CN1559403A - Method for preparing soft capsule prepn. contg. artemisine - Google Patents
Method for preparing soft capsule prepn. contg. artemisine Download PDFInfo
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- CN1559403A CN1559403A CNA2004100154260A CN200410015426A CN1559403A CN 1559403 A CN1559403 A CN 1559403A CN A2004100154260 A CNA2004100154260 A CN A2004100154260A CN 200410015426 A CN200410015426 A CN 200410015426A CN 1559403 A CN1559403 A CN 1559403A
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Abstract
A artemisine softgel is prepared through superfine pulverizing, suspending the fine particles in oily matrix, and including it by surface material at 25-38 deg.C.
Description
Affiliated technical field
The present invention relates to pharmaceutical preparation, particularly the preparation method of arteannuin soft capsule preparation.
Background technology
Arteannuin is the good antimalarial of China 1986 approval listing, has characteristics such as quick-acting, low toxicity, the strain of antagonism chloroquine protozoon be effective.Be with the arteannuin suppository listing at that time, other dosage form was not arranged.The back is because external pharmacodynamics test shows the high several times of potency ratio arteannuin of artemisinin derivative (two chlorine arteannuin, artesunate, Artemether), thus make the research and development of artemisinin-based drug abandon parent and monograph in its derivant.But the price of artemisinin derivative is higher more than 4 times than arteannuin, and its stability is all excellent not as good as arteannuin.
China's invention arteannuin malaria 30 years so far, but because the artemisinin derivative preparation high enterprise of price in the international market, can not enter the public medical institutions (except China, Vietnam) of developing country, thereby the malaria patient in the whole world 95% does not still use classic antimalarial arteannuin.
Recently, Li Guoqiao etc. prove that by clinical trial the malaria of arteannuin is tired completely different with the in vitro tests result in the patient body: isodose arteannuin and dihydroarteannuin do not have obvious difference in the intravital parasite killing speed of patient.This shows and is converted into dihydroarteannuin rapidly after arteannuin enters in the body and brings into play insecticidal action, under laboratory condition or commercial production also proved, be the synthetic dihydroarteannuin of raw material with the arteannuin, its yield is more than 90%.In view of this, arteannuin is directly made various preparations, comprise water solublity injection, oral agents, suppository and soft capsule preparation, can reduce cost greatly and extensively enter the public medical institutions of developing country, make global most of malaria patients can use arteannuin.Because the having good stability of arteannuin, the stability of existing several derivants be all not as arteannuin, thereby more have reason directly to develop with arteannuin certainly again the superiority of various preparations.
Summary of the invention
Purpose of the present invention be intended to overcome the deficiencies in the prior art and provide a kind of both can be oral, but also rectally, the bioavailability height, good stability, content is accurate, is convenient to the preparation method of the arteannuin soft capsule preparation of quality monitoring.
The present invention seeks to realize like this:
A kind of preparation method of arteannuin soft capsule preparation is earlier it evenly to be suspended in arteannuin to become capsule core material in the oleaginous base, be rolled into soft capsule with capsule material rubber at 25～28 ℃ of enclose again.
---the attritive powder of described arteannuin is good with 3～10 μ m, and the content of arteannuin is 20mg～200mg in every soft capsule.
---described oleaginous base is made up of vegetable oil, wax and ester, and its umber proportioning is:
93～99 parts of vegetable oil with Oleum Arachidis hypogaeae semen, Oleum Glycines or olive oil for well;
0.5～6 part in wax with Cera Flava or Cera Flava for well;
0.5～6 part of ester with tristearin or glyceryl monostearate for well.
---described capsule material rubber is made up of gelatin, G ﹠ W, and its umber proportioning is:
35～40 parts in gelatin
10～21 parts of glycerol
42～50 parts in water
---described capsule material rubber must dissolve the degassing at 40～60 ℃ when making, and viscosity is at 10500～11500cps.
---described oleaginous base and the mensuration of carrying out medicament contg after the arteannuin micropowder can separate fully with organic solvent, organic solvent with dehydrated alcohol, acetone or chloroform for well.
The present invention makes soft capsule preparation with arteannuin, its preparation method is with the insoluble drug arteannuin, pulverize to make with efficient crushing technology and be suspended in evenly that (excipient) is sealed in the oval capsule material in certain substrate, prepare with rolling, both can be oral, also can rectally, increased substantially the bioavailability and the therapeutic effect of arteannuin preparation, good stability, content is accurate.Set up quality inspection method, quality standard draft, can control its quality.
Description of drawings
Fig. 1 is preparation technology's flow chart of the present invention.
The specific embodiment
1. earlier arteannuin is crushed to 5 μ m through efficient powder machine;
2. with 94 parts of Oleum Arachidis hypogaeae semen, 3 parts in Cera Flava, 3 parts of glyceryl monostearates, be mixed into oleaginous base;
3. with 38 parts in gelatin, 17 parts of glycerol, 45 parts of mix homogeneously of water.Preparation is made soft capsule by Fig. 1 preparation technology flow process:
By the following method preparation is carried out quality monitoring:
Disintegration inspection technique:
With water is solvent, according to method inspection under Chinese Pharmacopoeia version appendix in 2000 the XA disintegrate item, and disintegration time＜20 minute.
Content assaying method:
1. spectrophotography (UV):
The sample solution preparation: get 20 soft capsules, accurate title is fixed, cuts off the capsule skin, and inclining capsule core material, grinds evenly (the accurate title of capsule skin is fixed), and precision takes by weighing in right amount (being equivalent to the 20mg arteannuin), the solubilizer dissolving.Filter, get subsequent filtrate Φ 0.22 μ m membrane filtration, precision is measured in right amount, adds NaOH solution, shakes up, and 50 ℃ of heating 30min are put and are chilled to room temperature, as sample solution.The reference substance solution preparation: precision takes by weighing arteannuin reference substance 20mg, the solubilizer dissolving." precision is measured in right amount, adds NaOH solution " rises with the sample solution manufacturing method, in contrast product solution.
Blank solution preparation: precision is measured solvent in right amount to the 25ml measuring bottle,, shakes up to scale with the NaOH solution dilution, and 50 ℃ of heating 30min are put and are chilled to room temperature, as blank solution.
Algoscopy at the wavelength place of 292nm, is measured reference substance solution and sample solution trap according to spectrophotography (two appendix IVA of Chinese Pharmacopoeia version in 2000) respectively, calculates, promptly.
2. high performance liquid chromatography (HPLC):
The sample solution preparation: get 20 soft capsules, accurate title is fixed, cuts off the capsule skin, and inclining capsule core material, grinds evenly (the accurate title of capsule skin is fixed), and precision takes by weighing in right amount (being equivalent to the 30mg arteannuin), the solubilizer dissolving.Filter, precision is measured in right amount, adds NaOH solution, with Φ 0.22 μ m membrane filtration, shakes up, and 50 ℃ of heating 30min are put and are chilled to room temperature, and precision is measured in right amount again, with mobile phase (acetonitrile-0.1mol/L KH
2PO
4Solution) dilution shakes up, and filters with the syringe-type nuclepore membrane filter, as sample solution.
The reference substance solution preparation: precision takes by weighing arteannuin reference substance 30mg, the solubilizer dissolving.Precision is measured in right amount, adds NaOH solution, shakes up, and " 50 ℃ of heating 30min " rises with the sample solution manufacturing method, in contrast product solution.
Algoscopy is set auto injection, measures each 20 μ l of reference substance solution and need testing solution respectively, injecting chromatograph, and the record chromatogram is pressed external standard method with calculated by peak area content.
Study on the stability:
40 ℃ ± 2 ℃ of accelerated test temperature under RH75% ± 5% condition, check that character do not have change in three months, do not detect related substance, and artemislnin content is constant substantially, illustrates that said preparation is more stable.
Claims (6)
1. the preparation method of an arteannuin soft capsule preparation is characterized in that earlier it evenly being suspended in arteannuin becomes capsule core material, be rolled into soft capsule with capsule material rubber at 25～28 ℃ of enclose again in the oleaginous base.
2. preparation method according to claim 1 is characterized in that the attritive powder of described arteannuin is good with 3～10 μ m, and the content of arteannuin is 20mg～200mg in every soft capsule.
3. preparation method according to claim 1 is characterized in that described oleaginous base is made up of vegetable oil, wax and ester, and its umber proportioning is:
93～99 parts of vegetable oil with Oleum Arachidis hypogaeae semen, Oleum Glycines or olive oil for well;
0.5～6 part in wax with Cera Flava or Cera Flava for well;
0.5～6 part of ester with tristearin or glyceryl monostearate for well.
4. preparation method according to claim 1 is characterized in that described capsule material rubber is made up of gelatin, G ﹠ W, and its umber proportioning is:
35～40 parts in gelatin
10～21 parts of glycerol
42～50 parts in water
5. preparation method according to claim 1 is characterized in that must dissolving the degassing at 40～60 ℃ when described capsule material rubber is made, and viscosity is at 10500～11500cps.
6. preparation method according to claim 1 is carried out the mensuration of medicament contg after it is characterized in that described oleaginous base and the arteannuin micropowder can separating fully with organic solvent, organic solvent with dehydrated alcohol, acetone or chloroform for well.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100154260A CN1559403A (en) | 2004-02-23 | 2004-02-23 | Method for preparing soft capsule prepn. contg. artemisine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100154260A CN1559403A (en) | 2004-02-23 | 2004-02-23 | Method for preparing soft capsule prepn. contg. artemisine |
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| Publication Number | Publication Date |
|---|---|
| CN1559403A true CN1559403A (en) | 2005-01-05 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2004100154260A Pending CN1559403A (en) | 2004-02-23 | 2004-02-23 | Method for preparing soft capsule prepn. contg. artemisine |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017016355A1 (en) * | 2015-07-30 | 2017-02-02 | 无限极（中国）有限公司 | Chinese medicine extract and preparation method and application thereof |
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2004
- 2004-02-23 CN CNA2004100154260A patent/CN1559403A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017016355A1 (en) * | 2015-07-30 | 2017-02-02 | 无限极（中国）有限公司 | Chinese medicine extract and preparation method and application thereof |
| US10675308B2 (en) | 2015-07-30 | 2020-06-09 | Infinitus (China) Company Ltd. | Chinese medicine extract and preparation method and application thereof |
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