CN101468100A - Method for preparing digitalis floating tablets and use thereof - Google Patents
Method for preparing digitalis floating tablets and use thereof Download PDFInfo
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- CN101468100A CN101468100A CNA2007103084333A CN200710308433A CN101468100A CN 101468100 A CN101468100 A CN 101468100A CN A2007103084333 A CNA2007103084333 A CN A2007103084333A CN 200710308433 A CN200710308433 A CN 200710308433A CN 101468100 A CN101468100 A CN 101468100A
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- floating
- digitalis
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- tablet
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Abstract
The invention disclosed floating film stomach digitalis preparation method and its application, the invention of new technologies are the drug, involving a new form of digitalis for the treatment of congestive heart failure and certain arrhythmias such as atrial fibrillation, atrial flutter and paroxysmal tachycardia in preparation methods and pharmaceutical preparations. The characteristics of the new formulations is that the gastric floating tablet containing a wide range of hydrophilic polymer material, in contact with gastric fluid temperature, the surface water into a gel, by volume expansion. At this point the weight of tablets is less than the buoyancy gastric juice to pills floating on the gastric juice, gastric retention time has been extended. The present invention has been floating piece of digitalis stomach with a simple, good stability and high bioavailability, compared with the general formulations to reduce the side effects of drug characteristics.
Description
Technical field
The invention belongs to the medicine new technical field, a kind of novel form that relates to Folium Digitalis Purpureae, be used for the treatment of congestive heart failure and some arrhythmia, after one's own heart atrial fibrillation is moving, pharmaceutical preparation of atrial flutter and paroxysmal tachycardia and preparation method thereof, specifically a kind of preparation method of digitalis floating tablets and application thereof.
Background technology
Folium Digitalis Purpureae, English Digitalis by name, another name: digitalis, Folium Digitalis have another name called: poison grass, pale reddish brown digitalis, fuchsia.Derive from the cured leaf powder of goatweed Digitalis purpurea L..Main component is digitophyllin (Digitoxin, C
41H
61O
13) gitoxin (gitoxin, Gitoxin, C
41H
64O
13) etc.1g tires and should be equivalent to 10 digitalis units.Folium Digitalis Purpureae is for being the dull gray green powder; Special Austria is arranged, bitter in the mouth.
" Xinhua's book on Chinese herbal medicine outline ": leaf: cardiac tonic.Be used for excited cardiac muscle, increase myocardial contraction, Syst blood output is increased, improve blood circulation.Heart arteries and veins edema patient there is diuresis.
Folium Digitalis Purpureae is the specific drug of the multiple heart failure of treatment, and it is former to be a kind of plant amedica.This plant amedica induced one, and clinical medicine is formal to be used, be Britain doctor Wei Selin (William Withering, 1741-1799), Wei Selin was through the experiment in 9 years, he has treated 163 patients altogether with Folium Digitalis Purpureae, has accumulated a large amount of experiences, 1785, he has delivered the monograph report that is entitled as " about Folium Digitalis Purpureae ", thereby for he has brought global fame.
Certainly, directly using Folium Digitalis Purpureae that many shortcomings are arranged, mainly is impure more, and is difficult for accurately grasping dosage again.Can directly affect the treatment like this, even make the lethal danger of people.Although Wei Selin has mentioned the untoward reaction of using Folium Digitalis Purpureae to occur in works.But still have some doctors, excessive because of using dosage, cause patient death, this has had a strong impact on applying of Folium Digitalis Purpureae.The basic way of dealing with problems is that the active ingredient that will extract Folium Digitalis Purpureae comes, and could strictly grasp dosage like this and prevent serious adverse.1874, and one of German classic medicine scholar Shi Midiboge (OswaldSchmiedeberg, 1838-1921), effective heart tonifying composition-a kind of glycosides (the same liver of sound) class of from the plant Folium Digitalis Purpureae, having purified finally.
So far, modern medicine often uses clinically, extracts the glycoside that gets from Folium Digitalis Purpureae exactly, is called cardiac glycoside.Folium Digitalis Purpureae is applied to clinical existing 200 years history, is still the active drug of treatment heart failure so far.
A large amount of chemical research shows, Folium Digitalis Purpureae positive inotropic action and " rapid commutative Ca
++The pond " increase be consistent.Folium Digitalis Purpureae triggers sarcoplasmic reticulum release Ca by causing that the property a crossed calcium increases
++, Ca
++Combine with troponin, remove the inhibition of tropomyosin to actin, impel the two combination, contractility strengthens, and suppresses Na
+-K
+Pump makes Na in the cell
+Increase, it may be that the contractile protein system is to Na that contractility strengthens
+Sensitivity or Na
+Pass through Na
+-Ca
++Exchange system remote-effects Ca
++Metabolism.
This product has following characteristics:
This product is an intra-gastric floating tablet, it is characterized in that this intra-gastric floating tablet owing to contain multiple hydrophilic high molecular material, and behind body temperature contact gastric juice, surface water changes into gel, and makes volumetric expansion.The weight of tablet floats on the gastric juice tablet less than the buoyancy of gastric juice at this moment, is prolonged gastric transit time.
The Entogastric lingering drug-supplying system is the novel drug-supplying system that grows up on common release drug-supplying system basis, it is the focus of current pharmaceutics research, be specially adapted to treat the medicine of disease of stomach, absorption site is at the medicine of stomach or small intestinal upper end, unsettled medicine in small intestinal or colonic environment, low or the undissolved medicine of dissolubility under small intestinal pH environment, and the bioavailability that improves common sustained-release preparation.The Entogastric lingering drug-supplying system is divided into drug-supplying systems such as floating in stomach, gastric bio-adhesive, gastric high density precipitation, gastric expansion and gastric magnetic guiding according to its Entogastric lingering mechanism; Can be divided into gastric residential tablet, gastric retention capsule and gastric retention micropill etc. according to dosage form.
The floating in stomach controlled release preparation (tablet or capsule) of applied fluid dynamics principle (HBSTM) preparation in recent years can discharge and absorb by the location that the prolongation preparation improves medicine in the holdup time of gastric.Composite materials such as hydrophilic gel commonly used and waxiness are made, and the floating in stomach system is wherein arranged, and permeate voltage-controlled release system etc. in the gastric expansion system stomach function regulating.Organic monoacid class medicine such as aspirin that some mainly absorb from stomach; Antacid Al (OH) 3 gel films etc.; Have vitamin B1, B2, B6 etc. that the active transport privileged sites absorb; Some greater than the medicine (norfloxacin, gentamycin etc.) of intestinal Digestive system and the medicine of particular requirement (gastritis that causes as anti-helicobacter pylori bacillus, the antibiotic of gastric ulcer and furazolidone etc.) clinically, all can be made into the Entogastric lingering floating sheet in gastric juice dissolving.Longer etc. utilize the bioadhesion effect that chlorothiazide and albumin bound are made the albumin granule of pastille, with poly-carbomer (PCP, 3:7) granule mixes and incapsulates, stripping shows in the body, the sustainable release 8h of capsule, but release surpasses 60% in the 2h.Behind the mice oral administration, produce very strong adhesiveness in gastric PCP hydration, PCP-albumin ball nearly 90% rests on gastric, compares with the albumin granule of taking medicated powder or pastille separately, and drug treating time prolongs, and bioavailability obviously improves.Also there is the people that the floating effect of bioadhesion effect stomach function regulating is combined and prepared floatable sotalol hydrochloride adhesion preparation.
Summary of the invention
In order to address the above problem, the dosage that the object of the present invention is to provide a kind of patient that can make person in middle and old age and take for a long time when reaching the identical treatment effect to take reduces, thereby reduces the digitalis floating tablets of side effect.
Another object of the present invention is to provide a kind of method for preparing digitalis floating tablets.Use the digitalis floating tablets that this method makes and it is characterized in that this intra-gastric floating tablet owing to contain multiple hydrophilic high molecular material, behind body temperature contact gastric juice, surface water changes into gel, and makes volumetric expansion.The weight of tablet floats on the gastric juice tablet less than the buoyancy of gastric juice at this moment, is prolonged gastric transit time.
Digitalis floating tablets provided by the invention can overcome takes blood drug level peak, the paddy phenomenon that occurs behind the common quick release sheet, can keep balance, persistent effective blood drug concentration in equal dosage and interval, thereby increase curative effect; Or reduce dosage when keeping equal drug effect, take the side effect that medicine brings to the patient thereby reduce; Particularly owing to slowly discharge, this not only can improve medicine and gastrointestinal contact area, makes drug absorption complete, thereby the bioavailability height, keeps long action time.
A kind of intra-gastric floating tablet that contains Folium Digitalis Purpureae of the present invention is made up of following component:
0.1 part of Folium Digitalis Purpureae
5 parts of HP-
Hydroxypropyl emthylcellulose K
4M20 parts
80 parts of hexadecanol
100 parts of microcrystalline Cellulose
5 parts of sodium bicarbonate
20 parts of Macrogol 4000s
2 parts of micropowder silica gels
A kind of intra-gastric floating tablet that contains Folium Digitalis Purpureae of the present invention is achieved through the following technical solutions:
(1) HP-with recipe quantity is dissolved in the suitable quantity of water
(2) with behind the good Folium Digitalis Purpureae of an amount of dissolve with ethanol, join while stirring in the HP-solution, 60 ℃ are stirred 30min.
(3) with the hydroxypropyl emthylcellulose K of recipe quantity
4M, hexadecanol, microcrystalline Cellulose, sodium bicarbonate, behind the Polyethylene Glycol mix homogeneously, 80 mesh sieve mixings
(4) (2) are joined in (3), stir the system soft material, cross 20 mesh sieves and granulate 60 ℃ of dryings.
(5) add micropowder silica gel, with 20 mesh sieve granulate, tabletting, product inspection, packing.
A kind of intra-gastric floating tablet that contains Folium Digitalis Purpureae that the present invention obtains has that method is simple, good stability, bioavailability height, compare the characteristics that reduced side effects of pharmaceutical drugs etc. with ordinary preparation.
Following examples explanation the present invention, but do not limit the present invention in any way.
Embodiment 1: 1000 of specifications
Prescription:
Folium Digitalis Purpureae 0.1g
HP-5g
Hydroxypropyl emthylcellulose K
4M20g
Hexadecanol 80g
Microcrystalline Cellulose 100g
Sodium bicarbonate 5g
Macrogol 4000 20g
Micropowder silica gel 2g
Method for making:
(1) HP-with recipe quantity is dissolved in the 15ml water
(2) with behind the good Folium Digitalis Purpureae of 2ml dissolve with ethanol, join while stirring in the HP-solution, 60 ℃ are stirred 30min.
(3) with the hydroxypropyl emthylcellulose K of recipe quantity
4M, hexadecanol, microcrystalline Cellulose, sodium bicarbonate, behind the Polyethylene Glycol mix homogeneously, 80 mesh sieve mixings
(4) (2) are joined in (3), stir the system soft material, cross 20 mesh sieves and granulate 60 ℃ of dryings.
(5) add micropowder silica gel, with 20 mesh sieve granulate, tabletting, product inspection, packing.
Embodiment 2: 10000 of specifications
Prescription:
Folium Digitalis Purpureae 1g
HP-50g
Hydroxypropyl emthylcellulose K
4M200g
Hexadecanol 800g
Microcrystalline Cellulose 1000g
Sodium bicarbonate 50g
Macrogol 4000 200g
Micropowder silica gel 20g
Method for making:
(1) HP-with recipe quantity is dissolved in the 150ml water
(2) with behind the good Folium Digitalis Purpureae of 15ml dissolve with ethanol, join while stirring in the HP-solution, 60 ℃ are stirred 30min.
(3) with the hydroxypropyl emthylcellulose K of recipe quantity
4M, hexadecanol, microcrystalline Cellulose, sodium bicarbonate, behind the Polyethylene Glycol mix homogeneously, 80 mesh sieve mixings
(4) (2) are joined in (3), stir the system soft material, cross 20 mesh sieves and granulate 60 ℃ of dryings.
(5) add micropowder silica gel, with 20 mesh sieve granulate, tabletting, product inspection, packing.
Claims (9)
1. the preparation method of digitalis floating tablets and application thereof, it is characterized in that this intra-gastric floating tablet is is the tablet that principal agent is made with the Folium Digitalis Purpureae, this intra-gastric floating tablet is owing to containing multiple hydrophilic high molecular material, behind body temperature contact gastric juice, surface water changes into gel, and makes volumetric expansion.The weight of tablet floats on the gastric juice tablet less than the buoyancy of gastric juice at this moment, is prolonged gastric transit time.
2. according to the preparation method and the application thereof of the described digitalis floating tablets of claim 1, it is characterized in that the floating adjuvant of stomach comprises hydrophilic gel material, auxiliary floating material, filler, foaming agent and release regulator, its weight ratio is 1.0:0.05～5.0:1.0～10.0:0～2.0:0.1～2.0.
3. according to the preparation method and the application thereof of the described digitalis floating tablets of claim 1, it is characterized in that each sheet contains Folium Digitalis Purpureae 0.01mg～10mg, preferred 0.05mg～1mg.
4. according to the preparation method and the application thereof of the described digitalis floating tablets of claim 1, it is characterized in that including but not limited to following pharmaceutically acceptable adjuvant: hydrophilic gel material hydroxypropyl cellulose, hydroxypropyl emthylcellulose, hydroxyethyl-cellulose, acroleic acid resin series, sodium alginate; Auxiliary floating material hexadecanol, stearic acid, glyceryl monostearate or Cera Flava; Foaming agent sodium bicarbonate or magnesium carbonate; Release regulator Polyethylene Glycol series, polyvidone series, mannitol or lactose etc.
5. according to the preparation method and the application thereof of the described digitalis floating tablets of claim 2, it is characterized in that the floating adjuvant of stomach comprises hydrophilic gel material hydroxypropyl emthylcellulose, auxiliary floating material hexadecanol or stearic acid, filler microcrystalline Cellulose or dextrin, foaming agent sodium bicarbonate or magnesium carbonate, release regulator Polyethylene Glycol, its weight ratio are 1.0:0.2～3.0:3.0～8.0:0.2～1.0:0.5～1.5.
6. according to the preparation method and the application thereof of the described digitalis floating tablets of claim 1, it is characterized in that this intra-gastric floating tablet is to be used for congestive heart failure and some arrhythmia, after one's own heart atrial fibrillation is moving, atrial flutter and paroxysmal tachycardia.
7. according to the preparation method and the application thereof of the described digitalis floating tablets of claim 5, the preparation that it is characterized in that tablet be not limited to adopt direct compression or granulate the back tabletting or with cyclodextrin (comprising beta-schardinger dextrin-, HP-etc.) wait with the containing of principal agent Folium Digitalis Purpureae afterwards tabletting make intra-gastric floating tablet, this floating tablets is formed including but not limited to following component:
0.1 part of Folium Digitalis Purpureae
5 parts of HP-
Hydroxypropyl emthylcellulose K
4M20 parts
80 parts of hexadecanol
100 parts of microcrystalline Cellulose
5 parts of sodium bicarbonate
20 parts of Macrogol 4000s
2 parts of micropowder silica gels
8. the preparation method of digitalis floating tablets according to claim 7 and application thereof, one of prescription that it is characterized in that this floating tablets is:
Folium Digitalis Purpureae 0.1g
HP-5g
Hydroxypropyl emthylcellulose K
4M20g
Hexadecanol 80g
Microcrystalline Cellulose 100g
Sodium bicarbonate 5g
Macrogol 4000 20g
Micropowder silica gel 2g
9. the preparation method of digitalis floating tablets according to claim 8 and application thereof is characterized in that including but not limited to following steps:
(1) HP-with recipe quantity is dissolved in the 15ml water
(2) with behind the good Folium Digitalis Purpureae of 2ml dissolve with ethanol, join while stirring in the HP-solution, 60 ℃ are stirred 30min.
(3) with the hydroxypropyl emthylcellulose K of recipe quantity
4M, hexadecanol, microcrystalline Cellulose, sodium bicarbonate, behind the Polyethylene Glycol mix homogeneously, 80 mesh sieve mixings
(4) (2) are joined in (3), stir the system soft material, cross 20 mesh sieves and granulate 60 ℃ of dryings.
(5) add micropowder silica gel, with 20 mesh sieve granulate, tabletting, product inspection, packing.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007103084333A CN101468100A (en) | 2007-12-29 | 2007-12-29 | Method for preparing digitalis floating tablets and use thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007103084333A CN101468100A (en) | 2007-12-29 | 2007-12-29 | Method for preparing digitalis floating tablets and use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101468100A true CN101468100A (en) | 2009-07-01 |
Family
ID=40826062
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2007103084333A Pending CN101468100A (en) | 2007-12-29 | 2007-12-29 | Method for preparing digitalis floating tablets and use thereof |
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| Country | Link |
|---|---|
| CN (1) | CN101468100A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103313698A (en) * | 2010-10-22 | 2013-09-18 | 梅利亚蒂斯公司 | Process for making multiparticulate gastroretentive dosage forms |
| CN101623377B (en) * | 2009-08-05 | 2013-10-16 | 锦州奥鸿药业有限责任公司 | Digitalis extract as well as preparation method and application thereof |
| CN103800297A (en) * | 2014-02-18 | 2014-05-21 | 四川农业大学 | Intragastric floating sustained release tablet of praziquantel composition and preparation method thereof |
| CN105998702A (en) * | 2016-07-11 | 2016-10-12 | 甘肃鑫晟源生物科技开发有限责任公司 | Traditional Chinese medicine Chinese rhubarb gastric floating tablets for treating alimentary tract hemorrhage and preparation method thereof |
-
2007
- 2007-12-29 CN CNA2007103084333A patent/CN101468100A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101623377B (en) * | 2009-08-05 | 2013-10-16 | 锦州奥鸿药业有限责任公司 | Digitalis extract as well as preparation method and application thereof |
| CN103313698A (en) * | 2010-10-22 | 2013-09-18 | 梅利亚蒂斯公司 | Process for making multiparticulate gastroretentive dosage forms |
| CN103800297A (en) * | 2014-02-18 | 2014-05-21 | 四川农业大学 | Intragastric floating sustained release tablet of praziquantel composition and preparation method thereof |
| CN103800297B (en) * | 2014-02-18 | 2016-05-11 | 四川农业大学 | A kind of praziquantel composition in-stomach floating type sustained-release sheet and preparation method thereof |
| CN105998702A (en) * | 2016-07-11 | 2016-10-12 | 甘肃鑫晟源生物科技开发有限责任公司 | Traditional Chinese medicine Chinese rhubarb gastric floating tablets for treating alimentary tract hemorrhage and preparation method thereof |
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| PB01 | Publication | ||
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Open date: 20090701 |