CN101972230A - Pirfenidone for suspension and preparation method - Google Patents
Pirfenidone for suspension and preparation method Download PDFInfo
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- CN101972230A CN101972230A CN 201010513545 CN201010513545A CN101972230A CN 101972230 A CN101972230 A CN 101972230A CN 201010513545 CN201010513545 CN 201010513545 CN 201010513545 A CN201010513545 A CN 201010513545A CN 101972230 A CN101972230 A CN 101972230A
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- pirfenidone
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Abstract
The invention provides a pirfenidone for suspension and a preparation method thereof, which belong to the technical field of pharmacy and are used for solving the problem of bioavailability of pirfenidone. The product mainly consists of a primary pharmaceutical pirfenidone and auxiliary materials and has the advantages of high pharmaceutical solubility, stable chemical property, good taste, convenient administration and high obedience of patients.
Description
Technical field
The present invention relates to a kind of dry suspension that comprises pirfenidone and preparation method thereof, belong to medical technical field.
Background technology
Pirfenidone (pirfenidone), 5-first class-1-phenyl-2-(1H)-pyridone, molecular formula is C
12H
11NO, molecular weight is 185.22, is the synthetic micromolecular compound seventies in 20th century, many result of the tests confirm that pirfenidone has anti-fibrosis effect.The preparation method of some N-replacement-2-1H-pyridone is disclosed among the USP3839346.Further described the preparation of Compound P irfenidone among USP3947281, USP4042699 and the USP4052509, this chemical compound can reduce the concentration of uric acid and glucose in the blood plasma, is used for people and mammiferous upper respiratory tract infection and skin infection.Pirfenidone can suppress the synthetic of collagen, reduces the generation of various kinds of cell kinetins, the former new hypertrophy of barrier fibers.The extensive use of pirfenidone aspect prevention and treatment fibrotic disease described among USP5310562 and the USP0383591.The prescription that discloses pirfenidone capsule among the WO2007038315 is formed and preparation technology.Pirfenidone is a kind of orally active small-molecule drug, Japan MHLW ratifies this medicine in October, 2008 and is used to treat idiopathic pulmonary fibrosis (IPF), pirfenidone is the medicine of first treatment IPF that gets the Green Light in the whole world, and has obtained the rare medicine of the U.S. and tight tracking relates to and European Orphan Drugs thing design is authorized.
Pirfenidone mainly carries out oral with tablet and capsular form, the administrated method of recommendation is a 200mg, and three times on the one, one after each meal can increase dosage to one time 400mg to 600mg, three times on the one after patient's tolerance gradually.It is reported that the main side effect of this product is phototoxicity and gastrointestinal reaction etc.As seen the dosage of pirfenidone is bigger, and pharmaceutical dosage form is more single, can not expire clinical requirement, is badly in need of the exploitation novel form.
Summary of the invention
The shortcoming of part patient's dysphagia that the specification that the objective of the invention is to overcome existing preparation is too big, volumes of formulation is big and cause, this provide that a kind of good stability, mouthfeel are good, the pirfenidone dry suspension of water solublity and bioavailability height, taking convenience.
Pirfenidone dry suspension among the present invention comprises principal agent pirfenidone and pharmaceutically acceptable other adjuvants, is characterised in that: described principal agent and various adjuvant are counted with unit of weight:
Pirfenidone 150-450 part
Water-soluble filler 440-520 part
Disintegrating agent 55-70 part
Suspending agent 5-10 part
Wherein said water-soluble filler be selected from sorbitol, sucrose,, a kind of or its compositions in the xylitol, mannitol; Described disintegrating agent is selected from one or more the mixture in carboxymethyl starch sodium, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone or the crosslinked carboxymethyl fecula sodium; Selected suspending agent is selected from one or more the compositions in polyvinylpyrrolidone, xanthan gum, the Resina persicae; Described binding agent is selected from the certain density alcoholic solution of ethanol or polyvinylpyrrolidone or hydroxypropyl level methyl fiber.
Water-soluble filler is sorbitol and mannitol more preferably; The preferred crospolyvinylpyrrolidone of disintegrating agent; Suspending agent preferably polyethylene ketopyrrolidine and xanthan gum.
Add the correctives of 5-5.3 unit of weight in the adjuvant recited above, described correctives is selected the compositions of one or more flavorants or edible glucin for use.More preferably fruit essence, A Sipa is sweet and the compositions of cyclamate.
Add the coloring agent of 0.2-0.3 unit of weight in the described adjuvant, coloring agent is selected the compositions of one or more food colorings for use.
The dried suspendible of pirfenidone of the present invention is realized as follows:
A. principal agent, adjuvant mix: the water-soluble filler in will filling a prescription, disintegrating agent, suspending agent are crossed 100 mesh sieves respectively, according to the recipe quantity weighing, and abundant mix homogeneously.
B. add correctives, the coloring agent of recipe quantity again, do not have mix homogeneously with above the mixing.
C. aluminum-plastic composite membrane is packed.
The pirfenidone suspensoid that utilizes the present invention to prepare, because add solubility adjuvant, correctives and sweeting agent, add suspending agent and bonding thickening agent, face with preceding adding suitable quantity of water or add in the suitable fruit juice and take behind the stirring suspendible, mouthfeel is good, taking convenience, patient's compliance are strong, is particularly useful for the old man and and by taking.
The specific embodiment
Embodiment 1
200 parts of pirfenidones
450 parts in mannitol
60 parts in crosslinked carboxymethyl fecula sodium
8 parts of polyvinylpyrrolidones
30 parts of xanthan gum
Hydroxypropyl methylcellulose is an amount of
Purified water is an amount of
Sweet 5.2 parts of aspa
0.25 part of Fructus Citri tangerinae powdered flavor
Preparation technology: 1. principal agent, adjuvant mix: the water-soluble filler in will filling a prescription, disintegrating agent, suspending agent are crossed 100 mesh sieves respectively, according to the recipe quantity weighing, and abundant mix homogeneously.
2. add correctives, coloring agent, binding agent: correctives, the coloring agent of getting recipe quantity stir.
3. add correctives, the coloring agent of recipe quantity again, do not have mix homogeneously with above the mixing.
4. aluminum-plastic composite membrane is packed.
Embodiment 2
400 parts of pirfenidones
200 parts in mannitol
280 parts of xylitol
55 parts of crospolyvinylpyrrolidone
8 parts of polyvinylpyrrolidones
32 parts of xanthan gum
Hydroxypropyl methylcellulose is an amount of
Purified water is an amount of
Sweet 2.5 parts of aspa
3.0 parts of cyclamates
0.35 part of Fructus Citri tangerinae powdered flavor
According to above-mentioned prescription, preparation technology similarly to Example 1 must do suspendible.
Embodiment 3
200 parts of pirfenidones
450 parts in mannitol
32 parts in crosslinked carboxymethyl fecula sodium
28 parts of polyvinylpyrrolidones
14 parts of carrageenans
Sodium carboxymethyl cellulose is an amount of
Purified water is an amount of
Sweet 5.2 parts of aspa
0.15 part of Fructus Citri tangerinae powdered flavor
0.3 part of Fructus Fragariae Ananssae powdered flavor
According to above-mentioned prescription, preparation technology similarly to Example 1 must do suspendible.
Embodiment 4
200 parts of pirfenidones
100 parts of sorbitol
450 parts of xylitol
55 parts of hydroxypropyl methylcellulose
4 parts of microcrystalline Cellulose
Hydroxypropyl methylcellulose is an amount of
Purified water is an amount of
Sweet 2.5 parts of aspa
3.0 parts of cyclamates
0.35 part of Fructus Citri tangerinae powdered flavor
According to above-mentioned prescription, preparation technology similarly to Example 1 gets dry suspension.
Pirfenidone dry suspension settling volume ratio of the present invention, content, study on the stability meet the pertinent regulations of oral suspensions under the Chinese Pharmacopoeia appendix item, specifically see embodiment 5
Embodiment 5
The stability study of dry suspension.
Sample among the embodiment is at 25 ℃, places 12 months and 40 ℃ in the environment of 60% relative humidity, and relative humidity is placement 6 months under 75% the condition, and detection level, related substance and moisture, settling volume prove that than equal no change product is stable.
Claims (5)
1. pirfenidone dry suspension, it mainly comprises principal agent pirfenidone and pharmaceutically acceptable other adjuvants, is characterised in that: described principal agent and various adjuvant are counted with unit of weight:
Pirfenidone 150-450 part
Water-soluble filler 440-520 part
Disintegrating agent 55-70 part
Suspending agent 5-10 part
Wherein said water-soluble filler be selected from sorbitol, sucrose,, a kind of or its compositions in the xylitol, mannitol; Described disintegrating agent is selected from one or more the mixture in carboxymethyl starch sodium, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone or the crosslinked carboxymethyl fecula sodium; Selected suspending agent is selected from one or more the compositions in polyvinylpyrrolidone, xanthan gum, the Resina persicae.
2. the dried suspendible of the described pirfenidone of claim 1 is characterized in that water-soluble filler more preferably sorbitol and mannitol; The preferred crospolyvinylpyrrolidone of disintegrating agent; Suspending agent preferably polyethylene ketopyrrolidine and xanthan gum; Binding agent preferred alcohol solution.
3. the right medicine requires the dried suspendible of 1 described pirfenidone, it is characterized in that adding in the described adjuvant correctives of 5-5.3 unit of weight, and described correctives is selected the compositions of one or more flavorants or edible glucin for use.More preferably fruit essence, A Sipa is sweet and the compositions of cyclamate.
4. the dried suspendible of the described pirfenidone of claim 1 is characterized in that adding in the described adjuvant coloring agent of 0.2-0.3 unit of weight, and coloring agent is selected the compositions of one or more food colorings for use.
5. the described pirfenidone dry suspension of claim 1, its preparation is characterised in that and comprises following steps:
A. principal agent, adjuvant mix: the water-soluble filler in will filling a prescription, disintegrating agent, suspending agent are crossed 100 mesh sieves respectively, according to the recipe quantity weighing, and abundant mix homogeneously.
B. add correctives, the coloring agent of recipe quantity again, with above mixture mix homogeneously.
C. aluminum-plastic composite membrane is packed.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201010513545 CN101972230A (en) | 2010-10-13 | 2010-10-13 | Pirfenidone for suspension and preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201010513545 CN101972230A (en) | 2010-10-13 | 2010-10-13 | Pirfenidone for suspension and preparation method |
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| Publication Number | Publication Date |
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| CN101972230A true CN101972230A (en) | 2011-02-16 |
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| CN 201010513545 Pending CN101972230A (en) | 2010-10-13 | 2010-10-13 | Pirfenidone for suspension and preparation method |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102558040A (en) * | 2011-12-28 | 2012-07-11 | 辰欣药业股份有限公司 | Method for preparing pirfenidone |
| CN102846555A (en) * | 2012-04-09 | 2013-01-02 | 珠海亿邦制药股份有限公司 | Solid preparation comprising pirfenidone as active component and application thereof |
| CN107961226A (en) * | 2016-10-19 | 2018-04-27 | 朱隆娅 | A kind of pirfenidone soft capsule |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1701793A (en) * | 2004-05-24 | 2005-11-30 | 上海睿星基因技术有限公司 | Usage of pirfenidone for treating hepatic injury and necrosis and acute lung injury |
| CN1775212A (en) * | 2004-11-16 | 2006-05-24 | 徐旗开 | Use of pirfenidone for treating psoriasis |
-
2010
- 2010-10-13 CN CN 201010513545 patent/CN101972230A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1701793A (en) * | 2004-05-24 | 2005-11-30 | 上海睿星基因技术有限公司 | Usage of pirfenidone for treating hepatic injury and necrosis and acute lung injury |
| CN1775212A (en) * | 2004-11-16 | 2006-05-24 | 徐旗开 | Use of pirfenidone for treating psoriasis |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102558040A (en) * | 2011-12-28 | 2012-07-11 | 辰欣药业股份有限公司 | Method for preparing pirfenidone |
| CN102846555A (en) * | 2012-04-09 | 2013-01-02 | 珠海亿邦制药股份有限公司 | Solid preparation comprising pirfenidone as active component and application thereof |
| CN107961226A (en) * | 2016-10-19 | 2018-04-27 | 朱隆娅 | A kind of pirfenidone soft capsule |
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Open date: 20110216 |