CN103933017A - Progesterone slow-release capsule - Google Patents
Progesterone slow-release capsule Download PDFInfo
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- CN103933017A CN103933017A CN201410116471.9A CN201410116471A CN103933017A CN 103933017 A CN103933017 A CN 103933017A CN 201410116471 A CN201410116471 A CN 201410116471A CN 103933017 A CN103933017 A CN 103933017A
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- slow releasing
- progesterone
- releasing capsule
- progesterone slow
- acrylic resin
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Abstract
A progesterone slow-release capsule is composed of, in percent by weight, 5-50% of progesterone, 55-90% of an excipient, 3-10% of a film coating material, 0-10% of a wetting agent and 1-2% of an adhesive. The preparation method of the progesterone slow-release capsule employs (1) extrusion-spheronization method, (2) powder coating method and (3) liquid-phase sedimentation method for preparing the progesterone slow-release capsule.
Description
Invention field
The present invention relates to a kind of slow releasing capsule, particularly a kind of Progesterone slow releasing capsule.
Background of invention
Progesterone, has another name called progesterone, gestogen, is a kind of progestogen, in menstrual phase, can make endometrial gland bulk-growth, metremia, and intimal thickening, for the implantable endocardial of germ cell is got ready.After germ cell is implanted, make it to produce Placenta Hominis, reduce simultaneously gravid uterus irritability, suppress its activity, so that fetal well-being growth.With estrogenic combined effect under, impel breast to reach full growth, for lactation is prepared.In addition, can also suppress ovary ovulation.Be applicable to dysfunctional uterine hemorrhage, dysmenorrhea, menorrhagia, amenorrhea, threatened abortion, habitual abortion and advanced breast cancer etc.Untoward reaction is even nauseating, vomiting, dizziness, headache etc., sometimes can cause distending pain of the breast.
Domestic existing progesterone preparation mainly comprises at present: capsule, soft gelatin capsule, gel, sustained-release gel, soft capsule, Transdermal absorption frost, injection etc.
Progesterone slow releasing capsule prepared by the present invention has the slow-release function of 24 hours, can effectively control the burst size of medicine, and safety, effectiveness are better; Because being pilule, large at gastrointestinal tract distribution area, improved Progesterone dissolubility, bioavailability is high, and zest is little; Can make blood drug level reach rapidly curative effect concentration, maintain steady, long valid density, blood concentration fluctuation is little; Be beneficial to the toxic and side effects that reduces medicine; Reduced patient's medicining times; Steady quality.
Summary of the invention
The object of the present invention is to provide a kind of Progesterone slow releasing capsule, it can overcome current Progesterone general formulation release amount of medicine can not effectively control, and causes safety, the poor shortcoming of effectiveness, and can reduce medication accumulated dose and good effect.Concrete technical scheme is as follows:
On the one hand, the present invention relates to a kind of Progesterone slow releasing capsule, it is comprised of Progesterone, excipient, thin film coating material, wetting agent, stabilizing agent and binding agent, wherein each component by weight Progesterone be 5～50%, excipient is 55～90%, thin film coating material is 3～10%, and wetting agent is 0～10% and binding agent 1～2%.
In some embodiments, Progesterone slow releasing capsule of the present invention, it is a kind of pilule with slow releasing function.
In some embodiments, Progesterone slow releasing capsule of the present invention, wherein, the excipient in described Progesterone slow releasing capsule is the one or more combination in cellulose family, starch, lactose and calcium bicarbonate.
In other embodiments, Progesterone slow releasing capsule of the present invention, wherein, the cellulose family excipient in described Progesterone slow releasing capsule is ethyl cellulose, hydroxypropyl emthylcellulose, microcrystalline Cellulose, acrylic resin I, acrylic resin II, acrylic resin III or acrylic resin IV.
Some embodiments therein, Progesterone slow releasing capsule of the present invention, wherein, the thin film coating material in described Progesterone slow releasing capsule is one or both combinations in Aquacoat and aqueous acrylic resin dispersion.
Some embodiments therein, Progesterone slow releasing capsule of the present invention, the wetting agent in wherein said Progesterone slow releasing capsule is one or both the mixing in water or ethanol.
Some embodiments therein, Progesterone slow releasing capsule of the present invention, wherein, the binding agent in described Progesterone slow releasing capsule is the one or more combination in cellulose family, resinae, saccharide, gelatin.
Some embodiments therein, Progesterone slow releasing capsule of the present invention, wherein, the cellulose family binding agent in described Progesterone slow releasing capsule is water or the alcoholic solution of hydroxypropyl emthylcellulose, ethyl cellulose.
Some embodiments therein, Progesterone slow releasing capsule of the present invention, wherein, the resinae binding agent in described Progesterone slow releasing capsule is acrylic resin I, acrylic resin II, acrylic resin III or acrylic resin IV.
Some embodiments therein, Progesterone slow releasing capsule of the present invention, wherein, the saccharide binding agent in described Progesterone slow releasing capsule is maltose.
The specific embodiment
The preparation technology of above-mentioned Progesterone slow releasing capsule, it adopts following several technique to prepare:
(1) extrude spheronization: utilize and extrude round as a ball comminutor, crude drug and mixed with excipients are crossed to 80 eye mesh screens, after with adhesive, mixed powder being squirted, extrude the round as a ball ball of making in extruding round as a ball comminutor, after being dried, sieve and obtain the pastille micropill that certain order is counted size.In fluidized bed coating pot, with Aquacoat, carry out coating and get final product;
(2) powder coating method: utilize atresia coating pan, Corm Eleocharitis type coating pan, fluid bed top spray (or end spray) seed-coating machine, fluid bed tangent line spray ball mechanism ball.The Corm Eleocharitis type coating pan of take is example: medicated powder and mixed with excipients are crossed to 80 eye mesh screens, get the micropill (sucrose ball or microcrystalline Cellulose ball) of certain order number and put into Corm Eleocharitis type coating pan, after micropill surface being squirted with adhesive, a small amount of mixed powder is sprinkled in pot, make mixed powder be wrapped in uniformly the surface of micropill, and then squirt micropill surface and add again powder, until mixed powder all adds, after being dried, sieve and obtain the pastille micropill that certain order is counted size.In fluidized bed coating pot, with Aquacoat, carry out coating and get final product;
(3) liquid phase deposition: can utilize atresia coating pan, Corm Eleocharitis type coating pan, fluid bed top spray (or end spray) seed-coating machine, fluid bed tangent line spray ball mechanism ball.The Corm Eleocharitis type coating pan of take is example: the micropill (sucrose ball or microcrystalline Cellulose ball) of getting certain order number is put into Corm Eleocharitis type coating pan, medicated powder and excipient is molten in adhesive, the Surface Edge spray limit that mixed liquor is sprayed onto to micropill is dry, until mixed liquor has all sprayed, after being dried, sieve and obtain the pastille micropill that certain order is counted size.In fluidized bed coating pot, with Aquacoat, carry out coating and get final product.
Embodiment
Embodiment 1:
A Progesterone slow releasing capsule, it is comprised of 20% Progesterone, 75% excipient, 3% thin film coating material, 1% wetting agent and 1% binding agent.Wherein excipient is microcrystalline Cellulose, and thin film coating material is Aquacoat, and wetting agent is 75% alcoholic solution, and binding agent is the aqueous solution of hydroxypropyl emthylcellulose.Make 1000.
Progesterone slow releasing capsule a preparation technology, it adopts following technique to prepare:
Spheronization is extruded in utilization: utilize and extrude round as a ball comminutor; crude drug was mixed to 80 eye mesh screens with microcrystalline Cellulose; after mixed powder being squirted with the aqueous solution of hydroxypropyl emthylcellulose, extrude the round as a ball ball of making in extruding round as a ball comminutor; after dry, sieve and obtain the pastille micropill that certain order is counted size, in fluidized bed coating pot, with Aquacoat, carry out coating and get final product.
Embodiment 2
A Progesterone slow releasing capsule, wherein, described slow releasing capsule is comprised of 5% Progesterone, 78% excipient, 10% thin film coating material, 5% wetting agent and 2% binding agent.Wherein excipient is starch, and thin film coating material is Aquacoat, and wetting agent is aqueous solution, and binding agent is the alcoholic solution of polyethylene pyrroles protective embankment ketone.Make 1000.
Progesterone slow releasing capsule a preparation technology, it adopts following technique to prepare:
Powder coating method: utilize atresia coating pan, Corm Eleocharitis type coating pan, fluid bed top spray (or end spray) seed-coating machine, fluid bed tangent line spray pellet processing machine to make ball.The Corm Eleocharitis type coating pan of take is example: medicated powder was mixed to 80 eye mesh screens with starch, get the micropill (sucrose ball or microcrystalline Cellulose ball) of 30-35 order number and put into Corm Eleocharitis type coating pan, after micropill surface being squirted with the alcoholic solution of polyethylene pyrroles protective embankment ketone, a small amount of mixed powder is sprinkled in pot, make mixed powder be wrapped in uniformly the surface of micropill, and then squirt micropill surface and add again powder, until mixed powder all adds, after being dried, sieve and obtain the pastille micropill that certain order is counted size.In fluidized bed coating pot, with Aquacoat, carry out coating and get final product.
Embodiment 3
A Progesterone slow releasing capsule, wherein, described slow releasing capsule is comprised of 10% Progesterone, 73% excipient, 5% thin film coating material, 10% wetting agent and 2% binding agent.Wherein excipient is starch, and thin film coating material is Aquacoat, and wetting agent is aqueous solution, and binding agent is the alcoholic solution of hydroxypropyl emthylcellulose.Make 1000.
A preparation technology for Progesterone slow releasing capsule, it adopts following technique to prepare:
Liquid phase deposition: can utilize atresia coating pan, Corm Eleocharitis type coating pan, fluid bed top spray (or end spray) seed-coating machine, fluid bed tangent line spray ball mechanism ball.The Corm Eleocharitis type coating pan of take is example: get certain 30-35 object micropill (sucrose ball or microcrystalline Cellulose ball) and put into Corm Eleocharitis type coating pan, medicated powder and excipient is molten in adhesive, the Surface Edge spray limit that mixed liquor is sprayed onto to micropill is dry, until mixed liquor has all sprayed, after being dried, sieve and obtain the pastille micropill that certain order is counted size.In fluidized bed coating pot, with Aquacoat, carry out coating and get final product.
Clinical case is analyzed
Clinical case analysis of the present invention: this product clinical trial, obtain good safety, efficiency evaluation, and bioavailability is high, in vivo sustainable 24 hours drug releases.Because Progesterone slow releasing capsule is that pilule is large at gastrointestinal tract distribution area, bioavailability is high, therefore irritating property is little, be subject to the digestive tract conveying food rhythm and pace of moving things to affect little (as pylorus is closed etc.), blood drug level can be reached rapidly to curative effect concentration, and maintain steady, long valid density, blood concentration fluctuation is little, be conducive to reduce the toxic and side effects of medicine, below adopt several routine typical clinical cases to analyze:
Clinical case l: patient A, female, 25 years old, had bleeding conceived February, uses Progesterone slow releasing capsule under doctor advised, takes every day 2 times, takes continuously 12 days, and symptom has obvious alleviation, and keeps fetus.Explanation thus: the features such as Progesterone slow releasing capsule drug effect is fast, and effect is lasting, and toxic and side effects is little.
Clinical case 2: patient B, female, 28 years old, Progesterone slow releasing capsule was used in amenorrhea 2 years under doctor advised, took every day 2 times, took continuously the rear eumenorrhea 28 days.Explanation thus: the features such as Progesterone slow releasing capsule drug effect is fast, and effect is lasting, and toxic and side effects is little.
Clinical case 3: patient C, female, 36 years old, amenorrhea 3 years started to take Progesterone slow releasing capsule under doctor's suggestion, takes every day 2 times, takes continuously the rear eumenorrhea 8 weeks.Explanation thus: Progesterone slow releasing capsule is rapid-action, and dosage is few, taking convenience, toxic and side effects is little.
Clinical case 4: patient D, female, 30 years old, has bleeding conceived March, under doctor's suggestion, start to take Progesterone slow releasing capsule, take every day 2 times, take continuously 12 days, after miscarriage, its dosage is little, reduces the toxic and side effects of medicine, through treatment patient symptom, obviously improves.
Therefore superiority of the present invention and technique effect are: (1) Progesterone slow releasing capsule has the slow-release function of 24 hours, can effectively control the burst size of medicine, and safety, effectiveness are better; (2) Progesterone slow releasing capsule is that pilule is large at gastrointestinal tract distribution area, and bioavailability is high, and zest is little; (3), because particle diameter is little, be subject to the digestive tract conveying food rhythm and pace of moving things to affect little (as pylorus is closed etc.); (4) Progesterone controlled release micro pill can make blood drug level reach rapidly curative effect concentration, and maintains steady, long valid density, and blood concentration fluctuation is little; (5) good fluidity of micropill, size evenly, is easy to process (as coating, divided dose); (6) Progesterone slow releasing capsule is conducive to reduce the toxic and side effects of medicine; (7) the Progesterone slow releasing capsule dosage form more common than this medicine reduced the accumulated dose of medication, reduced patient's medicining times; (8) new formula, steady quality have been adopted; (9) in the preparation process of Progesterone slow releasing capsule, can adopt framing structure, film control structure or skeleton blooming control structure.
Claims (10)
1. a Progesterone slow releasing capsule, it is comprised of Progesterone, excipient, thin film coating material, wetting agent and binding agent, wherein each component by weight Progesterone be 5～50%, excipient is 55～90%, thin film coating material is 3～10%, and wetting agent is 0～10% and binding agent 1～2%.
2. Progesterone slow releasing capsule according to claim 1, it is a kind of pilule with slow releasing function.
3. Progesterone slow releasing capsule according to claim 1, wherein, the excipient in described Progesterone slow releasing capsule is the one or more combination in cellulose family, starch, lactose and calcium bicarbonate.
4. Progesterone slow releasing capsule according to claim 3, wherein, the cellulose family excipient in described Progesterone slow releasing capsule is ethyl cellulose, hydroxypropyl emthylcellulose, microcrystalline Cellulose, acrylic resin I, acrylic resin II, acrylic resin III or acrylic resin IV.
5. Progesterone slow releasing capsule according to claim 1, wherein, the thin film coating material in described Progesterone slow releasing capsule is one or both combinations in Aquacoat and aqueous acrylic resin dispersion.
6. Progesterone slow releasing capsule according to claim 1, the wetting agent in wherein said Progesterone slow releasing capsule is one or both the mixing in water or ethanol.
7. Progesterone slow releasing capsule according to claim 1, wherein, the binding agent in described Progesterone slow releasing capsule is the one or more combination in cellulose family, resinae, saccharide, gelatin.
8. Progesterone slow releasing capsule according to claim 7, wherein, the cellulose family binding agent in described Progesterone slow releasing capsule is water or the alcoholic solution of hydroxypropyl emthylcellulose, ethyl cellulose.
9. Progesterone slow releasing capsule according to claim 7, wherein, the resinae binding agent in described Progesterone slow releasing capsule is acrylic resin I, acrylic resin II, acrylic resin III or acrylic resin IV.
10. Progesterone slow releasing capsule according to claim 7, wherein, the saccharide binding agent in described Progesterone slow releasing capsule is maltose.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410116471.9A CN103933017A (en) | 2014-03-26 | 2014-03-26 | Progesterone slow-release capsule |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410116471.9A CN103933017A (en) | 2014-03-26 | 2014-03-26 | Progesterone slow-release capsule |
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| Publication Number | Publication Date |
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| CN103933017A true CN103933017A (en) | 2014-07-23 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410116471.9A Pending CN103933017A (en) | 2014-03-26 | 2014-03-26 | Progesterone slow-release capsule |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106063783A (en) * | 2016-06-16 | 2016-11-02 | 浙江爱生药业有限公司 | A kind of Progesterone slow-releasing microcapsule preparation and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000013663A1 (en) * | 1998-09-09 | 2000-03-16 | Alza Corporation | Dosage form comprising liquid formulation |
| US20030143276A1 (en) * | 1999-12-28 | 2003-07-31 | Watson Pharmaceuticals, Inc. | Dosage forms and methods for oral delivery of progesterone |
| CN101224210A (en) * | 2006-12-13 | 2008-07-23 | 天津市弗兰德医药科技发展有限公司 | Mizolastine sustained release capsule |
-
2014
- 2014-03-26 CN CN201410116471.9A patent/CN103933017A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000013663A1 (en) * | 1998-09-09 | 2000-03-16 | Alza Corporation | Dosage form comprising liquid formulation |
| US20030143276A1 (en) * | 1999-12-28 | 2003-07-31 | Watson Pharmaceuticals, Inc. | Dosage forms and methods for oral delivery of progesterone |
| CN101224210A (en) * | 2006-12-13 | 2008-07-23 | 天津市弗兰德医药科技发展有限公司 | Mizolastine sustained release capsule |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106063783A (en) * | 2016-06-16 | 2016-11-02 | 浙江爱生药业有限公司 | A kind of Progesterone slow-releasing microcapsule preparation and preparation method thereof |
| CN106063783B (en) * | 2016-06-16 | 2019-03-12 | 浙江爱生药业有限公司 | A kind of progesterone slow-releasing microcapsule preparation and preparation method thereof |
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Application publication date: 20140723 |
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