CN1833650A - Jixuedai dispersion tablet having function of promoting wound reunion, and its prepn. method - Google Patents
Jixuedai dispersion tablet having function of promoting wound reunion, and its prepn. method Download PDFInfo
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- CN1833650A CN1833650A CN 200610000790 CN200610000790A CN1833650A CN 1833650 A CN1833650 A CN 1833650A CN 200610000790 CN200610000790 CN 200610000790 CN 200610000790 A CN200610000790 A CN 200610000790A CN 1833650 A CN1833650 A CN 1833650A
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- China
- Prior art keywords
- asiaticoside
- herba centellae
- total glycosides
- wound healing
- centellae total
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 238000000034 method Methods 0.000 title claims abstract description 20
- 239000006185 dispersion Substances 0.000 title claims description 14
- 230000001737 promoting effect Effects 0.000 title abstract 2
- WYQVAPGDARQUBT-FGWHUCSPSA-N Madecassol Chemical compound O([C@@H]1[C@@H](CO)O[C@H]([C@@H]([C@H]1O)O)OC[C@H]1O[C@H]([C@@H]([C@@H](O)[C@@H]1O)O)OC(=O)[C@]12CC[C@H]([C@@H]([C@H]1C=1[C@@]([C@@]3(CC[C@H]4[C@](C)(CO)[C@@H](O)[C@H](O)C[C@]4(C)[C@H]3CC=1)C)(C)CC2)C)C)[C@@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@H]1O WYQVAPGDARQUBT-FGWHUCSPSA-N 0.000 claims abstract description 27
- WYQVAPGDARQUBT-XCWYDTOWSA-N asiaticoside Natural products O=C(O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO[C@H]2[C@H](O)[C@H](O)[C@H](O[C@H]3[C@H](O)[C@H](O)[C@@H](O)[C@H](C)O3)[C@@H](CO)O2)O1)[C@@]12[C@@H]([C@@H](C)[C@H](C)CC1)C=1[C@](C)([C@@]3(C)[C@@H]([C@@]4(C)[C@H]([C@@](CO)(C)[C@@H](O)[C@H](O)C4)CC3)CC=1)CC2 WYQVAPGDARQUBT-XCWYDTOWSA-N 0.000 claims abstract description 27
- 229940022757 asiaticoside Drugs 0.000 claims abstract description 27
- QCYLIQBVLZBPNK-UHFFFAOYSA-N asiaticoside A Natural products O1C(C(=O)C(C)C)=CC(C)C(C2(C(OC(C)=O)CC34C5)C)C1CC2(C)C3CCC(C1(C)C)C45CCC1OC1OCC(O)C(O)C1O QCYLIQBVLZBPNK-UHFFFAOYSA-N 0.000 claims abstract description 27
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 52
- 229930182470 glycoside Natural products 0.000 claims description 44
- 150000002338 glycosides Chemical class 0.000 claims description 44
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 28
- 229920002472 Starch Polymers 0.000 claims description 25
- 239000008107 starch Substances 0.000 claims description 25
- 235000019698 starch Nutrition 0.000 claims description 25
- 230000000694 effects Effects 0.000 claims description 22
- 239000003795 chemical substances by application Substances 0.000 claims description 21
- 239000008187 granular material Substances 0.000 claims description 20
- 239000000203 mixture Substances 0.000 claims description 19
- 238000001035 drying Methods 0.000 claims description 17
- 239000000945 filler Substances 0.000 claims description 15
- 238000002360 preparation method Methods 0.000 claims description 15
- 230000029663 wound healing Effects 0.000 claims description 15
- 108010011485 Aspartame Proteins 0.000 claims description 14
- 239000000605 aspartame Substances 0.000 claims description 14
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 14
- 235000010357 aspartame Nutrition 0.000 claims description 14
- 229960003438 aspartame Drugs 0.000 claims description 14
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 10
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 10
- 239000011734 sodium Substances 0.000 claims description 10
- 229910052708 sodium Inorganic materials 0.000 claims description 10
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 9
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 6
- 239000004378 Glycyrrhizin Substances 0.000 claims description 6
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 6
- 229930195725 Mannitol Natural products 0.000 claims description 6
- UEDUENGHJMELGK-HYDKPPNVSA-N Stevioside Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O UEDUENGHJMELGK-HYDKPPNVSA-N 0.000 claims description 6
- LPLVUJXQOOQHMX-UHFFFAOYSA-N glycyrrhetinic acid glycoside Natural products C1CC(C2C(C3(CCC4(C)CCC(C)(CC4C3=CC2=O)C(O)=O)C)(C)CC2)(C)C2C(C)(C)C1OC1OC(C(O)=O)C(O)C(O)C1OC1OC(C(O)=O)C(O)C(O)C1O LPLVUJXQOOQHMX-UHFFFAOYSA-N 0.000 claims description 6
- 229960004949 glycyrrhizic acid Drugs 0.000 claims description 6
- UYRUBYNTXSDKQT-UHFFFAOYSA-N glycyrrhizic acid Natural products CC1(C)C(CCC2(C)C1CCC3(C)C2C(=O)C=C4C5CC(C)(CCC5(C)CCC34C)C(=O)O)OC6OC(C(O)C(O)C6OC7OC(O)C(O)C(O)C7C(=O)O)C(=O)O UYRUBYNTXSDKQT-UHFFFAOYSA-N 0.000 claims description 6
- 235000019410 glycyrrhizin Nutrition 0.000 claims description 6
- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 claims description 6
- 239000008101 lactose Substances 0.000 claims description 6
- 239000000594 mannitol Substances 0.000 claims description 6
- 235000010355 mannitol Nutrition 0.000 claims description 6
- 229940013618 stevioside Drugs 0.000 claims description 6
- OHHNJQXIOPOJSC-UHFFFAOYSA-N stevioside Natural products CC1(CCCC2(C)C3(C)CCC4(CC3(CCC12C)CC4=C)OC5OC(CO)C(O)C(O)C5OC6OC(CO)C(O)C(O)C6O)C(=O)OC7OC(CO)C(O)C(O)C7O OHHNJQXIOPOJSC-UHFFFAOYSA-N 0.000 claims description 6
- 235000019202 steviosides Nutrition 0.000 claims description 6
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 claims description 5
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 5
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims description 5
- 235000019700 dicalcium phosphate Nutrition 0.000 claims description 5
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 5
- 229940085605 saccharin sodium Drugs 0.000 claims description 5
- 239000000811 xylitol Substances 0.000 claims description 5
- 235000010447 xylitol Nutrition 0.000 claims description 5
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 5
- 229960002675 xylitol Drugs 0.000 claims description 5
- DHHFDKNIEVKVKS-FMOSSLLZSA-N Betanin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC(C(=C1)O)=CC(C[C@H]2C([O-])=O)=C1[N+]2=C\C=C\1C=C(C(O)=O)N[C@H](C(O)=O)C/1 DHHFDKNIEVKVKS-FMOSSLLZSA-N 0.000 claims description 4
- DHHFDKNIEVKVKS-MVUYWVKGSA-N Betanin Natural products O=C(O)[C@@H]1NC(C(=O)O)=C/C(=C\C=[N+]/2\[C@@H](C(=O)[O-])Cc3c\2cc(O)c(O[C@H]2[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O2)c3)/C1 DHHFDKNIEVKVKS-MVUYWVKGSA-N 0.000 claims description 4
- 239000001654 beetroot red Substances 0.000 claims description 4
- 235000012677 beetroot red Nutrition 0.000 claims description 4
- 235000002185 betanin Nutrition 0.000 claims description 4
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 3
- 235000011132 calcium sulphate Nutrition 0.000 claims description 3
- 238000007796 conventional method Methods 0.000 claims description 2
- 208000027418 Wounds and injury Diseases 0.000 abstract description 8
- 206010052428 Wound Diseases 0.000 abstract description 7
- 206010039710 Scleroderma Diseases 0.000 abstract description 5
- 206010040943 Skin Ulcer Diseases 0.000 abstract description 2
- 231100000019 skin ulcer Toxicity 0.000 abstract description 2
- 230000035876 healing Effects 0.000 abstract 1
- 239000007919 dispersible tablet Substances 0.000 description 20
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 16
- 239000002671 adjuvant Substances 0.000 description 16
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 16
- 239000008108 microcrystalline cellulose Substances 0.000 description 16
- 229940016286 microcrystalline cellulose Drugs 0.000 description 16
- 239000003814 drug Substances 0.000 description 14
- 239000003826 tablet Substances 0.000 description 9
- 239000000463 material Substances 0.000 description 7
- 239000000080 wetting agent Substances 0.000 description 7
- 229940079593 drug Drugs 0.000 description 6
- 238000012360 testing method Methods 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 238000012216 screening Methods 0.000 description 5
- 208000002260 Keloid Diseases 0.000 description 4
- 206010023330 Keloid scar Diseases 0.000 description 4
- 210000001117 keloid Anatomy 0.000 description 4
- 239000002245 particle Substances 0.000 description 4
- 239000002994 raw material Substances 0.000 description 4
- 229910019142 PO4 Inorganic materials 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 239000001257 hydrogen Substances 0.000 description 3
- 229910052739 hydrogen Inorganic materials 0.000 description 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 3
- 239000010452 phosphate Substances 0.000 description 3
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 229910052791 calcium Inorganic materials 0.000 description 2
- 210000000589 cicatrix Anatomy 0.000 description 2
- 239000002131 composite material Substances 0.000 description 2
- 230000007812 deficiency Effects 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- JEIPFZHSYJVQDO-UHFFFAOYSA-N ferric oxide Chemical compound O=[Fe]O[Fe]=O JEIPFZHSYJVQDO-UHFFFAOYSA-N 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 230000008595 infiltration Effects 0.000 description 2
- 238000001764 infiltration Methods 0.000 description 2
- 231100000252 nontoxic Toxicity 0.000 description 2
- 230000003000 nontoxic effect Effects 0.000 description 2
- 239000002674 ointment Substances 0.000 description 2
- 239000007909 solid dosage form Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 238000012795 verification Methods 0.000 description 2
- 244000063299 Bacillus subtilis Species 0.000 description 1
- 235000014469 Bacillus subtilis Nutrition 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 101001051969 Bos taurus Fibroblast growth factor 2 Proteins 0.000 description 1
- OYPRJOBELJOOCE-IGMARMGPSA-N Calcium-40 Chemical compound [40Ca] OYPRJOBELJOOCE-IGMARMGPSA-N 0.000 description 1
- 244000146462 Centella asiatica Species 0.000 description 1
- 235000004032 Centella asiatica Nutrition 0.000 description 1
- 102000029816 Collagenase Human genes 0.000 description 1
- 108060005980 Collagenase Proteins 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 101500025419 Homo sapiens Epidermal growth factor Proteins 0.000 description 1
- 241001597008 Nomeidae Species 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 206010002022 amyloidosis Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 229960002424 collagenase Drugs 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 210000002919 epithelial cell Anatomy 0.000 description 1
- 229940116978 human epidermal growth factor Drugs 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 235000013372 meat Nutrition 0.000 description 1
- GVUGOAYIVIDWIO-UFWWTJHBSA-N nepidermin Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C(C)C)C(C)C)C1=CC=C(O)C=C1 GVUGOAYIVIDWIO-UFWWTJHBSA-N 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 229940126701 oral medication Drugs 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
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Landscapes
- Medicinal Preparation (AREA)
Abstract
A dispersing tablet of asiaticoside for promoting healing of wound and treating burn, wound, skin ulcer, scleroderma, etc is prepared from asiaticoside and proper auxiliary. Its preparing process is also disclosed.
Description
Technical field
The present invention relates to a kind of dispersion tablet of asiaticoside and preparation method thereof, belong to technical field of Chinese medicine with promotion wound healing.
Technical background
Wound, operation wound, burn, keloid and scleroderma are clinical more common diseases, and wherein skin ulcer, keloid, scleroderma and amyloidosis cutis lack satisfied drug treatment.Current people promote the pharmaceutical requirements of wound healing effect constantly to increase the pursuit of quality of life to having.And chemical drugs and biological preparation such as asiaticoside sodium ointment, Contractubex gel, collagenase ointment, lyophilizing M-EGF, external recombinant human epidermal growth factor derivant, bFGF bovine basic fibroblast growth factor, bacillus subtilis active bacteria formulation etc. are this type of disease preparation of treatment, but only limit external mostly, and certain side effect is arranged; And the effect that now commercially available Chinese medicine preparation such as asiaticoside sheet have tangible promotion wound healing, determined curative effect and having no side effect.Herba Centellae (Centella asiatica) is used existing more than 2,000 year history in China as medicinal plants, and domestic aboundresources spreads all over areas to the south, the Yangtze river basin.Just Herba Centellae extract is used as the medicine that promotes wound healing in the seventies in 20th century abroad, through a large amount of clinical verifications, Herba Centellae total glycosides and preparation thereof, external or for oral administration, wound, operation wound, burn, keloid and scleroderma are had good effect, and almost non-toxic, side effect.Right commercially available asiaticoside sheet at present is a conventional tablet, and disintegration time is longer, and onset time is slower, and bioavailability is low, and dosage form falls behind, and the curative effect fluctuation is bigger, and is limited in clinical use.For this reason, develop the very big concern that a kind of bioavailability height, dosage form advanced person, the sure novel dosage form of curative effect just are subjected to medicine enterprise and research and development unit.
For this reason, the character of inventor's bound drug itself and the modern requirement of Chinese medicine preparation, through scientific appraisal, with its be developed as a kind of new quite being subjected to the patient like, bioavailability height, disintegrate dispersible tablet rapidly.By retrieval, this dispersible tablet still belongs to internal blank.
Summary of the invention
Based on asiaticoside sheet good clinical basis and the present deficiency that exists, the object of the present invention is to provide a kind of new pharmaceutical preparation and preparation method thereof, said preparation is longer at the conventional tablet disintegration time, onset time is slower, and bioavailability is hanged down and waited deficiency, is made into the dispersible tablet of the good reputation of Peroral solid dosage form liquid, not only can in cold water, form uniform suspension after the disintegrate fast, directly drink, also can directly swallow or sublingual administration taking convenience; Increased surface area simultaneously, drug release is fast, increases the infiltration rate and the bioavailability of Herba Centellae total glycosides, plays quick-acting and effect efficiently.
The present invention is achieved through the following technical solutions:
A kind of dispersion tablet of asiaticoside with promotion wound healing effect, it mainly is prepared from by Herba Centellae total glycosides, disintegrating agent, filler, correctives; Calculate Herba Centellae total glycosides (in asiaticoside) 6-10 part, disintegrating agent 40-90 part, correctives 0.5-2 part, filler 0-53.5 part according to parts by weight.Described Herba Centellae total glycosides is commercially available or conventional method makes, and Herba Centellae total glycosides content is not less than 60% in asiaticoside.Disintegrating agent be selected from the fine little element of crystallite, carboxymethyl starch sodium, crosslinked carboxymethyl fecula sodium, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone one or more; Filler is selected from one or more in starch, lactose, mannitol, xylitol, calcium sulfate, the calcium hydrogen phosphate; Correctives is selected from one or more in stevioside, betanin, aspartame, glycyrrhizin, the saccharin sodium.Preferred disintegrating agent is the fine little element of low-substituted hydroxypropyl cellulose, crystallite; Preferred filler is a starch; Preferred correctives is an aspartame.Preferred consumption is: count by weight, the fine little element of crystallite is 20-45 part; Low-substituted hydroxypropyl cellulose is counted 20-45 part by weight.Optimum amount is: count by weight, the fine little element of crystallite is 35-45 part; Low-substituted hydroxypropyl cellulose is 25-35 part.
A kind of preparation method with the dispersion tablet of asiaticoside that promotes wound healing is, gets Herba Centellae total glycosides and the adjuvant pulverize separately becomes fine powder, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 40～80% ethanol, and drying, compacting is in blocks, promptly.Specifically, get Herba Centellae total glycosides and disintegrating agent, filler, correctives,, granulate in right amount with 60% ethanol with the method mix homogeneously that equivalent increases progressively, drying, tabletting, promptly.
At prior art, Herba Centellae total glycosides has the activation epithelial cell, promotes normal meat dental tissue to form, and accelerates to hinder face and heals rapidly, has the fibrocellular propagation of inhibition, prevents that cicatrix from developing, and makes established cicatrix soften the effect of grade.A large amount of clinical verifications, Herba Centellae total glycosides and preparation thereof, no matter external or for oral administration all has good effect to wound, operation wound, burn, keloid and scleroderma, and almost non-toxic, side effect.It is right because most oral medication belongs to general formulation, exist disintegration time longer, absorb slowly, drawbacks such as bioavailability is low, bound drug character of the present invention and the modern requirement of Chinese medicine preparation are made into the dispersible tablet of the good reputation of Peroral solid dosage form liquid, not only can in cold water, form uniform suspension after the disintegrate fast, directly drink, also can directly swallow or sublingual administration taking convenience; Increased surface area simultaneously, drug release is fast, increases the infiltration rate and the bioavailability of Herba Centellae total glycosides, plays quick-acting and effect efficiently.
The inventor finds that in development process kind, the consumption of adjuvant have considerable influence to it, and for this reason, the applicant has carried out a series of experiments, and is rationally feasible, quality controllable with proof technology of the present invention, to guarantee the beneficial effect of medicine.
Experimental example 1: Study on Forming
1.1 the screening of wetting agent
Be that disintegrating agent, starch are filler with carboxymethyl starch sodium (CMS) at first, fixing prescription screens wetting agent, the results are shown in Table.
The screening of table wetting agent (unit: gram)
| Name of material | Prescription 1 | Name of material | Prescription 2 | Name of material | Prescription 3 |
| Asiaticoside raw material CMS starch phosphate hydrogen calcium 80% ethanol particle water content hardness (KG) outward appearance | 10 50 30 10 Q.S about 4% 2.8 are on a small quantity frangible | Asiaticoside raw material CMS starch phosphate hydrogen calcium 60% ethanol particle water content hardness (KG) outward appearance | 10 60 20 10 Q.S about 4% 3.6 are good | Asiaticoside raw material CMS starch phosphate hydrogen calcium 40% ethanol particle water content hardness (KG) outward appearance | 10 70 10 10 Q.S are about, and 4% 4.5 parts have pit |
More than experiment shows, each material is formed under the identical condition in prescription, and 40%～80% ethanol can both satisfy the preparation requirement substantially, but when being wetting agent with 80% ethanol, granule is looser, and the part tablet is frangible; When 40% ethanol was wetting agent, granule was hard, the part tablet has pit; 60% ethanol liquid is during as wetting agent, and granule viscosity is moderate, and the slice, thin piece that is pressed into has certain rigidity, and outward appearance is good.When doing this type of test with other adjuvant, also be same test effect.Therefore, preferred 60% ethanol is as wetting agent.
1.2 disintegrating agent screening
Through test, with in the fine little element of crystallite, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, the crospolyvinylpyrrolidone one or more is disintegrating agent, in starch, lactose, mannitol, xylitol, calcium sulfate, the calcium hydrogen phosphate one or more are filler, can make satisfactory dispersion tablet of asiaticoside; Experiment simultaneously finds that adopting composite auxiliary material low-substituted hydroxypropyl cellulose (L-HPC) and microcrystalline Cellulose (MCC) is disintegrating agent, starch is that filler can make easy-formation, the dispersible tablet that disintegration rate is fast, so preferred version is to be disintegrating agent with low-substituted hydroxypropyl cellulose (L-HPC) and microcrystalline Cellulose (MCC), starch is filler, below its consumption is examined or check, result of the test sees Table.
Table prescription screening tables of data (unit: gram)
| Name of material | Formula number | |||||||
| 1 | 2 | 3 | 4 | 5 | 6 | 7 | 8 | |
| Asiaticoside raw material L-HPC MCC starch 60% ethanol particle water content disintegration (branch) hardness (KG) | 10 30 40 20 Q.S about 4% 1.0 4.5 | 10 45 20 20 Q.S about 4% 1.2 3.9 | 10 20 45 20 Q.S about 4% 1.6 4.2 | 10 45 30 15 Q.S about 4% 1.7 4.3 | 10 30 35 25 Q.S about 4% 1.1 4.4 | 10 40 25 17 Q.S about 4% 1.4 4.6 | 10 25 45 20 Q.S about 4% 0.9 4.5 | 10 35 35 20 Q.S about 4% 0.8 4.4 |
From above result as can be known, composite auxiliary material low-substituted hydroxypropyl cellulose (L-HPC), microcrystalline Cellulose (MCC), starch effect in the dispersible tablet prescription is better, can make satisfactory dispersible tablet, the fine little element of the preferred crystallite of disintegrating agent, low-substituted hydroxypropyl cellulose.The fine little element of crystallite is counted 20-45 part by weight, and best umber is 35-45 part; Low-substituted hydroxypropyl cellulose is counted 20-45 part by weight, and best umber is 25-35 part.
1.3 correctives consumption screening
In view of Herba Centellae total glycosides in the side is bitter, add the sweeting agent flavoring so adopt, sweeting agent commonly used has: stevioside, betanin, aspartame (Aspartrame), glycyrrhizin and saccharin sodium etc.Through trial test, above-mentioned sweeting agent uses separately or is used and can both reach the flavoring purpose to some extent; Result of the test shows that aspartame is a sweeting agent, and not only mouthfeel is good, and can be fit to the use of diabetics simultaneously, so preferred aspartame is a correctives.Through its consumption examination being found by weight, the aspartame that adds 0.5-2 part can be corrected the bitterness of this medicine.
Concrete embodiment
Embodiment 1: Herba Centellae total glycosides 9.23g, low-substituted hydroxypropyl cellulose 30g, microcrystalline Cellulose 40g, aspartame 1g, starch 19.77g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 60% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 2: Herba Centellae total glycosides 9g, low-substituted hydroxypropyl cellulose 25g, calcium sulfate 45g, aspartame 0.5g, lactose 20.5g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 60% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 3: Herba Centellae total glycosides 8g, low-substituted hydroxypropyl cellulose 28g, calcium hydrogen phosphate 45g, stevioside 1.5g, lactose 17.5g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 60% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 4: Herba Centellae total glycosides 7g, microcrystalline Cellulose 28g, carboxymethyl starch sodium 10, crospolyvinylpyrrolidone 15, mannitol 25g, saccharin sodium 1.0g, glycyrrhizin 0.5g, lactose 20g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 60% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 5: Herba Centellae total glycosides 10g, low-substituted hydroxypropyl cellulose 30g, microcrystalline Cellulose 40g, aspartame 2g, xylitol 18g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 75% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 6: Herba Centellae total glycosides 6g, low-substituted hydroxypropyl cellulose 30g, microcrystalline Cellulose 40g, aspartame 1g, starch 20g, calcium hydrogen phosphate 3g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 65% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 7: Herba Centellae total glycosides 8g, low-substituted hydroxypropyl cellulose 30g, microcrystalline Cellulose 40g, stevioside 0.5g, glycyrrhizin 0.5g, starch 21g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 60% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 8: Herba Centellae total glycosides 7g, low-substituted hydroxypropyl cellulose 20g, microcrystalline Cellulose 45g, aspartame 0.5g, starch 27.5g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 60% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 9: Herba Centellae total glycosides 10g, low-substituted hydroxypropyl cellulose 25g, microcrystalline Cellulose 45g, aspartame 1.5g, starch 18.5g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 70% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 10: Herba Centellae total glycosides 10g, low-substituted hydroxypropyl cellulose 35g, microcrystalline Cellulose 35g, betanin 0.5g, starch 19.5g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 50% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 11: Herba Centellae total glycosides 8g, low-substituted hydroxypropyl cellulose 45g, microcrystalline Cellulose 20g, stevioside 1g, calcium sulfate 6g, mannitol 20g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 80% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 12: Herba Centellae total glycosides 6g, carboxymethyl starch sodium 20g, crosslinked carboxymethyl fecula sodium 20g, saccharin sodium 0.5g, xylitol 20.5g, mannitol 33g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 40% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Embodiment 13: Herba Centellae total glycosides 9.5g, crospolyvinylpyrrolidone 90g, glycyrrhizin 0.5g
Get the adjuvant in Herba Centellae total glycosides and the prescription, with the method mix homogeneously that equivalent increases progressively, granulate in right amount with 60% ethanol, drying is pressed into 1000, promptly gets dispersible tablet.
Claims (8)
1, a kind of dispersion tablet of asiaticoside with promotion wound healing effect is characterized in that it mainly is prepared from by Herba Centellae total glycosides, disintegrating agent, filler, correctives; Calculate Herba Centellae total glycosides (in asiaticoside) 6-10 part, disintegrating agent 40-90 part, correctives 0.5-2 part, filler 0-53.5 part according to parts by weight.
2, a kind of dispersion tablet of asiaticoside that promotes the wound healing effect that has according to claim 1 is characterized in that described Herba Centellae total glycosides is commercially available or conventional method makes, and Herba Centellae total glycosides content is not less than 60% in asiaticoside.
3, a kind of dispersion tablet of asiaticoside that promotes the wound healing effect that has according to claim 1, it is characterized in that, disintegrating agent be selected from the fine little element of crystallite, carboxymethyl starch sodium, crosslinked carboxymethyl fecula sodium, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone one or more; Filler is selected from one or more in starch, lactose, mannitol, xylitol, calcium sulfate, the calcium hydrogen phosphate; Correctives is selected from one or more in stevioside, betanin, aspartame, glycyrrhizin, the saccharin sodium.
4, a kind of dispersion tablet of asiaticoside that promotes the wound healing effect that has according to claim 3 is characterized in that, disintegrating agent is meant low-substituted hydroxypropyl cellulose, the fine little element of crystallite; Filler is meant starch; Correctives is meant aspartame.
5, according to claim 1,4 described a kind of dispersion tablet of asiaticoside that promote the wound healing effect that have, it is characterized in that count by weight, the fine little element of crystallite is 20-45 part; Low-substituted hydroxypropyl cellulose is counted 20-45 part by weight.
6, a kind of dispersion tablet of asiaticoside that promotes the wound healing effect that has according to claim 5 is characterized in that, counts by weight, and the fine little element of crystallite is 35-45 part; Low-substituted hydroxypropyl cellulose is 25-35 part.
7, a kind of preparation method with the dispersion tablet of asiaticoside that promotes wound healing according to claim 6 is characterized in that, gets Herba Centellae total glycosides and disintegrating agent, filler, correctives, with the method mix homogeneously that equivalent increases progressively, granulate drying in right amount with 40-80% ethanol, tabletting, promptly.
8, a kind of preparation method with the dispersion tablet of asiaticoside that promotes wound healing according to claim 7 is characterized in that, gets Herba Centellae total glycosides and reaches disintegrating agent, filler, correctives, with the method mix homogeneously that equivalent increases progressively, granulate drying in right amount with 60% ethanol, tabletting, promptly.
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| CN109303746B (en) * | 2018-12-13 | 2021-05-28 | 广州环亚化妆品科技有限公司 | Prebiotic composition and preparation method and application thereof |
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