CN106880604A - A kind of oral disnitegration tablet containing penfluridol and preparation method thereof - Google Patents
A kind of oral disnitegration tablet containing penfluridol and preparation method thereof Download PDFInfo
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- CN106880604A CN106880604A CN201510930895.3A CN201510930895A CN106880604A CN 106880604 A CN106880604 A CN 106880604A CN 201510930895 A CN201510930895 A CN 201510930895A CN 106880604 A CN106880604 A CN 106880604A
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- penfluridol
- oral disnitegration
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Biophysics (AREA)
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Abstract
The present invention relates to penfluridol oral disnitegration tablet and preparation method thereof, belong to pharmaceutical technology field.The oral disnitegration tablet contains penfluridol, hydrophilic filler, water-soluble binder, disintegrant, lubricant and flavouring etc., its preparation process is simple, convenient to take, rapid-action, and up to peak morning, curative effect is obvious.
Description
Technical field
The present invention relates to the oral disnitegration tablet that can be disintegrated rapidly and the method for producing the formulation that a kind of active component is penfluridol,
Belong to field of pharmaceutical preparations.
Background technology
Schizophrenia be mainly shown as manic uneasy, bigoted, depressed, phobic anxiety, phonism illusion, it is sensitive it is suspicious, force
Irritability, disturbance in thinking, talk nonsense, disorderly fall thing, impulsion hurt sb.'s feelings, it is off one's feet etc..Patient is likely to occur one when sick
Kind groundless wrong idea, suspects that someone will do harm to him and wait some illusory consciousness, thus it is final pessimistic desperate and commit suiside,
Greatly injury is brought to family, society.Schizophrenia does not have a single cause of disease, possible paathogenic factor include gene (heredity),
Complication during chemical balance imbalance, pregnancy and childbirth etc..
Penfluridol (penfluridol), chemical entitled 1- (4,4- double (4- fluorophenyls) butyl) -4- (the chloro- 3- of 4- (trifluoromethyl)
Phenyl) -4- piperidine alcohols, molecular formula is C28H27ClF5NO, is white or off-white color crystalline powder, and odorless is tasteless, almost
It is water insoluble.This product is oral depot antipsychotics, and antipsycholic action is strong and lasting, orally once can maintain a couple of days extremely
One week, for treating all kinds of schizophrenia, the maintaining treatment of the person that is more suitable for disease amelioration.
Penfluridol oral disnitegration tablet of the invention need not use water delivery service, and saliva can be disintegrated it, mask medicine in itself
Bad smell and bitter taste, improve the compliance of patient's Long-term taking medicine, be particularly suited for the elderly, children and other swallow it is tired
Difficult patient.Oral disnitegration tablet can rapidly be disintegrated before intestines and stomach are reached and be dispersed into fine particle, disperse more equal in the gastrointestinal tract
Even, diffusional area is big, can make the rapid dissolution of medicine, quick to absorb, rapid-action.As can be seen here, antidepression and schizophrenia
The oral disnitegration tablet of medicine is more more advantageous than other formulations.
The A of patent CN 104546784 disclose a kind of penfluridol tablet composition and preparation method thereof, composition disclosed in the document
Prepared coating tablet disintegration time limited is about 16min, patient's medication poor compliance.The A of patent CN 101732311 disclose one kind
Oral formulations containing penfluridol, the formulation included in document has capsule, granule, also poor to patient's Compliance.
The A of patent CN 104586780 disclose a kind of penfluridol oral freeze-dried slices and preparation method thereof, and the freeze-drying tablet described in document reaches
The disintegration time limited of oral disintegrating tablet has been arrived, but, technical sophistication high to production equipment requirement.
The content of the invention
It is an object of the invention to provide the oral disnitegration tablet formulation of penfluridol, the technical complexity that the production of the formulation need not be very high,
This formulation considers penfluridol low-solubility, is fast and efficiently given birth to producing the characteristics of by the rapid disintegration of oral disnitegration tablet
Thing availability, to obtain preferable clinical efficacy.
Penfluridol oral disnitegration tablet of the present invention, the pharmaceutical composition contains 1- (4,4- double (4- fluorophenyls) butyl) as follows
- 4- (4- chloro- 3- (trifluoromethyl) phenyl) -4- piperidine alcohols:
And hydrophilic filler, water-soluble binder, disintegrant, lubricant and flavouring;Wherein bulk drug and hydrophilicity condiment
Micronizing altogether, its ratio is 1:1-1:50(w/w);The disintegration time for using static disintegration time mensuration method to determine is 12-60s,
Preferably 14-45s.
The hydrophilicity condiment being micronized altogether with penfluridol in the present invention includes mannitol, cornstarch, microcrystalline cellulose, lactose
In one kind, its ratio be 1:1-1:50 (w/w), particularly preferred 1:2-1:20(w/w).The grain of penfluridol after being micronized altogether
Footpath is controlled in 1-50 μ ms, preferably in 1-30 μ ms.
The content of active component penfluridol is 2%-20%, preferably 5mg, 10mg, 20mg in the present invention.
Hydrophilic filler in the present invention is in lactose, sucrose, mannitol, microcrystalline cellulose, starch, dextrin, sorbierite
One or more, its consumption be 30%-95%, preferably one or more in lactose, mannitol, microcrystalline cellulose, starch,
The preferred 40%-90% of its consumption.
Water-soluble binder in the present invention is one or more in PVP, hydroxypropyl cellulose, hydroxypropyl methyl cellulose,
Its consumption is 0.2%-10%, preferably 0.5%-5%.
Disintegrant in the present invention is Ac-Di-Sol, PVPP, low-substituted hydroxypropyl cellulose, carboxymethyl form sediment
One or more in powder sodium, its consumption is 2%-50%, preferably 5%-40%.
Lubricant in the present invention for the one kind in silica, talcum powder, magnesium stearate, stearic acid, sodium stearyl fumarate or
Various, its consumption is 0.1%-5%, preferably 0.2%-1%.
Flavouring in the present invention is one or more in acesulfame potassium, Aspartame, menthol, Sucralose, essence class,
Its consumption is 0.1%-10%, preferably 0.5%-5%.
Penfluridol oral disnitegration tablet of the present invention, its piece weight 80-300mg, preferably 100-260mg;Hardness 2-7kgf,
Preferably 3-5kgf.
The advantage of the invention is that:
1) penfluridol oral disnitegration tablet of the invention, in preparation process, in penfluridol bulk drug and hydrophilic filler one
Kind or it is various carry out common micronizing, due to the hydrophilic nmature of filler, penfluridol with its altogether micronizing after enhance bulk drug
Dissolubility, and micronization technology effect in itself, also enhance the dissolubility of bulk drug simultaneously, improve penfluridol raw material
The property of medicine indissoluble.
2) it is 12-60s that penfluridol oral disnitegration tablet of the invention uses the disintegration time that static disintegration time mensuration method is determined,
Preferably 14-45s.Disintegration is rapid, has exceeded the disintegration time limited of oral disnitegration tablet in the prior art, for Clinical practice provide it is fast
The penfluridol oral disnitegration tablet of speed disintegration.
3) penfluridol oral disnitegration tablet of the invention need not use water delivery service, and saliva can be disintegrated it, mask medicine in itself
Bad smell and bitter taste, improve the compliance of patient's Long-term taking medicine, be particularly suited for the elderly, children and other swallow
Difficult patient.Oral disnitegration tablet can rapidly be disintegrated before intestines and stomach are reached and be dispersed into fine particle, disperse in the gastrointestinal tract more
Uniformly, diffusional area is big, can make the rapid dissolution of medicine, quick to absorb, rapid-action.As antidepression and schizophrenia drug
Oral disnitegration tablet it is more more advantageous than other formulations.
Specific embodiment
Further present disclosure is described in further detail with embodiment below.But this should not be interpreted as this hair
It is bright to be limited by specific embodiment.All technologies realized based on the above of the invention belong to the scope of the present invention.
Embodiment 1
Preparation technology:
(1) penfluridol and mannitol are total to micronization processes in proportion;
(2) penfluridol of recipe quantity is well mixed with mannitol, microcrystalline cellulose, sodium carboxymethyl starch in blender;
(3) to the wet softwood of hydroxypropylcellulose aqueous solution system that 4% is added in said mixture, granulation;
(4) above-mentioned particle drying converts the use of additional magnesium stearate, Mint Essence and Aspartame to moisture < 3% after whole grain
Amount, is well mixed with dried particle;
(5) total mixed rear granule content is determined, piece weight is converted, hardness 3-5kgf compressing tablets are controlled.It is prepared into 1000.
Embodiment 2
Preparation technology:
(1) penfluridol and mannitol are total to micronization processes in proportion;
(2) penfluridol of recipe quantity is well mixed with mannitol, microcrystalline cellulose, sodium carboxymethyl starch in blender;
(3) to the wet softwood of hydroxypropylcellulose aqueous solution system that 4% is added in said mixture, granulation;
(4) above-mentioned particle drying converts the use of additional magnesium stearate, Mint Essence and Aspartame to moisture < 3% after whole grain
Amount, is well mixed with dried particle;
(5) total mixed rear granule content is determined, piece weight is converted, hardness 3-5kgf compressing tablets are controlled.It is prepared into 1000.
Embodiment 3
Preparation technology:
(1) penfluridol and mannitol are total to micronization processes in proportion;
(2) penfluridol of recipe quantity is well mixed with mannitol, microcrystalline cellulose, sodium carboxymethyl starch in blender;
(3) to the wet softwood of hydroxypropylcellulose aqueous solution system that 4% is added in said mixture, granulation;
(4) above-mentioned particle drying converts the use of additional magnesium stearate, Mint Essence and Aspartame to moisture < 3% after whole grain
Amount, is well mixed with dried particle;
(5) total mixed rear granule content is determined, piece weight is converted, hardness 3-5kgf compressing tablets are controlled.It is prepared into 1000.
Embodiment 4
Preparation technology:
(1) penfluridol and mannitol are total to micronization processes in proportion;
(2) penfluridol of recipe quantity is well mixed with mannitol, microcrystalline cellulose, sodium carboxymethyl starch in blender;
(3) to the wet softwood of hydroxypropylcellulose aqueous solution system that 4% is added in said mixture, granulation;
(4) above-mentioned particle drying converts the use of additional magnesium stearate, Mint Essence and Aspartame to moisture < 3% after whole grain
Amount, is well mixed with dried particle;
(5) total mixed rear granule content is determined, piece weight is converted, hardness 3-5kgf compressing tablets are controlled.It is prepared into 1000.
Embodiment 5
Preparation technology:
(1) penfluridol and mannitol are total to micronization processes in proportion;
(2) penfluridol of recipe quantity is well mixed with mannitol, microcrystalline cellulose, sodium carboxymethyl starch in blender;
(3) to the wet softwood of hydroxypropylcellulose aqueous solution system that 4% is added in said mixture, granulation;
(4) above-mentioned particle drying converts the use of additional magnesium stearate, Mint Essence and Aspartame to moisture < 3% after whole grain
Amount, is well mixed with dried particle;
(5) total mixed rear granule content is determined, piece weight is converted, hardness 3-5kgf compressing tablets are controlled.It is prepared into 1000.
Embodiment 6
Preparation technology:
(1) penfluridol and lactose are total to micronization processes in proportion;
(2) penfluridol of recipe quantity is well mixed with lactose, microcrystalline cellulose, sodium carboxymethyl starch in blender;
(3) to the wet softwood of hydroxypropylcellulose aqueous solution system that 4% is added in said mixture, granulation;
(4) above-mentioned particle drying converts the use of additional magnesium stearate, Mint Essence and Aspartame to moisture < 3% after whole grain
Amount, is well mixed with dried particle;
(5) total mixed rear granule content is determined, piece weight is converted, hardness 3-5kgf compressing tablets are controlled.It is prepared into 1000.
Embodiment 7
Preparation technology:
(1) penfluridol and lactose are total to micronization processes in proportion;
(2) penfluridol of recipe quantity is well mixed with lactose, microcrystalline cellulose, sodium carboxymethyl starch in blender;
(3) to the wet softwood of hydroxypropylcellulose aqueous solution system that 4% is added in said mixture, granulation;
(4) above-mentioned particle drying converts the consumption of additional magnesium stearate, Mint Essence and acesulfame potassium to moisture < 3% after whole grain,
It is well mixed with dried particle;
(5) total mixed rear granule content is determined, piece weight is converted, hardness 3-5kgf compressing tablets are controlled.It is prepared into 1000.
2nd, quality assessment method
The disintegration time limited of oral disnitegration tablet checks
Take 2mL water (37 DEG C) to be placed in 5mL test tubes, add penfluridol oral disintegrating tablet, start timing, opened to complete disintegration
Into independent fine particle, stop, recording disintegration time, test tube should not be moved in disintegrating procedue, 6 are taken every time and is detected,
Take its average value.
Tablet friability is checked
According to《Chinese Pharmacopoeia》Method is detected that calculating subtracts under " tablet friability inspection technique " item in 2015 editions four 0923
Weight loss (%), and seen whether the abnormal conditions such as fracture, cracking and/or crushing.
Orally disintegrating is tested and mouthfeel inspection
Healthy volunteer 6 is chosen, oral disnitegration tablet is placed in and is started timing on lingual surface, stopped to during complete disintegration in the oral cavity
Timing, records disintegration time, and oneself is placed in mouth the intraoral sensation to after being disintegrated completely to experience slice, thin piece.
The penfluridol oral disnitegration tablet experimental result of table 1
3rd, evaluation result
Can be disintegrated rapidly using prescription of the present invention and the penfluridol oral disnitegration tablet of preparation by being known with upper table, sample hardness is closed
Lattice, it is in good taste, without obvious sand type, and special production equipment is not needed, with low production cost, carry, store, transport
It is defeated and take convenient feature, patient's drug compliance is improve, with actual application value higher.
Claims (10)
1. a kind of penfluridol oral disnitegration tablet, it is characterised in that contain penfluridol as follows in the oral disnitegration tablet:
Wherein also include hydrophilic filler, water-soluble binder, disintegrant, lubricant and flavouring.
2. penfluridol oral disnitegration tablet according to claim 1, it is characterised in that the content of penfluridol is 2%-20%.
3. penfluridol oral disnitegration tablet according to claim 1, it is characterised in that described hydrophilic filler is breast
One or more in sugar, sucrose, mannitol, microcrystalline cellulose, starch, dextrin, sorbierite;The hydrophilic filler
Consumption is 30%-95%;Preferably, the hydrophilic filler consumption is 40%-90%.
4. penfluridol oral disnitegration tablet according to claim 1, it is characterised in that described water-soluble binder is poly-
One or more in dimension ketone, hydroxypropyl cellulose, hydroxypropyl methyl cellulose;The water-soluble binder consumption is 0.2%-10%;
Preferably, the water-soluble binder consumption is 0.5%-5%.
5. penfluridol oral disnitegration tablet according to claim 1, it is characterised in that described disintegrant is crosslinking carboxylic first
One or more in base sodium cellulosate, PVPP, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch;The disintegrant
Consumption is 2%-50%;Preferably, the disintegrant consumption is 5%-40%.
6. penfluridol oral disnitegration tablet according to claim 1, it is characterised in that described lubricant be silica,
One or more in talcum powder, magnesium stearate, stearic acid, sodium stearyl fumarate;The lubricant quantity is 0.1%-5%;
Preferably, the lubricant quantity is 0.2%-1%.
7. penfluridol oral disnitegration tablet according to claim 1, it is characterised in that preparation prescription is:
8. the preparation method of the penfluridol oral disnitegration tablet described in claim 1, comprises the following steps:
(1) one or more in penfluridol and hydrophilic filler is carried out into common micronizing;
(2) penfluridol, hydrophilic filler, disintegrant are well mixed;
(3) to the wet softwood of aqueous solution system that water-soluble binder is added in said mixture, granulation;
(4) above-mentioned particle drying, whole grain, additional lubricant, flavouring are well mixed with dried particle;
(5) compressing tablet.
9. preparation method according to claim 8, it is characterised in that step (1) penfluridol bulk drug and hydrophily
Carry out common micronizing one or more in filler, its ratio is 1:1-1:50 (w/w), preferably 1:2-1:20(w/w).
10. preparation method according to claim 9, it is characterised in that the particle diameter of penfluridol 90% exists after micronizing altogether
In 1-50 μ ms, preferably in 1-30 μ ms.
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CN201510930895.3A CN106880604A (en) | 2015-12-15 | 2015-12-15 | A kind of oral disnitegration tablet containing penfluridol and preparation method thereof |
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CN201510930895.3A CN106880604A (en) | 2015-12-15 | 2015-12-15 | A kind of oral disnitegration tablet containing penfluridol and preparation method thereof |
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Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101732311A (en) * | 2009-12-15 | 2010-06-16 | 苏春华 | Penfluridol-containing oral preparation and application thereof |
CN104546784A (en) * | 2014-12-31 | 2015-04-29 | 康普药业股份有限公司 | Penfluridol tablet composition and preparation method thereof |
-
2015
- 2015-12-15 CN CN201510930895.3A patent/CN106880604A/en active Pending
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101732311A (en) * | 2009-12-15 | 2010-06-16 | 苏春华 | Penfluridol-containing oral preparation and application thereof |
CN104546784A (en) * | 2014-12-31 | 2015-04-29 | 康普药业股份有限公司 | Penfluridol tablet composition and preparation method thereof |
Non-Patent Citations (1)
Title |
---|
陈卫卫等: "《药剂学》", 31 January 2014 * |
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Application publication date: 20170623 |