CN101804145B - Garlic oil enteric pellet capsule and preparation method thereof - Google Patents
Garlic oil enteric pellet capsule and preparation method thereof Download PDFInfo
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- CN101804145B CN101804145B CN2009100958359A CN200910095835A CN101804145B CN 101804145 B CN101804145 B CN 101804145B CN 2009100958359 A CN2009100958359 A CN 2009100958359A CN 200910095835 A CN200910095835 A CN 200910095835A CN 101804145 B CN101804145 B CN 101804145B
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Abstract
The invention relates to the field of antibacterial agent, in particular to a garlic oil enteric pellet capsule and a preparation method thereof. Wherein the garlic oil pellet capsule is composed of a coated pellets and a coating layer, the coated pellets comprises pharmaceutically active ingredients of garlic oil and coated pellet minor ingredient; wherein the coated pellet minor ingredient comprises pellet core, bonding agent, absorbing agent, disintegrating agent, antioxygen agent and antiplastering aid while the coating layer comprises an enteric coating and an isolated layer; the coated pellet comprises the following components according to weight percentage: 5-40% of garlic oil, 10-60% of pellet core, 2-10% of binding agent, 20-50% of absorbing agent, 0.5-5% of antioxygen agent, 0.5-10% of disintegrating agent and 2-20% of antiplastering aid.Compared with the existing allicin dosage form, the garlic oil enteric pellet capsule of the invention enjoys more advanced dosage form, thus ensuring effectiveness and stability of the capsule and high bioavailability; in addition, with the enteric pellet capsule of the invention, harm done to gastric mucosa as the capsule is dissolved inside the stomach is avoided and the allicin is not damaged by gastric acid so that drug effect of the capsule is not affected.
Description
Technical field
The present invention relates to the antibacterial medicine preparation field, relate in particular to a kind of garlic oil enteric pellet capsule and preparation method thereof.
Background technology
Garlicin (Allicin) has another name called allicin, and chemical name diallyl trisulfide (CH2=CH2CH22S2S2S2CH22CH=CH2) is the volatility oily thing that from the spherical bulb of Bulbus Allii, extracts, and is the main effective ingredient of Bulbus Allii.Garlicin is except that having traditional antibiotic, the antiviral of Bulbus Allii, protozoacidal effect; Modern medicine proof its also have antitumor, with effects such as blood fat, human body immunity improving power; Be described as " natural broad ectrum antibiotic ", the bactericidal action of pure garlicin is 100 times of penicillin, is abused at current antibiotic; Under the continuous enhanced situation of antibiotic property, Oleum Bulbus Allii is considered to the alternative of desirable safety.In recent years, Chinese scholars has been carried out many-sided research to the chemistry of Bulbus Allii, pharmacology and clinical, proves that garlicin has remarkable effect.But Bulbus Allii oil volatility, unstability and the human body mucosa is had stronger zest limited being widely used of garlicin.At present, the Oleum Bulbus Allii preparation has dosage forms such as tablet, enteric coated tablet, capsule, enteric coated capsule, enteric soft gelatin capsule, soft capsule, injection, but all there are some defectives in these present dosage forms, are in particular in:
1, conventional tablet, capsule, soft capsule are in the stomach disintegrate, and principal agent is poor stability under acid condition, are prone to degraded, are difficult to bring into play due effect;
Though 2, enteric coated tablet can be avoided stomach acids destroy, long the micropill holdup time at gastric transit time, release does not have the micropill good uniformity in intestinal portion; Enteric coated capsule is opened at stomach easily, thereby part is destroyed.
3, the enteric soft gelatin capsule also might break because of the food extruding, even open in intestinal portion, the relative micropill of its drug distribution concentration will be concentrated manyly, is unfavorable for the absorption of medicine, thereby does not have the drug effect of pellet preparations under the Isodose.
Publication number is that one Chinese patent application garlicin enteric coated capsule and the compounding method thereof of CN101006994 discloses a kind of garlicin enteric coated capsule and compounding method thereof; This patent application be with Oleum Bulbus Allii with the beta-schardinger dextrin-bag with; And then process granule or micropill, and overlapping capsule shells at last and obtain, its micropill of this enteric coated capsule is after the enteral dissolving; Cost with beta-schardinger dextrin-bag and Oleum Bulbus Allii is higher, and the beta-schardinger dextrin-bag and bag and the bad easy stability to degradation of garlicin that causes of property bad.
Summary of the invention
The object of the present invention is to provide a kind of good stability, bioavailability height, dissolved garlic oil enteric pellet capsule in intestinal.
Another object of the present invention is to provide a kind of method for preparing of garlic oil enteric pellet capsule.
The present invention is the basis with the micropill technology, absorbs Oleum Bulbus Allii with adjuvant and makes it be completed into water miscible dispersion, and then at its outer parcel enteric solubility material, realize the present invention thereby overlap capsule shells at last.
In order to solve the problem that exists in the above-mentioned background technology, realize goal of the invention, the present invention adopts following technical scheme:
A kind of garlic oil enteric pellet capsule; By plain ball and coatings; Wherein plain ball comprises effective ingredient Oleum Bulbus Allii and plain ball adjuvant; Described plain ball adjuvant comprises ball core, binding agent, absorbent, disintegrating agent, antioxidant and antiplastering aid; Coatings comprises enteric coating and sealing coat, and each component is pressed following percentage by weight proportioning in the plain ball: 5%～40% Oleum Bulbus Allii, 10%～60% ball core, 2%～10% binding agent, 20%～50% absorbent, 0.5%～5% antioxidant, 0.5%～10% disintegrating agent, 2%～20% antiplastering aid.
Described plain ball comprises the component of following weight percentage ratio: 11.3% Oleum Bulbus Allii, 48.7% ball core, 8% binding agent, 24.3% absorbent, 1% antioxidant, 1.6% disintegrating agent and 4.7% antiplastering aid.
Described binding agent is PVP or CMCNa.
Described disintegrating agent is cross-linked pvp or crosslinked CMCNa.
Described ball core is sucrose ball core, starch ball core or microcrystalline Cellulose ball core.
Described absorbent is one or more mixing in starch, microcrystalline Cellulose, the lactose.
Enteric-coating material in the described coatings is Lac or acrylic resin.
The invention also discloses a kind of method for preparing of garlic oil enteric pellet capsule, comprise the steps:
A, get the plain ball adjuvant of recipe quantity, add Oleum Bulbus Allii after adding the abundant suspendible of 95% ethanol, stir 30min, add TW-80 and continue to stir more than the 30min, subsequent use;
B, get the ball core and place in the pellet processing machine, the material loading pill is processed micropill, and parameter is controlled as follows:
Rotating speed 350rpm.Temperature 24dec, whitewashing 25, the air quantity transfer is big;
C, get micropill and carry out coating, last enteric coating liquid, parameter is controlled as follows:
Rotating speed 400rpm, temperature 27dec, whitewashing 8, air quantity is big;
Finish the continued isolation coat, finish rewinding.
The present invention is the basis with the micropill technology; Take the adjuvant absorption method; Oleum Bulbus Allii (effective ingredient is allicin, i.e. garlicin) is processed the water solublity dispersion, outer again by acid resistance materials such as enteric material such as Lac; Pack into after processing in the conventional capsule, thereby accomplish the preparation of garlic oil enteric pellet capsule.The present invention adopts the adjuvant absorption process, Oleum Bulbus Allii is prepared into water miscible dispersion, changed Oleum Bulbus Allii traditionally with the beta-schardinger dextrin-bag and method.Improved the water solublity of Oleum Bulbus Allii greatly, the water miscible raising of Oleum Bulbus Allii makes it in intestinal, form dispersion to have improved the absorption of intestinal to garlicin, reduced the stimulation to intestinal mucosa.
Garlic oil enteric pellet capsule of the present invention and existing garlicin dosage form relatively have the dosage form advance; Thereby also can guarantee the effectiveness and the stability of medicine; Bioavailability is higher; And enteric coated micropill of the present invention has avoided medicine in the gastric dissolving gastric mucosa to be caused damage, and has guaranteed that also garlicin can not influenced its drug effect by stomach acids destroy simultaneously.
The specific embodiment
Below in conjunction with specific embodiment the present invention is done further elaboration.
Embodiment 1: present embodiment prepares garlic oil enteric pellet capsule, adopts prescription as follows:
Plain ball prescription:
The coating prescription:
Lac 149.2g adds 1500ml95% ethanol, and stirred overnight makes dissolving fully, and is subsequent use;
Contagion gown: 20gPVP, 6.7g Pulvis Talci add 500ml95% dissolve with ethanol, suspendible, and be subsequent use.
Concrete step of preparation process is following:
A, get the plain ball adjuvant of recipe quantity, add Oleum Bulbus Allii after adding the abundant suspendible of 95% ethanol, stir 30min, add TW-80 and continue to stir more than the 30min, subsequent use;
B, get the ball core and place in the pellet processing machine, the material loading pill is processed micropill, and parameter is controlled as follows:
Rotating speed 350rpm.Temperature 24dec, whitewashing 25, the air quantity transfer is big;
C, get micropill and carry out coating, last enteric coating liquid, parameter is controlled as follows:
Rotating speed 400rpm, temperature 27dec, whitewashing 8, air quantity is big;
Finish the continued isolation coat, finish rewinding, the cover capsule shells obtains.
The garlic oil enteric pellet capsule that obtains is measured, and the result is following:
Garlicin content is 4.15%, acid resistance 87.17%, enteric reclaim 0.59% dissolving fully.
Embodiment 2: present embodiment adopts following prescription:
Plain ball prescription:
The coating prescription:
Acrylic resin 149.2g adds 1500ml95% ethanol, and stirred overnight makes dissolving fully, and is subsequent use;
Contagion gown: 20gPVP, 6.7g Pulvis Talci add 500ml95% dissolve with ethanol, suspendible, and be subsequent use.
Technology is identical with embodiment 1.
Embodiment 3: present embodiment adopts following prescription:
Plain ball prescription:
The coating prescription:
Lac 149.2g adds 1500ml95% ethanol, and stirred overnight makes dissolving fully, and is subsequent use;
Contagion gown: 20gPVP, 6.7g Pulvis Talci add 500ml95% dissolve with ethanol, suspendible, and be subsequent use.
Technology is identical with embodiment 1.
Embodiment 4: the garlic oil enteric pellet capsule that embodiment 1～3 is made detects.
Test item: 1, outward appearance: ocular estimate;
2, release degree: by this quality draft standard method, should be up to specification;
3, content: by this quality draft standard method, should be up to specification.
4, result:
Can know that by above-mentioned experiment the garlic oil enteric pellet capsule of gained of the present invention meets the requirements fully on release degree and content, have the high characteristics of stability.
The present invention is the basis with the micropill technology; Take the adjuvant absorption method; Oleum Bulbus Allii (effective ingredient is allicin, i.e. garlicin) is processed the water solublity dispersion, outer again by acid resistance materials such as enteric material such as Lac; Pack into after processing in the conventional capsule, thereby accomplish the preparation of garlicin enteric-coated pellet capsule.The present invention adopts the adjuvant absorption process, Oleum Bulbus Allii is prepared into water miscible dispersion, changed Oleum Bulbus Allii traditionally with the beta-schardinger dextrin-bag and method.Improved the water solublity of Oleum Bulbus Allii greatly, the water miscible raising of Oleum Bulbus Allii makes it in intestinal, form dispersion to have improved the absorption of intestinal to garlicin, reduced the stimulation to intestinal mucosa.
Garlic oil enteric pellet capsule of the present invention and existing garlicin dosage form relatively have the dosage form advance; Thereby also can guarantee the effectiveness and the stability of medicine; Bioavailability is higher; And enteric coated micropill of the present invention has avoided medicine in the gastric dissolving gastric mucosa to be caused damage, and has guaranteed that also Oleum Bulbus Allii can not influenced its drug effect by stomach acids destroy simultaneously.
Claims (2)
1. garlic oil enteric pellet capsule; Form by plain ball and coatings; Wherein plain ball comprises effective ingredient Oleum Bulbus Allii and plain ball adjuvant; It is characterized in that described plain ball adjuvant comprises ball core, binding agent, absorbent, disintegrating agent, antioxidant and antiplastering aid; Coatings comprises enteric coating and sealing coat, and each component is pressed following percentage by weight proportioning in the plain ball: 5%～40% Oleum Bulbus Allii, 10%～60% ball core, 2%～10% binding agent, 20%～50% absorbent, 0.5%～5% antioxidant, 0.5%～10% disintegrating agent, 2%～20% antiplastering aid; Described binding agent is PVP or CMCNa; Described disintegrating agent is cross-linked pvp or crosslinked CMCNa; Described ball core is sucrose ball core, starch ball core or microcrystalline Cellulose ball core; Described absorbent is one or more mixing in starch, microcrystalline Cellulose, the lactose; Enteric-coating material in the described coatings is Lac or acrylic resin.
2. according to the method for preparing of any one described a kind of garlic oil enteric pellet capsule of claim 1, it is characterized in that comprising the steps:
A, get the plain ball adjuvant of recipe quantity except that the ball core, add Oleum Bulbus Allii after adding the abundant suspendible of 95% ethanol, stir 30min, add TW-80 and continue to stir more than the 30min, subsequent use;
B, get the ball core and place in the pellet processing machine, the material loading pill is processed micropill, and parameter is controlled as follows:
Rotating speed 350rpm, 24 ℃ of temperature, whitewashing 25, the air quantity transfer is big;
C, get micropill and carry out coating, last enteric coating liquid, parameter is controlled as follows:
Rotating speed 400rpm, 27 ℃ of temperature, whitewashing 8, air quantity is big;
Finish the continued isolation coat, finish rewinding.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100958359A CN101804145B (en) | 2009-02-12 | 2009-02-12 | Garlic oil enteric pellet capsule and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100958359A CN101804145B (en) | 2009-02-12 | 2009-02-12 | Garlic oil enteric pellet capsule and preparation method thereof |
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| Publication Number | Publication Date |
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| CN101804145A CN101804145A (en) | 2010-08-18 |
| CN101804145B true CN101804145B (en) | 2012-11-14 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN2009100958359A Active CN101804145B (en) | 2009-02-12 | 2009-02-12 | Garlic oil enteric pellet capsule and preparation method thereof |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN107802842B (en) * | 2016-09-07 | 2022-04-12 | 汤臣倍健股份有限公司 | Allicin flavouring preparation and its preparation method |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1200924A (en) * | 1997-05-29 | 1998-12-09 | 伊莱利利公司 | Fluoxetine enteric micropills |
| CN101006994A (en) * | 2006-01-23 | 2007-08-01 | 湖北金龙福药业有限公司 | Enteric-coated capsules of allimin and its preparation method |
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2009
- 2009-02-12 CN CN2009100958359A patent/CN101804145B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1200924A (en) * | 1997-05-29 | 1998-12-09 | 伊莱利利公司 | Fluoxetine enteric micropills |
| CN101006994A (en) * | 2006-01-23 | 2007-08-01 | 湖北金龙福药业有限公司 | Enteric-coated capsules of allimin and its preparation method |
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| CN101804145A (en) | 2010-08-18 |
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Address after: West Building in Hangzhou City, Zhejiang province 310052 Binjiang District Lake Road 1180 Huaye hi tech Industrial Park Building No. 2 Patentee after: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. Patentee after: HAINAN POLY PHARM. Co.,Ltd. Address before: West Building in Hangzhou City, Zhejiang province 310052 Binjiang District Lake Road 1180 Huaye hi tech Industrial Park Building No. 2 Patentee before: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. Patentee before: Hainan Poly Pharm Co.,Ltd. |
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Effective date of registration: 20230116 Address after: 571127 Guilin Ocean Economic Development Zone, Meilan District, Haikou City, Hainan Province Patentee after: HAINAN POLY PHARM. Co.,Ltd. Address before: West Building in Hangzhou City, Zhejiang province 310052 Binjiang District Lake Road 1180 Huaye hi tech Industrial Park Building No. 2 Patentee before: HANGZHOU SHARPLY PHARM R&D INSTIT. Co.,Ltd. Patentee before: HAINAN POLY PHARM. Co.,Ltd. |
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