CN1962639A - Lappaconitine hydrochoric acid, its production method and its uses in preparing analgetic - Google Patents
Lappaconitine hydrochoric acid, its production method and its uses in preparing analgetic Download PDFInfo
- Publication number
- CN1962639A CN1962639A CN 200510100907 CN200510100907A CN1962639A CN 1962639 A CN1962639 A CN 1962639A CN 200510100907 CN200510100907 CN 200510100907 CN 200510100907 A CN200510100907 A CN 200510100907A CN 1962639 A CN1962639 A CN 1962639A
- Authority
- CN
- China
- Prior art keywords
- lappaconitine
- hydrochoric acid
- crystallization
- hydrochoric
- acid
- 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.)
- Pending
Links
Abstract
The invention discloses a manufacturing method of alcaine high-sinomontanine and application in the anodyne, which comprises the following steps: dissolving high-sinomontanine through alcohol or carbinol; dripping alcaine solution; stewing; eluting; crystallizing; filtering; washing crystallization through little solvent; drying.
Description
Technical field
The present invention relates to a kind of new compound Lappaconitine hydrochoric acid, its production method and the application in the preparation anodyne thereof.
Background technology
Aconitum sinomontanum Nakai (Radix aconiti sinomontanea) is the dry taproot of ranunculaceae plant Aconitum sinomontanum Nakai (Aconitumsinomontanum Nakai), nature and flavor suffering, hardship, temperature, poisonous.The 1980s in the past never as the single medicine or be used for its effective constituent clinical.One of nineteen seventies applicant once studied the diterpenes alkaloid in the Aconitum sinomontanum Nakai, and therefrom extract several alkaloids, wherein the main component lappaconitine is lappaconitine (Lappaconitine) after measured, have good analgesic activity, and make Lappaconitine and be used for clinically, the result shows, it has stronger analgesic activity, and do not have habituation, accumulate poisoning also can not take place in no teratogenesis.The 1980s formally as medicinal application in clinical, through area, Lanzhou 12 tame hospitals, the checking of Shanghai liang man hospital clinical, the analgesic effect of various pain 385 examples, no matter quiet, intramuscular injection, oral, all effective in cure, obvious effective rate 49.09%, total effective rate 87.27%, its onset time is slow slightly than pethidine, but it is longer to hold time.
Because Lappaconitine is insoluble in water,, certain difficulty is arranged then if when the patient needs the aqueous injection of Lappaconitine of higher concentration when treatment; Because it is insoluble in water, therefore its absorption in vivo also has been subjected to influence, causes its onset of pain control slow simultaneously.In addition, dissociative bromonium ions has certain side effect in vivo, and can there be anaphylaxis in a few patients, it is reported that also there is suspicious carcinogenesis in bromide anion.
Summary of the invention
Purpose of the present invention be exactly for the onset of pain control that overcomes Lappaconitine slow, have the certain toxic side effect and the shortcoming of suspicious carcinogenesis, a kind of rapid-action, its production method of compound Lappaconitine hydrochoric acid that toxic side effect is little and the application in the preparation anodyne thereof are provided.
Lappaconitine hydrochoric acid of the present invention, its chemical name are (1 α, 14 α, 16 β)-20-ethyl-1,14,16-trimethoxy aconitane-4,8,9-triol 4-[2-(kharophen)] benzoic ether hydrochloride monohydrate.Its structural formula is:
Molecular formula: C
32H
44N
2O
8HClH
2O
Molecular weight: 639.19
Lappaconitine hydrochoric acid of the present invention, white crystals odorless, bitter, mp.205-207 ℃ of (dec.) [α]
D+ 32 ° ± 1 (C, 2; Methyl alcohol), Lappaconitine hydrochoric acid of the present invention dissolves in water, also dissolving in the methyl alcohol, and micro dissolution in ethanol, almost insoluble in chloroform.
Lappaconitine hydrochoric acid of the present invention is non-addicted analgesics, has stronger analgesic activity.Also have toponarcosis, cooling, analgesic and anti-inflammatory action.To compare analgesic effect suitable with Pethidine, and onset time is close, and it is longer to hold time; Analgesic activity is more than 7 times of antipyretic and analgesic pyramidon.
Lappaconitine hydrochoric acid of the present invention does not have teratogenesis through animal experiment, no mutagenesis and do not have carcinogenesis.
The producer genealogy of law of Lappaconitine hydrochoric acid of the present invention adopts the lappaconitine crystallization through Aconitum sinomontanum Nakai extraction, separation, purifying preparation, with ethanol or dissolve with methanol, dripping hydrochloric acid solution, makes congo-red test paper just become blue, place, separate out crystallization, filter, crystallization a small amount of solvent drip washing, drying, promptly.Filtrate can be continued as mother liquid recycle.
The present invention adopts conventional pharmaceutical carrier auxiliary material commonly used on the pharmaceutics, by pharmaceutics method commonly used, is prepared into any adoptable oral dosage form and injection type, includes but not limited to oral liquid, tablet, capsule, injection powder pin, injection liquid.
When the present invention adopted oral dosage form, the formulation amount was 5mg～10mg, every day 1～2 time;
When adopting injection type, dosage is 10mg, every day 1～2 time.
The invention will be further described below in conjunction with embodiment.
Embodiment
The preparation of embodiment 1 Lappaconitine hydrochoric acid
The production method of Lappaconitine hydrochoric acid of the present invention is used the method for 93100499.3 patents, system adopts through Aconitum sinomontanum Nakai through the ethanol submergence, heating and refluxing extraction, filter, be further purified, the lappaconitine crystallization of preparation gained, with ethanol or dissolve with methanol, filtrate decompression concentrates, and reclaims ethanol, and being concentrated into has crystallization to occur on the vessel wall; Leave standstill, separate out throw out; Dripping hydrochloric acid solution shakes up, and makes congo-red test paper just become blue, places, and separates out crystallization, filters, and crystallization is with small amount of ethanol or methanol solvate drip washing, and drying promptly gets Lappaconitine hydrochoric acid.
The analgesic test result of embodiment 2 Lappaconitine hydrochoric acids
Show that through mouse animal experiment the oral hydrochloride lappaconitine is fast slightly than the Lappaconitine analgesic activity, analgesia duration is suitable.
Claims (4)
1, Lappaconitine hydrochoric acid, its chemical name are (1 α, 14 α, 16 β)-20-ethyl-1,14,16-trimethoxy aconitane-4,8,9-triol 4-[2-(kharophen)] benzoic ether hydrochloride monohydrate.
Its structural formula is:
2, pharmaceutical composition wherein contains the Lappaconitine hydrochoric acid of claim 1, and contains the carrier of conventional medicine.
3, the production method of Lappaconitine hydrochoric acid is that employing is extracted the lappaconitine crystallization for preparing through Aconitum sinomontanum Nakai, with ethanol or dissolve with methanol, and dripping hydrochloric acid solution, make congo-red test paper just become blue, place, separate out crystallization, filter, crystallization a small amount of solvent drip washing is drying to obtain.
4, the application of Lappaconitine hydrochoric acid in the preparation anodyne.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510100907 CN1962639A (en) | 2005-11-07 | 2005-11-07 | Lappaconitine hydrochoric acid, its production method and its uses in preparing analgetic |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510100907 CN1962639A (en) | 2005-11-07 | 2005-11-07 | Lappaconitine hydrochoric acid, its production method and its uses in preparing analgetic |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1962639A true CN1962639A (en) | 2007-05-16 |
Family
ID=38081887
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200510100907 Pending CN1962639A (en) | 2005-11-07 | 2005-11-07 | Lappaconitine hydrochoric acid, its production method and its uses in preparing analgetic |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1962639A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107746387A (en) * | 2017-10-12 | 2018-03-02 | 西北师范大学 | A kind of trifluoroacetic acid lappaconitine and preparation method thereof |
| CN108409657A (en) * | 2017-11-24 | 2018-08-17 | 孙益民 | High-purity lappaconitine and preparation method thereof |
| CN112358487A (en) * | 2020-11-16 | 2021-02-12 | 中国科学院新疆理化技术研究所 | Lappaconitine derivative and preparation method and application thereof |
-
2005
- 2005-11-07 CN CN 200510100907 patent/CN1962639A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107746387A (en) * | 2017-10-12 | 2018-03-02 | 西北师范大学 | A kind of trifluoroacetic acid lappaconitine and preparation method thereof |
| CN108409657A (en) * | 2017-11-24 | 2018-08-17 | 孙益民 | High-purity lappaconitine and preparation method thereof |
| CN108409657B (en) * | 2017-11-24 | 2021-08-20 | 孙益民 | High-purity lappaconitine and preparation method thereof |
| CN112358487A (en) * | 2020-11-16 | 2021-02-12 | 中国科学院新疆理化技术研究所 | Lappaconitine derivative and preparation method and application thereof |
| WO2022099937A1 (en) * | 2020-11-16 | 2022-05-19 | 中国科学院新疆理化技术研究所 | Lappaconitine derivative, preparation method therefor, and use thereof |
| CN112358487B (en) * | 2020-11-16 | 2023-08-25 | 中国科学院新疆理化技术研究所 | Lappaconitine derivative, and preparation method and application thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN101297880B (en) | Active extract containing phlorizin and uses thereof | |
| CN103193772A (en) | Preparation method and application of substituted aryl propionic berberine ion-pair compound | |
| CN102283949B (en) | Spraying agent containing sodium gualenate for treating canker sore | |
| CN1962639A (en) | Lappaconitine hydrochoric acid, its production method and its uses in preparing analgetic | |
| CN109010341A (en) | A kind of compound oral solution and preparation method thereof containing dextromethorphan hydrobromide | |
| CN104784157A (en) | Stable Montelukast oral film preparation | |
| CN1931265A (en) | Externally applied Chinese medicine spray for treating burns and scalds | |
| CN103239586A (en) | Flavored agastache turbidity-dispelling external preparation as well as preparation method and application thereof | |
| Cao et al. | Pharmacodynamic comparison of pantoprazole enantiomers: inhibition of acid-related lesions and acid secretion in rats and guinea-pigs | |
| CN102319225B (en) | Trimetazidine hydrochloride sustained release tablet and preparation method thereof | |
| CN107375430A (en) | A kind of curcumin composition with preventing and treating diabetes and complication | |
| CN103040849A (en) | Tannic acid preparation for treating burn, bedsore and diaper dermatitis and preparation method thereof | |
| CN103142645A (en) | High stability composite guaiacol phenolsulfonic acid oral liquid and preparation method thereof | |
| CN1911293B (en) | Gel agent-Guzhining for treating osteoporosis and its preparation method | |
| CN102204976B (en) | Pummelo peel extract with hypoglycemic activity and preparation method thereof | |
| CN101468074A (en) | Antalgic gel patch and preparation method thereof | |
| CN101138590A (en) | Use of medicinal fatheadtree leaf in the preparation of antimicrobial anti-inflammation medicament | |
| CN1861131A (en) | Qingkailing dixinwan pill prepn. and its prepn. method | |
| CN102357122A (en) | Masking type Chailian oral liquid and preparation method thereof | |
| Sabina et al. | Analgesic, antipyretic and ulcerogenic effects of Indian Ayurvedic Herbal formulation Triphala | |
| CN112194624A (en) | Crystal form of isoquinoline compound and preparation method thereof | |
| CN105362090A (en) | Portable compound deodorant wet tissue | |
| CN104971100A (en) | Traditional Chinese medicine composition having effects of resisting inflammation and relieving pain, preparation method and application thereof | |
| CN100358506C (en) | Compound musk drip pill and its preparation method | |
| CN100375630C (en) | Compound drop pills with flavescent sophora root and its preparation method |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| 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 |
Open date: 20070516 |