920002472 Starch Polymers 0.000 claims description 18
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 18
- 238000004132 cross linking Methods 0.000 claims description 18
- 239000011734 sodium Substances 0.000 claims description 18
- 229910052708 sodium Inorganic materials 0.000 claims description 18
- 239000008107 starch Substances 0.000 claims description 18
- 235000019698 starch Nutrition 0.000 claims description 18
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 13
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 13
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 13
- 235000019359 magnesium stearate Nutrition 0.000 claims description 13
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 13
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 13
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 13
- 239000000741 silica gel Substances 0.000 claims description 13
- 229910002027 silica gel Inorganic materials 0.000 claims description 13
- 229930195725 Mannitol Natural products 0.000 claims description 12
- 239000000594 mannitol Substances 0.000 claims description 12
- 235000010355 mannitol Nutrition 0.000 claims description 12
- 239000011812 mixed powder Substances 0.000 claims description 10
- 239000007864 aqueous solution Substances 0.000 claims description 5
- 239000012467 final product Substances 0.000 claims description 5
- 229960001855 mannitol Drugs 0.000 claims description 5
- 239000000203 mixture Substances 0.000 claims description 5
- 239000008213 purified water Substances 0.000 claims description 5
- 239000000243 solution Substances 0.000 claims description 5
- 238000009492 tablet coating Methods 0.000 claims description 5
- 239000002700 tablet coating Substances 0.000 claims description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 5
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims description 3
- 206010006187 Breast cancer Diseases 0.000 abstract description 8
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 abstract description 5
- 230000000694 effects Effects 0.000 abstract description 5
- 239000003795 chemical substances by application Substances 0.000 abstract description 2
- 238000004519 manufacturing process Methods 0.000 abstract description 2
- 230000009245 menopause Effects 0.000 abstract description 2
- 239000004067 bulking agent Substances 0.000 abstract 1
- 238000001035 drying Methods 0.000 abstract 1
- 239000000314 lubricant Substances 0.000 abstract 1
- 229940085033 nolvadex Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 description 8
- 238000003556 assay Methods 0.000 description 7
- 238000000034 method Methods 0.000 description 6
- 238000012360 testing method Methods 0.000 description 6
- 102000014654 Aromatase Human genes 0.000 description 5
- 108010078554 Aromatase Proteins 0.000 description 5
- 208000026310 Breast neoplasm Diseases 0.000 description 4
- 229940011871 estrogen Drugs 0.000 description 4
- 239000000262 estrogen Substances 0.000 description 4
- 206010003439 Artificial menopause Diseases 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 description 2
- AEMFNILZOJDQLW-QAGGRKNESA-N androst-4-ene-3,17-dione Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 AEMFNILZOJDQLW-QAGGRKNESA-N 0.000 description 2
- 229960005471 androstenedione Drugs 0.000 description 2
- AEMFNILZOJDQLW-UHFFFAOYSA-N androstenedione Natural products O=C1CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 AEMFNILZOJDQLW-UHFFFAOYSA-N 0.000 description 2
- 201000008275 breast carcinoma Diseases 0.000 description 2
- 238000001514 detection method Methods 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000002207 metabolite Substances 0.000 description 2
- 238000011020 pilot scale process Methods 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 238000012216 screening Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 229960001603 tamoxifen Drugs 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- 210000002700 urine Anatomy 0.000 description 2
- DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 description 1
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 1
- 102000004506 Blood Proteins Human genes 0.000 description 1
- 108010017384 Blood Proteins Proteins 0.000 description 1
- DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 description 1
- 206010027336 Menstruation delayed Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 210000004100 adrenal gland Anatomy 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000003098 androgen Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 230000004087 circulation Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 238000007599 discharging Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 229960005309 estradiol Drugs 0.000 description 1
- 229930182833 estradiol Natural products 0.000 description 1
- 230000001076 estrogenic effect Effects 0.000 description 1
- 229960003399 estrone Drugs 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 230000012010 growth Effects 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 230000000937 inactivator Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 230000002427 irreversible effect Effects 0.000 description 1
- 125000000468 ketone group Chemical group 0.000 description 1
- 238000011031 large-scale manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 230000037323 metabolic rate Effects 0.000 description 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 239000006225 natural substrate Substances 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 210000002381 plasma Anatomy 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 239000012925 reference material Substances 0.000 description 1
- 230000003637 steroidlike Effects 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 229960003604 testosterone Drugs 0.000 description 1
- 238000010200 validation analysis Methods 0.000 description 1
Abstract
The invention provides an exemestane tablet and a preparation method thereof. The exemestane tablet contains a principal component of exemestane and auxiliary components of a disintegrating agent, a stuffing bulking agent, a lubricating agent and the like. The preparation method of the exemestane tablet comprises the following steps of manufacturing a binding agent, mixing, granulating, drying and the like. The exemestane tablet is used for advanced breast cancer of women, patient's condition of which still gets on after the treatment of nolvadex and nature or induced menopause, and has notable curative effect.
Description
Technical field
The present invention relates to a kind of Exemestane Tablets and preparation method thereof, belong to technical field of medicine.
Background technology
Exemestane is irreversible arimedex, can suppress the estrogen synthesis of postmenopausal women, thus stops breast cancer cell growth.
The growth of breast cancer cell can be dependent on estrogenic existence, and the androgen (androstenedione and testosterone) in adrenal gland and ovary is transformed primarily of the aromatase in peripheral tissues by the estrogen (estrone and estradiol) in female menopausal Posterior circle.Estrogen production is stoped to be a kind of method that effective as selective treats menopausal hormone independent mammary tumor by suppressing aromatase.Exemestane is a kind of irreversibility steroidal aromatase inactivator, similar to the natural substrates androstenedione of this enzyme in structure, for the pseudo-substrate of aromatase, make its inactivation by being irreversibly combined with the avtive spot of this enzyme, thus obviously reduce the estrogen level in menopausal women blood circulation.
According to reported literature, after the oral radiolabeled exemestane of healthy women of menopause, absorb rapidly, the exemestane of at least 42% is absorbed at gastrointestinal tract; After edible High fat meal, in blood plasma, exemestane level rises about 40%.Exemestane extensively distributes in each tissue, and its plasma protein binding rate is 90%.The metabolic rate of exemestane is extensive, metabolism is carried out mainly through the oxidation of 6-position methylene and 17-position ketone group reduction, metabolite non-activity or suppress aromatase activity more weak, its metabolite is mainly drained from urine and excrement, about respectively account for about 40%, the original shape medicine of discharging in urine is lower than 1% of dosage.The average terminal half-lives of exemestane is 24 hours.The more healthy postmenopausal women of absorption of breast carcinoma postmenopausal women in late period is fast, and peak time is respectively 1.2 hours and 2.9 hours.After repeat administration, the more healthy postmenopausal women of mean oral clearance rate of breast carcinoma patients with terminal is low by 45%, and circulation in level higher; Its average A UC is 2 times of healthy women.
Therefore, exemestane is used for after tamoxifen treatment, and after the nature that its state of an illness still gets along with or artificial menopause, the advanced breast cancer of women, has significant curative effect.
Summary of the invention
The object of this invention is to provide a kind of Exemestane Tablets and preparation method thereof.Medicine of the present invention is used for after tamoxifen treatment, and after the nature that its state of an illness still gets along with or artificial menopause, the advanced breast cancer of women, has significant curative effect.
Exemestane Tablets of the present invention is made up of the supplementary material medicine of following weight portion:
Exemestane 25, mannitol 50-70, microcrystalline Cellulose 3-6, cross-linking polyethylene pyrrolidone 1-3, carboxymethyl starch sodium 1-3, magnesium stearate 0.3-0.7, micropowder silica gel 0.3-0.7, hydroxypropyl emthylcellulose 0.3-0.7.
Preferably, the weight ratio of its supplementary material medicine is:
Exemestane 25, mannitol 60, microcrystalline Cellulose 4.5, cross-linking polyethylene pyrrolidone 2, carboxymethyl starch sodium 2, magnesium stearate 0.5, micropowder silica gel 0.5, hydroxypropyl emthylcellulose 0.5.
Or:
Exemestane 25, mannitol 70, microcrystalline Cellulose 6, cross-linking polyethylene pyrrolidone 3, carboxymethyl starch sodium 3, magnesium stearate 0.7, micropowder silica gel 0.7, hydroxypropyl emthylcellulose 0.7.
Or:
Exemestane 25, mannitol 50, microcrystalline Cellulose 3, cross-linking polyethylene pyrrolidone 1, carboxymethyl starch sodium 1, magnesium stearate 0.3, micropowder silica gel 0.3, hydroxypropyl emthylcellulose 0.3.
Present invention also offers the preparation method of above-mentioned Exemestane Tablets, it is made up of following steps:
A the preparation of () binding agent: the hydroxypropyl emthylcellulose taking prescription amount, adds purified water, is stirred to dissolve, makes the binder aqueous solution of 2%, for subsequent use;
B () mixes: get prescription amount exemestane, mannitol, microcrystalline Cellulose, the cross-linking polyethylene pyrrolidone of half amount and carboxymethyl starch sodium and put into wet mixing pelletizer mixing 10 minutes, obtain mixed-powder;
C () is granulated: using 2% binder solution of aequum as binding agent, join in mixed-powder and granulate;
D () granulate is dry: obtained granule is crossed 24 mesh sieves and granulate, dry, obtains dry granule;
E () always mixes: in dry granule, add remaining cross-linking polyethylene pyrrolidone and carboxymethyl starch sodium, then add magnesium stearate and micropowder silica gel, mixing;
F () compress tablet coating, to obtain final product.
The supplementary material part by weight of Exemestane Tablets of the present invention is through a large amount of strict screening test, process certification, just obtain after stability study, just can directly obtain not by preparation teaching material or other reference material, through screening test, process certification, stability study proved invention supplementary material ratio is reasonable, stable preparation process, finished product preparation is stablized, and meets the preparation guideline requirement for tablet of galenic pharmacy and State Food and Drug Administration.
After exemestane tablet preparation of the present invention completes, carry out quality research, work out the method for inspection of indices, and carried out the Method validation of each index detection method according to the guideline of Chinese Pharmacopoeia and new drug research, all methods all meet analysis of pharmaceutical dosage forms requirement, detect according to the Exemestane Tablets of these methods to development and study.
1, according to supplementary material formula and the preparation method of embodiment 1, obtained tablet, in laboratory indices testing result in table 1:
Table 1 laboratory detection result:
From table 1, the indices that laboratory records, all meets the relevant criterion of tablet.
2, according to supplementary material formula and the preparation method of embodiment 1, in three batches that produce under pilot-scale condition, the assay of test agent sees the following form 2.
Table 2 Exemestane Tablets pilot scale sample survey result
From table 2, Exemestane Tablets of the present invention and preparation method thereof, the every monitoring index of the Exemestane Tablets produced is all qualified, can produce the medicine meeting tablet formulation requirement.
3, the three batch sample accelerated tests assay of 6 months, that is: by commercially available back, place the assay of 6 months at 40 DEG C of temperature and relative humidity 75% ± 5% condition.In table 3.
The table 3 three batch sample accelerated test assay of 6 months
| Lot number | Outward appearance | Content (%) | Dissolution (%) | Disintegration (s) | Related substance (%) |
| 050601 | Unchanged | 99.33 | 98.74 | 52 | 0.48 |
| 050602 | Unchanged | 99.34 | 98.61 | 52 | 0.51 |
| 050603 | Unchanged | 99.42 | 98.63 | 53 | 0.47 |
4, three batch samples keep sample the assay of 36 months for a long time, that is: under commercially available back condition, room temperature places the assay after 36 months naturally.In table 4.
Table 4 Exemestane Tablets keeps sample 36 months assays for a long time
| Lot number | Outward appearance | Content (%) | Dissolution (%) | Disintegration (s) | Related substance (%) |
| 050701 | Unchanged | 99.94 | 99.62 | 51 | 0.31 |
| 050702 | Unchanged | 100.25 | 99.50 | 49 | 0.30 |
| 050703 | Unchanged | 100.18 | 99.51 | 50 | 0.32 |
From the result of table 3 and table 4, Exemestane Tablets of the present invention indices under extreme storage condition and room temperature naturalness still meets the formulation requirements of tablet, and visible Exemestane Tablets steady quality of the present invention, can large-scale production.
Detailed description of the invention
Following embodiment is for illustrating the preparation of medicine of the present invention, but it can not form any restriction to scope of the present invention.
Embodiment 1
Supplementary material part by weight: exemestane 25 grams, 60 grams, mannitol, microcrystalline Cellulose 4.5 grams, cross-linking polyethylene pyrrolidone 2 grams, carboxymethyl starch sodium 2 grams, magnesium stearate 0.5 gram, micropowder silica gel 0.5 gram, hydroxypropyl emthylcellulose 0.5 gram.
Preparation method: the preparation of (a) binding agent: the hydroxypropyl emthylcellulose taking prescription amount, adds purified water, is stirred to dissolve, makes the binder aqueous solution of 2%, for subsequent use; ;
B () mixes: get prescription amount exemestane, mannitol, microcrystalline Cellulose, the cross-linking polyethylene pyrrolidone of half amount and carboxymethyl starch sodium and put into wet mixing pelletizer and mix, obtain mixed-powder;
C () is granulated: using 2% binder solution of aequum as binding agent, join in step (b) gained mixed-powder and granulate;
D () granulate is dry: obtained granule is crossed 24 mesh sieves and granulate, dry, obtains dry granule;
E () always mixes: in the dry granule of step (d) gained, add remaining cross-linking polyethylene pyrrolidone and carboxymethyl starch sodium, then add magnesium stearate and micropowder silica gel, mixing.
F () compress tablet coating, to obtain final product.
Embodiment 2
Supplementary material part by weight: exemestane 25 grams, 70 grams, mannitol, microcrystalline Cellulose 6 grams, cross-linking polyethylene pyrrolidone 3 grams, carboxymethyl starch sodium 3 grams, magnesium stearate 0.7 gram, micropowder silica gel 0.7 gram, hydroxypropyl emthylcellulose 0.7 gram.
Preparation method: the preparation of (a) binding agent: the hydroxypropyl emthylcellulose taking prescription amount, adds purified water, is stirred to dissolve, makes the binder aqueous solution of 2%, for subsequent use; ;
B () mixes: get prescription amount exemestane, mannitol, microcrystalline Cellulose, the cross-linking polyethylene pyrrolidone of half amount and carboxymethyl starch sodium and put into wet mixing pelletizer and mix, obtain mixed-powder;
C () is granulated: using 2% binder solution of aequum as binding agent, join in step (b) gained mixed-powder and granulate;
D () granulate is dry: obtained granule is crossed 24 mesh sieves and granulate, dry, obtains dry granule;
E () always mixes: in the dry granule of step (d) gained, add remaining cross-linking polyethylene pyrrolidone and carboxymethyl starch sodium, then add magnesium stearate and micropowder silica gel, mixing.
F () compress tablet coating, to obtain final product.
Embodiment 3
Supplementary material part by weight: exemestane 25 grams, 50 grams, mannitol, microcrystalline Cellulose 3 grams, cross-linking polyethylene pyrrolidone 1 gram, carboxymethyl starch sodium 1 gram, magnesium stearate 0.3 gram, micropowder silica gel 0.3 gram, hydroxypropyl emthylcellulose 0.3 gram.
Preparation method: the preparation of (a) binding agent: the hydroxypropyl emthylcellulose taking prescription amount, adds purified water, is stirred to dissolve, makes the binder aqueous solution of 2%, for subsequent use; ;
B () mixes: get prescription amount exemestane, mannitol, microcrystalline Cellulose, the cross-linking polyethylene pyrrolidone of half amount and carboxymethyl starch sodium and put into wet mixing pelletizer and mix, obtain mixed-powder;
C () is granulated: using 2% binder solution of aequum as binding agent, join in step (b) gained mixed-powder and granulate;
D () granulate is dry: obtained granule is crossed 24 mesh sieves and granulate, dry, obtains dry granule;
E () always mixes: in the dry granule of step (d) gained, add remaining cross-linking polyethylene pyrrolidone and carboxymethyl starch sodium, then add magnesium stearate and micropowder silica gel, mixing.
F () compress tablet coating, to obtain final product.
Claims (1)
1. a preparation method for Exemestane Tablets, the supplementary material of described Exemestane Tablets is: exemestane 25 grams, 60 grams, mannitol, microcrystalline Cellulose 4.5 grams, cross-linking polyethylene pyrrolidone 2 grams, carboxymethyl starch sodium 2 grams, magnesium stearate 0.5 gram, micropowder silica gel 0.5 gram, hydroxypropyl emthylcellulose 0.5 gram; This preparation method comprises the steps:
A the preparation of () binding agent: the hydroxypropyl emthylcellulose taking prescription amount, adds purified water, is stirred to dissolve, makes the binder aqueous solution of 2%, for subsequent use;
B () mixes: get prescription amount exemestane, mannitol, microcrystalline Cellulose, the cross-linking polyethylene pyrrolidone of half amount and carboxymethyl starch sodium and put into wet mixing pelletizer and mix, obtain mixed-powder;
C () is granulated: using 2% binder solution of aequum as binding agent, join in step (b) gained mixed-powder and granulate;
D () granulate is dry: obtained granule is crossed 24 mesh sieves and granulate, dry, obtains dry granule;
E () always mixes: in the dry granule of step (d) gained, add remaining cross-linking polyethylene pyrrolidone and carboxymethyl starch sodium, then add magnesium stearate and micropowder silica gel, mixing;
F () compress tablet coating, to obtain final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN200910075202.1A CN101991553B (en) | 2009-08-21 | 2009-08-21 | Exemestane tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN200910075202.1A CN101991553B (en) | 2009-08-21 | 2009-08-21 | Exemestane tablet and preparation method thereof |
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| CN101991553B true CN101991553B (en) | 2015-02-25 |
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Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103961326A (en) * | 2014-04-18 | 2014-08-06 | 赵辉 | Exemestane orally disintegrating tablet and preparation method thereof |
| CN103948570A (en) * | 2014-04-18 | 2014-07-30 | 赵辉 | Exemestane sustained-release capsule |
| AU2015335375B2 (en) * | 2014-10-24 | 2020-09-10 | Launx Biomedical Co., Ltd. | Use of azelnidipine in preparing medicinal composition for treating cancers |
| CN114557975B (en) * | 2022-03-04 | 2023-04-25 | 河南省人民医院 | Sustained release tablet containing exemestane, process and use thereof |
| CN114948901B (en) * | 2022-05-06 | 2023-04-21 | 郑州大学第一附属医院 | Exemestane nanoparticle and preparation for synergistic treatment of breast cancer and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101039919A (en) * | 2004-10-13 | 2007-09-19 | 惠氏公司 | N-benzenesulfonyl substituted anilino-pyrimidine analogs |
| CN101468023A (en) * | 2007-12-26 | 2009-07-01 | 上海复星医药（集团）股份有限公司 | Exemestane tablet and technique for preparing the same |
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- 2009-08-21 CN CN200910075202.1A patent/CN101991553B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101039919A (en) * | 2004-10-13 | 2007-09-19 | 惠氏公司 | N-benzenesulfonyl substituted anilino-pyrimidine analogs |
| CN101468023A (en) * | 2007-12-26 | 2009-07-01 | 上海复星医药（集团）股份有限公司 | Exemestane tablet and technique for preparing the same |
Non-Patent Citations (1)
| Title |
|---|
| Oral pharmaceutical formulation for anti-neoplastic Agent;Disclosed anonymously;《Research Disclosure》;20071231;第1页 * |
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