CN101224210A - Mizolastine sustained release capsule - Google Patents
Mizolastine sustained release capsule Download PDFInfo
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- CN101224210A CN101224210A CNA2007101950904A CN200710195090A CN101224210A CN 101224210 A CN101224210 A CN 101224210A CN A2007101950904 A CNA2007101950904 A CN A2007101950904A CN 200710195090 A CN200710195090 A CN 200710195090A CN 101224210 A CN101224210 A CN 101224210A
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- mizolastine
- slow releasing
- releasing capsule
- acrylic resin
- capsule
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Abstract
A mizolastine sustained release capsule consists of 4-6wt percent of mizolastine, 60-90wt percent of excipient, 4-10wt percent of film coating material, 0-10wt percent of wetting agent, stabilizer and 1-2wt percent of adhesive. The preparation method comprises: (1) extrusion and rounding method, (2) powder coating method and (3) liquid phase deposition method. The invention has the advantage that the mizolastine sustained release capsule can release drugs in 12-24hours and control the release of the drugs effectively and has good safety and effect; the small pill capsule has wide spreading area in the gastrointestinal tract, high bioavailability and insignificant irritation; a blood drug concentration can quickly reach the medical treatment concentration and remain at an effective concentration stably in a long time with small fluctuation; the invention is beneficial for reducing toxic and side effect of the medicine and the pill taking times by patients and has stable quality.
Description
(1) technical field:
The present invention relates to a kind of slow releasing capsule, particularly a kind of mizolastine slow releasing capsule.
(2) background technology:
Mizolastine (Mizolastione) is a second filial generation antihistaminic, stronger antihistamine effect is not only arranged, and has an effect that suppresses other inflammation mediators, as suppress the generation of leukotriene, alleviate edema etc., thereby, theoretically, mizolastine had both had antihistamine, anti-allergic effects, and the anti-inflammatory activity effect is arranged again, was the preferred medicine of the treatment of acute urticaria.At present, mizolastine general formulation drug release can not effectively be controlled its dosage, and safety, effectiveness are relatively poor, and therefore, invention can reduce the mizolastine slow releasing capsule of medication accumulated dose, reduces patient's medicining times and is necessary.
(3) summary of the invention:
The object of the present invention is to provide a kind of mizolastine slow releasing capsule, it can overcome present mizolastine general formulation release amount of medicine can not effectively control, and causes safety, the relatively poor shortcoming of effectiveness, and can reduce medication accumulated dose and good effect.
Technical scheme of the present invention: a kind of mizolastine slow releasing capsule, it is characterized in that it is a kind of pilule with slow releasing function, it is made up of mizolastine, excipient, thin film coating material, wetting agent, stabilizing agent and binding agent, wherein each component by weight mizolastine be 4～6%, excipient is 60～90%, thin film coating material is 4～10%, and wetting agent is 0～10% and binding agent 1～2%.
Excipient in the component of above-mentioned said mizolastine slow releasing capsule is the one or more combination in cellulose family, starch, lactose and the calcium bicarbonate.
Cellulose family in the above-mentioned said excipient is ethyl cellulose, hydroxypropyl emthylcellulose, microcrystalline Cellulose, acrylic resin I, acrylic resin II, acrylic resin III or acrylic resin IV.
Thin film coating material in the component of above-mentioned said mizolastine slow releasing capsule is one or both combinations in Aquacoat and the acrylic resin aqueous dispersion.
Wetting agent in the component of above-mentioned said mizolastine slow releasing capsule is one or both solution that are mixed in proportion in water or the ethanol.
Binding agent in the component of above-mentioned said mizolastine slow releasing capsule is the one or more combination in cellulose family, resinae, saccharide, the animal acid.
Water or alcoholic solution that above-mentioned said cellulose family binding agent is hydroxypropyl emthylcellulose, ethyl cellulose.
Above-mentioned said resinae binding agent is acrylic resin I, acrylic resin II, acrylic resin III or acrylic resin IV.
Above-mentioned said saccharide binding agent is a maltose.
Above-mentioned said animal acid is gelatin.
The preparation technology of above-mentioned said mizolastine slow releasing capsule, it adopts following several technologies to prepare:
(1) extrude spheronization: utilize and to extrude round as a ball comminutor, crude drug and mixed with excipients are crossed 80 eye mesh screens, extrude the round as a ball ball of making after with adhesive mixed powder being squirted in extruding round as a ball comminutor, sieving after the drying obtains the pastille micropill that certain order is counted size.In the fluidized bed coating pot, carry out coating promptly with Aquacoat;
(2) powder coating method: utilize atresia coating pan, Corm Eleocharitis type coating pan, fluid bed top spray (or end spray) coating machine, fluid bed tangent line spray ball mechanism ball.With Corm Eleocharitis type coating pan is example: medicated powder and mixed with excipients are crossed 80 eye mesh screens, get the micropill (sucrose ball or microcrystalline Cellulose ball) of certain order number and put into Corm Eleocharitis type coating pan, after with adhesive the micropill surface being squirted the mixed with little amount powder is sprinkled in the pot, make mixed powder be wrapped in the surface of micropill uniformly, and then squirt the micropill surface and add powder again, all add until mixed powder, sieving after the drying obtains the pastille micropill that certain order is counted size.In the fluidized bed coating pot, carry out coating promptly with Aquacoat;
(3) liquid phase deposition: can utilize atresia coating pan, Corm Eleocharitis type coating pan, fluid bed top spray (or end spray) coating machine, fluid bed tangent line spray ball mechanism ball.With Corm Eleocharitis type coating pan is example: the micropill (sucrose ball or microcrystalline Cellulose ball) of getting certain order number is put into Corm Eleocharitis type coating pan, medicated powder and excipient is molten in adhesive, mixed liquor is sprayed onto the Surface Edge spray limit drying of micropill, all sprayed until mixed liquor, sieving after the drying obtains the pastille micropill that certain order is counted size.In the fluidized bed coating pot, carry out coating promptly with Aquacoat.
Clinical case analysis of the present invention: this medicine once was widely used in clinical, obtain safety preferably, efficiency evaluation, because of the mizolastine slow releasing capsule is that pilule is big at the gastrointestinal tract distribution area, the bioavailability height, so zest is little, be subjected to digestive tract to carry the food rhythm and pace of moving things to influence little (close as pylorus etc.), can make blood drug level reach curative effect concentration rapidly, and keep steadily, valid density for a long time, blood concentration fluctuation is little, help reducing the toxic and side effects of medicine, below adopt several routine typical clinical cases to analyze:
Case 1: the patient * * *, the man, 34 years old, extremity, waist and the facial limitation welt that takes place, the increase of scratching, number increases, and suffers from urticaria after diagnosing, takes the mizolastine slow releasing capsule under doctor's suggestion, medication is the minimizing of welt quantity after 3 hours, the pruritus degree alleviates, and drug effect can reach 12 hours, recovery from illness after five days.Explanation thus: mizolastine slow releasing capsule dosage is little, and toxic and side effects is little, and safety, effectiveness are better.
Clinical case 2: the patient * * *, the woman, 27 years old, suffer from allergic rhinitis, under doctor's suggestion, use the mizolastine slow releasing capsule, take twice every day, the nasal obstruction symptom is alleviated rapidly to some extent, and only treatment in a few days is almost recovered.Explanation thus: characteristics such as mizolastine slow releasing capsule drug effect is fast, and effect is lasting, and toxic and side effects is little.
Clinical case 3: the patient * * *, the woman, 17 years old, suffer from contact dermatitis after diagnosing, under doctor's suggestion, begin to take the mizolastine slow releasing capsule, the dermatitis symptom is alleviated to some extent after 4 hours, thoroughly recovery from illness after six days.Explanation thus: the mizolastine slow releasing capsule is rapid-action, and dosage is few, taking convenience, and toxic and side effects is little.
Clinical case 4: the patient * * *, the man 46 years old, suffers from chronic eczema after diagnosing, begin to take the mizolastine slow releasing capsule under doctor's suggestion, the pruritus degree alleviated in 2 hours, sustainable 12 hours of drug effect, dosage is little, reduces the toxic and side effects of medicine, obviously improves through treatment patient symptom.
Superiority of the present invention and technique effect are: (1) mizolastine slow releasing capsule has the slow-release function of 12 hours or 24 hours, therefore can effectively control the burst size of medicine, and safety, effectiveness are better; (2) the mizolastine slow releasing capsule is that pilule is big at the gastrointestinal tract distribution area, the bioavailability height, and zest is little; (3), be subjected to digestive tract to carry the food rhythm and pace of moving things to influence little (close as pylorus etc.) because particle diameter is little; (4) the mizolastine controlled release micro pill can make blood drug level reach curative effect concentration rapidly, and keeps steady, long valid density, and blood concentration fluctuation is little; (5) good fluidity of micropill, size evenly are easy to handle (as coating, divided dose); (6) the mizolastine slow releasing capsule helps reducing the toxic and side effects of medicine; (7) the mizolastine slow releasing capsule dosage form more common than this medicine reduced the accumulated dose of medication, reduced patient's medicining times; (8) new prescription, steady quality have been adopted; (9) can adopt framing structure, film control structure or skeleton blooming control structure in the preparation process of mizolastine slow releasing capsule.
(4) specific embodiment:
Embodiment 1: a kind of mizolastine slow releasing capsule is characterized in that it is made up of 4% mizolastine, 80% excipient, 5% thin film coating material, 9% wetting agent and 2% binding agent.
Wherein excipient is a microcrystalline Cellulose, and thin film coating material is an Aquacoat, and wetting agent is 75% alcoholic solution, and binding agent is the aqueous solution of hydroxypropyl emthylcellulose.
A kind of mizolastine slow releasing capsule preparation technology, it adopts following technology to prepare:
Spheronization is extruded in utilization: utilize and extrude round as a ball comminutor; crude drug was mixed 80 eye mesh screens with microcrystalline Cellulose; extrude the round as a ball ball of making after in extruding round as a ball comminutor, mixed powder being squirted with the aqueous solution of hydroxypropyl emthylcellulose; sieving after the drying obtains the pastille micropill that certain order is counted size, carries out coating promptly with Aquacoat in the fluidized bed coating pot.
Embodiment 2: a kind of mizolastine slow releasing capsule is characterized in that it is made up of 6% mizolastine, 72% excipient, 10% thin film coating material, 10% wetting agent and 2% binding agent.
Wherein excipient is a starch, and thin film coating material is an Aquacoat, and wetting agent is an aqueous solution, and binding agent is the alcoholic solution of polyvinylpyrrolidone.
A kind of mizolastine slow releasing capsule preparation technology, it adopts following technology to prepare:
Powder coating method: utilize atresia coating pan, Corm Eleocharitis type coating pan, fluid bed top spray (or end spray) coating machine, fluid bed tangent line spray pellet processing machine to make ball.With Corm Eleocharitis type coating pan is example: medicated powder was mixed 80 eye mesh screens with starch, get the micropill (sucrose ball or microcrystalline Cellulose ball) of 30-35 order number and put into Corm Eleocharitis type coating pan, after with the alcoholic solution of polyvinylpyrrolidone the micropill surface being squirted the mixed with little amount powder is sprinkled in the pot, make mixed powder be wrapped in the surface of micropill uniformly, and then squirt the micropill surface and add powder again, all add until mixed powder, sieving after the drying obtains the pastille micropill that certain order is counted size.In the fluidized bed coating pot, carry out coating promptly with Aquacoat.
Embodiment 3: a kind of mizolastine slow releasing capsule is characterized in that it is made up of 5% mizolastine, 70% excipient, 10% thin film coating material, 12% wetting agent and 3% binding agent.
Wherein excipient is a starch, and thin film coating material is an Aquacoat, and wetting agent is an aqueous solution, and binding agent is the alcoholic solution of hydroxypropyl emthylcellulose.
A kind of mizolastine slow releasing capsule preparation technology, it adopts following technology to prepare:
Liquid phase deposition: can utilize atresia coating pan, Corm Eleocharitis type coating pan, fluid bed top spray (or end spray) coating machine, fluid bed tangent line spray ball mechanism ball.With Corm Eleocharitis type coating pan is example: get certain 30-35 purpose micropill (sucrose ball or microcrystalline Cellulose ball) and put into Corm Eleocharitis type coating pan, medicated powder and excipient is molten in adhesive, mixed liquor is sprayed onto the Surface Edge spray limit drying of micropill, all sprayed until mixed liquor, sieving after the drying obtains the pastille micropill that certain order is counted size.In the fluidized bed coating pot, carry out coating promptly with Aquacoat.
Claims (10)
1. mizolastine slow releasing capsule, it is characterized in that it is a kind of pilule with slow releasing function, it is made up of mizolastine, excipient, thin film coating material, wetting agent, stabilizing agent and binding agent, wherein each component by weight mizolastine be 4～6%, excipient is 60～90%, thin film coating material is 4～10%, and wetting agent is 0～10% and binding agent 1～2%.
2. according to the said a kind of mizolastine slow releasing capsule of claim 1, it is characterized in that excipient in the said mizolastine slow releasing capsule is the one or more combination in cellulose family, starch, lactose and the calcium bicarbonate.
3. according to the said a kind of mizolastine slow releasing capsule of claim 1, it is characterized in that the cellulose family in the said mizolastine slow releasing capsule is ethyl cellulose, hydroxypropyl emthylcellulose, microcrystalline Cellulose, acrylic resin I, acrylic resin II, acrylic resin III or acrylic resin IV.
4. according to the said a kind of mizolastine slow releasing capsule of claim 1, it is characterized in that thin film coating material in the said mizolastine slow releasing capsule is one or both combinations in Aquacoat and the acrylic resin aqueous dispersion.
5. according to the said a kind of mizolastine slow releasing capsule of claim 1, it is characterized in that wetting agent in the said mizolastine slow releasing capsule is one or both solution that are mixed in proportion in water or the ethanol.
6. according to the said a kind of mizolastine slow releasing capsule of claim 1, it is characterized in that binding agent in the said mizolastine slow releasing capsule is the one or more combination in cellulose family, resinae, saccharide, the animal acid.
7. according to the said a kind of mizolastine slow releasing capsule of claim 6, it is characterized in that the cellulose family binding agent in the said mizolastine slow releasing capsule is the water or the alcoholic solution of hydroxypropyl emthylcellulose, ethyl cellulose.
8. according to the said a kind of mizolastine slow releasing capsule of claim 6, it is characterized in that the resinae binding agent in the said mizolastine slow releasing capsule is acrylic resin I, acrylic resin II, acrylic resin III or acrylic resin IV.
9. according to the said a kind of mizolastine slow releasing capsule of claim 6, it is characterized in that the saccharide binding agent in the said mizolastine slow releasing capsule is a maltose.
10. according to the said a kind of mizolastine slow releasing capsule of claim 6, it is characterized in that the animal acid in the said mizolastine slow releasing capsule is gelatin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007101950904A CN101224210A (en) | 2006-12-13 | 2007-12-12 | Mizolastine sustained release capsule |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200610130145 | 2006-12-13 | ||
| CN200610130145.9 | 2006-12-13 | ||
| CNA2007101950904A CN101224210A (en) | 2006-12-13 | 2007-12-12 | Mizolastine sustained release capsule |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101224210A true CN101224210A (en) | 2008-07-23 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2007101950904A Pending CN101224210A (en) | 2006-12-13 | 2007-12-12 | Mizolastine sustained release capsule |
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| CN (1) | CN101224210A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103735534A (en) * | 2013-12-25 | 2014-04-23 | 于运红 | Bilastine sustained-release capsule |
| CN103933017A (en) * | 2014-03-26 | 2014-07-23 | 邵娜 | Progesterone slow-release capsule |
| CN103948570A (en) * | 2014-04-18 | 2014-07-30 | 赵辉 | Exemestane sustained-release capsule |
| CN103948569A (en) * | 2014-04-18 | 2014-07-30 | 赵辉 | Anastrozole sustained-release capsule |
-
2007
- 2007-12-12 CN CNA2007101950904A patent/CN101224210A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103735534A (en) * | 2013-12-25 | 2014-04-23 | 于运红 | Bilastine sustained-release capsule |
| CN103933017A (en) * | 2014-03-26 | 2014-07-23 | 邵娜 | Progesterone slow-release capsule |
| CN103948570A (en) * | 2014-04-18 | 2014-07-30 | 赵辉 | Exemestane sustained-release capsule |
| CN103948569A (en) * | 2014-04-18 | 2014-07-30 | 赵辉 | Anastrozole sustained-release capsule |
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| PB01 | Publication | ||
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Open date: 20080723 |