CN103565776A - Stable lurasidone capsule pharmaceutical composition - Google Patents
Stable lurasidone capsule pharmaceutical composition Download PDFInfo
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- CN103565776A CN103565776A CN201210258269.0A CN201210258269A CN103565776A CN 103565776 A CN103565776 A CN 103565776A CN 201210258269 A CN201210258269 A CN 201210258269A CN 103565776 A CN103565776 A CN 103565776A
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- lurasidone
- lactose
- magnesium stearate
- sodium carboxymethyl
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Abstract
The invention discloses a lurasidone capsule pharmaceutical composition and a preparation method thereof. The lurasidone capsule pharmaceutical composition is characterized in that a formula for preparing 1000 pills comprises 1-6 g of lurasidone, 40-240 g of lactose (Meggle C80), 10-60 g of microcrystalline cellulose (JRS 12), 5-30 g of cross-linked sodium carboxymethyl cellulose and 0.2-1.2 g of magnesium stearate. The invention also relates to a preparation method for the lurasidone capsule pharmaceutical composition. The method includes drying raw materials and auxiliary materials respectively at 80 DEG C for 3 h, mixing uniformly according to an equal proportion, and filling capsules. The lurasidone capsule prepared by the formula and the preparation method has good fluidity, good dissolution rate, small filling-amount difference, high biological utilization rate and good curative effects.
Description
Technical field
The present invention relates to technical field of medicine, relate in particular to pharmaceutical composition comprising as the Lurasidone of active component and preparation method thereof.
Background technology
Lurasidone is applicable to treat adult's schizophrenia.Lurasidone is an atypical antipsychotic, i.e. 5-HT2/D2 dual antagonist.Lurasidone not only can effectively be treated the schizophrenia positive symptom (hallucination, vain hope, behavior are strange), reduce the generation of EPS simultaneously, and can improve negative symptoms of schizophrenia (emotion and language are flat, social withdrawal and lack attention).
Existing patent has only proposed the good medical usage of Lurasidone, and the formula that does not propose Lurasidone medical composition forms and preparation method.Suitable preparation method and process conditions, the selection of filler and disintegrating agent kind and consumption, and the result of extraction of the paired pharmaceutical composition of suitable groups of filler and disintegrating agent, mobility, content uniformity is most important.
How dissolution adjustment formula and the technique adjustment by described Lurasidone obtains better dissolution rate, how by suitable process, to improve its mobility, content uniformity, how to select suitable process conditions to make Lurasidone pharmaceutical composition there are good long-time stability, prior art does not all provide further prompting, in view of this, special proposition the present invention.
Summary of the invention
The present invention is intended to overcome the problems such as existing conventional capsule formulation flows is bad, content uniformity is obvious, has changed the large shortcoming of the little content uniformity of Lurasidone specification, has improved curative effect, and the good fluidity of the Lurasidone capsule providing, and content uniformity is little.According to existing adjuvant and working condition, guaranteeing to have lower production cost and simple preparation technology, be suitable under the prerequisite of large-scale industrial production, be necessary to work out a kind of suitable prescription and form and preparation technology, made Lurasidone there is good bioavailability.
Therefore, the object of the present invention is to provide a kind of Lurasidone capsule, it is characterized in that, the formula of making 1000 is composed as follows:
Lurasidone 1-6g
Lactose (Meggle C80) 40-240g
Microcrystalline Cellulose (JRS 12) 10-60g
Cross-linking sodium carboxymethyl cellulose 5-30g
Magnesium stearate 0.2-1.2g
preferably, it is composed as follows that Lurasidone capsule of the present invention is made the formula of 1000:
Lurasidone 6g
Lactose (Meggle C80) 240g
Microcrystalline Cellulose (JRS 12) 60g
Cross-linking sodium carboxymethyl cellulose 30g
Magnesium stearate 1.2g
Preferred, it is composed as follows that Lurasidone capsule of the present invention is made the formula of 1000:
Lurasidone 4g
Lactose (Meggle C80) 160g
Microcrystalline Cellulose (JRS 12) 400g
Cross-linking sodium carboxymethyl cellulose 20g
Magnesium stearate 0.8g
Another object of the present invention also comprises the preparation method of Lurasidone pharmaceutical composition, it is characterized in that described preparation method comprises the steps:
1) Lurasidone, lactose, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, magnesium stearate are dried to 3 hours under 80 ℃ of conditions.
2) according to recipe quantity, through the double Lurasidone that takes recipe quantity, lactose, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, the magnesium stearate checked.
3) Lurasidone is mixed homogeneously in the equivalent mode of progressively increasing with other adjuvants.
4) measure granule drug content.
5) according to content, adjust loading amount, capsule fill, obtains.
Below by conceptual design and formulation optimization and test data explanation the present invention:
The present invention determines that by prescription screening the assembly of lactose and microcrystalline Cellulose applies, and prepared Lurasidone capsule dissolubility is better, and content uniformity is little, and determines optimizing prescriptions of the present invention through adjuvant screening test.Prescription screening is tested and be the results are shown in down:
| Prescription number | 1 | 2 | 3 | 4 |
| Lurasidone | 6g | 6g | 6g | 6g |
| Lactose | 240g | 60g | 120g | 240g |
| Microcrystalline Cellulose | 60g | 240g | 120g | 60g |
| Cross-linking sodium carboxymethyl cellulose | 30g | 30g | 30g | 0g |
| Magnesium stearate | 1.2g | 1.2g | 1.2g | 0g |
| Make | 1000 | 1000 | 1000 | 1000 |
| Content uniformity | 2.4 | 8.2 | 5.4 | 2.8 |
| Stripping 5min(%) | 82.7 | 80.4 | 76.8 | 68.5 |
| Stripping 10min(%) | 99.0 | 98.8 | 95.6 | 90.2 |
| Stripping 30min(%) | 100.0 | 99.8 | 99.5 | 99.5 |
From above result of the test: 1 content uniformity or stripping trend is all better than other prescription no matter of writing out a prescription.
Lurasidone capsule of the present invention is a kind of medicine.The present invention take that content uniformity is little, the lactose of good fluidity, microcrystalline Cellulose are disintegrating agent as filler, cross-linking sodium carboxymethyl cellulose; Lubricant is magnesium stearate.Make Lurasidone capsule, have following advantage:
1) can cover the abnormal smells from the patient of the former medicine of Lurasidone: because medicine is wrapped in capsule, therefore can cover bitterness and the foul smell of medicine;
2) can improve the stability of Lurasidone: because medicine is wrapped in capsule, therefore can completely cut off contacting of medicine and light, air and dampness, raising medicine stability;
3) higher than tablet bioavailability, be equal to injection bioavailability: because excipient is not generally added in the preparation of capsule, also plus-pressure not, therefore in gastrointestinal, compared with pill, tablet, disperse fast, good absorbing;
4) preparation method of Lurasidone capsule provided by the present invention, not only well overcome the degradation problem that heating causes Lurasidone, and adopted that the method prepared Lurasidone capsule good fluidity, dissolution are good, content uniformity is not obvious.
Accompanying drawing explanation
Fig. 1 is preparation technology's flow chart of product Lurasidone capsule of the present invention.
The specific embodiment
Below in conjunction with embodiment, the present invention is described in further detail, but should understands the non-scope that only limits to these embodiment of scope of the present invention.
embodiment 1
Lurasidone 6g
Lactose (Meggle C80) 240g
Microcrystalline Cellulose (JRS 12) 60g
Cross-linking sodium carboxymethyl cellulose 30g
Magnesium stearate 1.2g
Preparation method comprises the steps:
1) Lurasidone, lactose, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, magnesium stearate are dried to 3 hours under 80 ℃ of conditions.
2) according to recipe quantity, through the double Lurasidone that takes recipe quantity, lactose, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, the magnesium stearate checked.
3) Lurasidone is mixed homogeneously in the equivalent mode of progressively increasing with other adjuvants.
4) measure granule drug content.
5) according to content, adjust loading amount, capsule fill, obtains.
embodiment 2
Lurasidone 4g
Lactose (Meggle C80) 160g
Microcrystalline Cellulose (JRS 12) 40g
Cross-linking sodium carboxymethyl cellulose 20g
Magnesium stearate 0.8g
Preparation method is with embodiment 1.
embodiment 3
Lurasidone 2g
Lactose (Meggle C80) 80g
Microcrystalline Cellulose (JRS 12) 20g
Cross-linking sodium carboxymethyl cellulose 10g
Magnesium stearate 0.4g
Preparation method is with embodiment 1.
embodiment 4
Lurasidone 1g
Lactose (Meggle C80) 40g
Microcrystalline Cellulose (JRS 12) 10g
Cross-linking sodium carboxymethyl cellulose 5g
Magnesium stearate 0.2g
Preparation method is with embodiment 1.
Claims (4)
1. a stable Lurasidone pharmaceutical capsules compositions, is characterized in that, the formula of making 1000 is composed as follows:
Lurasidone 1-6g
Lactose (Meggle C80) 40-240g
Microcrystalline Cellulose (JRS 12) 10-60g
Cross-linking sodium carboxymethyl cellulose 5-30g
Magnesium stearate 0.2-1.2g.
2. Lurasidone pharmaceutical capsules compositions according to claim 1, is characterized in that, the formula of making 1000 is composed as follows:
Lurasidone 6g
Lactose (Meggle C80) 240g
Microcrystalline Cellulose (JRS 12) 60g
Cross-linking sodium carboxymethyl cellulose 30g
Magnesium stearate 1.2g.
3. Lurasidone pharmaceutical capsules compositions according to claim 1, is characterized in that, the formula of making 1000 is composed as follows:
Lurasidone 4g
Lactose (Meggle C80) 160g
Microcrystalline Cellulose (JRS 12) 400g
Cross-linking sodium carboxymethyl cellulose 20g
Magnesium stearate 0.8g.
4. according to the preparation method of a kind of stable Lurasidone pharmaceutical capsules compositions described in claim 1 or 2 or 3, it is characterized in that process following steps:
1) Lurasidone, lactose, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, magnesium stearate are dried to 3 hours under 80 ℃ of conditions;
2) according to recipe quantity, through the double Lurasidone that takes recipe quantity, lactose, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, the magnesium stearate checked;
3) Lurasidone is mixed homogeneously in the equivalent mode of progressively increasing with other adjuvants;
4) measure granule drug content;
5) according to content, adjust loading amount, capsule fill, obtains.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210258269.0A CN103565776A (en) | 2012-07-25 | 2012-07-25 | Stable lurasidone capsule pharmaceutical composition |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210258269.0A CN103565776A (en) | 2012-07-25 | 2012-07-25 | Stable lurasidone capsule pharmaceutical composition |
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| CN103565776A true CN103565776A (en) | 2014-02-12 |
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| CN201210258269.0A Pending CN103565776A (en) | 2012-07-25 | 2012-07-25 | Stable lurasidone capsule pharmaceutical composition |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107875122A (en) * | 2017-12-17 | 2018-04-06 | 佛山市弘泰药物研发有限公司 | A kind of Lurasidone HCl self-micro emulsion formulation and preparation method thereof |
| CN107998105A (en) * | 2017-12-19 | 2018-05-08 | 佛山市弘泰药物研发有限公司 | A kind of Lurasidone HCl spansule and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012063513A1 (en) * | 2010-11-08 | 2012-05-18 | Dainippon Sumitomo Pharma Co., Ltd. | Method of treatment for mental disorders |
-
2012
- 2012-07-25 CN CN201210258269.0A patent/CN103565776A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012063513A1 (en) * | 2010-11-08 | 2012-05-18 | Dainippon Sumitomo Pharma Co., Ltd. | Method of treatment for mental disorders |
Non-Patent Citations (1)
| Title |
|---|
| 崔福德: "《药剂学》", 31 July 2003, 人民卫生出版社 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107875122A (en) * | 2017-12-17 | 2018-04-06 | 佛山市弘泰药物研发有限公司 | A kind of Lurasidone HCl self-micro emulsion formulation and preparation method thereof |
| CN107998105A (en) * | 2017-12-19 | 2018-05-08 | 佛山市弘泰药物研发有限公司 | A kind of Lurasidone HCl spansule and preparation method thereof |
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Application publication date: 20140212 |