CN1600316A - Drop Pills of cucurbitacin medication and preparation method - Google Patents
Drop Pills of cucurbitacin medication and preparation method Download PDFInfo
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- CN1600316A CN1600316A CN 03134669 CN03134669A CN1600316A CN 1600316 A CN1600316 A CN 1600316A CN 03134669 CN03134669 CN 03134669 CN 03134669 A CN03134669 A CN 03134669A CN 1600316 A CN1600316 A CN 1600316A
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- cucurbitacin
- drop pill
- drop
- ball
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Abstract
A dripping pill of cucurbitacin is prepared from cucurbitacin and water-soluble medicinal matrix chosen from polyethanediol, sodium stearate, glycerin gelatin and poloxamer through heating the matrix by water bath until it is fused, adding cucurbitacin powder, stirring, holding the temp at 80-90 deg.C, dripping in atoleine for shaping, removing surficial atoleine and drying.
Description
Technical field of the present invention
The present invention relates to cucurbitacin medicinal dropping ball of a kind of treatment hepatitis and preparation method thereof.
Background technology of the present invention
Hepatitis is a kind of commonly encountered diseases, and frequently-occurring disease is distributed in all over the world because be difficult to radical cure and endanger wide, and with cancer, acquired immune deficiency syndrome (AIDS) and claim " centuries three big pertinacious disease." China is the viral hepatitis district occurred frequently, only hepatitis b virus carrier just reaches 1.3 hundred million, and the chronic hepatitis patient more than 3,000 ten thousand is wherein arranged approximately.Hepatic fibrosis just might be taken place as can not effectively treating in these patients, and then liver cirrhosis." trilogy " that this is made up of " hepatitis → hepatic fibrosis → liver cirrhosis ", it is the common pathway that a kind of chronic hepatopathy causes serious consequence.And drop pills of cucurbitacine has effect of anti hepatic fibrosis, and 84 routine chronic hepatitis patients are carried out the fibrosis treatment, and total effective rate is 88.2%.Anti-hepatic fibrosis will have in the market: colchicine, poly phenolic acid of Radix Salviae Miltiorrhizae and salvianolic acid B, can not meet the need of market far away.The medicine that is used for the treatment of hepatocarcinoma has: eliminating mass the liver benefiting sheet, and the cucurbitacin sheet, cinobufacin and 5-fluorouracil, and drop pills of cucurbitacine treatment primary hepatocarcinoma total effective rate is 84.5%.With respect to cinobufacin and 5-Fu, and the drop pills of cucurbitacine toxicity is low weight.
Cucurbitacin is to extract from muskmelon pedicel.Muskmelon pedicel is stated from Shennong's Herbal the earliest, and ancient medical book record is turned to be yellow the jaundice YIN jaundice with nose-insufflating therapy treatment calentura.Useful muskmelon pedicel levigation nasal insufflation treatment acute, chronic hepatitis among the people.The cucurbitacin that extracts from muskmelon pedicel pharmacology in external body experimental results show that and be the effective ingredient of treatment hepatitis that how tame the cucurbitacin tablet is effective to acute, chronic hepatitis through clinical verification.The cucurbitacin tablet has been recorded in the 19 p223 page or leaf of Ministry of Public Health Chinese traditional patent formulation preparation.Change its tablet into drop pill, realize that medicine absorbs rapidly, quick acting improves human bioavailability, reduces the adjuvant use amount, the medication target of carrying taking convenience.
Drop pills of cucurbitacine of the present invention is a pharmaceutical carrier with the water-soluble base, and medicine and substrate are melted altogether, and disintegrate is rapid, and the bioavailability height relatively sees Table 1. table 2. tables 3 with the every index of the tablet of selling at present.
Table 1. preparation process relatively
Table 2. dissolution relatively
See Figure of description 1 by last table drafting figure
Table 3 LD50 ED50 bioavailability, clinical efficacy (total effective rate %) untoward reaction are relatively
As can be known from the above table, drop pills of cucurbitacine, it is simple to have preparation technology, absorb fast, bioavailability height, characteristics such as clinical efficacy is good, and untoward reaction is few..
Summary of the invention of the present invention
The present invention be a kind of with cucurbitacin as active pharmaceutical ingredient, make oral administration dripping pill with medicinal soluble substrate.The water-soluble base that can select for use is one or more in Macrogol 4000, polyethylene glycol 6000, polyethylene glycol 1500, PEG400, Macrogol 600, cetomacrogol 1000, sodium stearate, glycerin gelatine, the poloxamer.Its preparation process is as follows: it is an amount of to get substrate by ratio, be heated to 90-100 ℃ of heating in water bath fusion, treat whole fusions after, add cucurbitacin dry powder, after stirring, be incubated 80-90 ℃, use the water dropper of suitable bore to splash into condensation in the liquid paraffin, make drop pill, the drop pill drop of molding is most, and the erasing liquor paraffin body, drying, promptly getting heavily is the drop pill of 3～60mg.The cucurbitacin that comprises in the drop pill that makes by weight every contain 0.008-0.3mg; Cucurbitacin B by weight every contain 0.005-0.18mg, the substrate amount is 2.992-59.7mg.The drop pill rounding that makes with this law is smooth, and the ball method of double differences is different little, and disintegration time is short, rapid-action.
Cucurbitacin used among the present invention can be prepared by the known method of those skilled in the art, or with meeting the statutory standards commercially available product.Now the present invention will be described with following embodiment, but the present invention is not limited in this embodiment.
Embodiment
Embodiment 1
Prescription
Cucurbitacin (in Cucurbitacin B) 0.06g
PEG4000 20g
Make 1000
[method for making] crosses 60 orders with the cucurbitacin powder, and be standby.Substrate PEG4000 puts in the 90-100 ℃ of water-bath behind the heating and melting, add above-mentioned fine powder, mix homogeneously, the temperature of mixture is remained on 80-90 ℃, and the water dropper of the suitable bore of usefulness splashes into temperature maintenance in 0-5 ℃ liquid paraffin with the speed of 20-35d/min, keeps dripping apart from 3-8cm, the drop pill drop of molding is most, and the erasing liquor paraffin body, drying, promptly.
Every ball contains Cucurbitacin B 0.06mg.Oral, one time 1 ball～3 balls, 3 times on the one.The said preparation heat clearing away of detoxifying, the dampness removing jaundice eliminating.Be used for damp and hot poison contain due to the auxiliary treatment of chronic persistent hepatitis, chronic hepatitis and primary hepatocarcinoma.
Embodiment 2
Prescription
Cucurbitacin (in Cucurbitacin B) 0.06g
PEG6000 20g
Make 1000
Method for making: the same.
Embodiment 3
Prescription
Cucurbitacin (in Cucurbitacin B) 0.06g
PEG4000 16g
PEG400 4g
Make 1000
Method for making: the same.
Embodiment 4
Prescription
Cucurbitacin (in Cucurbitacin B) 0.06g
PEG6000 16g
PEG400 4g
Make 1000
Method for making: the same.
Embodiment 5
Prescription
Cucurbitacin (in Cucurbitacin B) 0.06g
Poloxamer 20g
Make 1000
Method for making: the same.
Description of drawings of the present invention
Fig. 1 is the drug release rate curve that changes along with the time, by this figure release height of drop pill as can be seen
Release in tablet.
Fig. 2 is a drop pills of cucurbitacine preparation technology flow chart.
Claims (8)
1, a kind of cucurbitacin medicinal dropping ball, it is characterized in that this drop pill be by the treatment effective dose cucurbitacin be active component and the made drop pill of medicinal soluble substrate.
2, drop pill as claimed in claim 1, the ball that it is characterized in that said drop pill heavily is 3～60mg.
3, medicinal dropping ball as claimed in claim 1 or 2 is characterized in that comprising water-soluble base and is in Macrogol 4000, polyethylene glycol 6000, polyethylene glycol 1500, PEG400, Macrogol 600, cetomacrogol 1000, sodium stearate, glycerin gelatine, the poloxamer one or more in said drop pill.
4, a kind of medicinal dropping ball as claimed in claim 1 or 2, it is characterized in that the cucurbitacin that comprises in the said drop pill by weight every contain 0.008-0.3mg; Cucurbitacin B by weight every contain 0.005-0.18mg, the substrate amount is 2.992-59.7mg.
5, drop pill as claimed in claim 1 is characterized in that said drop pill is to be prepared with following method:
It is an amount of to get substrate by ratio, be heated to 90-100 ℃ of heating in water bath fusion, treat whole fusions after, add cucurbitacin dry powder, after stirring, be incubated 80-90 ℃, use the water dropper of suitable bore to splash into condensation in the liquid paraffin, make drop pill, the drop pill drop of molding is most, and the erasing liquor paraffin body, drying, promptly.
6, as any described drop pill of claim in front, it is characterized in that this drop pill is oral, one time 1 to 36 ball, three times on the one.
7, cucurbitacin has the effect of heat-clearing and toxic substances removing in preparation, is used for the treatment of the application in the medicine of hepatitis.
8, application as claimed in claim 7, wherein said medicine is an oral drop pills.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03134669 CN1600316A (en) | 2003-09-25 | 2003-09-25 | Drop Pills of cucurbitacin medication and preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03134669 CN1600316A (en) | 2003-09-25 | 2003-09-25 | Drop Pills of cucurbitacin medication and preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1600316A true CN1600316A (en) | 2005-03-30 |
Family
ID=34659070
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03134669 Pending CN1600316A (en) | 2003-09-25 | 2003-09-25 | Drop Pills of cucurbitacin medication and preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1600316A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105663690A (en) * | 2016-03-11 | 2016-06-15 | 孙彪 | Health-aiding compound dropping pills and preparing method thereof |
| CN108042496A (en) * | 2018-01-18 | 2018-05-18 | 承德医学院 | A kind of Cucurbitacin B solid dispersions and preparation method thereof |
-
2003
- 2003-09-25 CN CN 03134669 patent/CN1600316A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105663690A (en) * | 2016-03-11 | 2016-06-15 | 孙彪 | Health-aiding compound dropping pills and preparing method thereof |
| CN105663690B (en) * | 2016-03-11 | 2019-11-08 | 孙彪 | One kind helping health compound dripping pill and preparation method thereof |
| CN108042496A (en) * | 2018-01-18 | 2018-05-18 | 承德医学院 | A kind of Cucurbitacin B solid dispersions and preparation method thereof |
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| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |