CN1861056B - Slow-releasing preparation containing gastrodin - Google Patents
Slow-releasing preparation containing gastrodin Download PDFInfo
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- CN1861056B CN1861056B CN2006100921261A CN200610092126A CN1861056B CN 1861056 B CN1861056 B CN 1861056B CN 2006100921261 A CN2006100921261 A CN 2006100921261A CN 200610092126 A CN200610092126 A CN 200610092126A CN 1861056 B CN1861056 B CN 1861056B
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- gastrodine
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Abstract
An orally taken slow-releases gastrodine for treating dizziness, neuralgia, headache, etc contains gastrodine (10-30 Wt%) and slow-releasing auxiliary chosen from 18 materials including sodium alginate, potassium alginate, hydroxypropyl methyl cellulose, hydroxymethyl cellulose sodium, beeswax, etc.
Description
Technical field:
The invention belongs to medical technical field, what relate to is the gastrodin slow release preparation that is widely used in treatment dizzy (Meniere, poison of drug vertigo, vestibular neuronitis, vertebro-basilar artery insufficiency etc.), neuralgia (trigeminal neuralgia, sciatica, neuralgia of greater occipital nerve etc.), headache diseases such as (neurasthenia and neurasthenia syndrome, the headache of blood vessel character, tension headache, combined external head injuries, migraine etc.) of a kind of administration every day 2 times.
Background technology:
Gastrodine is the main active of rare medicinal herbs Rhizoma Gastrodiae; Have calmness, convulsion, epilepsy, analgesia; The cerebral blood flow increasing amount is improved vertebra basilar artery, AICA, PICA, labyrinthine artery and internal ear blood supply insufficiency, the neuroprotective cell; Promote the function of myocardial cell energy metabolism, be used widely clinically.
The mainly middle part absorption on stomach and small intestinal of these article, absorption is rapid, complete, and age and sex are to absorbing no significant difference.The commercially available common solid preparation of gastrodine has tablet, capsule etc. at present.
Slow releasing preparation be with the curative effect of medicine only relevant with vivo medicine concentration and with the third generation dosage form of irrelevant this conceptual foundation development of administration time; Do not need frequent drug administration; Medicine can discharge at absorption site on request lentamente; Blood drug level is reached and remain on and treat within the concentration range, this can make side effects of pharmaceutical drugs be reduced to minimum degree and reduce administration frequency.In general, this kind preparation is compared with fast dissolving dosage form, and the safety and the advantages such as effectiveness and compliance of patients that improve medication are arranged.
Summary of the invention:
The gastrodin slow release preparation that the purpose of this invention is to provide a kind of blood drug level of in 12 hours, remaining valid.Its advantage is improved sense of taste for improving curative effect, reduces and takes number of times, reduces the side effect incidence rate, takes, easy to carry.
The objective of the invention is to realize like this:
Preparation of the present invention contains following component by weight percentage:
Gastrodine 10-30%
Play the adjuvant 30-90% of slow releasing function
Other adjuvant surplus
This preparation mainly comprises the various preparations of skeleton type sustained release preparation, gel-type slow releasing preparation, porous matrix type slow releasing preparation and film controlling type slow releasing preparation etc., also comprises and processes the various slow releasing preparation that micropill, microcapsule, microsphere etc. are processed preparation more earlier.
The above-mentioned adjuvant that plays slow releasing function is sodium alginate, potassium alginate, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, hydroxyethyl-cellulose, hydroxypropyl cellulose, methylcellulose; Polyvinylpyrrolidone, acrylic resin, Cera Flava, hard ester acid, Brazil wax, hydrogenated vegetable oil, glycerol monostearate, octadecanol, ethyl cellulose, polypropylene and polyethylene etc.Above-mentioned adjuvant is porogen, filler, binding agent, lubricant, membrane material, solvent or other adjuvant, and porogen can adopt sucrose, mannitol, starch, Pulvis Talci, silicon dioxide etc.; Filler can adopt lactose, starch, dextrin etc.; Binding agent can adopt the ethanol-water solution of polyvinylpyrrolidone, hypromellose, dehydrated alcohol, various concentration etc.; Wetting agent can adopt the ethanol-water solution of water, dehydrated alcohol, various concentration; Lubricant can adopt stearic acid, Pulvis Talci, magnesium stearate, starch, paraffin etc.; Membrane material can adopt polyvinyl alcohol, hydroxyl methylcellulose, hyetellose, hymetellose, methylcellulose etc.; Foaming agent can adopt basic magnesium carbonate, sodium bicarbonate etc.; Bleach activator can adopt hexadecanol, octadecanol, Cera Flava etc.; Solvent can adopt dehydrated alcohol, ethanol, water etc.
Advantage of the present invention is: curative effect improves, and sense of taste improves, and reduces and takes number of times, reduces the side effect incidence rate, takes, easy to carry.
Description of drawings:
Fig. 1 is the release in vitro curve according to the gastrodin slow release preparation of embodiment 1 preparation.
Fig. 2 is the interior plasma concentration curve of gastrodine body among the embodiment 1.
Practical implementation side executes
Embodiment 1:
Present embodiment 1 tablet that adopts the known method of pharmaceuticals industry to process contains following composition by weight percentage:
Stearic acid 4%
Lactose 15%
Hydroxypropyl methylcellulose 55%
Polyvinylpyrrolidone 5%
Magnesium stearate 1%
Dehydrated alcohol is an amount of
Preparation technology: with principal agent and hydroxypropyl methylcellulose, stearic acid, lactose, polyvinylpyrrolidone mix homogeneously, granulate with dehydrated alcohol, oven dry, granulate adds hard month purport acid magnesium mixing, tabletting.
The used framework material of present embodiment is the mixed matrix material of hydrophilic gel matrix material and bioerodable property framework material.
Embodiment 2:
Present embodiment 2 tablets that adopt the known method of pharmaceuticals industry to process contain following composition by weight percentage:
Gastrodine 15%
Microcrystalline Cellulose 15%
Acrylic resin 45%
Lactose 15%
Hydroxypropyl methylcellulose 9%
Magnesium stearate 1%
5% ethyl cellulose alcoholic solution is an amount of
Preparation technology: with principal agent and acrylic resin, hydroxypropyl methylcellulose, lactose, microcrystalline Cellulose, granulate with 5% ethyl cellulose alcoholic solution, oven dry, granulate adds the magnesium stearate tabletting.
This used framework material of writing out a prescription is the mixture of two kinds of hydrophilic gel matrix materials and insoluble framework material.
Embodiment 3:
Present embodiment 3 tablets that adopt the known method of pharmaceuticals industry to process contain following composition by weight percentage:
Polyvinylpyrrolidone 6%
Lactose 12%
Microcrystalline Cellulose 11%
Magnesium stearate 1%
Dehydrated alcohol is an amount of
Preparation technology: with principal agent and hydroxypropyl methylcellulose, lactose, microcrystalline Cellulose, polyvinylpyrrolidone mix homogeneously, granulate with dehydrated alcohol, oven dry, granulate adds the magnesium stearate mixing, tabletting.
Employed framework material is a hydrophilic gel matrix material in this prescription.
Embodiment 4:
Present embodiment 4 tablets that adopt the known method of pharmaceuticals industry to process contain following composition by weight percentage:
Polyvinylpyrrolidone 7%
Lactose 9%
Calcium hydrogen phosphate 9%
Hydroxypropyl methylcellulose 35%
Microcrystalline Cellulose 11%
Hard ester acid 8%
Magnesium stearate 1%
Dehydrated alcohol is an amount of
Preparation technology: with principal agent and hydroxypropyl methylcellulose, stearic acid, calcium hydrogen phosphate, polyvinylpyrrolidone, microcrystalline Cellulose mixing, granulate with dehydrated alcohol, oven dry, granulate adds the magnesium stearate mixing, tabletting.
This employed framework material of writing out a prescription is the composite material of hydrophilic gel matrix material and bioerodable property framework material.
Embodiment 5:
Present embodiment 5 tablets that adopt the known method of pharmaceuticals industry to process contain following composition by weight percentage:
Gastrodine 24%
Hydroxypropyl methylcellulose (low viscosity) 30%
Hydroxypropyl methylcellulose (high viscosity) 6%
Lactose 15%
Cross-linking sodium carboxymethyl cellulose 10%
Polyvinylpyrrolidone 4%
Magnesium stearate 1%
Dehydrated alcohol is an amount of
Preparation technology: with principal agent and hydroxypropyl methylcellulose, lactose, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, polyvinylpyrrolidone mixing, granulate with dehydrated alcohol, oven dry, granulate adds the magnesium stearate mixing, tabletting.
This used framework material of writing out a prescription is the mixture of two kinds of hydrophilic gel matrix materials.
Embodiment 6:
Present embodiment 6 tablets that adopt the known method of pharmaceuticals industry to process contain following composition by weight percentage:
Gastrodine 25%
Brazil wax 35%
Stearic acid 16%
Lactose 11%
Microcrystalline Cellulose 12%
Magnesium stearate 1%
Water is an amount of
Preparation technology: with principal agent and acrylic resin, stearic acid, lactose, microcrystalline Cellulose, water is granulated, oven dry, and granulate adds the magnesium stearate mixing, tabletting.
This used framework material of writing out a prescription is the mixture of hydrophilic gel matrix material and bioerodable property framework material.
Embodiment 7:
Adopt the gastric floating tablet of the present embodiment 7 of the known method preparation of pharmaceuticals industry to contain following composition by weight percentage:
Basic magnesium carbonate 8%
Lactose 21%
PVPK30 6％
Stearic acid 13%
Magnesium stearate 1%
Ethanol is an amount of
Preparation technology: with principal agent and HPMCK100LV, stearic acid, basic magnesium carbonate, lactose, PVPK
30, use alcohol granulation, oven dry, granulate adds the magnesium stearate mixing, tabletting.
This used HPMCK100LV that writes out a prescription is a hydrophilic polymer, meets gastric juice and expands and form the gel barrier, and the density of keeping skeleton is less than gastric content density, and floats on the gastric juice; Stearic acid is a bleach activator, and can reduce the hydration rate of skeleton; Basic magnesium carbonate is a foaming agent, meets gastric acid and produces CO
2, can further alleviate the density of preparation, thereby prolong the gastrodini holdup time under one's belt, reach the slow release purpose.
Embodiment 8:
Adopt the coating type preparation of the present embodiment 8 of the known method preparation of pharmaceuticals industry to contain following composition by weight percentage:
Gastrodine 12%
Polyacrylic resin II 34%
Lactose 50%
Magnesium stearate 1%
Anhydrous alcohol solution 3%
Preparation technology: earlier principal agent and lactose are pressed into label, wrap enteric coating (being polyacrylic resin II) again.
When medicine entering intestinal, the enteric coating dissolving discharges medicine and plays the delay release action, be i.e. the enteric film sustained release.
Embodiment 9:
Adopt the coating type preparation of the present embodiment 9 of the known method preparation of pharmaceuticals industry to contain following composition by weight percentage:
Icing Sugar 32%
Polyvinylpyrrolidone 8%
Each component is the core on it.
Hypromellose 12g
Titanium dioxide 3.5g
PEG6000 1g
Propylene glycol 3g
Pulvis Talci 2g
Water 120ml
More than each medicine be the coating aqueous suspension.
Preparation technology: earlier principal agent and Icing Sugar, microcrystalline Cellulose, polyvinylpyrrolidone and lubricant being processed piller is core, then outsourcing hydrophilic film clothing (HPMC etc.).
After oral, meet Digestive system, constitute the hydrophilic polymer water absorption and swelling of film-coat, form the gel barrier, controlled drug release.
Claims (1)
1. gastrodin slow release tablet, it is characterized in that: the percentage by weight of its each constituent is following:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2006100921261A CN1861056B (en) | 2006-06-05 | 2006-06-05 | Slow-releasing preparation containing gastrodin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2006100921261A CN1861056B (en) | 2006-06-05 | 2006-06-05 | Slow-releasing preparation containing gastrodin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1861056A CN1861056A (en) | 2006-11-15 |
| CN1861056B true CN1861056B (en) | 2012-03-07 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2006100921261A Expired - Fee Related CN1861056B (en) | 2006-06-05 | 2006-06-05 | Slow-releasing preparation containing gastrodin |
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Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012035409A1 (en) * | 2010-09-14 | 2012-03-22 | Rubicon Research Private Limited | Sustained release compositions of anti-alzheimer's agents |
| CN102228449B (en) * | 2011-06-27 | 2013-04-10 | 昆明制药集团股份有限公司 | Gastrodin chronopharmaceutical medicine delivery preparation |
| CN115779042B (en) * | 2022-12-21 | 2023-12-05 | 浙江中医药大学 | Gastrodia elata total polyphenol for preventing and treating migraine |
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2006
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| CN1861056A (en) | 2006-11-15 |
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Granted publication date: 20120307 Termination date: 20160605 |