CN104013594A - Cisapride controlled release tablet and preparation method thereof - Google Patents
Cisapride controlled release tablet and preparation method thereof Download PDFInfo
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- CN104013594A CN104013594A CN201410265797.8A CN201410265797A CN104013594A CN 104013594 A CN104013594 A CN 104013594A CN 201410265797 A CN201410265797 A CN 201410265797A CN 104013594 A CN104013594 A CN 104013594A
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- controlled release
- cisapride
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Abstract
The invention belongs to the technical field of a medicine, and discloses a cisapride controlled release tablet and a preparation method thereof. The cisapride controlled release tablet is used for relieving continuous moderate to severe pain. The novel dosage form is characterized in that the product is represented as a controlled release tablet which can slowly release drugs in water or a specified release medium at a constant speed or nearly at a constant speed.
Description
Invention field
The present invention relates to chemical pharmacy field, be specifically related to a kind of cisapride controlled release tablet and preparation method thereof.
Background of invention
Cisapride, English name Cisapride.A kind of gastrointestinal tract dynamia medicine, can strengthen and coordinate gastrointestinal motility, prevent food entrapment and anti-stream, its mechanism of action is mainly the release that optionally promotes place's acetylcholine after myenteron plexus nervorum joint (in time and quantitatively), thereby strengthens the motion of gastrointestinal; But do not affect submucosal nervous plexus, therefore do not change the secretion of mucosa.
Chinese Pharmacopoeia (version in 2005) has recorded cisapride conventional tablet.The present invention by repetition test, obtains cisapride controlled release tablet of the present invention, safety aspect, and patient feels sick, vomiting, constipation, dizzy and calm incidence rate are all lower, does not surpass 4%.Therefore applicant thinks, short-term or prolonged application cisapride controlled release tablet can effectively be strengthened and coordinate gastrointestinal motility for 5mg/ days, prevents food entrapment and anti-stream, and patient tolerability is better.
Cisapride controlled release tablet provided by the invention, can significantly strengthen and coordinate gastrointestinal motility, prevents food entrapment and anti-stream, and processing technology is simple, and the quality of the pharmaceutical preparations is reliable and stable.
Summary of the invention
The invention provides a kind of new cisapride controlled release tablet, can significantly strengthen and coordinate gastrointestinal motility, prevent food entrapment and anti-stream, processing technology is simple, and the quality of the pharmaceutical preparations is reliable and stable.
On the one hand, the invention provides a kind of cisapride controlled release tablet, wherein, this controlled release tablet is to take the tablet that cisapride makes as principal agent, and every contains cisapride 1mg～10mg.
Some embodiments therein, cisapride controlled release tablet of the present invention, wherein, this controlled release tablet constant speed or approach the release medicine of constant speed lentamente in water or in the release medium of regulation.
Some embodiments therein, cisapride controlled release tablet of the present invention, wherein, the preparation of tablet be not limited to adopt direct compression or granulate after tabletting, this controlled release tablet is comprised of following component:
The prescription of coating solution
Some embodiments therein, cisapride controlled release tablet of the present invention, wherein, described filler is one or more in dextrin, starch, microcrystalline Cellulose or lactose; Plasticizer is one or more in polyethylene, phthalic acid dibutyl ester; Binding agent is 70%pvp ethanol; Solubilizing agent is cellulose acetate; Emulsifying agent is polysorbate-80.
Some embodiments therein, cisapride controlled release tablet of the present invention, wherein, described filler: plasticizer: binding agent: solubilizing agent: emulsifying agent is l:0.02～0.5:0.3～5:0.01～1.5:0.01～0.5.
In other embodiments, cisapride controlled release tablet of the present invention, wherein, the prescription of this controlled release tablet
One of be:
The prescription of coating solution
On the other hand, the invention provides the preparation method of cisapride controlled release tablet of the present invention, it comprises the following steps: get cisapride, and dextrin, polyethylene mixes, and with 70%pvp ethanol, granulates, dry, granulate, tabletting.Get cellulose acetate, polysorbate-80, phthalic acid dibutyl ester is appropriate, with 90% ethanol-acetone mixed solvent 1000ml, dissolves and joins to obtain coating solution.Coating to every coating tablets layer is heavily 8.5～9mg.Product inspection, coating.
Excipient of the present invention comprises, but be not limited to, ion-exchanger, aluminum, aluminium stearate, lecithin, serum albumin, as human albumin, buffer substance is as phosphate, glycine, sorbic acid, potassium sorbate, the partial glycerol ester admixture of saturated vegetable fatty acid, water, salt or electrolyte, as protamine sulfate, sodium hydrogen phosphate, potassium hydrogen phosphate, sodium chloride, zinc salt, colloid silicon, magnesium trisilicate, polyvinylpyrrolidone, polyacrylate, wax, polyethylene-polyoxypropylene-blocking-up polymer, lanoline, sugar, as lactose, dextrose plus saccharose, starch is as corn starch and potato starch, the derivant of cellulose and it is as sodium carboxymethyl cellulose, ethyl cellulose and cellulose acetate, natural gum powder, Fructus Hordei Germinatus, gelatin, Pulvis Talci, adjuvant is as cocoa butter and suppository wax, oily as Oleum Arachidis hypogaeae semen, Oleum Gossypii semen, safflower oil, Oleum Sesami, olive oil, Semen Maydis oil and Oleum Glycines, glycols compound, as propylene glycol and Polyethylene Glycol, esters is as ethyl oleate and ethyl laurate, agar, buffer agent is as magnesium hydroxide and aluminium hydroxide, alginic acid, pyrogen-free water, Deng oozing salt, Lin Ge (family name) solution, ethanol, phosphate buffer solution, and other nontoxic proper lubrication agent are as sodium laurylsulfate and magnesium stearate, coloring agent, releasing agent, coating dress material, sweeting agent, flavoring agent and spice, antiseptic and antioxidant.
Pharmaceutical composition of the present invention can also optionally contain one or more diluent.The example of diluent comprises mannitol, sorbitol, biphosphate calcium dihydrate, microcrystalline Cellulose and efflorescence cellulose.Preferred diluent is microcrystalline Cellulose.Microcrystalline Cellulose can be obtained from several suppliers, comprises Avicel PH101, Avicel PH102, Avicel PH103, AvicelPH105 and Avicel PH200 that FMCCorporation manufactures.
Pharmaceutical composition of the present invention can also optionally contain disintegrating agent.Disintegrating agent can be a kind of in several modified starches, modified cellulose polymer or polycarboxylic acids, such as crosslinked Carboxymethyl cellulose sodium, Explotab, polacrilin potassium and calcium carboxymethylcellulose (CMCCalcium).In one embodiment, disintegrating agent is croscarmellose sodium.Croscarmellose sodium NF type A obtains with trade name " Ac-di-sol " on market.
Pharmaceutical composition of the present invention can also optionally contain one or more surfactants or wetting agent.Surfactant can be anion, cation or neutral surface active agent.Anion surfactant comprises sodium lauryl sulfate, dodecyl sodium sulfate, oleyl sodium sulfate and the sodium laurate mixing with stearate and Talcum.Cationic surfactant comprises benzalkonium chloride and alkyl trimethyl ammonium bromide.Neutral surface active agent comprises glycerol list olein, polyoxyethylene sorbitan fatty acid ester, polyvinyl alcohol and anhydro sorbitol fat.The embodiment of wetting agent comprises poloxamer, polyoxyethylene alkyl ether, castor oil derivatives and polyoxyethylene 8 stearate fat.
The present invention can also optionally join antioxidant in preparation, thereby gives its chemical stability.Antioxidant is selected from the extract of a-tocopherol, Y-tocopherol, S-tocopherol, tocopherol enrichment natural origin, sodium or calcium salt, the Vitamin C acyl cetylate of L-AA and it, amass wealth by heavy taxation propyl propionate, amass wealth by heavy taxation misery ester, amass wealth by heavy taxation sour dodecyl ester, Yoshinox BHT (BHT) and butylated hydroxyanisol (BHA).In one embodiment, antioxidant is BHT or BHA.
The preferred dosage form of drug composition of the present invention is the tablet of preparing by compression method.Described tablet can, with such as the mixture of hydroxypropyl cellulose and hydroxypropyl emthylcellulose is filmed, contain titanium dioxide and/or other coloring agent, such as ferrum oxide, dyestuff and Se Dian in this mixture; The mixture of polyvinyl alcohol (PVA) and Polyethylene Glycol (PEG), contains titanium dioxide and/or other coloring agent, such as ferrum oxide, dyestuff and Se Dian; Or any other suitable instant-free coating agent.Coating provides taste masked and other stability to final tablet.Commercially available film for Colorcon provide for preparation mixture of powders
The present invention can also add sweeting agent and/or fumet.
The specific embodiment
Below in conjunction with embodiment, further explain the present invention, but embodiment does not limit in any form to the present invention.
A kind of cisapride controlled release tablet of the present invention is comprised of following component:
The prescription of coating solution
A kind of cisapride controlled release tablet of the present invention is achieved through the following technical solutions:
Get cisapride, dextrin, polyethylene mixes, with 70./。Pvp ethanol is granulated, dry, granulate, tabletting.Get cellulose acetate, polysorbate-80, phthalic acid dibutyl ester is appropriate, with 90% ethanol-acetone mixed solvent 1000ml, dissolves and joins to obtain coating solution.Coating to every coating tablets layer is heavily 1.0～5mg.Product inspection, coating.
A kind of cisapride controlled release tablet that the present invention obtains has that method is simple, good stability, feature that quality is high.
Embodiment 1: 1000 of specifications
Prescription:
The prescription of coating solution
Method for making:
Get cisapride, dextrin, polyethylene mixes, and with 70%pvp ethanol, granulates, dry, granulate, tabletting.Get cellulose acetate, polysorbate-80, phthalic acid dibutyl ester is appropriate, with 90% ethanol-acetone mixed solvent 1000ml, dissolves and joins to obtain coating solution.Coating to every coating tablets layer is heavily 1.0～5mg.Product inspection, coating.
Embodiment 2:
1000 of specifications
Prescription:
The prescription of coating solution
Method for making:
Get cisapride, dextrin, polyethylene mixes, and with 70%pvp ethanol, granulates, dry, granulate, tabletting.Get cellulose acetate, polysorbate-80, phthalic acid dibutyl ester is appropriate, with 90% ethanol-acetone mixed solvent 1000ml, dissolves and joins to obtain coating solution.Coating to every coating tablets layer is heavily 1～5mg.Product inspection, coating.
Embodiment 3:
1000 of specifications
Prescription:
The prescription of coating solution
Method for making:
Get cisapride, dextrin, polyethylene mixes, and with 70%pvp ethanol, granulates, dry, granulate, tabletting.Get cellulose acetate, polysorbate-80, phthalic acid dibutyl ester is appropriate, with 90% ethanol-acetone mixed solvent 1000ml, dissolves and joins to obtain coating solution.Coating to every coating tablets layer is heavily 1～5mg.Product inspection, coating.
Cisapride controlled release tablet good stability of the present invention, quality is high, evident in efficacy, untoward reaction is little, the cisapride controlled release tablet that application said method makes constant speed or approach the release medicine of constant speed lentamente in water or in the release medium of regulation.
Biological activity test
By preparation technology of the present invention, make sample, the dissolution that this product of take was measured in 40 minutes in phosphate buffered solution (pH7.4) is investigation index, the results are shown in Table 1:
Table 1 cisapride controlled release tablet of the present invention and commercially available mass ratio
By known with commercially available product contrast, after using solubilizing agent, the character of medicine, related substance, content do not have much variations, and the dissolution of medicine obviously raises.Result of the test shows, the quality of product of the present invention is stablized controlled.
Although the present invention describes with reference to specific embodiment, this description not meaning that is construed as limiting the present invention.With reference to description of the invention, other distortion of the disclosed embodiments, all can expect for those skilled in the art.Therefore, such distortion can not depart from scope and the spirit that affiliated claim limits.
Claims (7)
1. a cisapride controlled release tablet, wherein, this controlled release tablet is to take the tablet that cisapride makes as principal agent, every contains cisapride 1mg～10mg.
2. according to the described cisapride controlled release tablet of claim 1, wherein, this controlled release tablet constant speed or approach the release medicine of constant speed lentamente in water or in the release medium of regulation.
3. according to the described cisapride controlled release tablet of claim 1, wherein, the preparation of tablet is not limited to adopt direct compression or the rear tabletting of granulating, and this controlled release tablet is comprised of following component:
The prescription of coating solution
4. according to the described cisapride controlled release tablet of claim 3, wherein, described filler is one or more in dextrin, starch, microcrystalline Cellulose or lactose; Plasticizer is one or more in polyethylene, phthalic acid dibutyl ester; Binding agent is 70%pvp ethanol; Solubilizing agent is cellulose acetate; Emulsifying agent is polysorbate-80.
5. according to the described cisapride controlled release tablet of claim 3, wherein, described filler: plasticizer: binding agent: solubilizing agent: emulsifying agent is 1: 0.02～0.5: 0.3～5: 0.01～1.5: 0.01～0.5.
6. cisapride controlled release tablet according to claim 3, wherein, one of prescription of this controlled release tablet is:
The prescription of coating solution
7. a preparation method for the cisapride controlled release tablet described in claim 1-6 any one, it comprises the following steps: get cisapride, dextrin, polyethylene mixes, and with 70%pvp ethanol, granulates, dry, granulate, tabletting.Get cellulose acetate, polysorbate-80, phthalic acid dibutyl ester is appropriate, with 90% ethanol-acetone mixed solvent 1000ml, dissolves and joins to obtain coating solution.Coating to every coating tablets layer is heavily 8.5～9mg.Product inspection, coating.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201410265797.8A CN104013594A (en) | 2014-06-13 | 2014-06-13 | Cisapride controlled release tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410265797.8A CN104013594A (en) | 2014-06-13 | 2014-06-13 | Cisapride controlled release tablet and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104000795A (en) * | 2014-06-03 | 2014-08-27 | 青岛市市立医院 | Diammonium glycyrrhizinate controlled release tablets and preparation method thereof |
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2014
- 2014-06-13 CN CN201410265797.8A patent/CN104013594A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104000795A (en) * | 2014-06-03 | 2014-08-27 | 青岛市市立医院 | Diammonium glycyrrhizinate controlled release tablets and preparation method thereof |
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