CN103127021A - Vitamin c dropping pill - Google Patents
Vitamin c dropping pill Download PDFInfo
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- CN103127021A CN103127021A CN2013100531561A CN201310053156A CN103127021A CN 103127021 A CN103127021 A CN 103127021A CN 2013100531561 A CN2013100531561 A CN 2013100531561A CN 201310053156 A CN201310053156 A CN 201310053156A CN 103127021 A CN103127021 A CN 103127021A
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- vitamin
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- clathrate
- dropping pill
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Abstract
The invention relates to a vitamin C dropping pill, in particular to a sustained-release dripping pill containing a vitamin C inclusion compound.
Description
Technical field
The application relates to a kind of drop pill, particularly, is the sustained-release dropping pill that comprises the vitamin C clathrate.
Background technology
Drop pill has the following characteristics: 1, equipment simple, easy to operate, be beneficial to labor protection, process cycle is short, productivity ratio is high; 2, process conditions are easy to control, steady quality, and dosage is accurate, and heated time is short, after easily oxidation and the volatile medicine of tool are dissolved in substrate, can increase its stability; 3, to hold the liquid drug amount large for substrate, therefore liquid drug is solidified; 4, the drop pill with the solid dispersion technology preparation has the characteristics rapid, that bioavailability is high that absorb.
Clathrate has the following advantages: cover bad stink, reduce zest; Increase drug dissolution and bioavailability; Improve medicine stability.
Vitamin C claims again ascorbic acid, be a kind of in the middle of antioxidant vitamins, its participates in hydroxylation reaction in body, and is essential by forming between skeleton, tooth, connective tissue and non-Epithelial cell sticking thing, can keep the normal function of tooth, skeleton, blood vessel, increase the resistivity to disease.Report that according to interrelated data vitamin C has shortage in various degree in each crowd.When some indispositions appear in health, just should in time replenish appropriate vitamin and mineral and improve food deficiency disease, especially person in middle and old age should comparatively pay attention to.Vitamin has preventive effect to numerous disease, and the generation of numerous disease may more or less have relation with ascorbic shortage, and vitamin C can also be treated some disease with many other drug drug combinations in addition.
The research of relevant vitamin C clathrate sustained-release dropping pill was not yet disclosed at present.
Summary of the invention
The present invention has invented vitamin C clathrate sustained-release dropping pill in order to solve existing Vitamin C preparation poor stability, shortcoming that bioavailability is low.
The application first is prepared into clathrate with vitamin C, and then is prepared into sustained-release dropping pill, and it is one that enclose, slow release and drop pill technology are closed three, the advantage of performance three aspects:.
Drop pill comprises the vitamin C clathrate, substrate, stabilizing agent.
The vitamin C clathrate comprises active component and enclose material, and active component is vitamin C, and the enclose material is beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, one or more of hydroxypropylβ-cyclodextrin.The part by weight of active component and enclose material is 4:1-1:4.
The preparation method of vitamin C clathrate comprises:
(1) in water or aquiferous ethanol medium, by a certain percentage, with vitamin C and alpha-cyclodextrin, beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, one or more reactions of hydroxypropylβ-cyclodextrin, gained solution through extremely clarification of filtering with microporous membrane, is isolated clathrate from mixture; Or
(2) with solid form, with vitamin C and alpha-cyclodextrin, beta-schardinger dextrin-, hydroxyl beta-schardinger dextrin-, one or more reactions of hydroxypropylβ-cyclodextrin; Or
(3) vitamin C and alpha-cyclodextrin, beta-schardinger dextrin-, the hydroxyl beta-schardinger dextrin-, high energy milling is carried out in one or more reactions of hydroxypropylβ-cyclodextrin.
The substrate of sustained-release dropping pill is to realize the key of slow release effect, through many-side research, select glyceryl monostearate, polyethylene glycol 6000 and stearic mixture as substrate, and three's part by weight is 1:1:1.5, can prepare the splendid dropping pill formulation of slow release effect, and the drop pill that makes becomes ball, roundness best.
The above-mentioned vitamin C clathrate for preparing is crossed the 100-200 mesh sieve, be mixed into solid dispersion system with substrate and stabilizing agent, splash into the condensed fluid of 0-20 ℃ under 65 ± 5 ℃, adsorption condensing liquid, the drop pill drying, and get final product.
The stabilizing agent of indication of the present invention comprises that phosphatic PH buffering is right, as sodium hydrogen phosphate and sodium dihydrogen phosphate.
The condensed fluid of indication of the present invention comprises condensed fluid dimethicone, liquid paraffin, Oleum Camelliae, vegetable oil etc.
Metering of the present invention is weight.
Embodiment 1
The prescription of drop pill is (by weight):
Vitamin C clathrate (vitamin C: hydroxypropylβ-cyclodextrin is 1:2) 4.2g
Glyceryl monostearate, polyethylene glycol 6000 and stearic mixture (three's part by weight is 1:1:1.5) 18g
Sodium hydrogen phosphate and sodium dihydrogen phosphate 0.2g
Condensed fluid is liquid paraffin.
Preparation method:
1. prepare by the following method the vitamin C clathrate:
(1) in water or aquiferous ethanol medium, in proportion, with vitamin C and hydroxypropylβ-cyclodextrin reaction, gained solution through extremely clarification of filtering with microporous membrane, is isolated clathrate from mixture; Or
(2) with solid form, with vitamin C and hydroxypropylβ-cyclodextrin reaction; Or
(3) high energy milling is carried out in the reaction of vitamin C and hydroxypropylβ-cyclodextrin.
2. the vitamin C clathrate was pulverized the 100-200 mesh sieve; Glyceryl monostearate, polyethylene glycol 6000, stearic acid, sodium hydrogen phosphate and sodium dihydrogen phosphate ground and mixed is even, heating and melting on water-soluble, and mixing; The vitamin C clathrate is added in the fused mass of glyceryl monostearate, polyethylene glycol 6000, stearic acid, sodium hydrogen phosphate and sodium dihydrogen phosphate, mixing, in the impouring material fluid bath, kept 65-70 ℃ of temperature 10 minutes, above-mentioned medicinal liquid is splashed in the liquid paraffin of 0-20 ℃ and form drop pill, absorb condensed fluid, dry drop pill, packing.
Matched group 1
The prescription of drop pill is (by weight):
Vitamin C clathrate (vitamin C: hydroxypropylβ-cyclodextrin is 1:2) 4.2g
Polyethylene glycol 6000 18g
Sodium hydrogen phosphate and sodium dihydrogen phosphate 0.2g
Condensed fluid is dimethicone.
Preparation method is the same.
Matched group 2
The prescription of drop pill is (by weight):
Vitamin C clathrate (vitamin C: hydroxypropylβ-cyclodextrin is 1:2) 4.2g
Glyceryl monostearate 18g
Sodium hydrogen phosphate and sodium dihydrogen phosphate 0.2g
Condensed fluid is liquid paraffin.
Preparation method is the same.
Matched group 3
The prescription of drop pill is (by weight):
Vitamin C clathrate (vitamin C: hydroxypropylβ-cyclodextrin is 1:2) 4.2g
Stearic acid 18g
Sodium hydrogen phosphate and sodium dihydrogen phosphate 0.2g
Condensed fluid is liquid paraffin.
Preparation method is the same.
Vitamin C clathrate drop pill experimental result
The method of pressing Chinese Pharmacopoeia (2000 editions) detects the smooth rounding rate of drop pill, the results are shown in Table 1.
Table 1
| Group | Smooth rounding rate (%) |
| Embodiment 1 | 97.52 |
| Matched group 1 | 85.11 |
| Matched group 2 | 82.37 |
| Matched group 3 | 78.95 |
Result shows, vitamin C clathrate drop pill provided by the invention meets Chinese Pharmacopoeia (2000 editions) about the regulation of drop pill.
The slow release effect in vivo test
Experimental animal: 40 of new zealand rabbits, body weight 2.0-2.6kg is provided by Dalian Medical Univ's Experimental Animal Center.
Test method: with 1 week of new zealand rabbit routine feeding, be divided at random 4 groups, 10 every group.Respectively oral administration embodiment 1 and matched group 1,2,3 drop pill.Dosage is 10mg/kg.After administration 0.5,1,6,24,72h and 1,2 weeks got blood 1ml from arteria auricularis, measure ascorbic concentration (mg/L) in the different time points blood sample with high performance liquid chromatograph.The results are shown in Table 2.
Table 2
| Time | Embodiment 1 | Matched group 1 | Matched group 2 | Matched group 3 |
| 0.5h | 1.52 | 2.21 | 2.23 | 2.45 |
| 1h | 3.39 | 6.23 | 6.52 | 6.33 |
| 6h | 2.09 | 0.68 | 0.71 | 0.34 |
| 24h | 1.12 | 0.02 | 0.01 | 0 |
| 72h | 0.56 | 0 | 0 | 0 |
| 1 week | 0.35 | 0 | 0 | 0 |
| 2 weeks | 0.10 | 0 | 0 | 0 |
By as seen from Table 2, the embodiment of the present invention 1 drop pill has good slow release effect, has particularly selected the embodiment 1 of particular substrate and ratio, has better slow release effect.
Claims (7)
1. preparation, wherein active component is vitamin C.
2. sustained-release dropping pill, wherein active component is vitamin C.
3. sustained-release dropping pill as claimed in claim 2, wherein vitamin C is clathrate, the enclose material is alpha-cyclodextrin, beta-schardinger dextrin-, the hydroxyl beta-schardinger dextrin-, one or more of hydroxypropylβ-cyclodextrin, the part by weight of vitamin C and enclose material is 4:1-1:4.
4. sustained-release dropping pill as claimed in claim 3, wherein drop pill comprises the vitamin C clathrate, substrate, stabilizing agent.
5. sustained-release dropping pill as claimed in claim 4, its mesostroma comprise one or more mixing of glyceryl monostearate, polyethylene glycol 6000, stearic acid, Macrogol 4000; Stabilizing agent comprises sodium hydrogen phosphate and sodium dihydrogen phosphate.
6. sustained-release dropping pill as claimed in claim 4, wherein Basic compose is glyceryl monostearate, polyethylene glycol 6000 and stearic mixture, and three's part by weight is 1:1:1.5.
7. sustained-release dropping pill as claimed in claim 4, wherein the prescription of drop pill is (by weight):
Vitamin C clathrate (vitamin C: hydroxypropylβ-cyclodextrin is 1:2) 4.2g
Glyceryl monostearate, polyethylene glycol 6000 and stearic mixture (three's part by weight is 1:1:1.5)
18g
Sodium hydrogen phosphate and sodium dihydrogen phosphate 0.2g
Condensed fluid is liquid paraffin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310053156.1A CN103127021B (en) | 2013-02-19 | 2013-02-19 | Vitamin c dropping pill |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310053156.1A CN103127021B (en) | 2013-02-19 | 2013-02-19 | Vitamin c dropping pill |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103127021A true CN103127021A (en) | 2013-06-05 |
| CN103127021B CN103127021B (en) | 2014-08-20 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310053156.1A Active CN103127021B (en) | 2013-02-19 | 2013-02-19 | Vitamin c dropping pill |
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| Country | Link |
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| CN (1) | CN103127021B (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106309565A (en) * | 2015-06-29 | 2017-01-11 | 北京海吉星医疗科技有限公司 | Zhenqifuzheng slow release dripping pills and preparation method thereof |
| US11491100B2 (en) | 2013-03-12 | 2022-11-08 | Primal Therapies, Inc. | Dermal composition comprising chelator and base |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1943563A (en) * | 2006-11-09 | 2007-04-11 | 庄洪波 | Vitamin dripping pill and its preparing method |
| CN102579318A (en) * | 2011-01-10 | 2012-07-18 | 杭州赛利药物研究所有限公司 | Stable vitamin C sustained release preparation and preparation method thereof |
-
2013
- 2013-02-19 CN CN201310053156.1A patent/CN103127021B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1943563A (en) * | 2006-11-09 | 2007-04-11 | 庄洪波 | Vitamin dripping pill and its preparing method |
| CN102579318A (en) * | 2011-01-10 | 2012-07-18 | 杭州赛利药物研究所有限公司 | Stable vitamin C sustained release preparation and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 李慧等: "精制芎归缓释滴丸的制备", 《中国中药杂志》, vol. 30, no. 10, 31 May 2005 (2005-05-31), pages 747 - 749 * |
| 钱佩佩等: "维生素C包合物的拉曼光谱验证", 《中国成人医药教育论坛[2010(3)]》, 28 September 2010 (2010-09-28), pages 99 - 104 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11491100B2 (en) | 2013-03-12 | 2022-11-08 | Primal Therapies, Inc. | Dermal composition comprising chelator and base |
| CN106309565A (en) * | 2015-06-29 | 2017-01-11 | 北京海吉星医疗科技有限公司 | Zhenqifuzheng slow release dripping pills and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN103127021B (en) | 2014-08-20 |
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Address after: 266103 Qingdao economic and Technological Development Zone, unity Road, No. 3601, Shandong Applicant after: Qingdao Zhengda Haier Pharmaceutical Co., Ltd. Address before: 266103 Haier Road, Shandong, Qingdao, No. 1 Applicant before: Qingdao Zhengda Haier Pharmaceutical Co., Ltd. |
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Address after: 266103 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Patentee after: Zhengda Pharmaceutical (Qingdao) Co., Ltd. Address before: 266103 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Patentee before: Qingdao Zhengda Haier Pharmaceutical Co., Ltd. |