CN101829068A - Water soluble medicament sustained-release tablets and preparation method thereof - Google Patents
Water soluble medicament sustained-release tablets and preparation method thereof Download PDFInfo
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Abstract
The invention discloses water soluble medicament sustained-release tablets, which comprise the following components in part by weight: water soluble medicament 1-30, octadecanol 5-70, Eudragite L 100-55 2-50, talcpowder 2-30 and lactose 2-30. The water soluble medicament may be galanthamine hydrobromide, captopril, metoprolol tartaric acid or pseudoephedrine hydrochloride. In the invention, the octadecanol serving as a hydrophobic auxiliary material and the Eudragite L 100-55 sreving as a water soluble polymer auxiliary are adopted, so the release speed of the medicament can be controlled properly. The Eudragite L 100-55 is insoluble in gastric juice, but dissolves in duodenal juice to make high-viscosity sticky liquid, and thus the release and diffusion speed of the medicament can be reduced. The talcpowder which is a hydrophilic matter insoluble in water plays a porogen role in the sustained-release tablets. In the invention, the release speed of the medicament is regulated by regulating the mixing ratio of the medicament to the auxiliary material. Thus, the release speed of an active medicament is controlled.
Description
Technical field
The present invention relates to a kind of water soluble medicament sustained-release tablets and preparation method thereof.
Background technology
Senile dementia claims Alzheimer (Alzheimer ' s disease again, AD) be a kind of PDCD that occurs in geratic period and presenium, refer to a kind of persistence higher nerve functional activity obstacle, promptly there be not under the state of disturbance of consciousness the obstacle of aspects such as memory, thinking, analytical judgment, visual space identification, emotion.Its characteristic pathological change is the cerebral cortex atrophy, and with the amyloid-beta deposition, neurofibrillary tangles, mass memory neuron number reduces.This disease course is longer, is about 3～20 years, is " the fourth-largest killer " of the aged health after cardiovascular diseases, cerebrovascular and cancer.In the U.S., AD is only second to heart disease and cancer, expends the disease of medical expense more than the 3rd.Along with the quickening of aged tendency of population process, number of patients increasing, AD will become 21 century and threaten one of serious disease of human health.The definite cause of disease of AD and pathogenesis are comparatively complicated, still not fully aware of so far, and this disease research and control are still a global problem that remains to be broken through.Once the medicine that was used for clinical treatment has the agent of brain metabolic activation, cholinomimetic, potassium channel antagonists, glutamate receptor adjusting control agent, 5-HT3 receptor antagonist, Chinese medicine class etc., but effect is all not obvious.Acetyl choline content is relevant closely with memory in the existing known brain, the acetylcholine amount reduces in old age or the dementia human brain, replenish the choline medicine and can improve its memory and ability of thinking, but directly give choline or lecithin and can not make acetylcholine increase in the brain, so the most sophisticated at present Therapeutic Method is to adopt acetylcholine esterase (ChE) inhibitor for treating, stop the degraded of endogenous acetylcholine, and cholinesterase inhibitor is a unique up to now class is used for the treatment of AD by drugs approved by FDA a medicine.
Galanthamine hydrobromide is the reversibility cholinesterase inhibitor, it has double action mechanism, nicotine receptor site in acetylcholine esterase inhibition and the adjusting brain delays the process that function of brain cell goes down preferably, significantly improves cognitive function light, moderate AD patients.Reported that from the U.S. in 1988 galantamine can improve the mouse memory obstacle, infer its to senile dementia central cholinergic system obstacle may be effectively after, many countries have just begun the clinical research of galanthamine hydrobromide treatment AD.This medicine of calendar year 2001 U.S. FDA official approval is used for the treatment of AD, now 25 country's listings, and dosage forms such as existing slow releasing tablet, slow releasing capsule, but the dosage form of China's listing only has tablet, capsule and injection, dosage forms such as no slow releasing tablet, slow releasing capsule.Because AD is a chronic disease, need take medicine for a long time, so blood drug level is stable, untoward reaction is few, effect is lasting, take the few galantamine slow release formulation of number of times, suddenly wait to develop.And galanthamine hydrobromide is a water soluble drug, is used alone hydrophobicity or the hydrophilic framework material can not obtain slow release effect preferably.
Water soluble drug captopril (Cap) is generally coated tablet or ordinary tablet, because its biological half-life only is 1.9h, needs day clothes 3 times, and effect only can be kept 6～8h when the absorption total amount is 37.5～75.0mg.Single dose po50mg, peak concentration can reach more than the 600 μ g/L, and its treatment concentration is 50 μ g/L.This bigger peak valley concentration difference may be cause dizzy, headache, the reason of untoward reaction such as intestines and stomach disorder.For reducing peak valley difference and administration number of times, alleviate untoward reaction, be necessary it is made as slow release formulation.External existing Cap slow releasing capsule listing, because the stripping of water soluble drug own is very fast, it discharges difficult blocked, the domestic slow release kind listing of still not having Cap.The Cap of external listing is slow, controlled release preparation mostly is capsule, and its mechanism and technology mainly contain: the erodible skeleton piller of fatty acid ester; With the Eudragit S100 film-coat of common pastille piller bag, mix the dress capsule by proper proportion again with different-thickness; Or fused pastille solid dispersion is directly adorned capsule form.
Summary of the invention
At above-mentioned prior art, the invention provides a kind of water soluble medicament sustained-release tablets, it has the peak valley phenomenon of avoiding effective blood drug concentration, reduce toxic and side effects, keep effective haemoconcentration time long, therapeutic effect is good and characteristics such as administration once a day, increase patient compliance.
The present invention is achieved by the following technical solutions:
A kind of water soluble medicament sustained-release tablets is made up of the component of following weight portion: 1～30 part of water soluble drug, 5～70 parts of octadecanol, 2～50 parts of Youteqi L100-55,2～30 parts of Pulvis Talci, 2～30 parts of lactose.
Preferably, form: 5～25 parts of water soluble drugs, 10～50 parts of octadecanol, 5～30 parts of Youteqi L100-55,5～30 parts of Pulvis Talci, 5～25 parts of lactose by the component of following weight portion.
Described water soluble drug is galanthamine hydrobromide, captopril, spectinomycin hydrochloride or pseudoephedrine hydrochloride.
Described octadecanol is medicinal octadecanol.
Described Youteqi L100-55 derives from the auspicious medical technology company limited of Shanghai moral (import packing, German Romo Co.,Ltd).
Described Pulvis Talci is a medicinal Pulvis Talci.
A kind of compound method of water soluble medicament sustained-release tablets may further comprise the steps:
(1) raw material, adjuvant are all crossed 80 mesh sieves earlier;
(2) Pulvis Talci of octadecanol, Youteqi L100-55, lactose and the formula ratio 30～60% of formula ratio is crossed 60 mesh sieves, mixing;
(3) adjuvant that raw material and above-mentioned steps are obtained is with the equivalent abundant mixing of method of rising progressively;
(4) add 60% ethanol (V/V) in the material behind above-mentioned mixing and make soft material, granulate 45 ℃～50 ℃ dry 2h with 30 mesh sieves;
(5), add the residue Pulvis Talci, mix homogeneously with 30 mesh sieve granulate;
(6) with the conventional tabletting of tablet machine, promptly get water soluble medicament sustained-release tablets.
Described step (6) adopts the stamping of 5.5mm scrobicula, and Hardness Control is at 4.0-5.0Kg/cm
2
The whole operation process should be operated under the lucifuge condition as far as possible.
The present invention has adopted hydrophobic auxiliary octadecanol and water soluble polymer adjuvant Youteqi L100-55, can make the rate of release of medicine be subjected to suitable control.Youteqi L100-55 is insoluble in gastric juice, and dissolving becomes the big thick shape liquid of viscosity in duodenal juice, can slow down the release and the diffusion velocity of medicine.Pulvis Talci is water-fast hydroaropic substance, plays porogen in slow releasing tablet.Lactose has good water-solubility, flowability and compressibility, is used to regulate drug releasing rate and granule character and makes tablet specious.The present invention regulates drug releasing rate by the ratio of adjusting medicine, adjuvant, thereby has reached the purpose of control active medicine rate of release.
Compared with prior art, the present invention has the following advantages: (1) can avoid the peak valley phenomenon of effective blood drug concentration, can effectively reduce the toxic and side effects of medicine, and it is long to keep effective haemoconcentration time, and therapeutic effect is good; (2) administration once a day increases patient's compliance.
Description of drawings
Fig. 1 is Galantamin hydrobromide sustained-release sheet related substance own control (0 a day) HPLC collection of illustrative plates;
Fig. 2 is Galantamin hydrobromide sustained-release sheet determination of related substances (0 a day) HPLC collection of illustrative plates;
Fig. 3 quickens determination of related substances HPLC collection of illustrative plates in January for the Galantamin hydrobromide sustained-release sheet;
Fig. 4 quickens determination of related substances HPLC collection of illustrative plates in February for the Galantamin hydrobromide sustained-release sheet;
Fig. 5 quickens determination of related substances HPLC collection of illustrative plates in March for the Galantamin hydrobromide sustained-release sheet;
Fig. 6 quickens determination of related substances HPLC collection of illustrative plates in June for the Galantamin hydrobromide sustained-release sheet;
Fig. 7 is Galantamin hydrobromide sustained-release sheet determination of related substances HPLC in a long-term March collection of illustrative plates;
Fig. 8 is Galantamin hydrobromide sustained-release sheet determination of related substances HPLC in a long-term June collection of illustrative plates;
Fig. 9 is the long-term JIUYUE determination of related substances of a Galantamin hydrobromide sustained-release sheet HPLC collection of illustrative plates;
Figure 10 is the long-term December determination of related substances of a Galantamin hydrobromide sustained-release sheet HPLC collection of illustrative plates;
Figure 11 is long-term 18 months determination of related substances HPLC collection of illustrative plates of Galantamin hydrobromide sustained-release sheet.
The specific embodiment
The present invention is further illustrated below by embodiment.
Embodiment 1: preparation Galantamin hydrobromide sustained-release sheet:
Prescription is: made by following component for per 1000:
Galanthamine hydrobromide 10.0g
Octadecanol 25.0g
Youteqi L100-55 9.0g
Pulvis Talci 10.0g
Lactose 8.0g
60% ethanol 14ml
Above-mentioned galanthamine hydrobromide is meant the galanthamine hydrobromide that extracts from the plant Bulbus Lycoridis Radiatae, is buied by Zhejiang Yixin Pharmaceutical Co. Ltd..Octadecanol is to be buied by Shanghai traditional Chinese medicines group (import packing); Youteqi L100-55 is buied by the auspicious medical technology company limited of Shanghai moral (import packing, German Romo Co.,Ltd); Pulvis Talci is to be buied by three the Pulvis Talci factories in LONGSHENG IN GUANGXI county.
Preparation technology is as follows:
(1) raw material, adjuvant are all crossed 80 mesh sieves earlier;
(2) 9.0g Youteqi L100-55,25.0g octadecanol, 5.0g Pulvis Talci and lactose 8.0g are crossed 60 mesh sieve mixings;
(3) with galanthamine hydrobromide and above-mentioned adjuvant with the equivalent abundant mixing of method of rising progressively;
(4) add 60% ethanol liquid and make suitable soft material, granulate 45 ℃～50 ℃ dry 2h with 30 mesh sieves;
(5) with 30 mesh sieve granulate, add remaining 5.0g Pulvis Talci, mix homogeneously;
(6) with the stamping of 5.5mm scrobicula, Hardness Control is at 4.0-5.0Kg/cm
2, promptly get the Galantamin hydrobromide sustained-release sheet.
The whole operation process lucifuge of trying one's best.
Embodiment 2: preparation captopril slow releasing tablet:
Prescription is: made by following component for per 1000:
Captopril 12.5g
Octadecanol 27.0g
Youteqi L100-55 10.5g
Pulvis Talci 10.0g
Lactose 8.0g
60% ethanol 15ml
Above-mentioned captopril is buied by Wuhan Hezhong Bio-chemical Manufature Co., Ltd..Octadecanol is to be buied by Shanghai traditional Chinese medicines group (import packing); Youteqi L100-55 is buied by the auspicious medical technology company limited of Shanghai moral (import packing, German Romo Co.,Ltd); Pulvis Talci is to be buied by three the Pulvis Talci factories in LONGSHENG IN GUANGXI county.
Preparation technology is as follows:
(1) raw material, adjuvant are all crossed 80 mesh sieves earlier;
(2) Pulvis Talci and the lactose 8.0g with 10.5g Youteqi L100-55,27.0g octadecanol, 5.0g crosses 60 mesh sieve mixings;
(3) with captopril and above-mentioned adjuvant with the equivalent abundant mixing of method of rising progressively;
(4) add 60% ethanol liquid and make suitable soft material, granulate 45 ℃～50 ℃ dry 2h with 30 mesh sieves;
(5) with 30 mesh sieve granulate, add remaining 5.0g Pulvis Talci, mix homogeneously;
(6) with the stamping of 5.5mm scrobicula, Hardness Control is at 4.0-5.0Kg/cm
2, promptly get the Galantamin hydrobromide sustained-release sheet.
The whole operation process lucifuge of trying one's best.
Embodiment 3: preparation spectinomycin hydrochloride slow releasing tablet:
Prescription is: made by following component for per 1000:
Spectinomycin hydrochloride 100.0g
Octadecanol 80.0g
Youteqi L100-55 50.0g
Pulvis Talci 20.0g
Lactose 10.0g
3% carboxylic propyl methocel alcoholic solution (80%, V/V) 32ml
Above-mentioned spectinomycin hydrochloride is buied by Wuhan Hezhong Bio-chemical Manufature Co., Ltd.'s company limited.Octadecanol is to be buied by Shanghai traditional Chinese medicines group (import packing); Youteqi L100-55 is buied by the auspicious medical technology company limited of Shanghai moral (import packing, German Romo Co.,Ltd); Pulvis Talci is to be buied by three the Pulvis Talci factories in LONGSHENG IN GUANGXI county.
Preparation technology is as follows:
(1) raw material, adjuvant are all crossed 80 mesh sieves earlier;
(2) Pulvis Talci and the lactose 10.0g with 50.0g Youteqi L100-55,80.0g octadecanol, 10.0g crosses 60 mesh sieve mixings;
(3) with spectinomycin hydrochloride and the abundant mixing of above-mentioned adjuvant;
(4) add 3% carboxylic propyl methocel alcoholic solution (80%, V/V) make suitable soft material, with the granulation of 30 mesh sieves, 45 ℃～50 ℃ dry 2h;
(5) with 30 mesh sieve granulate, add remaining 10.0g Pulvis Talci, mix homogeneously;
(6) with the stamping of 8.0mm scrobicula, Hardness Control is at 4.0-5.0Kg/cm
2, promptly get the spectinomycin hydrochloride slow releasing tablet.
The whole operation process lucifuge of trying one's best.
Embodiment 4: preparation pseudoephedrine hydrochloride slow release sheet:
Prescription is: made by following component for per 1000:
Pseudoephedrine hydrochloride 120.0g
Octadecanol 110.0g
Youteqi L100-55 220.0g
Pulvis Talci 20.0g
Lactose 7.0g
4% ethyl cellulose alcoholic solution (75%, V/V) 55ml
Above-mentioned pseudoephedrine hydrochloride is buied by Zhejiang Kangyu Pharmaceutical Co., Ltd.'s company limited.Octadecanol is to be buied by Shanghai traditional Chinese medicines group (import packing); Youteqi L100-55 is buied by the auspicious medical technology company limited of Shanghai moral (import packing, German Romo Co.,Ltd); Pulvis Talci is to be buied by three the Pulvis Talci factories in LONGSHENG IN GUANGXI county.
Preparation technology is as follows:
(1) raw material, adjuvant are all crossed 80 mesh sieves earlier;
(2) Pulvis Talci and the lactose 7.0g with 220.0g Youteqi L100-55,110.0g octadecanol, 10.0g crosses 60 mesh sieve mixings;
(3) with pseudoephedrine hydrochloride and above-mentioned adjuvant with the equivalent abundant mixing of method of rising progressively;
(4) add 4% ethyl cellulose alcoholic solution (75%, V/V) make suitable soft material, with the granulation of 30 mesh sieves, 45 ℃～50 ℃ dry 2h;
(5) with 30 mesh sieve granulate, add remaining 10.0g Pulvis Talci, mix homogeneously;
(6) with the stamping of 10.0mm scrobicula, Hardness Control is at 4.0-5.0Kg/cm
2, promptly get the pseudoephedrine hydrochloride slow release sheet.
The whole operation process lucifuge of trying one's best.
Embodiment 5: the performance test of Galantamin hydrobromide sustained-release sheet:
Get slow releasing tablet, according to drug release determination method (two appendix X of Chinese Pharmacopoeia version in 2005 D, first method), adopt the device of dissolution method (two appendix X of Chinese Pharmacopoeia version in 2005 C three therapeutic methods of traditional Chinese medicine), release medium (pure water, the pH1.2 hydrochloric acid solution, the pH6.8 phosphate buffer) 250ml, rotating speed is that per minute 100 changes, operation in accordance with the law, at 1 hour, 2 hours, 6 hours, 12 hours, get solution 10ml in 16 hours respectively, filter, get subsequent filtrate, according to ultraviolet visible spectrophotometry (two appendix IV of Chinese Pharmacopoeia version in 2010 A), measure absorbance (seeing Table 1) respectively at the wavelength place of 289nm; In addition precision is measured the about 10mg of galanthamine hydrobromide reference substance, puts in the measuring bottle of 250ml, with the release medium dissolving and be diluted to scale, shakes up, and makes the solution that contains 40 μ g among every 1ml approximately, with method mensuration absorbance.Adopt the specific absorbance method to calculate stripping quantity, and calculate every cumulative release amount (seeing Table 2) respectively in different time points.Every of slow releasing tablet of the present invention is at 1 hour, and 2 hours, 6 hours, be respectively more than 10%～30%, 20%～45%, 40%～65%, 65%～85% and 75% of labelled amount with 16 hours cumulative release amount in 12 hours, all should be up to specification.
According to high performance liquid chromatography (two appendix V of Chinese Pharmacopoeia version in 2010 D).
Chromatographic condition and system suitability test octadecylsilane chemically bonded silica are filler, (contain the 1ml triethylamine in every 910ml water with acetonitrile-water-oxolane (170: 910: 30), 1.8g sodium heptanesulfonate, transfer PH to 2.6 with 85% phosphoric acid) as mobile phase, the detection wavelength is 289nm, column temperature is a room temperature, and number of theoretical plate should be not less than 2000 by the galanthamine hydrobromide peak.The separating degree at galanthamine hydrobromide peak and other peaks should meet the requirements.
It is an amount of to get the slow releasing tablet fine powder, adds the mobile phase ultrasonic dissolution and is diluted to the solution that every 1ml contains 1mg, filters, and gets subsequent filtrate as need testing solution; It is an amount of that precision is measured subsequent filtrate, adds mobile phase and be diluted to the solution that every 1ml contains 10 μ g, in contrast product solution.Get contrast solution 20 μ l and inject chromatograph of liquid, regulate instrumental sensitivity, make the peak height at main constituent peak be about 10% of monitor full scale, get need testing solution 20 μ l again and inject chromatograph of liquid, the record chromatogram is to 2 times of main constituent peak retention time.If any impurity peaks, each impurity peak area sum must not be greater than 2.5 times of the main peak areas (2.5%) of contrast solution in the need testing solution chromatogram.
Test 3: uniformity of dosage units
Get 10 of slow releasing tablet, put in the porcelain evaporating dishes respectively, grind, be transferred in the 200ml measuring bottle, water gradation washing evaporating dish, washing liquid is incorporated in the measuring bottle, ultrasonicly make galanthamine hydrobromide dissolving and be diluted to scale, filter, get subsequent filtrate according to assay item method mensuration content down, should meet (two appendix XE of Chinese Pharmacopoeia version in 2010) regulation, see Table 3.
Test 4: assay
Get 20 of slow releasing tablet, the accurate title, decide, porphyrize, precision is measured in right amount (being equivalent to galanthamine hydrobromide 2.5mg approximately), puts in the 50ml measuring bottle, adds water and dissolves in ultrasonic 20 minutes and be diluted to scale, filter, get subsequent filtrate,, measure absorbance at the wavelength place of 289nm according to ultraviolet visible spectrophotometry (two appendix IV of Chinese Pharmacopoeia version in 2005 A); In addition precision is measured the about 10mg of galanthamine hydrobromide reference substance, puts in the measuring bottle of 200ml, with water dissolution and be diluted to scale, shakes up, and makes the solution that contains 50 μ g among every 1ml approximately, measures absorbance with method, and calculating promptly should be 90.0%～110.0% of labelled amount.
Test result:
Adopt said method to test and study on the stability, draw following result:
One, check
1. release: the result is shown in table 1, table 2
Table 1 Galantamin hydrobromide sustained-release sheet absorbance table
Table 2 Galantamin hydrobromide sustained-release sheet cumulative release amount (%) table
| ??pH1.2 | ??18.31 | ??26.57 | ??46.54 | ??68.04 | ??81.80 |
| ??pH1.2 | ??20.00 | ??24.35 | ??43.99 | ??64.88 | ??76.60 |
| ??pH6.8 | ??17.14 | ??25.92 | ??48.16 | ??69.70 | ??82.45 |
| ??pH6.8 | ??16.82 | ??26.53 | ??48.78 | ??72.23 | ??82.28 |
| ??pH6.8 | ??17.45 | ??25.31 | ??47.50 | ??65.92 | ??76.66 |
| ??pH6.8 | ??18.06 | ??27.52 | ??50.11 | ??71.74 | ??81.47 |
| ??pH6.8 | ??16.51 | ??28.07 | ??50.69 | ??73.29 | ??79.96 |
| ??pH6.8 | ??17.45 | ??25.00 | ??48.12 | ??68.43 | ??76.46 |
2. related substance
After measured, related substance is 0.79%, sees accompanying drawing 1,2.
3. uniformity of dosage units: as shown in table 3
Table 3 Galantamin hydrobromide sustained-release sheet Determination of Content Uniformity result
| Numbering | Content % |
| ??1 | ??93.13 |
| ??2 | ??92.14 |
| ??3 | ??92.14 |
| ??4 | ??99.59 |
| ??5 | ??100.58 |
| ??6 | ??96.36 |
| ??7 | ??95.86 |
| ??8 | ??98.84 |
| ??9 | ??96.11 |
| ??10 | ??99.84 |
| Average content % | ??96.46 |
| Numbering | Content % |
| Standard deviation S | ??3.21 |
| The A=|100-average content | | ??3.54 |
| ??A+1.80S | ??9.318 |
4. assay
After measured, slow releasing tablet content is 99.63% of labelled amount, and is up to specification.
Therefore slow releasing tablet release, related substance, uniformity of dosage units and the assay of pressing the preparation of the prescription of embodiment 1 and preparation method are all up to specification.
Two, study on the stability
1. accelerated test
Condition: 40 ℃ ± 2 ℃, relative humidity are 75% ± 5%
Sample is placed above-mentioned environment, in 0,1,2,3, June every index of taking a sample to check, the results are shown in Table 4 and accompanying drawing 1～6.
Table 4 Galantamin hydrobromide sustained-release sheet accelerated test result
2. long term test
It is to preserve under 60% ± 10% condition that sample is placed 25 ℃ ± 2 ℃, relative humidity, respectively at 3,6,9,12,18 months relevant indexs of sampling and measuring, the results are shown in Table 5 and accompanying drawing 1,2,7～11.
The long-term result of the test of table 5 Galantamin hydrobromide sustained-release sheet
Above result shows:
1, the Galantamin hydrobromide sustained-release sheet is to deposit 6 months under 75% ± 5% condition at 40 ℃ 2 ± 2 ℃, relative humidity, and character, release do not have significant change, and content descends, and related substance raises, but all in acceptability limit.
2, the Galantamin hydrobromide sustained-release sheet is to deposit 6 months under 60% ± 10% condition at 25 ℃ ± 2 ℃, relative humidity, and character, release do not have significant change, and content descends, and related substance raises, but all in acceptability limit.
3,, find that its related substances increases gradually, but each impurity peak area sum is all less than 2.5 times of the main peak areas (2.5%) of contrast solution by above-mentioned test.
Claims (6)
1. a water soluble medicament sustained-release tablets is characterized in that, is made up of the component of following weight portion: 1～30 part of water soluble drug, 5～70 parts of octadecanol, 2～50 parts of Youteqi L100-55,2～30 parts of Pulvis Talci, 2～30 parts of lactose.
2. a kind of water soluble medicament sustained-release tablets according to claim 1 is characterized in that, is made up of the component of following weight portion: 5～25 parts of water soluble drugs, 10～50 parts of octadecanol, 5～30 parts of Youteqi L100-55,5～30 parts of Pulvis Talci, 5～25 parts of lactose.
3. a kind of water soluble medicament sustained-release tablets according to claim 1 and 2 is characterized in that: described water soluble drug is galanthamine hydrobromide, captopril, spectinomycin hydrochloride or pseudoephedrine hydrochloride.
4. the compound method of claim 1 or 2 described a kind of water soluble medicament sustained-release tablets is characterized in that, may further comprise the steps:
(1) raw material, adjuvant are all crossed 80 mesh sieves earlier;
(2) Pulvis Talci of octadecanol, Youteqi L100-55, lactose and the formula ratio 30～60% of formula ratio is crossed 60 mesh sieves, mixing;
(3) adjuvant that raw material and above-mentioned steps are obtained is with the equivalent abundant mixing of method of rising progressively;
(4) add 60% ethanol (V/V) in the material behind above-mentioned mixing and make soft material, granulate 45 ℃～50 ℃ dry 2h with 30 mesh sieves;
(5), add the residue Pulvis Talci, mix homogeneously with 30 mesh sieve granulate;
(6) with the conventional tabletting of tablet machine, promptly get water soluble medicament sustained-release tablets.
5. compound method according to claim 4 is characterized in that: the whole operation process is operated under the lucifuge condition.
6. compound method according to claim 4 is characterized in that: described step (6) adopts the stamping of 5.5mm scrobicula, and Hardness Control is at 4.0-5.0Kg/cm
2
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103385862A (en) * | 2012-05-08 | 2013-11-13 | 重庆国中医药有限公司 | Metoprolol tartrate sustained-release tablet and preparation method thereof |
| CN111233877A (en) * | 2018-11-29 | 2020-06-05 | 鲁南制药集团股份有限公司 | Galanthamine pamoate and preparation method thereof |
| CN111233878A (en) * | 2018-11-29 | 2020-06-05 | 鲁南制药集团股份有限公司 | Galanthamine pamoate and preparation method thereof |
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| CN103385862A (en) * | 2012-05-08 | 2013-11-13 | 重庆国中医药有限公司 | Metoprolol tartrate sustained-release tablet and preparation method thereof |
| CN103385862B (en) * | 2012-05-08 | 2015-09-30 | 重庆国中医药有限公司 | A kind of metoprolol tartrate extended release tablets and preparation method thereof |
| CN111233877A (en) * | 2018-11-29 | 2020-06-05 | 鲁南制药集团股份有限公司 | Galanthamine pamoate and preparation method thereof |
| CN111233878A (en) * | 2018-11-29 | 2020-06-05 | 鲁南制药集团股份有限公司 | Galanthamine pamoate and preparation method thereof |
| CN111233877B (en) * | 2018-11-29 | 2022-09-13 | 鲁南制药集团股份有限公司 | Galanthamine pamoate and preparation method thereof |
| CN111233878B (en) * | 2018-11-29 | 2022-09-13 | 鲁南制药集团股份有限公司 | Galanthamine pamoate and preparation method thereof |
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