CN1180521A - Medicinal composite containing megestrol acetate - Google Patents
Medicinal composite containing megestrol acetate Download PDFInfo
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- CN1180521A CN1180521A CN 97118976 CN97118976A CN1180521A CN 1180521 A CN1180521 A CN 1180521A CN 97118976 CN97118976 CN 97118976 CN 97118976 A CN97118976 A CN 97118976A CN 1180521 A CN1180521 A CN 1180521A
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- megestrol acetate
- starch
- polyethylene glycol
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- magnesium stearate
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Abstract
A medicinal composition containg megace in the form of capsule or tablet features large dosage but small size. Its preparing process includes fusing polyethylene glycol or dissolving polyethylene glycol in alcohol, addition of powdered megestrol acetate and starch, and making capsules or tablets.
Description
The present invention relates to progestogens medicine megestrol acetate is the Pharmaceutical composition of main component preparation, is heavy dose of specification megestrol acetate capsule and tablet and preparation method thereof specifically.
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, nineteen ninety-five version begin to record 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 has effect of malignant tumors such as treatment breast carcinoma, carcinoma of endometrium, and can improve patient's appetite, and weight increase improves cancer patient's life quality.Adapt to heavy dose of clinically needs of using, U.S. Shi Guibao company (Bristol-Mgers Squibb Company) has released heavy dose of specification of 160mg/ sheet, enters Chinese Hospitals the nineties and uses.But the pharmaceutical formulation of this big specification tablet and preparation technology do not see record in open source literature.
Use megestrol acetate treatment malignant tumor, its consumption can reach 1600mg every day, each 400mg.Use conventional tablet, will take tens of at every turn, even up to a hundred.The big specification tablet of 160mg/ sheet that uses U.S. Shi Guibao company to produce, though it is few to take a number at every turn, every is big as Semen arachidis hypogaeae, patient is difficult to swallow.Particularly did the cancer patient after radiotherapy, the chemotherapy, had a delicate constitution, the just difficulty more of granule is big, total amount is big tablet of swallowing several times every day, even can not accomplish.
Simultaneously, because megestrol acetate belongs to acidic drug, when low dose was in the past used, it was faint to acid stimulation of gastrointestinal.Along with the use of treatment malignant tumor, its consumption is increasing, just stimulates significantly to get up to gastrointestinal is acid, becomes the heavy dose of obstacle that uses of restriction.Though it is well-known, make capsule, particularly enteric coated capsule can subtract the acidity stimulation of medicine to stomach, but presses usual method, for example using hydroxy methocel, starch, micropowder silica gel etc. is main adjuvant, and made megestrol acetate granule all can not directly incapsulate.Its difficulty has two: one, and amount is too big, both has been No. 1 capsule with the capacity maximum, and 1 also is unable to hold and contains the amount of formulation of megestrol acetate 160mg; The 2nd, its particulate flowability is too poor, can not carry out the operation of dress capsule.In the pharmacopeia of Chinese Pharmacopoeia and world major country, all there is not the record of megestrol acetate capsule so far.
The object of the present invention is to provide a kind of megestrol acetate preparation, said preparation is under the prerequisite that guarantees the principal agent heavy dose, by selecting adjuvant and formulation method for use, make the finished medicines volume little, simultaneously have good dissolution again, reach high bioavailability, adapt to the needs of clinical practice.
The technical scheme that realizes the object of the invention is, selecting an amount of Polyethylene Glycol for use is the basic adjuvant of pharmacy, with its fusion or be dissolved in alcoholic solution, mix with the principal agent megestrol acetate, drink with other adjuvants such as amount of starch and magnesium stearate, make the less heavy dose of specification megestrol acetate capsule of volume, also can make tablet.
The prescription of megestrol acetate preparation of the present invention is,
Megestrol acetate 100 weight portion Polyethylene Glycol 2-40 weight portions
Starch 2-50 weight portion magnesium stearate 0.2-30 weight portion
In the pharmaceutical formulation of the present invention, be 100 weight portions with the consumption of megestrol acetate, used Polyethylene Glycol is the 2-40 weight portion.If the consumption of Polyethylene Glycol is less than 2 weight portions, then the principal agent megestrol acetate is difficult to be uniformly dispersed, and its volume can not reduce significantly, does not reach the purpose that makes the preparation finished-product volume little; If the consumption of Polyethylene Glycol has also increased the volume of patent medicine greater than 400 weight fraction.Usually the consumption of Polyethylene Glycol is the 30-40 weight portion, with 33 weight portions for the suitableeest.
Use amount of starch to play filling effect in the preparation of the present invention, improve the particulate dispersion situation of pharmacy, make the disintegration of preparation, dissolution all reach level preferably.When the consumption of megestrol acetate was 100 weight portions, the consumption of starch was the 2--50 weight portion.If the starch consumption is less than 2 weight portions, then the content difference of principal agent megestrol acetate can be bigger in every patent medicine; If the consumption of starch is greater than 50 weight portions then unnecessarily increased the weight and volume of patent medicine.When producing capsule, the consumption of starch in low ratio, is generally the 10--20 weight portion in above-mentioned scope, with 15 weight portions for the suitableeest.When producing tablet, the consumption of starch by higher proportion, is generally the 30--50 weight portion in above-mentioned scope, with 40 weight portions for the suitableeest.
Use magnesium stearate to increase the particulate flowability of pharmacy in the preparation of the present invention, be convenient to produce the operation of capsule fashionable dress capsule.When the consumption of megestrol acetate was 100 weight portions, the consumption of magnesium stearate was the 0.2-30 weight portion.When its consumption was less than 0.2 weight portion, then the particulate flowability of pharmacy was too poor, was difficult to carry out the dress capsule operation of capsule; If the consumption of Polyethylene Glycol greater than 30 weight portions, has then unnecessarily increased the weight and volume of patent medicine.Usually the consumption of magnesium stearate is the 2-5 weight portion, with 3 weight portions for the suitableeest.When producing tablet, can use magnesium stearate in the above ratio of producing capsule, also can not use magnesium stearate.
In the pharmaceutical technology, key is the processing to the adjuvant Polyethylene Glycol.Its preferable methods is to utilize Polyethylene Glycol 60 ℃ of-63 ℃ of fused characteristics, and heating once adds required megestrol acetate and starch with the Polyethylene Glycol fusion, stir, at room temperature add magnesium stearate again after the cooling, stir evenly, incapsulate or make tablet.Another kind method is earlier Polyethylene Glycol to be dissolved in Different concentrations of alcohol solution, adds required megestrol acetate and starch, stirs, and drying and granulating adds magnesium stearate again, stirs evenly, and incapsulates or make tablet.
The invention will be further described by the following examples.
Embodiment 1 produces 1000 of megestrol acetate 160mg capsules
Get
Megestrol acetate 160g Polyethylene Glycol-6000 50g
Starch 25g magnesium stearate 3g
1. megestrol acetate, starch are crossed 100 mesh sieves respectively, standby.
2. Polyethylene Glycol-6000 is heated to 60-63 ℃, treat that its complete fusion is for liquid, above-mentioned powdered megestrol acetate and the starch of getting ready is poured into, stir, place room temperature and cross 40 mesh sieves after 5 hours, add magnesium stearate again, stir evenly, branch was packed 1000 capsules into promptly after chemical examination content met the pharmacopeia required standard.Every capsules contains megestrol acetate 160mg.
Embodiment 2 produces 1000 in megestrol acetate 160mg tablet
Get
Megestrol acetate 160g Polyethylene Glycol-6000 50g
Starch 80g magnesium stearate 3g
1. megestrol acetate, starch are crossed 100 mesh sieves respectively, standby.
2. Polyethylene Glycol-6000 is joined in 2000 milliliters of 40% alcoholic solution, stirs, treat that it dissolves fully after, add above-mentioned megestrol acetate of getting ready and starch, stir, dry granulate, chemical examination content meets after the pharmacopeia required standard 1000 of tablettings, and every contains megestrol acetate 160mg.
Megestrol acetate preparation of the present invention can be made 160mg/ capsules (or sheet), even 240mg/ capsules (or sheet).The particulate flowability of preparation process Chinese medicine, dispersibility are all better.The volume and weight of patent medicine has only U.S. Shi Guibao company with about 1/2nd of dosage specification tablet, is convenient to patient and swallows.Simultaneously, capsule of the present invention can be avoided the acidity of stomach is stimulated when using enteric coated capsule fully.When using conventional capsule, also can avoid substantially the acidity of stomach is stimulated.
Claims (9)
1. contain the Pharmaceutical composition of megestrol acetate, it is characterized in that, contain megestrol acetate, Polyethylene Glycol, starch in the said preparation.
2. the Pharmaceutical composition that contains megestrol acetate as claimed in claim 1 is characterized in that, when megestrol acetate content was 100 weight portions, the content of Polyethylene Glycol was the 2-40 weight portion.
3. the Pharmaceutical composition that contains megestrol acetate as claimed in claim 1 is characterized in that, when megestrol acetate content was 100 weight portions, contents of starch was the 2-50 weight portion.
4. the Pharmaceutical composition that contains megestrol acetate as claimed in claim 1 is characterized in that it also contains magnesium stearate.
5. as claim 1 and the 4 described Pharmaceutical compositions that contain megestrol acetate, it is characterized in that when megestrol acetate content was 100 weight portions, the content of magnesium stearate was the 0.2-30 weight portion.
6. as claim 1 and the 4 described Pharmaceutical compositions that contain megestrol acetate, it is characterized in that its finished medicines is a capsule.
7. as claim 1, the 4 and 6 described Pharmaceutical compositions that contain megestrol acetate, it is characterized in that its preparation technology is first with the Polyethylene Glycol heating and melting, adds megestrol acetate and starch, add magnesium stearate after the cooling again, incapsulating becomes capsule formulation.
8. as claim 1, the 4 and 6 described Pharmaceutical compositions that contain megestrol acetate, it is characterized in that, its preparation technology is dissolved in alcoholic solution with Polyethylene Glycol earlier, add megestrol acetate and starch, dry granulate, add magnesium stearate again, stir evenly into granule and incapsulate and become capsule formulation.
9. the Pharmaceutical composition that contains megestrol acetate as claimed in claim 1 is characterized in that, its preparation technology is dissolved in alcoholic solution with Polyethylene Glycol earlier, adds megestrol acetate and starch, and dry granulate is pressed into tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 97118976 CN1180521A (en) | 1997-10-09 | 1997-10-09 | Medicinal composite containing megestrol acetate |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 97118976 CN1180521A (en) | 1997-10-09 | 1997-10-09 | Medicinal composite containing megestrol acetate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1180521A true CN1180521A (en) | 1998-05-06 |
Family
ID=5175101
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 97118976 Pending CN1180521A (en) | 1997-10-09 | 1997-10-09 | Medicinal composite containing megestrol acetate |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1180521A (en) |
Cited By (3)
| 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 |
| CN100434077C (en) * | 2002-02-09 | 2008-11-19 | 浙江万联药业有限公司 | Megestrol acetate capsule composition |
| CN108186586A (en) * | 2018-03-01 | 2018-06-22 | 常州市第四制药厂有限公司 | A kind of Allylestrenol tablet and preparation method thereof |
-
1997
- 1997-10-09 CN CN 97118976 patent/CN1180521A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100434077C (en) * | 2002-02-09 | 2008-11-19 | 浙江万联药业有限公司 | Megestrol acetate capsule composition |
| CN100423724C (en) * | 2006-03-31 | 2008-10-08 | 程雪翔 | Medicine for treating endometriosis and its prepn |
| CN108186586A (en) * | 2018-03-01 | 2018-06-22 | 常州市第四制药厂有限公司 | A kind of Allylestrenol tablet and preparation method thereof |
| CN108186586B (en) * | 2018-03-01 | 2020-12-29 | 常州市第四制药厂有限公司 | Allylestrenol tablet and preparation method thereof |
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| SE01 | Entry into force of request for substantive examination | ||
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| C01 | Deemed withdrawal of patent application (patent law 1993) | ||
| WD01 | Invention patent application deemed withdrawn after publication |