CN103933037B - Dehydrocavidine-containing pharmaceutical composition and preparation method thereof - Google Patents
Dehydrocavidine-containing pharmaceutical composition and preparation method thereof Download PDFInfo
- Publication number
- CN103933037B CN103933037B CN201410148314.6A CN201410148314A CN103933037B CN 103933037 B CN103933037 B CN 103933037B CN 201410148314 A CN201410148314 A CN 201410148314A CN 103933037 B CN103933037 B CN 103933037B
- Authority
- CN
- China
- Prior art keywords
- pharmaceutical composition
- agent
- deydrokaividing
- mixture
- granulate
- 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.)
- Active
Links
Abstract
The invention provides a dehydrocavidine-containing pharmaceutical composition. The pharmaceutical composition is in a form of dispersible tablet and comprises 1 to 150 parts by weight of dehydrocavidine and pharmaceutical excipients, wherein the pharmaceutical excipients comprise 10 to 200 parts by weight of disintegrating agent, 0.1 to 10 parts by weight of lubricating agent, 0.1 to 10 parts of flow aid, 0 to 200 parts of filling agent, 0 to 100 parts of adhesive, 0 to 200 parts of swelling agent, 0 to 50 parts of surface active agent, and 0 to 200 parts of corrigent. The dehydrocavidine-containing pharmaceutical composition (dispersible tablet) solves the problem of low dissolution rate of dehydrocavidine, and is high in disintegrative performance and dissolution performance, outstanding in dispersing uniformity, great in taste, convenient to take, high in adaptability, highly obvious in drug utilization rate, fast to act, and obvious in medical function.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition, particularly relate to a kind of pharmaceutical composition containing deydrokaividing and preparation method thereof, this pharmaceutical composition is dispersible tablet.
Background technology
Hepatitis B (Hepatitis B) is a kind of infectious disease being main manifestations with liver inflammatory pathological changes caused addicted to liver sexually transmitted disease (STD) poison (HBV) by DNA, there is infectiousness strong, route of transmission is complicated, popular wide, sickness rate high, very large to human health risk, be a worldwide public health difficult problem.The whole world about has 400,000,000 people to be hepatitis B virus chronic infection, is mainly distributed in Asia, non-country.China is viral hepatitis hotspot, based on HBV infection.Epidemiologic data shows, there is HBsAg carrier 1.2 hundred million people in China, about has 3,000 ten thousand chronic hepatitis B patients to need treatment, has had a strong impact on the life of people, employment, even marriage etc.Although Hepatitis B virus vaccine widely uses, there is preventive effect to hepatitis B to a certain extent, also exist and do not reply and untoward reaction.In addition, chronic viral hepatitis B patient about had 12% can develop into liver cirrhosis after 5 ~ 20 years, in patient with liver cirrhosis, about 20% patient finally develops into liver failure, about 5% develops into hepatocarcinoma, the whole world about has 2,713 ten thousand people to die from HBV relevant disease every year, belonging to great, common multiple, the infectious disease threatening human survival at present, is the key areas of medicine research and development.
At present, there is no the specific drug for the treatment of hepatitis B both at home and abroad.Get the Green Light for the treatment of hepatitis B in the world, they are Interferon Alpha-2b, lamivudine, Peg-IFN alpha-2b α-2a, adefovirdipivoxil, Entecavir.But due to the integrity problem of side reaction and curative effect, as nucleoside medicine medicine short-term administration has certain antivirus action, but it is still uncertain to the scavenging action of covalently closed circle HBV-DNA, guanosine class and gland aminoglycoside slightly strong to the scavenging action of HBV-DNA, but after drug withdrawal easy " knock-on ", and easily producing drug resistance phenomenon, side reaction is comparatively strong, affects clinical prolonged application; And the effective percentage of interferon is between 30 ~ 50%, and have very strong side effect, so, all non-recommendation interferon for the treatment of guidelines of " viral hepatitis control prece (trying) " (2007) specification and nucleotide antiviral agent thing.Current Chinese patent medicine, immunoregulation agent and hepatoprotective, to alleviation clinical symptoms, improve liver function and virus replication also has certain curative effect, but also there is the weak and high deficiency of knock-on rate of curative effect.Therefore, research is efficient, and safety, knock-on rate is low, untoward reaction is little, the treatment viral hepatitis new drug that not easily tolerates is current new drug development vital task.
Deydrokaividing alkaloid formulations be my company there is independent intellectual property right grinding new product, structural formula is:
My company has " preparation method of deydrokaividing, Dehydroapocavidine and compositions thereof, pharmaceutical composition " (patent No.: US7732458B2); The preparation method (patent No.: ZL200410099269.6) of deydrokaividing, Dehydroapocavidine and compositions thereof; The granted patent such as deydrokaividing compounds and the application in medicine (patent No.: ZL200410099271.3) thereof, may be used for disease such as treatment hepatitis, liver cirrhosis etc.Deydrokaividing alkaloid is from Corydalis thalictrifolia Franch. (Radix Corydalis Thalictrifoliae), extract the effective ingredient that this composition makes, and its content is greater than 90%.Its dissolubility in water is poor; oral administration bioavailability is lower; limit its application; because preparation method and pharmacodynamics effect are our company's Late Cambrian; and have corresponding patent protection; so this product so far, this composition, without any other patents, does not invade the right of other any companies or individual.
At present, the preparation being not also effective ingredient with deydrokaividing monomer component is reported.According to the research of our company to this product, find that the disintegrate of deydrokaividing ordinary preparation is comparatively slow, dissolution rate is slow, can not reach effective therapeutic dose.Therefore, exploitation drug release rate is fast, and bioavailability is high, determined curative effect, oral solid formulation easy to use are very necessary, is also the problem that the present invention needs to solve.
Summary of the invention
The object of the invention is to overcome above-mentioned deficiency, a kind of pharmaceutical composition containing deydrokaividing and preparation method thereof is provided, this pharmaceutical composition is dispersible tablet, and drug release rate is fast, and bioavailability is high, determined curative effect, toxic and side effects are little, easy to use and carry.
First aspect of the present invention is to provide a kind of pharmaceutical composition containing deydrokaividing, described pharmaceutical composition is dispersible tablet, containing deydrokaividing and pharmaceutic adjuvant, count by weight, deydrokaividing is 1-150 part, and pharmaceutic adjuvant comprises: disintegrating agent 10-200 part, lubricant 0.1-10 part, fluidizer 0.1-10 part, filler 0-200 part, binding agent 0-100 part, sweller 0-200 part, surfactant 0-50 part and sweeting agent 0-200 part.
In described pharmaceutical composition, deydrokaividing is preferably 10-120 part, is more preferably 30-100 part, is more preferably 50-80 part.
In described pharmaceutical composition, disintegrating agent is preferably 20-180 part, is more preferably 40-120 part, is more preferably 60-100 part.
In described pharmaceutical composition, lubricant is preferably 0.1-10 part, is more preferably 0.5-8 part, is more preferably 1-7 part, is more preferably 3-5 part.
In described pharmaceutical composition, fluidizer is preferably 0.1-10 part, is more preferably 0.5-8 part, is more preferably 1-7 part, is more preferably 3-5 part.
In described pharmaceutical composition, filler is preferably 1-200 part, is more preferably 20-180 part, is more preferably 40-120 part, is more preferably 60-100 part.
In described pharmaceutical composition, binding agent is preferably 0.1-50 part, is more preferably 1-40 part, is more preferably 5-30 part, is more preferably 10-20 part.
In described pharmaceutical composition, sweller is preferably 0.1-180 part, is more preferably 1-150 part, is more preferably 10-100 part, is more preferably 20-80 part.
In described pharmaceutical composition, surfactant is preferably 0.1-40 part, is more preferably 0.5-35 part, is more preferably 1-30 part, is more preferably 5-20 part.
In described pharmaceutical composition, sweeting agent is preferably 0.01-50 part, is more preferably 0.1-40 part, is more preferably 0.5-20 part, is more preferably 1-10 part.
Can contain wetting agent in described pharmaceutical composition, the content of described wetting agent is lower than 10% of described pharmaceutical composition gross weight.
In foregoing of the present invention, described filler comprises the mixture of one or more in microcrystalline Cellulose, lactose, starch, pregelatinized Starch, mannitol, calcium sulfate, calcium hydrogen phosphate and medicinal calcium carbonate.
In foregoing of the present invention, described binding agent comprises one or more in polyvinylpyrrolidone, hydroxypropyl cellulose, methylcellulose.
In foregoing of the present invention, described disintegrating agent comprises the mixture of one or more in carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, microcrystalline Cellulose.
In foregoing of the present invention, described lubricant comprises the mixture of one or more in magnesium stearate, Pulvis Talci, micropowder silica gel, sodium lauryl sulphate, Stepanol MG.
In foregoing of the present invention, described fluidizer comprises the mixture of one or more in magnesium stearate, Pulvis Talci, micropowder silica gel, sodium lauryl sulphate, Stepanol MG.
In foregoing of the present invention, described sweller comprises the mixture of one or more in pregelatinized Starch, alginate, guar gum, XANTHAN GUM, glucosan.
In foregoing of the present invention, described surfactant comprises the mixture of one or more in sodium lauryl sulphate, polysorbate, hexadecyl methylamine and magnesium stearate sulphonic acid ester.
In foregoing of the present invention, described sweeting agent comprises the mixture of one or more of sugar, saccharin sodium, Calcium o-benzolsulfimide, aspartame, Radix Asparagi phthalein amine, glycyrrhizin, alcohol sugar and radix asparagi sweet extract.
In foregoing of the present invention, described wetting agent comprises one or both the mixture in water, ethanol.
In one preferred embodiment, described pharmaceutical composition comprises deydrokaividing 1-300 part, pregelatinized Starch 0-200 part, polyvinylpyrrolidone 0-100 part, starch 1-200 part, cross-linking sodium carboxymethyl cellulose 0-100 part, microcrystalline Cellulose 0.1-100 part, micropowder silica gel 0.1-10 part, magnesium stearate 0.1-10 part, sodium lauryl sulphate 0.1 part-20 parts, sweeting agent 0.01-5 part, Yi Jishui, wherein, the content of water is lower than 10% of described pharmaceutical composition gross weight.
Second aspect of the present invention is to provide the preparation method of the pharmaceutical composition containing deydrokaividing described in a kind of the present invention first aspect, comprises the following steps:
Step 1, takes disintegrating agent, filler, sweller, surfactant and sweeting agent, pulverizes, sieves, mix homogeneously;
Step 2, adds the wetting agent being dissolved with binding agent and prepares soft material, granulates;
Step 3, dry;
Step 4, sieve granulate, adds lubricant and fluidizer, mix homogeneously, and tabletting both obtained.
It should be noted that step 3, in drying, most of wetting agent is removed, and makes the content of wetting agent in finished product lower than 10% of gained pharmaceutical composition gross weight.
Wherein, granulate in step 2 and adopted 16-24 mesh sieve to granulate, or use fluidized bed granulation.
Preferably, in step 1, sieve as crossing 80 mesh sieves.
Preferably, the granulate that sieves in step 4 was 16-24 mesh sieve.
The deydrokaividing dispersible tablet that contains of the present invention, compared with deydrokaividing ordinary tablet, has the following advantages:
1, there is good disintegrative and dissolving out capability.
Deydrokaividing medicine water solublity is poor, needs to add solubilizing agent in its injection, but the compliance of injection is very poor.Oral solid formulation is made in the present invention, the speed limit process of its onset is exactly disintegrate and process in leaching, dispersible tablet of the present invention meets water can disintegrate rapidly, and the fine grained be separated into by No. 2 sieves, there is the incomparable disintegrate ability of ordinary solid preparation and dissolving out capability, and dispersible tablet of the present invention makes the dissolution rate of medicine greatly improve, take rear absorption soon, bioavailability is high.
2, there is good dispersing uniformity: due to effective ingredient and major auxiliary burden co-grinding and by 80 orders, supplementary material is more tiny, pelletizing press sheet again, containing excellent disintegrating agent, dispersant, wetting agent etc. in sheet, make this dispersible tablet in water can rapidly disintegrate and dispersed be granule, effective ingredient is fully exposed, impels and absorb quickening, bioavailability raising.
3, good mouthfeel, taking convenience, compliance is good.The present invention is oral solid formulation, there is compared with injection the compliance of having followed, more general oral liquid has better stability and property easy to carry, and the taste of the present invention to dispersible tablet adjusts, outside making directly to swallow, to there being the patient of dysphagia can also add aqueous dispersion deutostoma clothes, add compliance.
4, this product tablet oral administration biaavailability is poor, and through improvement of the present invention, the bioavailability of this product is significantly improved, and onset time accelerates, and drug effect is more obvious.
Pharmaceutical composition (dispersible tablet) containing deydrokaividing provided by the invention, there is good disintegrative and dissolving out capability, there is good dispersing uniformity, good mouthfeel, taking convenience, compliance is good, and drug availability is significantly improved, onset time accelerates, and drug effect is more obvious.
Accompanying drawing explanation
Fig. 1 for embodiment 18 provide containing the pharmaceutical composition of deydrokaividing and common plain sheet dissolution comparison diagram.
Detailed description of the invention
With reference to the accompanying drawings, the invention will be further described in conjunction with specific embodiments, to understand the present invention better.
Embodiment 1
Take deydrokaividing 5mg, pre-paying starch 15mg, microcrystalline Cellulose 10mg, sodium lauryl sulphate 0.1mg, polyvinylpolypyrrolidone 5mg, cross-linking sodium carboxymethyl cellulose 1mg, appropriate sweeting agent, cross 80 mesh sieves, mix homogeneously, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, and moisture reaches 0.5-10%, granulate, add magnesium stearate 0.1mg, mix homogeneously, tabletting both obtained.
Embodiment 2
Take deydrokaividing 5mg, pre-paying starch 15mg, microcrystalline Cellulose 10mg, sodium lauryl sulphate 0.1mg, polyvinylpolypyrrolidone 5mg, cross-linking sodium carboxymethyl cellulose 1mg, appropriate sweeting agent, cross 80 mesh sieves, mix homogeneously, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, and moisture reaches 0.5-10%, granulate, add micropowder silica gel 0.1mg, mix homogeneously, tabletting both obtained.
Embodiment 3
Take deydrokaividing 25mg, pre-paying starch 15mg, lactose 50mg, sodium lauryl sulphate 0.5mg, polyvinylpolypyrrolidone 5mg, cross-linking sodium carboxymethyl cellulose 10mg, appropriate sweeting agent, cross 80 mesh sieves, mix homogeneously, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, and moisture reaches 0.5-10%, granulate, add magnesium stearate 1.2mg, mix homogeneously, tabletting both obtained.
Embodiment 4
Take deydrokaividing 25mg, pre-paying starch 15mg, microcrystalline Cellulose 50mg, sodium lauryl sulphate 0.5mg, polyvinylpolypyrrolidone 5mg, cross-linking sodium carboxymethyl cellulose 10mg, appropriate sweeting agent, cross 80 mesh sieves, mix homogeneously, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, and moisture reaches 0.5-10%, granulate, add magnesium stearate 1.2mg, mix homogeneously, tabletting both obtained.
Embodiment 5
Take deydrokaividing 50mg, pre-paying starch 25mg, microcrystalline Cellulose 50mg, sodium lauryl sulphate 0.5mg, polyvinylpolypyrrolidone 10mg, cross-linking sodium carboxymethyl cellulose 3mg, appropriate sweeting agent, cross 80 mesh sieves, mix homogeneously, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, moisture 0.5%-10%s, granulate, add magnesium stearate 1.2mg, mix homogeneously, tabletting both obtained.
Embodiment 6
Take deydrokaividing 50mg, pre-paying starch 50mg, microcrystalline Cellulose 20mg, sodium lauryl sulphate 0.5mg, polyvinylpolypyrrolidone 20mg, cross-linking sodium carboxymethyl cellulose 3mg, appropriate sweeting agent, cross 80 mesh sieves, mix homogeneously, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, moisture 0.5%-10%s, granulate, add magnesium stearate 1.2mg, mix homogeneously, tabletting both obtained.
Embodiment 7
Take deydrokaividing 100mg, pre-paying starch 40mg, corn starch 50mg, sodium lauryl sulphate 2.5mg, calcium sulfate 50mg, cross-linking sodium carboxymethyl cellulose 16mg, appropriate sweeting agent, cross 80 mesh sieves, mix homogeneously, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, and moisture reaches 0.5-10%, granulate, add magnesium stearate 1.2mg, mix homogeneously, tabletting both obtained.
Embodiment 8
Take deydrokaividing 100mg, pre-paying starch 100mg, microcrystalline Cellulose 40mg, polyvinylpolypyrrolidone 30mg, appropriate sweeting agent, crosses 80 mesh sieves, mix homogeneously, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, and moisture reaches 0.5-10%, granulate, add magnesium stearate 1.2mg, mix homogeneously, tabletting both obtained.
Embodiment 9
Take deydrokaividing 100mg, pre-paying starch 40mg, microcrystalline Cellulose 100mg, polyvinylpolypyrrolidone 20mg, appropriate sweeting agent, mix homogeneously, crosses 80 mesh sieves, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, and moisture reaches 0.5-10%, granulate, add micropowder silica gel 2mg, mix homogeneously, tabletting both obtained.
Embodiment 10
Take deydrokaividing 100mg, pre-paying starch 100mg, lactose 80mg, polyvinylpolypyrrolidone 20mg, appropriate sweeting agent, crosses 80 mesh sieves, mix homogeneously, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, and moisture reaches 0.5-10%, granulate, add magnesium stearate 1.2mg, mix homogeneously, tabletting both obtained.
Embodiment 11
Take deydrokaividing 100mg, starch 40mg, microcrystalline Cellulose 100mg can be pressed, polyvinylpolypyrrolidone 20mg, cross-linking sodium carboxymethyl cellulose 10mg, appropriate sweeting agent, crosses 80 mesh sieves, mix homogeneously, drips 5% aqueous povidone solution soft material, crosses 24 mesh sieves and granulates, granule is dry under 45-80 DEG C of condition, moisture reaches 0.5-10%, granulate, adds micropowder silica gel 2mg, mix homogeneously, tabletting both obtained.
Embodiment 12
Take deydrokaividing 10mg, pre-paying starch 40mg, corn starch 40mg, sodium lauryl sulphate 2.0mg, cross-linking sodium carboxymethyl cellulose 20mg, appropriate sweeting agent, crosses 80 mesh sieves, mix homogeneously, drips 5% aqueous povidone solution soft material, crosses 24 mesh sieves and granulates, granule is dry under 45-80 DEG C of condition, moisture reaches 0.5-10%, granulate, adds magnesium stearate 1.2mg, mix homogeneously, tabletting both obtained.
Embodiment 13
Take deydrokaividing 10mg, microcrystalline Cellulose 30mg, lactose 30mg, polyvinylpolypyrrolidone 20mg, appropriate sweeting agent, crosses 80 mesh sieves, mix homogeneously, drip 5% aqueous povidone solution soft material, cross 24 mesh sieves to granulate, granule is dry under 45-80 DEG C of condition, and moisture reaches 0.5-10%, granulate, add micropowder silica gel 1mg, mix homogeneously, tabletting both obtained.
Embodiment 14
Take deydrokaividing 10mg, microcrystalline Cellulose 60mg, lactose 20mg, trehalose 10mg, polyvinylpolypyrrolidone 20mg, appropriate sweeting agent, crosses 80 mesh sieves, mix homogeneously, drips 5% aqueous povidone solution soft material, crosses 24 mesh sieves and granulates, granule is dry under 45-80 DEG C of condition, moisture reaches 0.5-10%, granulate, adds micropowder silica gel 1mg, mix homogeneously, tabletting both obtained.
Embodiment 15
Take deydrokaividing 10mg, microcrystalline Cellulose 10mg, pre-paying starch 10mg, polyvinylpolypyrrolidone 5mg, appropriate sweeting agent, crosses 80 mesh sieves, mix homogeneously, with 5% aqueous povidone solution for binding agent, adopt boiling granulating method, one-step palletizing, granule is dry under 45-80 DEG C of condition, moisture reaches 0.5-10%, granulate, adds magnesium stearate 1mg, mix homogeneously, tabletting both obtained.
Embodiment 16
Take deydrokaividing 25mg, pre-paying starch 15mg, lactose 50mg, sodium lauryl sulphate 0.5mg, polyvinylpolypyrrolidone 5mg, cross-linking sodium carboxymethyl cellulose 10mg, appropriate sweeting agent, cross 80 mesh sieves, mix homogeneously, with 5% aqueous povidone solution for binding agent, adopt boiling granulating method, one-step palletizing, granule is dry under 45-80 DEG C of condition, moisture reaches 0.5-10%, granulate, adds magnesium stearate 1.0mg, mix homogeneously, tabletting both obtained.
Embodiment 17
Take deydrokaividing 50mg, pre-paying starch 25mg, microcrystalline Cellulose 50mg, sodium lauryl sulphate 0.5mg, polyvinylpolypyrrolidone 10mg, cross-linking sodium carboxymethyl cellulose 3mg, appropriate sweeting agent, cross 80 mesh sieves, mix homogeneously, with 5% aqueous povidone solution for binding agent, adopt boiling granulating method, one-step palletizing, granule is dry under 45-80 DEG C of condition, moisture 0.5%-10%s, granulate, adds magnesium stearate 1.2mg, mix homogeneously, tabletting both obtained.
Embodiment 18
Take deydrokaividing 100mg, pre-paying starch 100mg, microcrystalline Cellulose 40mg, polyvinylpolypyrrolidone 30mg, appropriate sweeting agent, crosses 80 mesh sieves, mix homogeneously, with 5% aqueous povidone solution for binding agent, adopt boiling granulating method, one-step palletizing, granule is dry under 45-80 DEG C of condition, moisture reaches 0.5-10%, granulate, adds magnesium stearate 1.2mg, mix homogeneously, tabletting both obtained.
Pharmaceutical composition containing deydrokaividing prepared by Example 1-18 carries out slaking test and dispersing uniformity measures, and wherein, reference examples 1 is deydrokaividing ordinary tablet, and result is as shown in table 1.
Pharmaceutical composition containing deydrokaividing prepared by Example 1-18 carries out dispersing uniformity mensuration, be specially: get 6 pharmaceutical compositions of the present invention and common plain sheet (reference examples 2), be placed in 250ml beaker respectively, add the water of 100ml 15-25 DEG C, jolting, make it by No. 2 sieves, result is as shown in table 1.
Pharmaceutical composition containing deydrokaividing prepared by Example 1-18 carries out dissolution detection, reference examples 1 is deydrokaividing ordinary tablet, according to dissolution method (Chinese Pharmacopoeia version in 2010 two annex XC second methods), with 900ml water for solvent, rotating speed is 50 turns per minute, operate in accordance with the law, at 2min, 5min, 10min, 20min, 30min, 45min, 60min timing sampling 5ml, supplement the liquid of same media, get dissolution fluid and be about 50ml filtration, get subsequent filtrate as test liquid.Result as shown in Table 2 and Figure 1.
Table 1 slaking test result and dispersing uniformity measurement result
| Disintegration time | Dispersing uniformity | |
| Embodiment 1 | 42s | Jolting 2.4 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 2 | 46s | Jolting 2.6 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 3 | 76s | Jolting 2.7 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 4 | 45s | Jolting 2.5 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 5 | 54s | Jolting 2.8 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 6 | 47s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 7 | 88s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 8 | 54s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 9 | 49s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 10 | 75s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 11 | 93s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 12 | 48s | Jolting 2.8 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 13 | 51s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 14 | 57s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 15 | 46s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 16 | 62s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 17 | 48s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Embodiment 18 | 49s | Jolting 3 minutes, dispersible tablet is all by No. 2 sieves |
| Reference examples 1 | 463s | -- |
| Reference examples 2 | -- | Jolting 15 minutes, plain sheet part is by No. 2 sieves |
As shown in Table 1, the pharmaceutical composition containing deydrokaividing provided by the invention has good disintegrative and dispersive property.
Table 2 dissolution testing result
As shown in Table 2, the dissolution rate of the pharmaceutical composition containing deydrokaividing provided by the invention and degree are obviously better than ordinary tablet.
Be described in detail specific embodiments of the invention above, but it is just as example, the present invention is not restricted to specific embodiment described above.To those skilled in the art, any equivalent modifications that the present invention is carried out and substituting also all among category of the present invention.Therefore, equalization conversion done without departing from the spirit and scope of the invention and amendment, all should contain within the scope of the invention.
Claims (8)
1. the pharmaceutical composition containing deydrokaividing, it is characterized in that, described pharmaceutical composition is dispersible tablet, containing deydrokaividing and pharmaceutic adjuvant, count by weight, deydrokaividing is 1-150 part, and pharmaceutic adjuvant comprises: disintegrating agent 10-200 part, lubricant 0.1-10 part, fluidizer 0.1-10 part, filler 0-200 part, binding agent 0-100 part, sweller 0-200 part, surfactant 0-50 part and sweeting agent 0-200 part; Also containing wetting agent in described pharmaceutical composition, the content of described wetting agent is lower than 10% of described pharmaceutical composition gross weight.；
Described filler is selected from the mixture of one or more in microcrystalline Cellulose, lactose, starch, pregelatinized Starch, mannitol, calcium sulfate, calcium hydrogen phosphate and medicinal calcium carbonate;
Described binding agent comprises one or more in polyvinylpyrrolidone, hydroxypropyl cellulose, methylcellulose;
Described disintegrating agent comprises the mixture of one or more in carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, microcrystalline Cellulose;
Described lubricant comprises the mixture of one or more in magnesium stearate, Pulvis Talci, micropowder silica gel, sodium lauryl sulphate, Stepanol MG;
Described fluidizer comprises the mixture of one or more in magnesium stearate, Pulvis Talci, micropowder silica gel, sodium lauryl sulphate, Stepanol MG;
Described sweller comprises the mixture of one or more in pregelatinized Starch, alginate, guar gum, XANTHAN GUM, glucosan;
Described surfactant comprises the mixture of one or more in sodium lauryl sulphate, polysorbate, hexadecyl methylamine and magnesium stearate sulphonic acid ester;
Described sweeting agent comprises the mixture of one or more of sugar, saccharin sodium, Calcium o-benzolsulfimide, aspartame, Radix Asparagi phthalein amine, glycyrrhizin, alcohol sugar and radix asparagi sweet extract;
Described wetting agent comprises one or both the mixture in water, ethanol.
2. pharmaceutical composition according to claim 1, is characterized in that, deydrokaividing is 10-120 part, disintegrating agent is 20-180 part, lubricant is 0.1-10 part, fluidizer is 0.1-10 part.
3. pharmaceutical composition according to claim 1, is characterized in that, filler 1-200 part, binding agent 0.1-50 part, sweller 0.1-180 part, surfactant 0.1-40 part and sweeting agent 0.01-50 part in described pharmaceutical composition.
4. pharmaceutical composition according to claim 1, it is characterized in that, hydrogen Ka Weiding is 30-100 part, and disintegrating agent is 40-120 part, and lubricant is 0.5-8 part, fluidizer is 0.5-8 part, filler is 20-180 part, and binding agent is 1-40 part, and sweller is 1-150 part, surfactant is 0.5-35 part, and sweeting agent 0.1-40 part.
5. pharmaceutical composition according to claim 1, it is characterized in that, described pharmaceutical composition comprises deydrokaividing 1-150 part, pregelatinized Starch 0-200 part, polyvinylpyrrolidone 0-100 part, starch 1-200 part, cross-linking sodium carboxymethyl cellulose 0-100 part, microcrystalline Cellulose 0.1-100 part, micropowder silica gel 0.1-10 part, magnesium stearate 0.1-10 part, sodium lauryl sulphate 0.1 part-20 parts, correctives 0.01-5 part, Yi Jishui, wherein, the content of water is lower than 10% of described pharmaceutical composition gross weight.
6. a preparation method for the pharmaceutical composition containing deydrokaividing in claim 1-5 described in any one, is characterized in that, comprise the following steps:
Step 1, takes deydrokaividing, disintegrating agent, filler, sweller, surfactant and sweeting agent, pulverizes, sieves, mix homogeneously;
Step 2, adds the wetting agent being dissolved with binding agent and prepares soft material, granulates;
Step 3, dry;
Step 4, sieve granulate, adds lubricant and fluidizer, mix homogeneously, and tabletting both obtained.
7. preparation method according to claim 6, is characterized in that, granulating in step 2 adopted 16-24 mesh sieve to granulate, or used fluidized bed granulation.
8. preparation method according to claim 6, is characterized in that, in step 1, sieve as crossing 80 mesh sieves, the granulate that sieves in step 4 was 16-24 mesh sieve.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410148314.6A CN103933037B (en) | 2014-04-14 | 2014-04-14 | Dehydrocavidine-containing pharmaceutical composition and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410148314.6A CN103933037B (en) | 2014-04-14 | 2014-04-14 | Dehydrocavidine-containing pharmaceutical composition and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103933037A CN103933037A (en) | 2014-07-23 |
| CN103933037B true CN103933037B (en) | 2015-06-17 |
Family
ID=51181095
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410148314.6A Active CN103933037B (en) | 2014-04-14 | 2014-04-14 | Dehydrocavidine-containing pharmaceutical composition and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103933037B (en) |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100595200C (en) * | 2004-12-29 | 2010-03-24 | 中国人民解放军第二军医大学 | Compound of dehydrogenated cavidine group and application in medication |
| CN100554270C (en) * | 2004-12-29 | 2009-10-28 | 中国人民解放军第二军医大学 | Deydrokaividing, dehydrogenation apocavidine and preparation of compositions method thereof |
-
2014
- 2014-04-14 CN CN201410148314.6A patent/CN103933037B/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| CN103933037A (en) | 2014-07-23 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN102198110B (en) | Tenofovir disoproxil fumarate dispersible tablets and preparation method thereof | |
| CN104000789A (en) | Adefovir dipivoxil dispersible tablet and preparation method thereof | |
| KR101562608B1 (en) | Compound chemical medicine acting on respiratory disease, preparation process and use thereof | |
| CN103893258A (en) | Oral solid preparation containing desmodium styracifolium general flavone and application thereof | |
| CN104586798A (en) | Gefitinib dispersible tablet and preparation method thereof | |
| CN101433610A (en) | Shan ju coated dispersible tablet for releasing pressure and preparation method thereof | |
| CN100542528C (en) | Bicyclol micronization and controlled release formulations for oral administration | |
| CN1903183A (en) | Dispersion tablets of telbivudine and its prepn. method | |
| CN103933037B (en) | Dehydrocavidine-containing pharmaceutical composition and preparation method thereof | |
| CN103933195B (en) | A kind of Chinese medicine composition and preparation prevent and treat the application in hepatopathy medicine | |
| CN101254177A (en) | Dantrolene sodium chewable tablet and method of preparing the same | |
| CN100348199C (en) | Silicibinin-N-methylglucamine disperser for treating hepatitis, and its prepn. method | |
| CN101953773B (en) | Lamivudine liposome solid preparation | |
| CN103919743B (en) | Pharmaceutical composition containing cavidine total alkali and preparation method of pharmaceutical composition | |
| CN101156856A (en) | Falacyclovir dispersion piece and its preparation method | |
| CN1546046A (en) | Adefovir dipivoxil dispersing tablet and its preparation | |
| CN1228051C (en) | Medicinal composition for treating cardiovascular disease | |
| CN102370621A (en) | Solid preparation with cefotiam hexetil as active component | |
| CN108785273B (en) | Entecavir capsule pharmaceutical composition and preparation method thereof | |
| CN101028273A (en) | Improved Enticawer suspension granules and their preparation | |
| CN111000807B (en) | A dripping pill containing ginkgolide as effective component and its preparation method | |
| CN101011383A (en) | Dispersible tablet of coumarin derivative and its preparation method | |
| CN101890057A (en) | Herba Pteridis Multifidae preparation that treatment gastrointestinal tract, urinary tract infection and the heart, cerebrovascular disease are used and preparation method thereof | |
| CN1439371A (en) | Matrine sustained releasing agent and its preparing process | |
| CN1927372A (en) | Antiviral dispersant tablet and method for making same |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20221116 Address after: No.6 Dongbo Road, East District, Guangzhou Economic and Technological Development Zone, Guangdong 510000 Patentee after: GUANGZHOU YIPINHONG PHARMACEUTICAL Co.,Ltd. Patentee after: GUANGDONG ZERUI PHARMACEUTICAL Co.,Ltd. Patentee after: Guangzhou Lianrui Pharmaceutical Co.,Ltd. Patentee after: Guangzhou Runlin Pharmaceutical Technology Co.,Ltd. Patentee after: Euphorbia Biological Medicine Co.,Ltd. Address before: Building 1, No. 6, Dongbo Road, Guangzhou Economic and Technological Development Zone, 510000 Guangdong Patentee before: GUANGZHOU YIPINHONG PHARMACEUTICAL Co.,Ltd. |
|
| TR01 | Transfer of patent right |