CN1562056A - Slow and control release preparation for thromus - Google Patents
Slow and control release preparation for thromus Download PDFInfo
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- CN1562056A CN1562056A CN 200410033144 CN200410033144A CN1562056A CN 1562056 A CN1562056 A CN 1562056A CN 200410033144 CN200410033144 CN 200410033144 CN 200410033144 A CN200410033144 A CN 200410033144A CN 1562056 A CN1562056 A CN 1562056A
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- slow
- controlled release
- xuesaitong
- release preparation
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Abstract
A slowly-releasing (or release-controllable) Xusaitong for treating thrombus contains sanchisaponin and slow-releasing additive.
Description
Technical field
The present invention relates to a kind of XUESAITONG medicine and preparation method thereof, relate in particular to that a kind of XUESAITONG is slow, controlled release preparation and preparation method thereof.
Background technology
Radix Notoginseng is a rare Chinese medicine, is the dry root of panax araliaceae plant Panaxnotoginseng (BURK.) F.H.Chen, now records in " one one of Chinese pharmacopoeia version in 2000, the hemostasis of function dissipating blood stasis, subduing swelling and relieving pain.Be used for spitting of blood, spit blood, epistaxis is had blood in stool, metrorrhagia, traumatic hemorrhage, breast ventral spine pain, tumbling and swelling.Domestic Radix Notoginseng research is started from last century at the beginning of, the big quantity research through last 100 years shows that its main effective ingredient is a Radix Notoginseng total arasaponins, comprises the Ginsenoside Rb
1, the Ginsenoside Rb
2, ginsenoside Rc, ginsenoside Rd, ginsenoside Rh
2, ginsenoside Re, panaxoside Rg
1, panaxoside Rg
2, ginsenoside Rh
1, arasaponin R
1Deng.Pharmacological research shows that Radix Notoginseng total arasaponins has the effect of tangible anti-cardiac-cerebral ischemia, antiarrhythmic effect more widely, certain vasorelaxation action, the hemorheology of improvement and microcirculatory effect are arranged, antiplatelet aggregation and anti-thrombosis function are arranged, certain effect for reducing fat and study of anti-atherogenic effect etc. are preferably arranged.
XUESAITONG is the preparation that Radix Notoginseng total arasaponins is made, and XUESAITONG PIAN, XUESAITONG JIAONANG, XUESAITONG KELI and four kinds of preparations of XUESAITONG ZHUSHEYE are arranged in the market, the function blood circulation promoting and blood stasis dispelling, and it is active to promote blood circulation, anticoagulant and cerebral blood flow increasing amount.Be used for the stasis of blood resistance of brain road, apoplectic hemiplegia, the resistance of the heart arteries and veins stasis of blood, obstruction of qi in the chest and cardialgia; Apoplexy sequela, angina pectoris belong to above-mentioned patient.The XUESAITONG ZHUSHEYE onset is rapid, but needs the intramuscular injection administration, is not easy to the patient; XUESAITONG PIAN, XUESAITONG JIAONANG, XUESAITONG KELI are oral administration, but all big (4-6 sheet of single administration dosage and administration frequency, 3 times on the one), not only use inconvenience, and blood drug level rises and falls very big, " peak valley " phenomenon is arranged, easily exceed or be lower than the treatment window, produce toxic and side effects or lessen the curative effect.
Goal of the invention
The objective of the invention is to problem at the existing preparation existence of XUESAITONG, a kind of XUESAITONG slow releasing preparation is provided, overcomes the shortcoming of the existing oral formulations of XUESAITONG, form steady persistent blood drug level, thereby reduce dosage and administration frequency, improve drug effect and safety.
The present invention also aims to provide that described XUESAITONG is slow, the preparation method of controlled release preparation.
XUESAITONG of the present invention is slow, controlled release preparation mainly comprises following effective ingredient:
Radix Notoginseng total arasaponins 1-10 weight portion
Slow, controlled release adjuvant 20-200 weight portion
XUESAITONG of the present invention is slow, the controlled release preparation effective ingredient can only comprise slow-released part, also can comprise rapid release and slow release two parts, form immediate release section by the part Radix Notoginseng total arasaponins, form slow-released part by remainder Radix Notoginseng total arasaponins and slow, controlled release adjuvant.
Described slow, controlled release adjuvant of the present invention is one of cellulose derivative or two or more.Cellulose derivative is sodium carboxymethyl cellulose, hydroxypropyl methyl fiber methyl element, hydroxypropyl cellulose, methyl hydroxyethylcellulose, methylcellulose, ethyl cellulose.
Described slow, controlled release adjuvant of the present invention is for also can be one of one of acrylic resin, polyvinylpyrrolidone, alkanols, polyethylene glycols or two kinds or two kinds.
Described XUESAITONG of the present invention is slow, controlled release preparation can be made and comprise gel matrix tablet, wax class matrix tablet, insoluble matrix tablet, slow, controlled release granule compressed tablet, the Entogastric lingering sheet, and biological adhesive tablet is in interior tablet, capsule, granule dosage form.
Described XUESAITONG of the present invention is slow, controlled release preparation also comprises filler 30%-70% (prescription total amount meter), disintegrating agent 5%-20% (prescription total amount meter), binding agent or wetting agent 5%-10% (prescription total amount meter), lubricant 0.1%-1% (prescription total amount meter).Filler is one of starch, dextrin, Icing Sugar, lactose or two or more, disintegrating agent is one of carboxymethyl starch sodium, microcrystalline Cellulose, hydroxypropyl emthylcellulose or two or more, binding agent is one of starch slurry, gelatine size, PVP rubber cement, sodium carboxymethyl cellulose, wetting agent is one of water, ethanol, and lubricant is one of magnesium stearate, Pulvis Talci, micropowder silica gel.
XUESAITONG of the present invention is slow, the preparation method when controlled release preparation only comprises slow-released part is:
With Radix Notoginseng total arasaponins, slow, controlled release adjuvant, filler mix homogeneously, add wetting agent and granulate, cross the 14-22 mesh sieve, 80-100 ℃ of drying, 12-18 mesh sieve granulate adds disintegrating agent, mix lubricant is even, makes tablet, capsule or granule.
XUESAITONG of the present invention is slow, the preparation method when controlled release preparation comprises immediate release section and slow-released part is:
(1) preparation of immediate release section: Radix Notoginseng total arasaponins, filler are crossed the 60-100 mesh sieve respectively, mix all, add binding agent, cross 14-22 mesh sieve system granule, 80-100 ℃ of drying, 12-18 mesh sieve granulate, adding disintegrating agent, mix lubricant are even.
(2) preparation of slow-released part: with Radix Notoginseng total arasaponins, slow, controlled release adjuvant, filler mix homogeneously, add wetting agent and granulate, cross the 14-22 mesh sieve, 80-100 ℃ of drying, 12-18 mesh sieve granulate adds disintegrating agent, mix lubricant is even.
(3) immediate release section and slow-released part are made tablet, capsule or granule in the prescription ratio.
XUESAITONG of the present invention is slow, controlled release preparation kind and consumption slow by regulating, the controlled release adjuvant, can obtain ideal slow, controlled-release effect, thereby overcome the peak valley phenomenon that the existing oral formulations of Rhizoma Corydalis Decumbentis produces, form effective blood drug concentration steadily special of a specified duration, reduce drug dose and administration frequency, improve drug effect and safety, help patient's treatment.
The specific embodiment:
The present invention is described in detail below in conjunction with embodiment.
Embodiment 1: the preparation gel matrix tablet
Prescription: immediate release section: Radix Notoginseng total arasaponins 12.5g
Lactose 50g
Starch 50g
Slow-released part: Radix Notoginseng total arasaponins 37.5g
Hydroxypropyl emthylcellulose 75g
Starch 25g
Make 1000
Its preparation technology is:
(1) immediate release section: the Radix Notoginseng total arasaponins, the lactose that take by weighing recipe quantity are crossed 80 mesh sieve mix homogeneously respectively, and 10% starch slurry is crossed 18 mesh sieves and granulated as binding agent, 80 ℃ of dryings, and 16 mesh sieve granulate add starch, an amount of mixing of magnesium stearate.
(2) slow-released part: with Radix Notoginseng total arasaponins, hydroxypropyl emthylcellulose, lactose mix homogeneously, 95% ethanol is made lubricant, and cross 18 mesh sieves and granulate, 80 ℃ of dryings, 16 mesh sieve granulate add starch, an amount of mixing of magnesium stearate.
(3) immediate release section and slow-released part are pressed into double-layer tablet in the prescription ratio.
Embodiment 2, prepare insoluble matrix tablet
Prescription: Radix Notoginseng total arasaponins 50g
Ethyl cellulose 150g
Hydroxypropyl emthylcellulose 15g
Starch 15g
Polyethylene glycol 6000 7.5g
Make 1000
Its preparation technology is made for: (1) takes by weighing the recipe quantity hydroxypropyl emthylcellulose, crosses 80 mesh sieves, mix homogeneously behind the starch pulverize separately.(2) Radix Notoginseng total arasaponins and the ethyl cellulose that takes by weighing recipe quantity is dissolved in the 10ml95% ethanol, and a few hours are left standstill in the sealing shading, adds in the mixed accessories in (1), the system soft material is crossed 18 mesh sieves and is granulated, and 16 mesh sieve granulate are crossed in 80 ℃ of dry backs, add an amount of mix homogeneously of magnesium stearate, tabletting.
Embodiment 3, preparation Entogastric lingering sheet
Prescription: Radix Notoginseng total arasaponins 50g
Hydroxypropyl emthylcellulose 100g
Hexadecanol 50g
Acrylic resin 20g
Magnesium stearate 1g
Make 1000
Its preparation technology is: precision takes by weighing medicine and adjuvant fully mixes the back with 2% hydroxypropyl emthylcellulose aqueous solution system soft material, crosses 18 orders and granulates, and 80 ℃ of dryings are crossed 16 mesh sieve granulate, tabletting behind the adding magnesium stearate mix homogeneously.
Embodiment 4, preparation slow releasing capsule
Prescription: immediate release section: Radix Notoginseng total arasaponins 12.5g
Lactose 50g
Slow-released part: Radix Notoginseng total arasaponins 37.5g
Hydroxypropyl emthylcellulose 100g
Starch 50g
Make 1000
Its preparation technology is:
(1) immediate release section: the Radix Notoginseng total arasaponins, the lactose that take by weighing recipe quantity are crossed 80 mesh sieves respectively, mix homogeneously, and 10% starch slurry is made binding agent, crosses 18 orders and granulates, and 80 ℃ of dryings are crossed 16 mesh sieve granulate, and adding starch, magnesium stearate are mixed in right amount.
(2) slow-released part: with Radix Notoginseng total arasaponins, hydroxypropyl emthylcellulose, lactose mix homogeneously, the lubricated humectant of 95% ethanol work is crossed 18 orders and is granulated, and 80 ℃ of dryings are crossed 16 mesh sieve granulate, and adding starch, magnesium stearate are mixed in right amount.
(4) immediate release section and slow-released part is even by the prescription mixed, the hard capsule of packing into.
Claims (8)
1, slow, the controlled release preparation of a kind of XUESAITONG, it is characterized in that: effective ingredient comprises:
Radix Notoginseng total arasaponins 1-10 weight portion
Slow, controlled release adjuvant 20-200 weight portion
2, slow, the controlled release preparation of XUESAITONG according to claim 1, it is characterized in that: effective ingredient comprises immediate release section and slow-released part, form immediate release section by the part Radix Notoginseng total arasaponins, by the remainder Radix Notoginseng total arasaponins, and slow, controlled release adjuvant form slow-released part.
3, slow, the controlled release preparation of XUESAITONG according to claim 1 and 2, it is characterized in that: slow, controlled release adjuvant is one of cellulose derivative or two or more.
4, slow, the controlled release preparation of XUESAITONG according to claim 1 and 2, it is characterized in that: cellulose derivative is sodium carboxymethyl cellulose, hydroxypropyl methyl fiber methyl element, hydroxypropyl cellulose, methyl hydroxyethylcellulose, methylcellulose, ethyl cellulose.
5, slow, the controlled release preparation of XUESAITONG according to claim 1 and 2 is characterized in that: slow, controlled release adjuvant is one of acrylic resin, polyvinylpyrrolidone, alkanols, polyethylene glycols or two kinds.
6, slow, the controlled release preparation of XUESAITONG according to claim 1 and 2, it is characterized in that: can make and comprise gel matrix tablet, wax class matrix tablet, insoluble matrix tablet, slow, controlled release granule compressed tablet, the Entogastric lingering sheet, biological adhesive tablet is in interior tablet, capsule, granule dosage form.
7, slow, the controlled release preparation of XUESAITONG according to claim 1 and 2, it is characterized in that: also comprise filler 30%-70% (prescription total amount meter), disintegrating agent 5%-20% (prescription total amount meter), binding agent or wetting agent 5%-10% (prescription total amount meter), lubricant 0.1%-1% (prescription total amount meter).
8, slow, the controlled release preparation of XUESAITONG according to claim 5, it is characterized in that: filler is one of starch, dextrin, Icing Sugar, lactose or two or more, disintegrating agent is one of carboxymethyl starch sodium, microcrystalline Cellulose, hydroxypropyl emthylcellulose or two or more, binding agent is one of starch slurry, gelatine size, PVP rubber cement, sodium carboxymethyl cellulose, wetting agent is one of water, ethanol, and lubricant is one of magnesium stearate, Pulvis Talci, micropowder silica gel.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410033144 CN1562056A (en) | 2004-04-07 | 2004-04-07 | Slow and control release preparation for thromus |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410033144 CN1562056A (en) | 2004-04-07 | 2004-04-07 | Slow and control release preparation for thromus |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1562056A true CN1562056A (en) | 2005-01-12 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410033144 Pending CN1562056A (en) | 2004-04-07 | 2004-04-07 | Slow and control release preparation for thromus |
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|---|---|
| CN (1) | CN1562056A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100444845C (en) * | 2005-06-03 | 2008-12-24 | 中国医学科学院药用植物研究所 | Biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract |
| CN102948418A (en) * | 2011-08-26 | 2013-03-06 | 浙江海洋学院 | Tea saponin tablet and preparation method thereof |
| CN115192595A (en) * | 2022-07-25 | 2022-10-18 | 昆明医科大学第一附属医院 | Application of notoginsenoside Rd in pharmacy |
-
2004
- 2004-04-07 CN CN 200410033144 patent/CN1562056A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100444845C (en) * | 2005-06-03 | 2008-12-24 | 中国医学科学院药用植物研究所 | Biologic adhesion preparation of total saponin of notoginseng for gastrointestinal tract |
| CN102948418A (en) * | 2011-08-26 | 2013-03-06 | 浙江海洋学院 | Tea saponin tablet and preparation method thereof |
| CN102948418B (en) * | 2011-08-26 | 2015-10-21 | 浙江海洋学院 | A kind of tea saponin tablet and preparation method thereof |
| CN115192595A (en) * | 2022-07-25 | 2022-10-18 | 昆明医科大学第一附属医院 | Application of notoginsenoside Rd in pharmacy |
| CN115192595B (en) * | 2022-07-25 | 2023-08-22 | 昆明医科大学第一附属医院 | Application of notoginsenoside Rd in pharmacy |
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