CN1799544A - Compound bergenin pills and its preparation method - Google Patents
Compound bergenin pills and its preparation method Download PDFInfo
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- CN1799544A CN1799544A CN 200410079652 CN200410079652A CN1799544A CN 1799544 A CN1799544 A CN 1799544A CN 200410079652 CN200410079652 CN 200410079652 CN 200410079652 A CN200410079652 A CN 200410079652A CN 1799544 A CN1799544 A CN 1799544A
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- bergeninum
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Abstract
The invention relates to a novel medicinal dosage for treating chronic bronchitis and common cold, and its preparing process, which comprises medicinal active constituents and medicinal auxiliary materials, wherein the active components of the medicament include Bergenin 8-42 wt% and chlorpheniramine 0.001-0.01 wt%, and balancing medicinal auxiliary materials.
Description
Technical field
The present invention relates to this medicine of a kind of medicine for the treatment of chronic bronchitis and cold cough, especially novel form and preparation method thereof.
Background technology
Bergeninum is a kind of extract of plant amedica, has the effect of relieving cough and expelling phlegm, can be used for treating chronic bronchitis.Curative effect can be affirmed, but onset time is slower.Main cause is that Bergeninum is a poorly water soluble drugs, and it is slow to make tablet stripping in human body with general disintegrating process, and bioavailability is low, thereby influences the performance of optimal efficacy.Therefore the bioavailability that how to improve behind the Bergeninum preparation oral is an important difficult problem in this field, is not resolved as yet so far.
Summary of the invention
The objective of the invention is to overcome the deficiencies in the prior art, a kind of oral back dissolution height is provided, bioavailability is compound bergenin pills preferably.
Another object of the present invention provides the preparation method of this compound bergenin pills.
Compound bergenin pills of the present invention is made up of active constituents of medicine and pharmaceutic adjuvant, described active constituents of medicine is Bergeninum and chlorphenamine, and its percentage by weight is: Bergeninum 8-42%, chlorphenamine 0.001-0.01%, surplus are pharmaceutic adjuvant.
Above-mentioned Bergeninum claims bergenin again, is the active ingredient of extracting from saxifragaceae plant Rhizoma Seu Herba Bergeniae BergrniaPurpurascens (Hook.f.et.Thoms.) Engl. or Yunnan Rhizoma Seu Herba Bergeniae Bergrnia Purpurascens (Hook.f.et.Thoms.) Engl.Vardelavayi (Franch) Engl.etirm rhizome.Bergeninum and chlorphenamine are prior art.
Above-mentioned pharmaceutic adjuvant is Polyethylene Glycol (PEG) 6000, Polyethylene Glycol (PEG) 4000, lecithin (PC).Can be wherein one or more.
The preparation method of compound bergenin pills of the present invention is divided into two kinds of fusion method and solvent methods.
The preparation method of compound bergenin pills of the present invention is made up of following steps:
One, gets the abundant mixing of Bergeninum, chlorphenamine and pharmaceutic adjuvant, put in 60 ℃-95 ℃ the water-bath fully thermosol;
Two, pour in the drop pill organizational security temperature charging apparatus, 60 ℃-90 ℃ of holding temperatures splash in the condensed fluid with per minute 40-90,5 ℃-16 ℃ of condensate temperatures;
Three, drip off the back and with filter paper the condensing agent of drop pill surface attachment inhaled and gone, put in the baking oven in 30 ℃-45 ℃ dry 12-24 hour, get product after the packing.
Above-mentioned condensed fluid is liquid Paraffin, vegetable oil, methyl-silicone oil etc.
The preparation method of compound bergenin pills of the present invention is made up of following steps:
One, gets Bergeninum and chlorphenamine, add in 60 ℃ of-80 ℃ of ethanol and dissolve, treat that medicine is all molten intact;
Two, get it filled and pour in the above-mentioned solution with adjuvant, the limit edged is stirred to dissolving fully, reclaims ethanol to there not being the alcohol flavor;
Three, pour in the drop pill organizational security temperature charging apparatus, 60 ℃-90 ℃ of holding temperatures splash in the condensed fluid with per minute 40-90,5 ℃-16 ℃ of condensate temperatures;
Four, drip off the back and with filter paper the condensing agent of drop pill surface attachment inhaled and gone, put in the baking oven in 30 ℃-45 ℃ dry 12-24 hour, get product after the packing.
Above-mentioned concentration of alcohol is 75%-95%, and its addition is Bergeninum and chlorphenamine 10-30 a times.Above-mentioned condensed fluid is liquid Paraffin, vegetable oil, methyl-silicone oil etc.
It is very close with the dispersity relation of medicine that solution of the present invention is based on the release-absorption of insoluble drug in the pharmaceutical preparation, very big to its medicine absorption in vivo influence, with the dispersity powder that general breaking method makes, often bioavailability is lower in vivo.This just need reach the purpose that improves bioavailability by changing the dispersity that methods such as dosage form, composition and technical process change medicine.
The present invention is exactly by changing dosage form, add macromolecule carrier (substrate), change preparation process, utilize solid dispersion technology, improve the dissolution of Bergeninum, improving its bioavailability in vivo.The dispersion technology of solid drugs, particularly insoluble drug when solid dispersion technology is meant the preparation preparation.Solid dispersion is meant the medicine high degree of dispersion in carrier, forms a kind of disperse system that exists with solid form.Insoluble drug is dispersed in the solid dispersion that obtains medicine one carrier in the carrier of a kind of no physiologically active (water soluble polymer substrate) by certain method, medicine is superfine colloid and ultrafine dust in solid dispersion, even molecularity exists.
Study of pharmacy and part pharmacological research:
1, the present invention and compound bergenin pills dissolution contrast test
Compound bergenin pills (Kunming biological preparation factory, lot number: 20020201) dissolution (%) measurement result:
| Time | Measure number of times | Date processing | |||||
| T (branch) | 1 | 2 | 3 | 4 | 5 | X | SD |
| 3 | 39.6 | 43.2 | 28.8 | 32.4 | 18 | 32.4 | 9.8590 |
| 5 | 46.8 | 72 | 54 | 57.6 | 32.4 | 52.56 | 14.5343 |
| 8 | 61.2 | 57.6 | 61.2 | 61.2 | 46.8 | 57.6 | 7.2000 |
| 10 | 60.15 | 75 | 46.8 | 72 | 46.8 | 60.15 | 15.4638 |
| 15 | 64.2 | 79.2 | 68.4 | 68.4 | 61.8 | 68.28 | 6.8200 |
| 20 | 72 | 82.8 | 79.2 | 82.8 | 68.4 | 77.04 | 6.5397 |
| 30 | 87.3 | 86.4 | 108 | 86.4 | 68.4 | 87.3 | 16.2000 |
| 45 | 82.8 | 86.4 | 79.2 | 86.4 | 75.6 | 82.08 | 4.6938 |
| 60 | 72 | 90 | 72 | 97.2 | 67.5 | 79.74 | 13.0360 |
Dissolution of the present invention (%) measurement result:
| Time | Measure number of times | Date processing | |||||
| T (branch) | 1 | 2 | 3 | 4 | 5 | X | SD |
| 3 | 18 | 32.4 | 25.2 | 10.2 | 28.8 | 28.8 | 8.8832 |
| 5 | 43.2 | 46.8 | 57.6 | 39.6 | 57.6 | 48.96 | 8.2878 |
| 8 | 72 | 79.2 | 86.4 | 64.8 | 82.8 | 77.04 | 8.6699 |
| 10 | 104.4 | 93.6 | 86.4 | 86.4 | 90 | 92.16 | 7.4651 |
| 15 | 93.6 | 97.2 | 100.8 | 86.4 | 97.2 | 95.04 | 5.4597 |
| 20 | 108 | 101.6 | 108 | 93.6 | 97.2 | 101.68 | 6.4274 |
| 30 | 104.4 | 82.8 | 97.2 | 90 | 100.8 | 95.04 | 8.6699 |
| 45 | 111.6 | 82.8 | 108 | 104.4 | 100.8 | 101.52 | 11.2121 |
| 60 | 90 | 109.6 | 100.8 | 100.8 | 97.2 | 99.68 | 7.0846 |
Above compound bergenin pills, five dissolutions of compound bergenin pills (%) meansigma methods are carried out date processing with weighted least-squares method, calculate T50, the Td of compound bergenin pills and compound bergenin pills, the dissolution time of T70, T80 respectively:
The result shows that dissolution of the present invention is better and complete than compound bergenin pills.
2, the present invention and compound bergenin pills bioavailability contrast test
Method according to the pharmacopeia regulation, carry out the present invention and compound bergenin pills (Kunming biological preparation factory with rat, lot number: 20020201) Isodose contrast test, as testing index, the result shows that bioavailability of the present invention is than compound bergenin pills height with Bergeninum (the Chinese biological goods are identified the 1532-200202 of institute).
3, the present invention and compound bergenin pills (Kunming biological preparation factory, lot number 20020201) cough-relieving test
Method: get white mice, body weight 18-22g is divided into blank group, positive administration group, the basic, normal, high dosage group of the present invention, compound bergenin pills group at random.Behind the gastric infusion 1 hour, place strong aqua ammonia to draw mice and cough in the device, make mice quantitatively regularly suck strong aqua ammonia and cause and cough, observe mouse cough number of times in the incubation period and 3 minutes that begins to occur coughing, the result adopts the t check to handle relatively:
| Group | Number of animals (only) | Dosage (mg/Kg) | The cough number of times | Cough latent period (second) |
| The blank group | 20 | 31.6±15.86 | 39.2±18.77 | |
| Carbetapentane citrate tablet | 10 | 20 | 15.4±7.38 | 66.95±32.5 |
| Compound bergenin pills | 10 | 80.4 | 20.2±8.84 | 55.1±21.36 |
| The drop pill low dosage | 20 | 40.2 | 17.2±12.33 | 54±26.26 |
| Dosage in the drop pill | 20 | 80.4 | 15.70±11.6 | 54.15±21.48 |
| The drop pill high dose | 10 | 160.8 | 13.50±5.78 | 64.8±25.36 |
Show that antitussive action of the present invention is better than compound bergenin pills.
The specific embodiment
Embodiment 1: get 30 parts of Bergeninums, and 0.48 part of chlorphenamine, 269.52 parts of PEG6000 promptly get every drop pill finished product that contains the plain 3mg of Rhizoma Seu Herba Bergeniae by above-mentioned fusion legal system.
Embodiment 2: get 45 parts of Bergeninums, and 0.72 part of chlorphenamine, 254.28 parts of PEG4000 promptly get every drop pill finished product that contains the plain 4.5mg of Rhizoma Seu Herba Bergeniae by above-mentioned fusion legal system.
Embodiment 3: get 60 parts of Bergeninums, and 0.96 part of chlorphenamine, 239.04 parts of PEG6000 promptly get every drop pill finished product that contains the plain 6mg of Rhizoma Seu Herba Bergeniae by above-mentioned fusion legal system.
Embodiment 4: get 75 parts of Bergeninums, and 1.2 parts of chlorphenamines, 223.8 parts of PEG4000 promptly get every drop pill finished product that contains the plain 7.5mg of Rhizoma Seu Herba Bergeniae by above-mentioned fusion legal system.
Embodiment 5: get 90 parts of Bergeninums, and 1.44 parts of chlorphenamines, 208.56 parts of PEG6000 promptly get every drop pill finished product that contains the plain 9mg of Rhizoma Seu Herba Bergeniae by above-mentioned fusion legal system.
Embodiment 6: get 105 parts of Bergeninums, and 1.68 parts of chlorphenamines, 193.32 parts of PEG4000 promptly get every drop pill finished product that contains the plain 10.5mg of Rhizoma Seu Herba Bergeniae by above-mentioned solvent legal system.
Embodiment 7: get 120 parts of Bergeninums, and 1.92 parts of chlorphenamines, 178.08 parts of PEG6000 promptly get every drop pill finished product that contains the plain 12mg of Rhizoma Seu Herba Bergeniae by above-mentioned solvent legal system.
Embodiment 8: get 90 parts of Bergeninums, and 1.44 parts of chlorphenamines, 104.28 parts of PEG6000,104.28 parts of PEG4000 promptly get every drop pill finished product that contains the plain 9mg of Rhizoma Seu Herba Bergeniae by above-mentioned solvent legal system.
Embodiment 9: get 105 parts of Bergeninums, and 1.68 parts of chlorphenamines, 32.22 parts of PEG6000,161.10 parts of PEG4000 promptly get every drop pill finished product that contains the plain 10.5mg of Rhizoma Seu Herba Bergeniae by above-mentioned solvent legal system.
Embodiment 10: get 120 parts of Bergeninums, and 1.92 parts of chlorphenamines, 4,000 176.18 parts of PEG, 1.9 parts of PC promptly get every drop pill finished product that contains the plain 12mg of Rhizoma Seu Herba Bergeniae by above-mentioned solvent legal system.
Content of the present invention is not limited to embodiment.
Claims (6)
1, a kind of compound bergenin pills, it is characterized in that forming by active constituents of medicine and pharmaceutic adjuvant, described active constituents of medicine is Bergeninum and chlorphenamine, and its percentage by weight is: Bergeninum 8-42%, chlorphenamine 0.001-0.01%, surplus are pharmaceutic adjuvant.
2,, it is characterized in that described pharmaceutic adjuvant is polyethylene glycol 6000, Macrogol 4000, lecithin according to the described compound bergenin pills of claim 1.
3,, it is characterized in that forming by following steps according to the preparation method of the described compound bergenin pills of claim 1:
One, gets the abundant mixing of Bergeninum, chlorphenamine and pharmaceutic adjuvant, put in 60 ℃-95 ℃ the water-bath fully thermosol;
Two, pour in the drop pill organizational security temperature charging apparatus, 60 ℃-90 ℃ of holding temperatures splash in the condensed fluid with per minute 40-90,5 ℃-16 ℃ of condensate temperatures;
Three, drip off the back and with filter paper the condensing agent of drop pill surface attachment inhaled and gone, put in the baking oven in 30 ℃-45 ℃ dry 12-24 hour, get product after the packing.
4,, it is characterized in that described condensed fluid is liquid Paraffin, vegetable oil, methyl-silicone oil according to the preparation method of the described compound bergenin pills of claim 3.
5,, it is characterized in that forming by following steps according to the preparation method of the described compound bergenin pills of claim 1:
One, gets Bergeninum and chlorphenamine, add in 60 ℃ of-80 ℃ of ethanol and dissolve, treat that medicine is all molten intact;
Two, get it filled and pour in the above-mentioned solution with adjuvant, the limit edged is stirred to dissolving fully, reclaims ethanol to there not being the alcohol flavor;
Three, pour in the drop pill organizational security temperature charging apparatus, 60 ℃-90 ℃ of holding temperatures splash in the condensed fluid with per minute 40-90,5 ℃-16 ℃ of condensate temperatures;
Four, drip off the back and with filter paper the condensing agent of drop pill surface attachment inhaled and gone, put in the baking oven in 30 ℃-45 ℃ dry 12-24 hour, get product after the packing.
6,, it is characterized in that described condensed fluid is liquid Paraffin, vegetable oil, methyl-silicone oil according to the preparation method of the described compound bergenin pills of claim 5.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100796525A CN100341507C (en) | 2004-12-31 | 2004-12-31 | Compound bergenin pills and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100796525A CN100341507C (en) | 2004-12-31 | 2004-12-31 | Compound bergenin pills and its preparation method |
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| Publication Number | Publication Date |
|---|---|
| CN1799544A true CN1799544A (en) | 2006-07-12 |
| CN100341507C CN100341507C (en) | 2007-10-10 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100796525A Expired - Fee Related CN100341507C (en) | 2004-12-31 | 2004-12-31 | Compound bergenin pills and its preparation method |
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| CN (1) | CN100341507C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105832752A (en) * | 2016-04-08 | 2016-08-10 | 王金霞 | Pharmaceutical composition for clinical nursing of upper respiratory infection |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH06100640A (en) * | 1992-09-22 | 1994-04-12 | Kansai Paint Co Ltd | Actinic-radiation-during colored coating composition for vacuum-formable film, vacuum-formable film and vacuum-formed article |
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- 2004-12-31 CN CNB2004100796525A patent/CN100341507C/en not_active Expired - Fee Related
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105832752A (en) * | 2016-04-08 | 2016-08-10 | 王金霞 | Pharmaceutical composition for clinical nursing of upper respiratory infection |
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| Publication number | Publication date |
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| CN100341507C (en) | 2007-10-10 |
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Granted publication date: 20071010 Termination date: 20201231 |