CN1287799C - Bean curd fruit glycocide softcapsule - Google Patents
Bean curd fruit glycocide softcapsule Download PDFInfo
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- CN1287799C CN1287799C CN 03135874 CN03135874A CN1287799C CN 1287799 C CN1287799 C CN 1287799C CN 03135874 CN03135874 CN 03135874 CN 03135874 A CN03135874 A CN 03135874A CN 1287799 C CN1287799 C CN 1287799C
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Abstract
The present invention provides a helicid soft capsule which is composed of liquid medicine and capsule wall materials. The present invention is characterized in that the liquid medicine contains 50 to 200 mg of helicid whose particle diameter is smaller than 200 mu m by weight and the rest is medicinal or edible auxiliary materials used as solvent substrates. Since raw material, namely helicid, is ultra-finely refined in advance, the specific surface area of helicid is increased so that the helicid soft capsule has the characteristics of rapid dissolution, good biological availability, etc.; in addition, the helicid soft capsule contactd with the intestinal wall easily to accelerate the absorption of a human body, and therefore, the helicid soft capsule fully exerts the effects of tranquilization and sedation. In addition, the helicid soft capsule also has the advantages of preferable external appearance, stable effect and obvious sedation effect, and takes effect in 2 hours; the capsule improves sleep quality, obviously reduces waking frequency at night and has strong anti-inflammatory effect. Compared with the conventional tablets, the biological availability of the present invention is increased by 10 to 59%.
Description
Technical field
The present invention relates to a kind of helicide soft capsule of regulating nerve and blood circulation function that has.
Background technology
Helicide (Hilieidum) claims hilieidum, Helicid etc. again, is the natural plants monomer component that extraction separation goes out from the fruit of Yunnan Jingpo Nationality medicine wood bundle (Helicia erratica Hock.F).These product have only a kind of tablet of helicide sheet so far, and existing 20 years of clinical practice, are to be used to calm the nerves the main medicine of abirritative at present.Because the water solublity of helicide is relatively poor relatively, in hot water, dissolve, but become the pasty state insoluble matter after the cooling, the other biological chemical characteristic of glycosides compound is also not ideal in addition, so all there is the relatively poor problem of bioavailability in existing helicide oral formulations.Especially existing tablet all directly allocate into helicide medicinal or edible adjuvant in suppress and form, not only dosage is less, and its medicinal effective ingredient is not fully exerted, thereby cause this product use inconvenient, curative effect is relatively poor, can't satisfy the calm the nerves demand of abirritative particular patients ' of those urgent needs.
Summary of the invention
Purpose of the present invention is exactly in order to solve the problems referred to above that helicide exists, and provides that a kind of oral artifact utilization is better, stability of drug products good, helicide soft capsule easy to use, evident in efficacy.
Helicide soft capsule provided by the invention is made of medicinal liquid and capsule material, it is characterized in that medicinal liquid every helicide 50-200mg that contains particle diameter less than 200 μ m by weight, and surplus is the medicinal or edible adjuvant as solvent substrate.
Described medicinal or edible adjuvant is one or more in concise Testa oryzae oil, safflower oil, linoleic acid, alpha-linolenic acid, gamma-Linolenic acid, polyunsaturated fatty acid, Semen Tritici aestivi germ oil, Radix Oenotherae erythrosepalae oil, perilla oil, Oleum Hippophae, Semen Lini oil, bathypelagic fish oil, eicosapentaenoic acid, docosahexenoic acid, Semen Maydis oil, Oleum Vitis viniferae, Folium et Cacumen Artemisiae Halodendri seed oil, walnut oil, soybean oil, the Oleum Arachidis hypogaeae semen.
Also contain in the edible or medicinal pigment of the Carthamus yellow, amaranth, brilliant black etc. of promising increase product colour one or more in described medicinal liquid or the capsule material, perhaps one or more in the edible or medicinal flavours for the NINGMENGXIANG that increases product taste or fragrance, Fructus Citri tangerinae perfume (or spice), vanillin, Mentholum, muscone etc.
Helicide soft capsule provided by the invention may further comprise the steps:
Helicide is carried out ultra fine, make particle diameter, the helicide of super-refinement is added in the solvent substrate, fully stir, after the mixing emulsifying, filter, the degassing, deliver in the jar of filling machine top less than 200 μ m, stand-by;
After the dissolving of capsule material, under 40-50 ℃ of temperature, be incubated, stand-by;
Under 10,000 grades, 21 ℃-25 ℃, the condition of RH%:39-41%, with rotating mould press pelleting, the soft capsule of making is cleaned, 28 ± 2 ℃ dry 19-27 hour down, packing, pack and get product.
Advantage of the present invention and effect are: owing to raw material-helicide is carried out ultra fine in advance, remove the specific surface area that increases it, product is had outside the characteristics such as stripping is fast, bioavailability is good, product is easily contacted with intestinal wall, quicken the absorption of human body to it, the abirritative medicinal efficacy of calming the nerves is given full play to, and in addition, product also has outward appearance and stable performance preferably.Concrete manifestation is as follows:
1, sedation: all occur calm indexs such as drowsiness sense, the appearance of electroencephalogram slow wave, the obvious minimizing of alpha index behind the oral product of the present invention of 20 routine normal persons.
2, this product onset time is within 2 hours, the long-term bad old people of 10 example sleeps is arranged, after taking this product three times every day, sleep quality improves greatly, can obviously reduce night and wake up number of times, 3 examples are by waking up 6 times every night, reduce to 3-4 time, 4 examples are reduced to 1-3 time by waking up 4-6 time every night, 3 examples are reduced to below 1 time by waking up 3-5 time every night.Above-mentioned patient all feels to take after three days spiritual fine.
3, convulsion: this product can obviously reduce incidence rate, the incubation period that prolongs generation, the number of times that alleviates outbreak, the shortening outbreak time-histories that coriamyrtin is fainted from fear.
4, show that with " writhing method " and " hot plate method " this product has analgesic activity; With vascular permeation method, acute and chronic arthrocele method and cotton ball granular swelling, prove that this product has stronger antiinflammatory action.
5, improve bioavailability: compare with conventional tablet, the bioavailability of this product can improve 10-59%.
Embodiment 1
Prescription (1000):
Ultra-fine helicide (particle diameter less than 200 μ m, as follows) 25g
Soybean oil 100g
By above-mentioned prescription it is made every soft capsule finished product that contains helicide 25mg.
Embodiment 2,
Prescription (1000):
Ultra-fine helicide 5g
PEG-400 6g
Oleum Arachidis hypogaeae semen 30g
Perilla oil 25g
By above-mentioned prescription it is made every soft capsule finished product that contains helicide 5mg.
Embodiment 3,
Prescription (1000):
Ultra-fine helicide 200g
Alpha-linolenic acid 350g
Safflower oil 600g
By above-mentioned prescription it is made every soft capsule finished product that contains helicide 200mg.
Embodiment 4,
Prescription (1000):
Ultra-fine helicide 100g
Concise Testa oryzae oil 500g
Ethyl hydroxybenzoate 2g
Vanillin 1g
By above-mentioned prescription it is made every soft capsule finished product that contains helicide 100mg.
Adding amaranth and brilliant black are modulated into aubergine and then can get mauve helicide soft capsule in the capsule material.
Embodiment 5,
Prescription (1000):
Ultra-fine helicide 100g
Docosahexenoic acid 400g
Oleum Hippophae 200g
Carthamus yellow 1g
Vanillin 2g
By above-mentioned prescription it is made and to have fragrance and xanchromatic every soft capsule finished product that contains helicide 100mg.
The concrete processing method of the various embodiments described above is:
1, helicide is carried out ultra fine with existing breaking methods such as comminution by gas stream or ball mill pulverizing earlier, make particle diameter, in the helicide adding solvent substrate with super-refinement less than 200 μ m, fully after stirring, the mixing emulsifying, filter, outgas, deliver in the jar of filling machine top, stand-by:
2, with after the dissolving of capsule material, put into the insulation jar of soft capsule filling machine top, under 40-50 ℃ of temperature, be incubated, stand-by;
3, under 10,000 grades, 21 ℃-25 ℃, the condition of RH%:39-41%, medicinal liquid and capsule material are carried out pelleting, the soft capsule of making are cleaned with the rotating mould press, 28 ± 2 ℃ dry 19-27 hour down, packing, packing get product.
For showing drug action of the present invention, the present invention is through animal experiment, and its result is as follows:
1, the helicide soft capsule causes the effect of mice convulsion to coriamyrtin
Use the coriamyrtin model, 60 of female mice 20 ± 1g are divided into 3 groups at random, and 20 every group, behind mice fasting 8h, ig helicide soft capsule content (is amounted to helicide I group: 300mg, II group: 600mg).Suddenly the whole body twitch occurring with animal behind the injection coriamyrtin is preclinical observation index, with facial spasm, ear tremble, extremity stretch, tail perk etc. is the index of light-duty outbreak, with the strong spasm of whole body, roll fall down to the ground, jump, running is the index of heavy type outbreak, observes the behavior performance of animal respectively.Each group is observed 1.5h continuously behind the intramuscular injection coriamyrtin.Result such as following table:
| Group | Incidence rate (%) | Incubation period (min) | Attack rate (%) | Light-duty outbreak (s) | Attack rate (%) | Heavy outbreak (s) | Mortality rate (%) |
| Contrast I group II group | 100 95 88 | 24.1±7.8 31.0±7.9 32.2±8.8 | 91 78 47 | 12.5±9.7 10.0±9.0 8.4±6.9 | 23 12 7 | 2.6±14.8 21.3±12.7 16.1±4.6 | 7 0 0 |
Conclusion:
1, the helicide soft capsule can prolong the incubation period of coriamyrtin convulsions generation, also reduce the incidence rate and the mortality rate of fainting from fear;
2, capsule has the effect that alleviates coriamyrtin convulsive attack degree, and is dose-effect relationship within the specific limits.
2, the analgesic activity of helicide soft capsule
Mouse writhing method:
60 of mices are divided into 4 groups at random, and 15 every group, 60min after the ig administration, mouse peritoneal inject 0.7% acetic acid 0.1ml/10g, and record 5 ~ 15min mouse writhing reaction times is calculated and comparable group differences significance, the results are shown in following table:
| Group | Body weight | Dosage (mg/Kg) | Turn round the body number of times | Suppression ratio |
| Blank group morphine group soft capsule soft capsule | 20±1.1 20±0.9 20±1.2 20±1.0 | Equal-volume 10 300 600 | 30.8±8.00 2.4±1.49 24.6±5.39 10.0±2.02 | 92.2％ 41.1％ 72.0％ |
Conclusion: this product has certain analgesic activity, and is heavy effect relationship within the specific limits.
3, helicide soft capsule antiinflammatory action
Use the Whttle method, 60 of mices are divided into 4 groups at random, 15 every group, 60min after the ig administration, the blue 0.2ml/ of mouse tail vein injection 0.5% ivens is the timely lumbar injection 0.7% acetic acid 0.2ml/10g in back only, puts to death mice behind the 15min, and intraperitoneal injection of saline 5ml gently rubs the back and extracts peritoneal fluid, centrifugal, supernatant is measured optical density value in the 620nm place, calculate and comparable group differences significance, the results are shown in following table:
| Group | Body weight | Dosage (mg/Kg) | Optical density value | Suppression ratio |
| Blank group aspirin soft capsule group soft capsule group | 20±1.1 20±1.3 20±1.2 20±1.0 | Equal-volume 200 300 600 | 0.29±0.06 0.12±0.04 0.20±0.04 0.13±0.03 | 61.0％ 39.6％ 47.8％ |
Conclusion: the helicide soft capsule has the obvious anti-inflammatory and anti effect, with the blank group difference of highly significant is arranged relatively, and is dose-effect relationship within the specific limits.
Claims (5)
1, a kind of helicide soft capsule is characterized in that by weight components:
Particle diameter is less than the ultra-fine helicide 25g of 200 μ m
Soybean oil 100g
Make 1000 of every soft capsules that contains helicide 25mg.
2, a kind of helicide soft capsule is characterized in that by weight components:
Particle diameter is less than the ultra-fine helicide 5g of 200 μ m
PEG-400 6g
Oleum Arachidis hypogaeae semen 30g
Perilla oil 25g
Make 1000 of every soft capsules that contains helicide 5mg.
3, a kind of helicide soft capsule is characterized in that by weight components:
Particle diameter is less than the ultra-fine helicide 200g of 200 μ m
Alpha-linolenic acid 350g
Safflower oil 600g
Make 1000 of every soft capsules that contains helicide 200mg.
4, a kind of helicide soft capsule is characterized in that by weight components:
Particle diameter is less than the ultra-fine helicide 100g of 200 μ m
Concise Testa oryzae oil 500g
Ethyl hydroxybenzoate 2g
Vanillin 1g
Make 1000 of every soft capsules that contains helicide 100mg.
5, a kind of helicide soft capsule is characterized in that by weight components:
Particle diameter is less than the ultra-fine helicide 100g of 200 μ m
Docosahexenoic acid 400g
Oleum Hippophae 200g
Carthamus yellow 1g
Vanillin 2g
Make 1000 of every soft capsules that contains helicide 100mg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03135874 CN1287799C (en) | 2003-09-20 | 2003-09-20 | Bean curd fruit glycocide softcapsule |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03135874 CN1287799C (en) | 2003-09-20 | 2003-09-20 | Bean curd fruit glycocide softcapsule |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1596903A CN1596903A (en) | 2005-03-23 |
| CN1287799C true CN1287799C (en) | 2006-12-06 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03135874 Expired - Fee Related CN1287799C (en) | 2003-09-20 | 2003-09-20 | Bean curd fruit glycocide softcapsule |
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| CN (1) | CN1287799C (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101550173B (en) * | 2009-05-12 | 2012-02-15 | 四川大学 | 4-(4-beta-D-allopyranosid-phenyl)-2-aryl-5-nitrilyl-6-methoxyl pyridine and preparation method and application thereof |
| CN101550174B (en) * | 2009-05-12 | 2012-02-22 | 四川大学 | 2-amino-4-(4-beta-D-allopyranosid-phenyl)-6-phenyl-pyrimidine, preparation method and application thereof |
| CN103564429A (en) * | 2012-08-10 | 2014-02-12 | 余尚学 | Novel soft capsule oily liquid accessory capable of improving sleep |
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2003
- 2003-09-20 CN CN 03135874 patent/CN1287799C/en not_active Expired - Fee Related
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| Publication number | Publication date |
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| CN1596903A (en) | 2005-03-23 |
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