CN101991619A - Pomegranate controlled-release pellets and preparation method thereof - Google Patents
Pomegranate controlled-release pellets and preparation method thereof Download PDFInfo
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- CN101991619A CN101991619A CN2009101009534A CN200910100953A CN101991619A CN 101991619 A CN101991619 A CN 101991619A CN 2009101009534 A CN2009101009534 A CN 2009101009534A CN 200910100953 A CN200910100953 A CN 200910100953A CN 101991619 A CN101991619 A CN 101991619A
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- Prior art keywords
- punica granatum
- slow
- preparation
- release micro
- ball core
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- 235000014360 Punica granatum Nutrition 0.000 title claims abstract description 61
- 238000002360 preparation method Methods 0.000 title claims abstract description 29
- 241000219991 Lythraceae Species 0.000 title abstract description 11
- 239000008188 pellet Substances 0.000 title abstract description 6
- 238000013270 controlled release Methods 0.000 title abstract 3
- 244000294611 Punica granatum Species 0.000 claims description 52
- 239000006187 pill Substances 0.000 claims description 23
- 239000008118 PEG 6000 Substances 0.000 claims description 9
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 claims description 9
- 229920002472 Starch Polymers 0.000 claims description 9
- 239000011230 binding agent Substances 0.000 claims description 9
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 claims description 9
- 239000008107 starch Substances 0.000 claims description 9
- 235000019698 starch Nutrition 0.000 claims description 9
- 229930006000 Sucrose Natural products 0.000 claims description 7
- 239000005720 sucrose Substances 0.000 claims description 7
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims description 6
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 claims description 6
- 239000000843 powder Substances 0.000 claims description 6
- 239000000463 material Substances 0.000 claims description 5
- 230000002572 peristaltic effect Effects 0.000 claims description 5
- 239000007921 spray Substances 0.000 claims description 5
- 239000004834 spray adhesive Substances 0.000 claims description 5
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 239000002994 raw material Substances 0.000 claims description 4
- 239000002904 solvent Substances 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 3
- 229920003081 Povidone K 30 Polymers 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 238000002156 mixing Methods 0.000 claims description 2
- 125000000185 sucrose group Chemical group 0.000 claims description 2
- 239000003814 drug Substances 0.000 abstract description 6
- 229940079593 drug Drugs 0.000 abstract description 6
- 239000007767 bonding agent Substances 0.000 abstract 1
- 230000036470 plasma concentration Effects 0.000 abstract 1
- 229940109529 pomegranate extract Drugs 0.000 abstract 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 5
- 239000008280 blood Substances 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 4
- 230000001476 alcoholic effect Effects 0.000 description 3
- 235000013399 edible fruits Nutrition 0.000 description 3
- AFSDNFLWKVMVRB-UHFFFAOYSA-N Ellagic acid Chemical compound OC1=C(O)C(OC2=O)=C3C4=C2C=C(O)C(O)=C4OC(=O)C3=C1 AFSDNFLWKVMVRB-UHFFFAOYSA-N 0.000 description 2
- ATJXMQHAMYVHRX-CPCISQLKSA-N Ellagic acid Natural products OC1=C(O)[C@H]2OC(=O)c3cc(O)c(O)c4OC(=O)C(=C1)[C@H]2c34 ATJXMQHAMYVHRX-CPCISQLKSA-N 0.000 description 2
- 229920002079 Ellagic acid Polymers 0.000 description 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 2
- 241001083505 Punica Species 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 229960002852 ellagic acid Drugs 0.000 description 2
- 235000004132 ellagic acid Nutrition 0.000 description 2
- FAARLWTXUUQFSN-UHFFFAOYSA-N methylellagic acid Natural products O1C(=O)C2=CC(O)=C(O)C3=C2C2=C1C(OC)=C(O)C=C2C(=O)O3 FAARLWTXUUQFSN-UHFFFAOYSA-N 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 239000003075 phytoestrogen Substances 0.000 description 2
- 238000013268 sustained release Methods 0.000 description 2
- 239000012730 sustained-release form Substances 0.000 description 2
- 208000017897 Carcinoma of esophagus Diseases 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 229930003451 Vitamin B1 Natural products 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000003712 anti-aging effect Effects 0.000 description 1
- 230000003064 anti-oxidating effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000009509 drug development Methods 0.000 description 1
- 201000005619 esophageal carcinoma Diseases 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 229960003512 nicotinic acid Drugs 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
- 239000011664 nicotinic acid Substances 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 230000035764 nutrition Effects 0.000 description 1
- 235000008935 nutritious Nutrition 0.000 description 1
- 238000000643 oven drying Methods 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 229960003495 thiamine Drugs 0.000 description 1
- DPJRMOMPQZCRJU-UHFFFAOYSA-M thiamine hydrochloride Chemical compound Cl.[Cl-].CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N DPJRMOMPQZCRJU-UHFFFAOYSA-M 0.000 description 1
- 239000011691 vitamin B1 Substances 0.000 description 1
- 235000010374 vitamin B1 Nutrition 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention relates to pomegranate controlled-release pellets and a preparation method thereof. The pellets are prepared from 20-50wt% of main drug of pomegranate extract, 20-50wt% of pellet core and 0.5-3wt% of bonding agent. The invention solves the problem that a pomegranate preparation in the background technology has low bioavailability because the pomegranate preparation cannot maintain stable plasma concentration, and provides the pomegranate controlled-release pellets with high bioavailability.
Description
Technical field
The present invention relates to pharmaceutical preparation and preparation method thereof, relate in particular to a kind of Punica granatum L. slow-release micro-pill and preparation method thereof.
Background technology
Punica granatum L. have another name called pomegranate, Calamina pomegranate, if pomegranate, golden small-mouthed jar, red if, day slurry, English name: Pomegranate.Punicaceae (Punicaceae) Punica (Punica L.) plant, fruit is attractive in appearance bright-coloured, and is nutritious.Punica granatum L. contains abundant vitamin B1, B2, B6, VC and nicotinic acid and phytoestrogen, wherein ascorbic content is higher 1～2 times than Fructus Mali pumilae, human body is highly profitable, and particularly phytoestrogen especially is concerned by people to the effect of diseases such as female dimacteric syndrome, osteoporosis.Ellagic acid content is 123.76mg/g in the Punica granatum L., has effects such as opposing pulmonary carcinoma, the esophageal carcinoma, antioxidation IC, and Northwestern Univ USA's medical college is being studied this acid, is used for preventing curing cancers.And the nutrition consultant Ao Cijia West Asia of the Equino health club in New York says that becoming is " the human known thing that has anti-aging effects most " to ellagic acid.The Punica granatum L. aboundresources extensively has cultivation in China various places.Punica granatum L. is as one of domestic fruit of giving priority to, and the regular modelling of cultivated area develops.And Punica granatum L. is only edible as fruit in certain areas, causes the serious wasting of resources.Should further strengthen the pharmacological component research of Punica granatum L. from now on, provide a new effective natural drug for clinical, for new drug development is laid a good foundation.The clear and definite pharmacological action of Punica granatum L. more and more has been subjected to people's attention, believes along with going deep into of studying, and will have the excellent development prospect.
The pharmaceutical preparation of Punica granatum L. at present mainly contains the Punica granatum L. vegetarian piece, does not have the Punica granatum L. sustained-release pellet preparation, and the Punica granatum L. vegetarian piece can not keep stable blood drug level in human body, cause its bioavailability not high.
Summary of the invention
The invention provides a kind of energy and keep stable blood drug level, the Punica granatum L. slow-release micro-pill that bioavailability is high.
Another object of the present invention is to provide a kind of preparation method of Punica granatum L. slow-release micro-pill.
In order to solve the problem that exists in the background technology, realize the foregoing invention purpose, the invention provides following technical scheme:
A kind of Punica granatum L. slow-release micro-pill, this micropill comprise 20%～50% principal agent Punica granatum L. extract, 20%～50% ball core and 0.5%～3% binding agent by weight percentage.
This micropill also comprises 10%～40% excipient.
This micropill also comprises 10～45% solubilizing agents.
Described ball core is sucrose ball core, starch ball core or microcrystalline Cellulose ball core.
Described binding agent is one or more mixing among 30 POVIDONE K 30 BP/USP 30, PEG400, the PEG6000.
Described solubilizing agent is PEG400, PEG6000.
Described excipient is a starch.
The invention also discloses a kind of preparation method of Punica granatum L. slow-release micro-pill, this preparation method comprises the steps:
(1) pretreatment of raw material and binder solution preparation;
(2) adjust each parameter of centrifuge, put into the ball core;
(3) mixture of Punica granatum L. extract and starch is put into the centrifuge hopper, the setting rotating speed is 3～7r/min;
(4) beginning shows spray adhesive solution to the ball core, and the setting rotating speed is 5～11r/min, when the ball core shows enough moistening and adhesion, begins to start blanking device and prepares micropill;
(5) after the hopper material uses up, close the hydrojet peristaltic pump and for the powder switch, allow the micropill of preparation rotate in centrifuge 5 minutes, oven dry promptly then.
During pretreatment of raw material Punica granatum L. extract crossed 200 mesh sieves.
The adjustment centrifuge parameters is: air quantity " little " is set, and rotating speed is 220r/min, and temperature control " pass " is put into and adjusted the spray gun position behind the ball core, and the setting atomizing pressure is 0.05mpa.
Punica granatum L. slow-release micro-pill of the present invention has solved that the Punica granatum L. preparation can not cause the not high problem of its bioavailability keeping stable blood drug level in the background technology, provides a kind of bioavailability high Punica granatum L. slow-release micro-pill.
The specific embodiment
The present invention will be further described below by specific embodiment.
Embodiment 1:
Prescription: Punica granatum L. extract 200g sucrose ball core 200g
Starch 200g polyvidone k30 7.5g
Preparation technology:
The 50% alcoholic solution preparation of (1) 3% polyvidone k30 is as binding agent;
(2) supplementary material is carried out pretreatment, Punica granatum L. extract is crossed 200 mesh sieves, and starch is crossed 120 mesh sieves, mixes after sieve;
(3) centrifuge air quantity " little " is set, rotating speed is 220r/min; Temperature control " pass " is put into pot with sucrose ball core, adjusts the spray gun position, and the setting atomizing pressure is 0.05mpa;
(4) Punica granatum L. extract powder and starch mixture are put into the centrifuge hopper, the setting rotating speed is 5r/min;
(5) beginning shows spray adhesive to the ball core, and the setting rotating speed is 8r/min, during enough moistening and adhesion, begins to start blanking device when the ball wicking surface, begins to prepare micropill;
(6) after the hopper material uses up, close the hydrojet peristaltic pump and, allow the micropill for preparing after centrifuge is relayed to 5 minutes, take out micropill, make moisture≤6% promptly get the Punica granatum L. slow-release micro-pill in 40 ± 5 ℃ circulation oven drying for the powder switch.
The micropill that obtains is filled to promptly gets the Punica granatum L. sustained-release micro-pill capsules in the capsule shells.
The Punica granatum L. slow-release micro-pill that the present invention obtains slowly discharges in human body, keeps the stable of blood drug level, the bioavailability height.
Embodiment 2:
Prescription: Punica granatum L. extract 200g PEG400 120G
PEG6000 120g sucrose ball core 200g polyvidone k30 20g
Preparation method:
(1) 50% alcoholic solution of preparation 1.5% polyvidone k30 adds PEG400, PEG6000, stirs, and is prepared into binding agent;
(2) to supplementary material pretreatment respectively, Punica granatum L. extract is crossed 200 mesh sieves;
(3) centrifuge air quantity " little " is set, rotating speed is 220r/min; Temperature control " pass " is put into pot with sucrose ball core, adjusts the spray gun position, and the setting atomizing pressure is 0.05mpa;
(4) Punica granatum L. extract is put into the centrifuge hopper, the setting rotating speed is 7r/min;
(5) beginning is to ball wicking surface spray adhesive, and settings rotating speed is 9r/min, and during enough moistening and adhesion, the unlatching blanking device begins to prepare micropill when the ball wicking surface;
(6) after the hopper material uses up, close the hydrojet peristaltic pump and for the powder switch, allow the micropill of preparation in centrifuge, rotate 5 minutes after, the taking-up micropill with 40 ± 5 ℃ of oven dry, makes moisture≤6% promptly get the Punica granatum L. slow-release micro-pill in the circulation baking oven.
Embodiment 3:
Prescription: Punica granatum L. extract 200g PEG6000 70g
Microcrystalline Cellulose ball core 300g
Preparation technology: 50% alcoholic solution of (1) preparation 50%PEG6000, as binding agent;
(2) to supplementary material pretreatment respectively, Punica granatum L. extract is crossed 200 mesh sieves;
(3) centrifuge air quantity " little " is set, rotating speed is 220r/min; Temperature control " pass " is put into pot with sucrose ball core, adjusts the spray gun position, and the setting atomizing pressure is 0.05mpa;
(4) Punica granatum L. extract is put into the centrifuge hopper, the setting rotating speed is 7r/min;
(5) beginning is to ball wicking surface spray adhesive, and settings rotating speed is 9r/min, and during enough moistening and adhesion, the unlatching blanking device begins to prepare micropill when the ball wicking surface;
(6) after the hopper material uses up, close the hydrojet peristaltic pump and for the powder switch, allow the micropill of preparation in centrifuge, rotate 5 minutes after, the taking-up micropill with 40 ± 5 ℃ of oven dry, makes moisture≤6% promptly get the Punica granatum L. slow-release micro-pill in the circulation baking oven.
Embodiment 4:
Prescription: Punica granatum L. extract 100g PEG6000 200g
Microcrystalline Cellulose ball core 300g
Preparation method is identical with embodiment 3.
Claims (10)
1. a Punica granatum L. slow-release micro-pill is characterized in that this micropill comprises 20%～50% principal agent Punica granatum L. extract, 20%～50% ball core and 0.5%～3% binding agent by weight percentage.
2. a kind of Punica granatum L. slow-release micro-pill according to claim 1 is characterized in that this micropill also comprises 10%～40% excipient.
3. a kind of Punica granatum L. slow-release micro-pill according to claim 1 is characterized in that this micropill also comprises 10～45% solubilizing agents.
4. a kind of Punica granatum L. slow-release micro-pill according to claim 1 is characterized in that described ball core is sucrose ball core, starch ball core or microcrystalline Cellulose ball core.
5. a kind of Punica granatum L. slow-release micro-pill according to claim 1 is characterized in that described binding agent is one or more mixing among 30 POVIDONE K 30 BP/USP 30, PEG400, the PEG6000.
6. a kind of Punica granatum L. slow-release micro-pill according to claim 1 is characterized in that described solubilizing agent is PEG400, PEG6000.
7. a kind of Punica granatum L. slow-release micro-pill according to claim 1 is characterized in that described excipient is a starch.
8. according to the preparation method of any one described a kind of Punica granatum L. slow-release micro-pill of claim 1～4, it is characterized in that this preparation method comprises the steps:
(1) pretreatment of raw material and binder solution preparation;
(2) adjust each parameter of centrifuge, put into the ball core;
(3) mixture of Punica granatum L. extract and starch is put into the centrifuge hopper, the setting rotating speed is 3～7r/min;
(4) beginning shows spray adhesive solution to the ball core, and the setting rotating speed is 5～11r/min, when the ball core shows enough moistening and adhesion, begins to start blanking device and prepares micropill;
(5) after the hopper material uses up, close the hydrojet peristaltic pump and for the powder switch, allow the micropill of preparation rotate in centrifuge 5 minutes, oven dry promptly then.
9. the preparation method of a kind of Punica granatum L. slow-release micro-pill according to claim 7 when it is characterized in that pretreatment of raw material is crossed Punica granatum L. extract 200 mesh sieves.
10. the preparation method of a kind of Punica granatum L. slow-release micro-pill according to claim 7, it is characterized in that adjusting centrifuge parameters is: air quantity " little " is set, and rotating speed is 220r/min, temperature control " pass ", adjust the spray gun position after putting into the ball core, the setting atomizing pressure is 0.05mpa.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009101009534A CN101991619B (en) | 2009-08-10 | 2009-08-10 | Pomegranate controlled-release pellets and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009101009534A CN101991619B (en) | 2009-08-10 | 2009-08-10 | Pomegranate controlled-release pellets and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101991619A true CN101991619A (en) | 2011-03-30 |
| CN101991619B CN101991619B (en) | 2013-09-25 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2009101009534A Active CN101991619B (en) | 2009-08-10 | 2009-08-10 | Pomegranate controlled-release pellets and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101991619B (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1823804A (en) * | 2005-12-30 | 2006-08-30 | 刘展欣 | Clamycin fast release micropill and its preparation method |
| CN101254223A (en) * | 2008-03-04 | 2008-09-03 | 东莞市竟恒流通研究所 | New use of pericarpium Granati and semen Granati extract for improving prostate symptom |
| CN101396348A (en) * | 2008-10-25 | 2009-04-01 | 浙江华义医药有限公司 | Omeprazole enteric-coated micro-pill |
-
2009
- 2009-08-10 CN CN2009101009534A patent/CN101991619B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1823804A (en) * | 2005-12-30 | 2006-08-30 | 刘展欣 | Clamycin fast release micropill and its preparation method |
| CN101254223A (en) * | 2008-03-04 | 2008-09-03 | 东莞市竟恒流通研究所 | New use of pericarpium Granati and semen Granati extract for improving prostate symptom |
| CN101396348A (en) * | 2008-10-25 | 2009-04-01 | 浙江华义医药有限公司 | Omeprazole enteric-coated micro-pill |
Non-Patent Citations (1)
| Title |
|---|
| 钟玲; 许小红; 杨胜玉; 苏青: "中药微丸的药学研究进展", 《时珍国医国药》 * |
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| Publication number | Publication date |
|---|---|
| CN101991619B (en) | 2013-09-25 |
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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 Applicant after: Hangzhou Saili Medicine Inst. Co., Ltd. Applicant after: Hainan Pulin Pharmaceutical Co., Ltd. Applicant after: Zhejiang Poly Pharmaceutical 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 Applicant before: Hangzhou Saili Medicine Inst. Co., Ltd. Applicant before: Hainan Pulin Pharmaceutical Co., Ltd. Applicant before: Zhejiang Ridae Pharmaceutical Co., Ltd. |
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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 Saili Medicine Inst. Co., Ltd. Patentee after: Hainan Puli Pharmacy stock Co., Ltd Patentee after: Zhejiang Poly Pharmaceutical 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 Saili Medicine Inst. Co., Ltd. Patentee before: Hainan Pulin Pharmaceutical Co., Ltd. Patentee before: Zhejiang Poly Pharmaceutical Co., Ltd. |