CN1298318C - Sodium ferulic acid osmosis pump controlled release formulation and its preparation method - Google Patents
Sodium ferulic acid osmosis pump controlled release formulation and its preparation method Download PDFInfo
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- CN1298318C CN1298318C CNB031442501A CN03144250A CN1298318C CN 1298318 C CN1298318 C CN 1298318C CN B031442501 A CNB031442501 A CN B031442501A CN 03144250 A CN03144250 A CN 03144250A CN 1298318 C CN1298318 C CN 1298318C
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- sodium
- sodium ferulate
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Abstract
The present invention relates to a preparation method for sodium ferulate osmotic pump controlled release preparation which comprises sodium ferulate core as an effective active component, a semi-transparent coating film, medicine-releasing holes and a damp-proof film, wherein the core contains 40 wt% to 90 wt% of sodium ferulate, 30 wt% to 95 wt% of penetrating agent, 1 wt% to 8 wt% adhesive, 2 wt% to 10 wt% disintegrating agent and 0.5 wt% to 3 wt% of lubricating agent. The present invention overcomes the defects of existing preparations and the osmotic pump preparation is prepared by using the film control technology; the medicine is released constantly, and the effective plasma drug concentration in vivo can maintain for 24 hours; the frequency of taking medicine is reduced so that patients only need take medicine once per day; the present invention has the advantages of zero-order medicine release, stable plasma drug concentration and little side effect.
Description
Technical field:
The present invention relates to a kind of preparation method of sodium ferulate penetration pump type controlled release
Background technology:
Sodium ferulate (sodium Ferulate) is the water-soluble active ingredient that extracts from Radix Angelicae Sinensis or Rhizoma Chuanxiong, chemistry 3-methoxyl group by name-4 hydroxyls-Sodium Cinnamate, be the common drug of treatment cardiovascular and cerebrovascular disease, its pharmaceutical dosage form has conventional tablet, regular dosage forms such as powder and aqueous solution.Because the sodium ferulate biological half-life is short, oral post-absorption is fast, and therefore elimination is also fast in vivo, and for keeping effective blood drug concentration, necessary balance administration so just can be produced the Wave crest and wave trough phenomenon in the hematopoietic.Chinese patent CN138515151 discloses a kind of slow releasing tablet.But because the sodium ferulate good water solubility, between the general 8-10 of its gel matrix tablet hour, medicine discharges fully.Want controlled release constant release in 24 hours, be difficult to realize.So develop controlled release preparation once-a-day, meet the needs of clinical development fully.
Summary of the invention:
The purpose of this invention is to provide a kind of sodium ferulate penetration pump type controlled release and preparation method, the present invention can overcome the defective of existing preparation choosing, the selective membrane control techniques, and osmotic pump preparation can constant release, and effective blood drug concentration can be kept 24 hours in the body.Can reduce medicining times, once a day, nearly zero-order release, blood drug level is steady, and side effect is little.
The present invention includes the label of effective active composition sodium ferulate, semi-transparent coating membrane, drug release hole and damp-proof membrane constitutes;
The weight of described label is formed:
Sodium ferulate 40%-90%
Penetrating agent 30%-95%
Binding agent 1%-8%
Disintegrating agent 2%-10%
Lubricant 0.5%-3%
Described semi-transparent coating membrane weight is formed:
Macromolecular material 50-100 part
Plasticizer 5-50 weight portion
Described drug release hole is in label one side laser boring;
It is that Opadry model opadryII stomach dissolution type coating materials is prepared the back coating in accordance with regulations that described damp-proof membrane is formed.
Described penetrating agent is:
Low molecule saccharide: sucrose, mannitol or sorbitol;
Inorganic salt: sodium chloride, potassium chloride, magnesium chloride, potassium sulfate or sodium sulfate; Or
Other short saturating active substances: polyvinylpyrrolidone, sodium carboxymethyl cellulose, Polyethylene Glycol, carbamide or tartaric acid.
Described binding agent is polyvinylpyrrolidone, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose or methylcellulose.
Described disintegrating agent is crosslinked Carboxymethyl cellulose sodium or polyvinylpolypyrrolidone.
Described lubricant is: magnesium stearate, Pulvis Talci or Polyethylene Glycol.
Described semipermeable membrane coating macromolecular material is: ethyl cellulose, cellulose acetate, polyoxyethylene or polyvinyl alcohol.
In the described semipermeable membrane coating membrane, plasticizer is diethyl phthalate, triglyceride, Polyethylene Glycol-1000, Polyethylene Glycol-4000, Polyethylene Glycol-6000, triethyl citrate or succinate.
Described damp-proof membrane consists of Opadry model opadryII, and coating materials (production of the happy Kanggong of Shanghai card department) is coating weightening finish 2%-6% in accordance with regulations.
Described laser boring diameter 100-600 micron.
The preparation method of sodium ferulate controlled releasing penetrant pump may further comprise the steps:
1) by metering formulation selection label prescription, semipermeable membrane and moistureproof mould, the laser boring diameter, with medicine adhesive, disintegrating agent, the penetrating agent crushing screening, fully mixing adds ethanol: water (1: 1) system soft material, the granulation of 20 orders, 45 degrees centigrade of drying baker dryings, 16 orders are put dried granule in order and are added lubricant and be pressed into label;
2) semipermeable membrane coating macromolecular material and plasticizer are dissolved in acetone, in the mixed solvent of chloroform, label are placed in the tangent line spray fluid bed, carry out coating;
3), coating membrane was solidified in 24 hours with coated tablet to 40 degree centigrade drying baker inner drying;
4) use the aperture of laser-beam drilling machine diameter between 100-600 micron of side preparation of label, place bag damp-proof membrane in the tangent line spray fluid bed again, 40 degrees centigrade of drying baker inner dryings 8 hours promptly get sodium ferulate laser boring osmotic pump type controlled release tablet.
Advantage of the present invention is: utilize advanced film control techniques, make sodium ferulate laser boring controlled release tablet, can reduce medicining times, once a day.The said preparation release is not subjected to the influence of PH.External stripping test, 1-18 hour constant release, blood drug level is steady, reduces toxic and side effects, improves patient's compliance, is fit to the needs of clinical development.
Description of drawings
Fig. 1: be sodium ferulate laser boring osmotic pump controlled release tablet stripping curve figure of the present invention.
The specific embodiment:
Embodiment 1
The label prescription:
Sodium ferulate 150g
Sodium chloride 150g
Cross-linking sodium carboxymethyl cellulose 9g
30 POVIDONE K 30 BP/USP 30 12g
Magnesium stearate 1.5g
The semipermeable membrane prescription:
Cellulose acetate 15g
Polyethylene Glycol-1000 3g
Damp-proof membrane prescription Opadry model opadryII collocation method: solvent is placed container, and solvent is a water, slowly Opadry model opadryII is added in the solvent under condition of stirring, and solid content is 8%-20%
Preparation technology:
With the sodium ferulate in the prescription, cross-linking sodium carboxymethyl cellulose, 30 POVIDONE K 30 BP/USP 30, magnesium stearate is sieving for standby respectively, and sodium chloride is pulverized sieving for standby, and main ingredient is put in the container, and fully mixing adds lubricant ethanol: water (1: 1), system soft material.20 mesh sieves are granulated, and 45 degrees centigrade of drying baker dryings are used 16 mesh sieve granulate.Add tabletting behind the magnesium stearate lubricant, label is put in the tangent line spray fluidized-bed coating machine.
With coated tablet to 40 degree centigrade drying baker inner drying, coating membrane was solidified in 24 hours;
Use the aperture of laser-beam drilling machine diameter between 100-600 micron of side preparation of label, place bag damp-proof membrane in the tangent line spray fluid bed again, 40 degrees centigrade of drying baker inner dryings 8 hours get final product.
Embodiment 2
The label prescription:
Sodium ferulate 1500g
Sodium chloride 750g
Sucrose 750g
Cross-linking sodium carboxymethyl cellulose 90g
30 POVIDONE K 30 BP/USP 300 120g
Magnesium stearate 15g
The semipermeable membrane prescription:
Cellulose acetate 150g
Polyethylene Glycol-4000 20g
Damp-proof membrane prescription Opadry model opadryII collocation method: solvent is placed container, and solvent is a water, slowly Opadry model opadryII is added in the solvent under condition of stirring, and solid content is 8%-20%
Preparation technology:
With the sodium ferulate in the prescription, cross-linking sodium carboxymethyl cellulose, 30 POVIDONE K 30 BP/USP 30, magnesium stearate is sieving for standby respectively, and sodium chloride is pulverized sieving for standby, and main ingredient is put in the container, and fully mixing adds lubricant ethanol: water (1: 1), system soft material.20 mesh sieves are granulated, and 45 degrees centigrade of drying baker dryings are used 16 mesh sieve granulate.Add tabletting behind the magnesium stearate lubricant, label is put in the tangent line spray fluidized-bed coating machine.
With coated tablet to 40 degree centigrade drying baker inner drying, coating membrane was solidified in 24 hours;
Use the aperture of laser-beam drilling machine diameter between 100-600 micron of side preparation of label, place bag damp-proof membrane in the tangent line spray fluid bed again, 40 degrees centigrade of drying baker inner dryings 8 hours get final product.
Embodiment 3
The label prescription
Sodium ferulate 450g
Sodium chloride 225g
Sucrose 225g
Cross-linking sodium carboxymethyl cellulose 27g
30 POVIDONE K 30 BP/USP 30 36g
Magnesium stearate 15g
The semipermeable membrane prescription:
Cellulose acetate 45g
Polyethylene Glycol-6000 4.5g
Damp-proof membrane prescription Opadry model opadryII collocation method: solvent is placed container, and solvent is a water, slowly Opadry model opadryII is added in the solvent under condition of stirring, and solid content is 8%-20%
Preparation technology
With the sodium ferulate in the prescription, cross-linking sodium carboxymethyl cellulose, 30 POVIDONE K 30 BP/USP 30, magnesium stearate is sieving for standby respectively, and sodium chloride is pulverized sieving for standby, and main ingredient is put in the container, and fully mixing adds lubricant ethanol: water (1: 1), system soft material.20 mesh sieves are granulated, and 45 degrees centigrade of drying baker dryings are used 16 mesh sieve granulate.Add tabletting behind the magnesium stearate lubricant, label is put in the tangent line spray fluidized-bed coating machine.
With coated tablet to 40 degree centigrade drying baker inner drying, coating membrane was solidified in 24 hours; Use the aperture of laser-beam drilling machine diameter between 100-600 micron of side preparation of label, place bag damp-proof membrane in the tangent line spray fluid bed again, 40 degrees centigrade of drying baker inner dryings 8 hours get final product.
Embodiment 1 its accumulation discharges the time mapping, sees Fig. 1
Illustrate that the release of embodiment 1 sodium ferulate laser boring osmotic pump controlled release tablet is not influenced by PH, release is steady, meets the zero-order release process, sees Table 1, table 1: be the release of sodium ferulate laser boring osmotic pump controlled release tablet of the present invention in different medium.
Table 2
Claims (10)
1, a kind of sodium ferulate controlled releasing penetrant pump is characterized in that it is that the label that comprises effective active component sodium ferulate, semi-transparent coating membrane, drug release hole and damp-proof membrane constitute;
The weight of described label is formed:
Sodium ferulate 46-46.5%
Penetrating agent 46-46.5%
Binding agent 2.8%
Disintegrating agent 3.7%
Lubricant 0.5-1.5%
Described semi-transparent coating membrane weight is formed:
Semipermeable membrane coating macromolecular material 50-100 part
Plasticizer 5-50 weight portion
Described drug release hole is in label one side laser boring;
It is that Opadry model opadryII stomach dissolution type coating materials disposes the back coating in accordance with regulations that described damp-proof membrane is formed.
2, sodium ferulate controlled releasing penetrant pump according to claim 1 is characterized in that described penetrating agent is: low molecule saccharide: sucrose, mannitol or sorbitol;
Inorganic salt: sodium chloride, potassium chloride, magnesium chloride, potassium sulfate or sodium sulfate; Or other short saturating active substances: polyvinylpyrrolidone, sodium carboxymethyl cellulose, Polyethylene Glycol, carbamide or tartaric acid.
3,, it is characterized in that described binding agent is polyvinylpyrrolidone, sodium carboxymethyl cellulose, hydroxypropyl emthylcellulose or methylcellulose according to the described sodium ferulate controlled releasing penetrant pump of claim 1.
4,, it is characterized in that described disintegrating agent is crosslinked Carboxymethyl cellulose sodium or polyvinylpolypyrrolidone according to the described sodium ferulate controlled releasing penetrant pump of claim 1.
5, sodium ferulate controlled releasing penetrant pump according to claim 1 is characterized in that described lubricant is: magnesium stearate, Pulvis Talci or Polyethylene Glycol.
6, sodium ferulate controlled releasing penetrant pump according to claim 1 is characterized in that described semipermeable membrane coating macromolecular material is: ethyl cellulose, cellulose acetate, polyoxyethylene or polyvinyl alcohol.
7, the described sodium ferulate controlled releasing penetrant pump of root a tree name claim 1, it is characterized in that in the described semipermeable membrane coating membrane that plasticizer is diethyl phthalate, triglyceride, Polyethylene Glycol-1000, Polyethylene Glycol-4000, Polyethylene Glycol-6000, triethyl citrate or succinate.
8, the described sodium ferulate controlled releasing penetrant pump of root a tree name claim 1 is characterized in that described damp-proof membrane consists of Opadry model opadryII, and coating materials is coating weightening finish 2%-6% in accordance with regulations.
9, the described sodium ferulate controlled releasing penetrant pump of root a tree name claim 1 is characterized in that described laser boring diameter 100-600 micron.
10, the preparation method of the described sodium ferulate controlled releasing penetrant pump of claim 1 is characterized in that it may further comprise the steps:
1) by metering formulation selection label prescription, semipermeable membrane and moistureproof mould, the laser boring diameter, and with medicine adhesive, disintegrating agent, the penetrating agent crushing screening, abundant mixing, with 1: 1 ethanol and water mixed liquid system soft material, 20 orders are granulated, 45 degrees centigrade of drying baker dryings, 16 orders are put dried granule in order and are added lubricant and be pressed into label;
2) semipermeable membrane coating macromolecular material and plasticizer are dissolved in acetone, in the mixed solvent of chloroform, label are placed in the tangent line spray fluid bed, carry out coating;
3), coating membrane was solidified in 24 hours with coated tablet to 40 degree centigrade drying baker inner drying;
4) use the aperture of laser-beam drilling machine diameter between 100-600 micron of side preparation of label, place bag damp-proof membrane in the tangent line spray fluid bed again, 40 degrees centigrade of drying baker inner dryings 8 hours promptly get sodium ferulate laser boring osmotic pump type controlled release tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB031442501A CN1298318C (en) | 2003-09-08 | 2003-09-08 | Sodium ferulic acid osmosis pump controlled release formulation and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB031442501A CN1298318C (en) | 2003-09-08 | 2003-09-08 | Sodium ferulic acid osmosis pump controlled release formulation and its preparation method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1522693A CN1522693A (en) | 2004-08-25 |
| CN1298318C true CN1298318C (en) | 2007-02-07 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| CNB031442501A Expired - Fee Related CN1298318C (en) | 2003-09-08 | 2003-09-08 | Sodium ferulic acid osmosis pump controlled release formulation and its preparation method |
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| CN (1) | CN1298318C (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101152228B (en) * | 2006-09-28 | 2010-08-18 | 成都中医药大学 | Genseng total sapnin micropore permeation pump, and its preparing method |
| CN102670548A (en) * | 2011-03-14 | 2012-09-19 | 北京天衡药物研究院 | Paroxetine hydrochloride osmotic pump type enteric controlled release tablet |
| CN110025589A (en) * | 2019-01-16 | 2019-07-19 | 武汉长联来福制药股份有限公司 | A kind of sodium ferulate controlled release tablet and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1385151A (en) * | 2002-05-16 | 2002-12-18 | 中国人民解放军第二军医大学 | Slow-released dosage form of sodium ferulate and preparation process thereof |
| CN1415287A (en) * | 2002-11-28 | 2003-05-07 | 沈阳药科大学 | Hydrochloric ambroxol osmotic pump type controlled release formulation and its preparation method |
-
2003
- 2003-09-08 CN CNB031442501A patent/CN1298318C/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1385151A (en) * | 2002-05-16 | 2002-12-18 | 中国人民解放军第二军医大学 | Slow-released dosage form of sodium ferulate and preparation process thereof |
| CN1415287A (en) * | 2002-11-28 | 2003-05-07 | 沈阳药科大学 | Hydrochloric ambroxol osmotic pump type controlled release formulation and its preparation method |
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| Publication number | Publication date |
|---|---|
| CN1522693A (en) | 2004-08-25 |
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