CN100434077C - Megestrol acetate capsule composition - Google Patents
Megestrol acetate capsule composition Download PDFInfo
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- CN100434077C CN100434077C CNB021042101A CN02104210A CN100434077C CN 100434077 C CN100434077 C CN 100434077C CN B021042101 A CNB021042101 A CN B021042101A CN 02104210 A CN02104210 A CN 02104210A CN 100434077 C CN100434077 C CN 100434077C
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- megestrol acetate
- soft capsule
- glycerol
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Abstract
The present invention relates to a stable liquid soft capsule composition containing a soft capsule which is suitable for the preparation of megestrol acetate; more specifically, the present invention relates to a liquid content which is suitable for the preparation of soft capsules. Megestrol acetate is used as an active ingredient, and glycerol is used as an auxiliary surface active agent, a solvent component and a surface active agent. The present invention also relates to a soft capsule preparation which comprises a suspensoid content. The present invention relates to a megestrol acetate soft capsule which comprises main medicine of megestrol acetate, the sufficient quantity of glycerol, the proper quantity of solvent, the surface active agent, etc. which are prepared into suspensoid liquid for oral administration, wherein the megestrol acetate in the capsule is differentiated, and thus, the megestrol acetate of medicines without water solubility has high biological availability and fast effect taking, and overcomes the defect of low biological availability of conventional tablets. Simultaneously, the product is used as a novel preparation, and can provide the possibility of the selection of new and good preparations for patients and doctors.
Description
The present invention relates to contain the stable liquid capsule composition of the soft capsule that is suitable for preparing megestrol acetate.More particularly, the present invention relates to a kind of liquid content that is suitable for being mixed with soft capsule, it contains megestrol acetate as active component, and glycerol also relates to the soft capsule preparation that contains described suspendible shape content as cosurfactant, solvent composition and surfactant.
Megestrol acetate (Megestrol Acetate) is a kind of progestogens medicine of U.S. Searle company nineteen fifty-nine invention, is used for the treatment of gynaecopathias such as menoxenia.Chinese Pharmacopoeia records its crude drug since version in 1985, and 1996 and version in 2000 are recorded its tablet, but its specification only is the low dose of specification of 1mg, 4mg.After the eighties, medical circle finds that heavy dose of megestrol acetate is used for the treatment of treatment for cancer such as hormone-sensitive type cancer such as carcinoma of endometrium, breast carcinoma, carcinoma of prostate, renal carcinoma, have stimulate appetite, weight increase, improve the life quality and the dyscrasic effect of AIDS VICTIMS of patient with advanced cancer; And heavy dose of megestrol acetate that uses also has the effect of the chronic pain that alleviates the cancer patient, and its analgesic effect does not rely on anticancer effect, has dependency preferably between analgesic effect and blood drug level.Neoplastic bone cancerometastasis patient's pain often is difficult to be alleviated by NSAID (non-steroidal anti-inflammatory drug), and heavy dose of megestrol acetate has better pain relieving effect.Recorded in the national essential drugs handbook.The oral formulations that present China uses clinically is the tablet Megace megace (trade name) that U.S. Shi Guibao company produces, and specification is the 160mg/ sheet, and the tablet specification that the Shi Guibao company that American Pharmacopeia records produces is 40mg and 20mg.The patent that in December, 1992 U.S. Bristol-Myers SquibbCompany345 Park Avenue has applied for the flocculation suspensoid (aqueous) of megestrol acetate, the patent No. is: 0519351A2, the patent that calendar year 2001 JIUYUE Pharmaceutical Resources Inc has also applied for the flocculation suspensoid (aqueous) of megestrol acetate, application number is US2001/0048931A1.Do not see the report of the patent of relevant megestrol acetate capsule so far as yet.
Use megestrol acetate treatment malignant tumor, its consumption per day every day is 40mg～320mg, once or part vic, this product is a megestrol acetate capsule, wherein in the preparation megestrol acetate through micronized, can guarantee water-insoluble drug megestrol acetate high bioavailability, and rapid-action, overcome the lower shortcoming of conventional tablet bioavailability; Simultaneously, this product can provide the possibility of a kind of renewal, better dosage form selection for doctor and patient as a kind of novel form.
The object of the present invention is to provide a kind of megestrol acetate novel formulation, said preparation is guaranteeing under the suitable prerequisite of principal agent dosage, by selecting adjuvant and formulation method for use, megestrol is made suspension to be wrapped in and to make soft capsule in the rubber, help oral, the absorption of medicine, reach high bioavailability.Simultaneously, also be clinical a kind of renewal, the better dosage form selection of providing.
Soft capsule preparation of the present invention, soft capsule content mainly are made up of following material and weight ratio:
Megestrol acetate 1
Glycerol 1.2～3
Vegetable oil or Polyethylene Glycol 7～10
In tween, span, Cera Flava, stearic acid, the arabic gum one or more 0.8～2.
The preferred soybean oil of vegetable oil wherein.The preferred PEG400 of Polyethylene Glycol wherein.Preferably contain 40 milligrams of megestrol acetates in every soft capsule.
Be described more specifically the present invention by the following example.But these embodiment should not be construed as the restriction to any aspect of the present invention.
Embodiment 1
The 4.0g megestrol acetate is added in the 7.0g glycerol.Stirring is dispersed in the glycerol megestrol acetate, adds the soybean oil of 4.0g Arlacel-80 and 30g again, fully stirs, and is A liquid; Get in the soybean oil that the 0.40g Cera Flava is dissolved in 10g, be B liquid; Merge A liquid and B liquid, cross colloid mill and grind up to becoming the uniform solution of suspendible.The suspension that obtains like this is incorporated in the machine of preparation soft capsule, regulates this machine and make the suspendible medicinal liquid that injects 0.55g in each soft capsule, preparation contains the soft capsule of megestrol acetate suspension in gelatin shell.
Embodiment 2
Preparing the soft capsule with following composition according to same steps as among the embodiment 1, is the consumption difference as the glycerol of cosurfactant.
2-A constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 40
Arlacel-80 40
Cera Flava 4.0
Soybean oil 400
Amount to 524mg
2-B constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 100
Arlacel-80 40
Cera Flava 4.0
Soybean oil 400
Amount to 584mg
Embodiment 3
Prepare soft capsule according to embodiment 1 identical step, just the composition of surfactant and its changes of contents with following composition.
3-A constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Arlacel-80 60
Cera Flava 4.0
Soybean oil 400
Amount to 574mg
3-B constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Arlacel-80 100
Cera Flava 5.0
Soybean oil 400
Amount to 615mg
3-C constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Arlacel-80 40
Tween 80 10
Stearic acid 5.0
Soybean oil 400
Amount to 565mg
3-D constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Arlacel-80 30
Tween-60 25
Cera Flava 5.0
Soybean oil 400
Amount to 570mg
3-E constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Arlacel-60 30
Tween 80 20
Cera Flava 4.0
Soybean oil 400
Amount to 564mg
3-F constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Methylcellulose 15
Tween-40 45
Arabic gum 5.0
Soybean oil 400
Amount to 570mg
Embodiment 4
Composition and the preparation of its consumption according to surfactant among preparation of the same steps as of embodiment 1 and the embodiment 3 have following soft capsule, just oily changes of contents.
4-A constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Arlacel-80 60
Cera Flava 4.0
Soybean oil 300
Amount to 474mg
4-B constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Arlacel-80 100
Cera Flava 5.0
Soybean oil 250
Amount to 465mg
4-C constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Arlacel-80 40
Tween 80 10
Stearic acid 5.0
Soybean oil 300
Amount to 465mg
Embodiment 5
Composition and its consumption soft capsule of having following solvent and different surfaces activating agent according to the same steps as preparation of embodiment 1.
5-A constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Tween 80 40
Arlacel-80 15
Cera Flava 5.0
PEG400 400
Amount to 570mg
5-B constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Tween 80 60
Arlacel-60 10
Cera Flava 4.0
PEG400 300
Amount to 484mg
5-C constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Tween-60 80
Arlacel-20 20
Stearic acid 5.0
PEG400 300
Amount to 515mg
5-D constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Tween 80 45
Methylcellulose 15
Arabic gum 5.0
PEG400 300
Amount to 475mg
5-E constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Tween 80 85
Cera Flava 5.0
Liquid Macrogol
Amount to 500mg
Embodiment 6
The soft capsule that has following composition according to embodiment 1 identical step preparation.
6-A constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Arlacel-80 30
Soybean oil 3 50
Amount to 490mg
6-B constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Stearic acid 5.0
Soybean oil 300
Amount to 415mg
6-C constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Arabic gum 10
Soybean oil 300
Amount to 420mg
6-D constituent content (mg/ grain)
Megestrol acetate 40
Glycerol 70
Cera Flava 5.0
Polyethylene Glycol 350
Amount to 465mg
Claims (4)
1, the soft capsule preparation of megestrol acetate, soft capsule content mainly is made up of following material and weight ratio:
Micronized megestrol acetate 1
Glycerol 1.2～3
Vegetable oil or Polyethylene Glycol 7～10
In tween, span, Cera Flava, stearic acid, the arabic gum one or more 0.8～2.
2, the soft capsule preparation of claim 1, wherein vegetable oil is a soybean oil.
3, the soft capsule preparation of claim 1, wherein Polyethylene Glycol is a PEG400.
4, the soft capsule preparation of claim 1 wherein contains 40 milligrams of megestrol acetates in every soft capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021042101A CN100434077C (en) | 2002-02-09 | 2002-02-09 | Megestrol acetate capsule composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021042101A CN100434077C (en) | 2002-02-09 | 2002-02-09 | Megestrol acetate capsule composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1436534A CN1436534A (en) | 2003-08-20 |
| CN100434077C true CN100434077C (en) | 2008-11-19 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB021042101A Expired - Fee Related CN100434077C (en) | 2002-02-09 | 2002-02-09 | Megestrol acetate capsule composition |
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Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100423724C (en) * | 2006-03-31 | 2008-10-08 | 程雪翔 | Medicine for treating endometriosis and its prepn |
| CN105878205A (en) * | 2014-12-31 | 2016-08-24 | 天津康鸿医药科技发展有限公司 | Oral preparation for treating asthma |
| CN106109435B (en) * | 2016-07-09 | 2018-11-06 | 南京臣功制药股份有限公司 | A kind of megestrol acetate capsule and preparation method thereof |
| CN107875135A (en) * | 2017-11-29 | 2018-04-06 | 浙江安宝药业有限公司 | Megestrol acetate capsule and preparation method |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1180521A (en) * | 1997-10-09 | 1998-05-06 | 海南诚成药业有限公司 | Medicinal composite containing megestrol acetate |
| US6028065A (en) * | 1998-04-20 | 2000-02-22 | Pharmaceutical Resources, Inc. | Flocculated suspension of megestrol acetate |
-
2002
- 2002-02-09 CN CNB021042101A patent/CN100434077C/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1180521A (en) * | 1997-10-09 | 1998-05-06 | 海南诚成药业有限公司 | Medicinal composite containing megestrol acetate |
| US6028065A (en) * | 1998-04-20 | 2000-02-22 | Pharmaceutical Resources, Inc. | Flocculated suspension of megestrol acetate |
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| CN1436534A (en) | 2003-08-20 |
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