CN1579410A - Oral total notoginsenoside blending preparation - Google Patents
Oral total notoginsenoside blending preparation Download PDFInfo
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- CN1579410A CN1579410A CN 03132238 CN03132238A CN1579410A CN 1579410 A CN1579410 A CN 1579410A CN 03132238 CN03132238 CN 03132238 CN 03132238 A CN03132238 A CN 03132238A CN 1579410 A CN1579410 A CN 1579410A
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Abstract
The invention is a notoginseng saponin slow release preparation, which includes effective ingredient notoginseng saponin and release regulator, diluter, lubricant and glidant. Its character lies in: the slow release preparation contains cellulose polymer framework material. In order to control and regulate the medicine release better, the surface active agent and diluter can be added into the preparation. The preparation can release notoginseng saponin 50% in 4-6 hours, and the releasing rate is not affected by media pH value. After the medicine is taken, the effective ingredients will be released with slow release medicine formulation character, in order to achieve the aim of release regulation. Its meaning lies in: it reduces the peak density of the medicine, prolongs the half life of medicine, and upgrades the compliance of medicine.
Description
One, technical field
The present invention relates to a kind of pharmaceutical composition, particularly relate to a kind of Peroral solid dosage form pharmaceutical preparation of middle pharmaceutically active ingredient, exactly is a kind of oral Radix Notoginseng total glycosides solid adjustment release preparation that contains the cellulosic polymer skeleton.
Two, background technology
Radix Notoginseng is Chinese traditional rare Chinese medicine, and " A Supplement to the Compendium of Materia Medica " of Qing Dynasty's ZHAO Xue-Min thought: Radix Notoginseng " Radix Notoginseng enriches blood the first for class Radix Ginseng quite, ginseng qi-tonifying the first, flavor with and merit also with, the old friend also claims to say Radix Notoginseng, Radix Notoginseng is the most precious person in the medicine ".And say " greatly the effect that has cured the wound and come back to life as the fist person, valency and gold etc. ".Radix Notoginseng total arasaponins is the total effective ingredient that extracts from the Chinese medicine Radix Notoginseng; it is clinical cardiovascular and cerebrovascular vessel medication commonly used; gone on the market at present use oral ordinary tablet, capsule arranged; dosage forms such as injection; because its determined curative effect; be put into the national essential drugs catalogue, and all kinds of having gone on the market are all classified Chinese medicine protection kind as.The medication of the kind of having gone on the market routine is to be administered three times every day.These oral ordinary preparation releases are rapid, effective ingredient is at blood samples of patients concentration a middle or short term height (peak value), and the accent release formulation only is administered once every day, can avoid such peak value, make the equalization of concentration of effective ingredient in blood samples of patients and stable, thus the side effect of avoiding peak value to cause.Patient's biological compliance also improves greatly.
The Radix Notoginseng total arasaponins that the present invention is used is the effective ingredient that extracts from the Chinese medicine Radix Notoginseng, its extraction process is in full accord with the extraction process of the ordinary preparation that has gone on the market.
Three, summary of the invention
Oral Radix Notoginseng total arasaponins provided by the present invention is transferred release formulation, comprise effective ingredient Radix Notoginseng total arasaponins and diluent, lubricant and fluidizer, it is characterized in that: cellulose polymeric skeleton material in this accent release formulation, described cellulosic polymer is made of at least a hydrophilic polymer or hydrophobic polymer.
The effective ingredient Radix Notoginseng total arasaponins accounts for 25～70% of total formulation weight amount.
Described hydrophilic polymer is hypromellose, low substituted cellulose, Hydroxypropyl methyl cellulose phtalate, alginate etc.
Described hydrophobic polymer is ethyl cellulose or cellulose acetate etc.
Described framework material accounts for 10%～60% of total formulation weight amount, is good with 15～45% particularly.
For controlling the rate of release of Radix Notoginseng total arasaponins better, can also add surfactant in this accent release formulation, they can be sodium lauryl sulphate, polyethylene glycols or Tweens etc.1～20% of surfactant comprise total formulation weight amount is good with 2～10%.
Described diluent adopts starch, dextrin, low substituted cellulose, and conventional adjuvants such as microcrystalline Cellulose, lactose, calcium hydrogen phosphate, calcium sulfate are preferably dextrin.Diluent accounts for 5～40% of total formulation weight amount, is good with 10～30% especially.
Described lubricant adopts known stearic acid or its salt, preferred magnesium stearate.Lubricant accounts for 3～5% of total formulation weight amount.
Described fluidizer is selected known micronized silica for use.Fluidizer accounts for 1～2% of total formulation weight amount.
Oral Radix Notoginseng total arasaponins provided by the present invention transfers release formulation to prepare by the routine fashion of matrix tablet.Here it is at first with Radix Notoginseng total arasaponins and cellulosic polymer, diluent and surfactant mix homogeneously, makes wet granular with suitable binders, behind the hot air drying, adds lubricant and fluidizer and mix
Evenly, granulate, measure granule content after, tabletting or encapsulated getting final product.
Oral Radix Notoginseng total arasaponins provided by the present invention is transferred release formulation, adopts cellulosic polymer framework material and surfactant and diluent to make up, and its release in vitro meets the requirement of controlled release or slow release.Radix Notoginseng total arasaponins discharged 50% of total amount between 4～6 hours, and was not subjected to the influence (seeing accompanying drawing) of release medium pH value.
Four, description of drawings
Figure 1 shows that the release curve of example 2 made tablets in pH6.8, pH7.4 and pure water.Its release is not subjected to the influence of pH value.
Figure 2 shows that the oral back of example 2 made tablets and conventional tablet domesticated dog blood drug level-time graph.The ordinary tablet peak value is obvious.
Five, the specific embodiment
To prepare 1000, every contains Radix Notoginseng total arasaponins 100mg is example, and non-limiting examples is described below:
Example 1, prescription:
Radix Notoginseng total arasaponins 100g
Sodium alginate 55g
Calcium hydrogen phosphate 30g
Sodium lauryl sulphate 8g
Micropowder silica gel 2g
Magnesium stearate 7g
Make 1000 (grains)
Operation: take by weighing Radix Notoginseng total arasaponins, sodium alginate and calcium hydrogen phosphate by recipe quantity and put in the pulverizer, mixing is pulverized the back and is crossed 100～120 mesh sieves, puts in the step comminutor to stir, and the ethanol of adding 95% is made even, tiny granule.Wet grain below 3%, adds magnesium stearate, micropowder silica gel behind the dried granule 24-30 mesh sieve granulate in 50 ℃ ± 10 ℃ hot air dryings to moisture content, measures granule content behind the mixing, and 8mm is flat to strike out 1000 or irritate 1000 capsules.
Example 2, prescription:
Radix Notoginseng total arasaponins 100g
HPMC4000 33g
HPMC100 17g
Dextrin 33g
Sodium lauryl sulphate 10g
Micropowder silica gel 2g
Magnesium stearate 7g
Make 1000 (grains)
Operation: take by weighing Radix Notoginseng total arasaponins, hypromellose and dextrin by recipe quantity and put in the pulverizer, mixing is pulverized the back and is crossed the 100-120 mesh sieve, puts in the step comminutor to stir, and the ethanol of adding 25ml 95% is made even, tiny granule.Wet grain below 3%, adds magnesium stearate, micropowder silica gel behind the dried granule 24-30 mesh sieve granulate in 50 ℃ ± 10 ℃ hot air dryings to moisture content, measures granule content behind the mixing, and 8mm is flat to strike out 1000 or irritate 1000 capsules.
Example 3, prescription:
Radix Notoginseng total arasaponins 100g
Ethyl cellulose 65g
Starch 25g
Sodium lauryl sulphate 10g
Magnesium stearate 4g
Micropowder silica gel 2g
Make 1000 (grains)
Operation: with embodiment 1 or 2.
Example 4, prescription:
Radix Notoginseng total arasaponins 100g
Cellulose acetate 55g
Calcium sulfate 30g
Polyethylene glycol 6000 10g
Magnesium stearate 6g
Micropowder silica gel 2g
Make 1000 (grains)
Operation: with embodiment 1 or 2.
Example 5, prescription:
Radix Notoginseng total arasaponins 100g
HPMC4000 30g
HPMC100 0g
Dextrin 56g
Sodium lauryl sulphate 5g
Micropowder silica gel 2g
Magnesium stearate 7g
Make 1000 (grains)
Operation is with example 3.
Example 6, prescription:
Radix Notoginseng total arasaponins 100g
HPMC4000 90g
HPMC100 85g
Sodium lauryl sulphate 20g
Micropowder silica gel 2g
Magnesium stearate 7g
Make 1000 (grains)
Operation is with example 3.
Example 7, example 1～5 made tablet is measured release by two appendix XD of 2000 editions Chinese Pharmacopoeias drug release determination method, hanging basket, 100 rev/mins, medium: pure water, measure temperature: 37 ± 1 ℃; Behind each point in time sampling, with high effective liquid chromatography for measuring ginsenoside Rb1's the accumulation amount of being released into.
Sample time example 1 example 2 examples 3 examples 4 examples 5 examples 6
1 hour (%) 16 15.4 17. 16.3 30 4
2 hours (%) 30.5 31.2 35.3 34 58 11
4 hours (%) 49 50.1 58 51.2 75 20
6 hours (%) 69.6 72 85.3 64 95 31
8 hours (%) 92 95.5 99 74.2 40
10 hours (%) 98.8 101 89 47
Example 8, will give 6 of domesticated dogs by example 2 prepared tablets, 1 of every dog is after the administration
The concentration of ginsenoside Rg1 in the blood is measured in the different time blood sampling, the data of being measured are added up, the result: summit concentration (Cmax) is 2.1 ± 1.0ug/ml, it is 4.5 ± 0.91 hours, eliminating the half-life is 8.2 ± 1.4 hours, bioavailability is 25.6 ± 12.7ug.min/ml, has sustained releasing character.Blood drug level-time graph is seen accompanying drawing 2.
Claims (7)
1, a kind of oral Radix Notoginseng total arasaponins is transferred release formulation, comprises effective ingredient, diluent, surfactant, lubricant and fluidizer, it is characterized in that: contain the cellulosic polymer framework material in this accent release formulation.
2, accent release formulation according to claim 1 is characterized in that:
Radix Notoginseng total arasaponins 25～70%
Framework material 10～60%
Diluent 5～40%
Surfactant 1～20%.
3, accent release formulation according to claim 2 is characterized in that:
Radix Notoginseng total arasaponins 30～60%
Framework material 15～45%
Diluent 10～30%
Surfactant 2～10%.
4, according to claim 1 or 2 or 3 described accent release formulations, it is characterized in that: also contain 3～5% lubricant and 1～2% fluidizer in the said preparation.
5, accent release formulation according to claim 4 is characterized in that: described cellulosic polymer is at least a in hydrophilic polymer hypromellose, low substituted cellulose, Hydroxypropyl methyl cellulose phtalate, alginate or hydrophobic polymer ethyl cellulose, the cellulose acetate.
6, accent release formulation according to claim 4 is characterized in that: described diluent is starch, dextrin, low substituted cellulose, microcrystalline Cellulose, lactose, calcium hydrogen phosphate, calcium sulfate.
7, accent release formulation according to claim 4 is characterized in that: described surfactant is sodium lauryl sulphate, polyethylene glycols or Tweens.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03132238 CN1579410A (en) | 2003-07-31 | 2003-07-31 | Oral total notoginsenoside blending preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03132238 CN1579410A (en) | 2003-07-31 | 2003-07-31 | Oral total notoginsenoside blending preparation |
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| Publication Number | Publication Date |
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| CN1579410A true CN1579410A (en) | 2005-02-16 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03132238 Pending CN1579410A (en) | 2003-07-31 | 2003-07-31 | Oral total notoginsenoside blending preparation |
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Cited By (2)
| 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 |
| CN103127020A (en) * | 2013-02-19 | 2013-06-05 | 青岛正大海尔制药有限公司 | Alfacalcidol sustained-release preparation and preparation method thereof |
-
2003
- 2003-07-31 CN CN 03132238 patent/CN1579410A/en active Pending
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 |
| CN103127020A (en) * | 2013-02-19 | 2013-06-05 | 青岛正大海尔制药有限公司 | Alfacalcidol sustained-release preparation and preparation method thereof |
| CN103127020B (en) * | 2013-02-19 | 2014-07-23 | 青岛正大海尔制药有限公司 | Alfacalcidol sustained-release preparation and preparation method thereof |
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