CN102319228B - Dutasteride liquid hard capsule and preparation method thereof - Google Patents
Dutasteride liquid hard capsule and preparation method thereof Download PDFInfo
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- CN102319228B CN102319228B CN2011102317101A CN201110231710A CN102319228B CN 102319228 B CN102319228 B CN 102319228B CN 2011102317101 A CN2011102317101 A CN 2011102317101A CN 201110231710 A CN201110231710 A CN 201110231710A CN 102319228 B CN102319228 B CN 102319228B
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Abstract
The invention discloses a dutasteride liquid hard capsule which comprises a hard capsule shell and contents, and the contents comprise dutasteride, a diluent and an anti-oxidant. The invention also discloses a preparation method of the dutasteride liquid hard capsule, which comprises the following steps: weighing dutasteride, the diluent and the anti-oxidant according to the weight composition of the contents, dissolving by stirring, well mixing to obtain a mixture which is the contents, filling the mixture into a hard capsule shell, sealing to obtain the dutasteride liquid hard capsule. The dutasteride liquid hard capsule of the invention has the characteristics of high disintegration and dissolution rate, and good stability, and the preparation method has the characteristics of simple operation, low production cost, and controllable quality.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, be specifically related to a kind of dutasteride's liquid hard capsule and preparation method thereof.
Background technology
The dutasteride is a kind of 5 alpha reductase inhibitors, and 5 alpha-reductases have two hypotypes, i.e. I type and II type, and I type isozyme plays a role to reproductive system, and the testosterone that II type isozyme mainly acts on skin and liver transforms.The dutasteride is 60 times of finasteride to suppressing the 5 alpha-reductase effects of I type, and also very strong to the effect of II type, the dutasteride can suppress testosterone and change dihydrotestosterone (DHT) into, and then suppresses the generation of male DHT, therefore suppresses the prostatic growth of BPH patient.Be mainly used in the treatment of prostatauxe, male pattern alopecia, seborrheic alopecia, hereditary alopecia clinically.
Dutasteride's chemical name:: (5 α, 17 β)-(2, two (trifluoromethyl) phenyl of 5-)-3-oxygen-4-azepine-androstane-1-alkene-17-Methanamide, its chemical structural formula is:
On physical property, the dutasteride is a kind of white and off-white color crystalline powder, and water solublity is relatively poor, and is well-known, the bad stripping that limits the dutasteride of water solublity, and then also limited it and absorb at gastrointestinal.And dutasteride's stability is also bad, is easy to oxidized.
(trade name: An Luda, English name: Avodart), the GlaxoSmithKline PLC product first in U.S.'s listing, was mainly used in anti-prostatic hyperplasia in 2003 to dutasteride's soft capsule.The product and relevant report that also do not have at present dutasteride's liquid hard capsule.
Summary of the invention
The object of the present invention is to provide that a kind of drug release, dissolution rate are fast, dutasteride's liquid hard capsule of good stability.
Another object of the present invention is to provide a kind of method for preparing of dutasteride's liquid hard capsule easy and simple to handle.
The present invention has adopted following technical scheme:
A kind of dutasteride's liquid hard capsule comprises hard capsule case and content, it is characterized in that the weight of said content consists of:
1 part of dutasteride
500～640 parts of diluent
0.1～0.2 part in antioxidant
Said diluent is one or both in sad/certain herbaceous plants with big flowers acid glyceride, the Rikemal B 200;
Said antioxidant is one or both in BHA (BHA), the fourth hydroxy-methylbenzene (BHT).
The weight of the preferred a kind of content of the present invention consists of:
1 part of dutasteride
Sad/640 parts of certain herbaceous plants with big flowers acid glycerides
0.1 part of fourth hydroxy-methylbenzene.
The weight of the preferred another kind of content of the present invention consists of:
1 part of dutasteride
500 parts of Rikemal B 200s
0.1 part of fourth hydroxy-methylbenzene.
The weight of preferred another content of the present invention consists of:
The weight of the present invention is also preferred a kind of content consists of:
1 part of dutasteride
Sad/640 parts of certain herbaceous plants with big flowers acid glycerides
0.2 part of BHA.
The invention also discloses a kind of method for preparing of dutasteride's liquid hard capsule: form by the weight of said content and get dutasteride, diluent and antioxidant; With alr mode dissolving, mixing; The mixture that obtains is content; The mixture filling in hard capsule case, is promptly got dutasteride's liquid hard capsule after the sealing.
Beneficial effect of the present invention has:
(1) adopts diluent of the present invention, can improve dutasteride's dissolubility, and then improve dutasteride's dissolution;
(2) adopt antioxidant of the present invention, can improve dutasteride's stability, it is oxidized that it is not easy under the condition of high temperature and strong illumination;
(3) liquid hard capsule is faster than the disintegration rate of soft capsule in water, thereby has improved the rate of release of medicine;
(4) easy and simple to handle, production cost is low, quality is more stable more, controlled than soft capsule.
The specific embodiment
Further specify the present invention below in conjunction with embodiment.
Embodiment 1: a kind of dutasteride's liquid hard capsule, comprise hard capsule case and content, and wherein, the weight of said content consists of:
Dutasteride 0.5g
Sad/certain herbaceous plants with big flowers acid glyceride 320g
BHT 0.05g
Method for preparing is: form by the weight of said content and get dutasteride, sad/certain herbaceous plants with big flowers acid glyceride and BHT, dutasteride, BHT are joined in sad/certain herbaceous plants with big flowers acid glyceride, mechanical agitation dissolving, mixing; In order to accelerate dissolved speed; Can under 30 ℃～50 ℃, stir, the mixture that obtains is content, with the mixture filling in hard capsule case; Promptly get dutasteride's liquid hard capsule with gelatin-sealed, process 1000 altogether.
Embodiment 2: the weight of content consists of:
Dutasteride 0.5g
Rikemal B 200 250g
BHT 0.05g
Method for preparing is with embodiment 1.
Embodiment 3: the weight of content consists of:
Method for preparing is with embodiment 1.
Embodiment 4: the weight of content consists of:
Dutasteride 0.5g
Sad/certain herbaceous plants with big flowers acid glyceride 320g
BHA 0.1g
Method for preparing is with embodiment 1.
Embodiment 5: the weight of content consists of:
Method for preparing is with embodiment 1.
Embodiment 6 (Comparative Examples): the weight of content consists of:
Dutasteride 0.5g
Sad/certain herbaceous plants with big flowers acid glyceride 320g
Method for preparing is with embodiment 1.
Test Example 1: the screening test of diluent kind and consumption.
This test mixes the 50mg dutasteride respectively with sad/certain herbaceous plants with big flowers acid glyceride, the Rikemal B 200 of different amounts, observe the dissolving situation of dutasteride in different diluent, and result of the test is seen table 1.
The dissolubility test of table 1 dutasteride in diluent
Can find out from last table, when with the 50mg dutasteride sad with 32g/certain herbaceous plants with big flowers acid glyceride or 25g Rikemal B 200 or 15g be sad/when certain herbaceous plants with big flowers acid glyceride and 12g Rikemal B 200 mixed, solute effect was best.
Test Example 2: the dissolution contrast test of dutasteride's liquid hard capsule and dutasteride's soft capsule.
Table 2 dutasteride's liquid hard capsule of the present invention stripping curve
Can find out that from last table the dissolution rate of dutasteride's liquid hard capsule of embodiment 1～4 is obviously faster than dutasteride's soft capsule.
Test Example 3: the stable contrast test of dutasteride's liquid hard capsule and dutasteride's soft capsule.
With dutasteride's liquid hard capsule and dutasteride's soft capsule respectively 60 ℃ with the high temperature of 6000LX and strong illumination condition held 10 days, detection dutasteride's content.Testing result and the testing result after the off-test before on-test are seen table 3,4,5 respectively.
The testing result of table 3 before on-test
| Project | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Comparative Examples | Soft capsule |
| Content | 99.2％ | 99.8％ | 99.4％ | 99.2％ | 98.6 | 100.2％ |
10 days testing results of 60 ℃ of tests of table 4 influence factor high temperature
| Project | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Comparative Examples | Soft capsule |
| Content | 98.4％ | 100.1％ | 99.1％ | 99.6％ | 93.2％ | 98.4％ |
10 days testing results of table 5 influence factor strong illumination test
| Project | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Comparative Examples | Soft capsule |
| Content | 98.8％ | 99.3％ | 100.2％ | 99.6％ | 96.2％ | 98.4％ |
Can find out that from table 3,4,5 content of embodiment 1～4 is highly stable, and the Comparative Examples content that does not add antioxidant declines by a big margin.Simultaneously, the content of soft capsule also has a declining tendency, and shows that the antioxidant that the present invention screens is better than the antioxidant effect in the existing soft capsule.
Claims (4)
1. dutasteride's liquid hard capsule comprises hard capsule case and content, it is characterized in that said content is made up of dutasteride, diluent, antioxidant, and said diluent is one or both in caprylic/capric glyceride, the Rikemal B 200; Said antioxidant is one or both in BHA, the fourth hydroxy-methylbenzene, and the weight of said content consists of:
2. dutasteride's liquid hard capsule according to claim 1 is characterized in that the weight of said content consists of:
1 part of dutasteride
640 parts of caprylic/capric glyceride
0.1 part of fourth hydroxy-methylbenzene.
3. dutasteride's liquid hard capsule according to claim 1 is characterized in that the weight of said content consists of:
1 part of dutasteride
640 parts of caprylic/capric glyceride
0.2 part of BHA.
4. according to the method for preparing of each described dutasteride's liquid hard capsule in the claim 1～3; It is characterized in that getting dutasteride, diluent and antioxidant by the weight composition of said content; With alr mode dissolving, mixing; The mixture that obtains is content, and the mixture filling in hard capsule case, is promptly got dutasteride's liquid hard capsule after the sealing.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN2011102317101A CN102319228B (en) | 2011-08-12 | 2011-08-12 | Dutasteride liquid hard capsule and preparation method thereof |
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| CN2011102317101A CN102319228B (en) | 2011-08-12 | 2011-08-12 | Dutasteride liquid hard capsule and preparation method thereof |
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| Publication Number | Publication Date |
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| CN102319228A CN102319228A (en) | 2012-01-18 |
| CN102319228B true CN102319228B (en) | 2012-11-28 |
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| CN103830201A (en) * | 2012-11-20 | 2014-06-04 | 重庆医药工业研究院有限责任公司 | Dutasteride liquid soft capsules |
| CN104069084B (en) * | 2013-03-25 | 2019-06-25 | 重庆华邦制药有限公司 | A kind of dutasteride's soft capsule that quality is stable |
| CN104257665A (en) * | 2014-09-01 | 2015-01-07 | 南京正大天晴制药有限公司 | Oral solid preparation of dutasteride and preparation method thereof |
| CN109394723B (en) * | 2017-08-17 | 2020-11-24 | 海南皇隆制药股份有限公司 | Dutasteride soft capsule and preparation method thereof |
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| CN102145003B (en) * | 2010-02-08 | 2015-04-22 | 张立英 | Medicinal composition containing insoluble medicament |
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Address after: 430056, No. three, No. 9, Maple Road, Wuhan economic and Technological Development Zone, Hubei, Wuhan Patentee after: Ferguson (Wuhan) Biological Technology Co., Ltd. Address before: 430056, building 8, hi tech Industrial Park, Wuhan economic and Technological Development Zone, Wuhan, Hubei Patentee before: Ferguson (Wuhan) Biological Technology Co., Ltd. |
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Address after: 430056, No. three, No. 9, Maple Road, Wuhan economic and Technological Development Zone, Hubei, Wuhan Patentee after: FERGUSON (WUHAN) BIOTECHNOLOGY CO., LTD. Address before: 430056, No. three, No. 9, Maple Road, Wuhan economic and Technological Development Zone, Hubei, Wuhan Patentee before: Ferguson (Wuhan) Biological Technology Co., Ltd. |