CN104546768B - Chewing tablet composition containing lipase inhibitor and preparation method thereof - Google Patents
Chewing tablet composition containing lipase inhibitor and preparation method thereof Download PDFInfo
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- CN104546768B CN104546768B CN201410838551.5A CN201410838551A CN104546768B CN 104546768 B CN104546768 B CN 104546768B CN 201410838551 A CN201410838551 A CN 201410838551A CN 104546768 B CN104546768 B CN 104546768B
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Abstract
The invention discloses the chewing tablet composition containing lipase inhibitor, the component comprising following weight percents is：Lipase inhibitor 3%~20%, filler 20%~80%, adhesive 1%~10%, flavouring 5%~40%, surfactant 0.5%~8%, disintegrant 2%~8%, lubricant 1%~5%.Chewable tablets preparation method of composition containing lipase inhibitor of the invention includes：Sieving, mixing, compressing tablet.Compared with prior art, the single impurity of lipase inhibitor chewable tablets of the invention and total impurities content are lower, moisture is lower, it is to avoid medicine meets damp and hot degraded, improve medicine stability, it is ensured that product quality.
Description
Technical field
The invention belongs to pharmaceutical technology field, more specifically to the chewing tablet composition containing lipase inhibitor
And preparation method thereof.
Background technology
Orlistat is reversible gastrointestinal lipases inhibitor, by fatty with gastric lipase in stomach and small intestinal lumen and pancreas
The active ser position of enzyme forms covalent bond makes enzyme inactivate and play therapeutic action, and the enzyme of inactivation can not be by the fat in food
（Mainly triglycerides）It is hydrolyzed to absorbable free fatty and monoacylglycerol.Indigested triglycerides can not be by body
Body absorbs, so that energy intake is reduced, control body weight.The medicine by systemic Absorption without playing drug effect.
Orlistat is white or off-white color crystalline powder, in 0.1mol/L hydrochloric acid, 0.1mol/L sodium hydroxide solutions
It is almost insoluble with water, in methyl alcohol, acetonitrile, glacial acetic acid, chloroform, DMF and dimethyl sulfoxide (DMSO) easily
To wet and hot unstable, easily there is crystal transfer and degraded in dissolving, 42~46 DEG C of fusing point.
When preparing containing orlistat composition and in placement process, orlistat crystal formation easily changes and produces
Degraded, impurity increases, and quality is unstable.
The content of the invention
The invention provides chewing tablet composition containing lipase inhibitor and preparation method thereof, product is both reduced
Degraded, improves the stability of product, it is ensured that the security of product；Meanwhile, the preparation method that the present invention is provided, process is simple, peace
It is complete controllable, can be mass-produced.
It is an object of the invention to provide a kind of chewing tablet composition containing lipase inhibitor.
It is a further object to provide the preparation method of the chewing tablet composition containing lipase inhibitor.
Technical solution of the present invention is as follows：
In one embodiment of the present invention, the invention provides the chewing tablet composition containing lipase inhibitor,
Said composition contains lipase inhibitor, filler, adhesive, flavouring, surfactant, disintegrant, lubricant.
In one embodiment of the present invention, the invention provides the chewing tablet composition containing lipase inhibitor,
Wherein, the described chewable tablets composition weight percent composition containing lipase inhibitor is：Lipase inhibitor 3%~
20%th, filler 20%~80%, adhesive 1%~10%, flavouring 5%~40%, surfactant 0.5%~8%, disintegrant 2%~
8%th, lubricant 1%~5%.
In a kind of preferred embodiment of the invention, the invention provides the chewable tablets combination containing lipase inhibitor
Thing, wherein, the described preferred weight percent composition of chewing tablet composition containing lipase inhibitor is：Fatty enzyme level
Agent 3%~10%, filler 30%~80%, adhesive 2%~8%, flavouring 10%~30%, surfactant 0.5%~5%, collapse
Solution agent 2%~6%, lubricant 1%~3%.
In a kind of more preferred of the invention, the invention provides the chewable tablets group containing lipase inhibitor
Compound, wherein, the described chewing further preferred weight percent composition of tablet composition containing lipase inhibitor is：Fat
Fat enzyme inhibitor 4%~7%, filler 50%~80%, adhesive 3%~6%, flavouring 10%~30%, surfactant 2%~
4%th, disintegrant 2%~6%, lubricant 1%~3%.
In embodiments of the invention, the invention provides the chewing tablet composition containing lipase inhibitor, wherein,
Described lipase inhibitor is orlistat, i.e.,（(S) -2- formamidos -4- methvl-pentanoic acids (S) -1- [[(2S, 3S) -
3- hexyl -4- ketone -2- oxetanylmethoxies] methyl]-dodecyl ester）.
In the solution of the present invention, the invention provides the chewing tablet composition containing lipase inhibitor, wherein, it is described
Filler be selected from the SD of mannitol 200, microcrystalline cellulose pH102, lactose monohydrate, cellulose milk sugar, Lactis Anhydrous, starch, pre-
One or more in gelling starch, Icing Sugar；It is preferred that the one kind in the SD of mannitol 200, microcrystalline cellulose pH102, Lactis Anhydrous
Or it is several.
In the solution of the present invention, the invention provides the chewing tablet composition containing lipase inhibitor, wherein, it is described
Adhesive be selected from Hydroxypropyl methylcellulose, PVP, copolyvidone S630.It is preferred that copolyvidone S630.
In the solution of the present invention, the invention provides the chewing tablet composition containing lipase inhibitor, wherein, it is described
Flavouring be selected from xylitol, sorbierite.It is preferred that xylitol.
In the solution of the present invention, the invention provides the chewing tablet composition containing lipase inhibitor, wherein, it is described
Surfactant be selected from lauryl sodium sulfate, sucrose palmitate；Preferably sucrose palmitate.
In the solution of the present invention, the invention provides the chewing tablet composition containing lipase inhibitor, wherein, it is described
Disintegrant is received selected from cross-linked carboxymethyl cellulose, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose；It is preferred that sodium carboxymethyl starch.
In the solution of the present invention, the invention provides the chewing tablet composition containing lipase inhibitor, wherein, it is described
Lubricant is selected from sodium stearyl fumarate, magnesium stearate, superfine silica gel powder, talcum powder, Compritol 888 ATO；It is preferred that magnesium stearate.
In a kind of preferred embodiment of the invention, the invention provides the chewable tablets combination containing lipase inhibitor
Thing, wherein, the lipase inhibitor chewable tablets contains lipase inhibitor, filler, adhesive, flavouring, surface-active
Agent, disintegrant and lubricant；
Here, the fatty enzyme level is orlistat；The filler is selected from mannitol, microcrystalline cellulose, anhydrous lactitol
It is sugared a kind of and more than；Described adhesive is selected from copolyvidone S630；The flavouring is selected from xylitol；The surfactant choosing
From sucrose palmitate；The disintegrant is selected from sodium carboxymethyl starch；The lubricant is selected from magnesium stearate.
In a kind of preferred embodiment of the invention, chewing tablet composition of the present invention containing lipase inhibitor,
It contains the component of following weight percents：Lipase inhibitor 3%~20%, filler 20%~80%, adhesive 1%~10%,
Flavouring 5%~40%, surfactant 0.5%~8%, disintegrant 2%~8% and lubricant 1%~5%；
Here, the lipase inhibitor is selected from orlistat；The filler is selected from the SD of mannitol 200, microcrystalline cellulose
One kind in plain pH102, lactose monohydrate, cellulose milk sugar, Lactis Anhydrous, starch, pregelatinized starch, Icing Sugar and more than；Bonding
Agent is selected from Hydroxypropyl methylcellulose, PVP, copolyvidone S630, and flavouring is selected from xylitol, sorbierite；Surfactant is selected from
Lauryl sodium sulfate, sucrose palmitate；Disintegrant is received selected from cross-linked carboxymethyl cellulose, sodium carboxymethyl starch, low substitution
Hydroxypropylcellulose；Lubricant is selected from sodium stearyl fumarate, magnesium stearate, superfine silica gel powder, talcum powder, Compritol 888 ATO.
In a kind of preferred embodiment of the invention, the invention provides the chewable tablets combination containing lipase inhibitor
Thing, it contains the component of following weight percents：Lipase inhibitor 3%~10%, filler 30%~80%, adhesive 2%~
8%th, flavouring 10%~20%, surfactant 0.5%~5%, disintegrant 2%~6%, lubricant 1%~3%；
Here, the lipase inhibitor is selected from orlistat；The filler is selected from the SD of mannitol 200, microcrystalline cellulose
Plain pH102, Lactis Anhydrous it is a kind of and more than；Adhesive is selected from copolyvidone S630, and flavouring is selected from xylitol, surfactant
Selected from sucrose palmitate, disintegrant is selected from sodium carboxymethyl starch, and lubricant is selected from magnesium stearate.
In a kind of preferred embodiment of the invention, the invention provides the chewable tablets combination containing lipase inhibitor
Thing, it contains the component of following weight percents：Orlistat 4%~7%, filler 50%~80%, copolyvidone S630 3%~
6%th, xylitol 10%~30%, sucrose palmitate 2%~4%, sodium carboxymethyl starch 2%~6%, magnesium stearate 1%~3%；It is described to fill out
Fill agent be selected from the SD of mannitol 200, microcrystalline cellulose pH102, Lactis Anhydrous it is a kind of and more than.
The chewing tablet composition containing lipase inhibitor that the present invention is provided, its preparation method is comprised the following steps：
（1）, by lipase inhibitor, filler, adhesive, flavouring, surfactant, disintegrant, lubricant difference
Sieving, average grain diameter is 75 μm 249 μm；
（2）, by weight proportion, by lipase inhibitor, filler, adhesive, flavouring, surfactant, disintegrant,
Lubricant, with 820 revs/min of rotating speed, mixes 1545 minutes in mixer, obtains intermediate products；
（3）, intermediate products carry out compressing tablet, control slice, thin piece hardness 510kg, obtain orlistat chewable tablets.In the present invention
Embodiment in, the present invention provide the chewing tablet composition containing lipase inhibitor, its preparation method include following step
Suddenly：
（1）, pretreatment：By lipase inhibitor, filler, adhesive, flavouring, surfactant, disintegrant, lubrication
Agent is sieved respectively, and average grain diameter is respectively 75 μm~249 μm mesh, standby；
（2）, by weight, by lipase inhibitor, filler, adhesive 1%~10%, flavouring, surfactant collapses
Solution agent, lubricant, are put into mixer, with 820 revs/min of rotating speed, mix 1545 minutes, are well mixed, and obtain middle product
Product, detect intermediate products content；
（3）, piece weight determined according to the content of intermediate products, carry out compressing tablet according to prior art, control hardness 5~
10kg, obtains lipase inhibitor chewable tablets；
（4）, lipase inhibitor chewable tablets is carried out detection proterties, crystal formation, relevant material, dissolution rate, content；And by fat
Fat enzyme inhibitor chewable tablets carries out bottled, obtains lipase inhibitor chewable tablets finished product.
In the lipase inhibitor chewable tablets preparation method of composition that the present invention is provided, wherein, described contains fat
The chewable tablets composition weight percent composition of enzyme inhibitor is：Lipase inhibitor 3%~20%, filler 20%~80%, glue
Mixture 1%~10%, flavouring 5%~40%, surfactant 0.5%~8%, disintegrant 2%~8%, lubricant 1%~5%.
In the lipase inhibitor chewable tablets preparation method of composition that the present invention is provided, as one kind side of being preferable to carry out
Case, wherein, the described preferred weight percent composition of chewing tablet composition containing lipase inhibitor is：Fatty enzyme level
Agent 3%~10%, filler 30%~80%, adhesive 2%~8%, flavouring 10%~30%, surfactant 0.5%~5%, collapse
Solution agent 2%~6%, lubricant 1%~3%.
In the lipase inhibitor chewable tablets preparation method of composition that the present invention is provided, as one kind side of being preferable to carry out
Case, wherein, the described chewing further preferred weight percent composition of tablet composition containing lipase inhibitor is：Fat
Enzyme inhibitor 4%~7%, filler 50%~80%, adhesive 3%~6%, flavouring 10%~30%, surfactant 2%~4%,
Disintegrant 2%~6%, lubricant 1%~3%.
In the lipase inhibitor chewable tablets preparation method of composition that the present invention is provided, as one kind side of being preferable to carry out
Case, wherein, described lipase inhibitor is orlistat, i.e.,（(S) -2- formamidos -4- methvl-pentanoic acids (S) -1-
[[(2S, 3S) -3- hexyl -4- ketone -2- oxetanylmethoxies] methyl]-dodecyl ester）.
In the lipase inhibitor chewable tablets preparation method of composition that the present invention is provided, as one kind side of being preferable to carry out
Case, wherein, described filler is selected from the SD of mannitol 200, microcrystalline cellulose pH102, lactose monohydrate, cellulose milk sugar, anhydrous
One or more in lactose, starch, pregelatinized starch, Icing Sugar；It is preferred that the SD of mannitol 200, microcrystalline cellulose pH102, anhydrous
One or more in lactose；
Described adhesive is selected from Hydroxypropyl methylcellulose, PVP, copolyvidone S630.It is preferred that copolyvidone S630；
Described flavouring is selected from xylitol, sorbierite；It is preferred that xylitol；
Described surfactant is selected from lauryl sodium sulfate, sucrose palmitate；Preferably sucrose palmitate.
The disintegrant is received selected from cross-linked carboxymethyl cellulose, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose；It is preferred that carboxylic
Methyl starch sodium；
The lubricant is selected from sodium stearyl fumarate, magnesium stearate, superfine silica gel powder, talcum powder, Compritol 888 ATO；It is preferred that
Magnesium stearate.
In the lipase inhibitor chewable tablets preparation method of composition that the present invention is provided, as one kind side of being preferable to carry out
Case, wherein, the lipase inhibitor chewable tablets contains lipase inhibitor, filler, adhesive, flavouring, surface-active
Agent, disintegrant and lubricant；
Here, the fatty enzyme level is orlistat；The filler is selected from mannitol, microcrystalline cellulose, anhydrous lactitol
It is sugared a kind of and more than；Described adhesive is selected from copolyvidone S630；The flavouring is selected from xylitol；The surfactant choosing
From sucrose palmitate；The disintegrant is selected from sodium carboxymethyl starch；The lubricant is selected from magnesium stearate.
In the lipase inhibitor chewable tablets preparation method of composition that the present invention is provided, as one kind side of being preferable to carry out
Case, wherein, the chewing tablet composition containing lipase inhibitor of the invention, it contains the component of following weight percents：Fat
Fat enzyme inhibitor 3%~20%, filler 20%~80%, adhesive 1%~10%, flavouring 5%~40%, surfactant 0.5%
~8%, disintegrant 2%~8% and lubricant 1%~5%；
Here, the lipase inhibitor is selected from orlistat；The filler is selected from the SD of mannitol 200, microcrystalline cellulose
One kind in plain pH102, lactose monohydrate, cellulose milk sugar, Lactis Anhydrous, starch, pregelatinized starch, Icing Sugar and more than；Bonding
Agent is selected from Hydroxypropyl methylcellulose, PVP, copolyvidone S630, and flavouring is selected from xylitol, sorbierite；Surfactant is selected from
Lauryl sodium sulfate, sucrose palmitate；Disintegrant is received selected from cross-linked carboxymethyl cellulose, sodium carboxymethyl starch, low substitution
Hydroxypropylcellulose；Lubricant is selected from sodium stearyl fumarate, magnesium stearate, superfine silica gel powder, talcum powder, Compritol 888 ATO.
In the lipase inhibitor chewable tablets preparation method of composition that the present invention is provided, as one kind side of being preferable to carry out
Case, wherein, the chewing tablet composition containing lipase inhibitor that the present invention is provided, it contains the group of following weight percents
Point：Lipase inhibitor 3%~10%, filler 30%~80%, adhesive 2%~8%, flavouring 10%~20%, surface-active
Agent 0.5%~5%, disintegrant 2%~6%, lubricant 1%~3%；
Here, the lipase inhibitor is selected from orlistat；The filler is selected from the SD of mannitol 200, microcrystalline cellulose
Plain pH102, Lactis Anhydrous it is a kind of and more than；Adhesive is selected from copolyvidone S630, and flavouring is selected from xylitol, surfactant
Selected from sucrose palmitate, disintegrant is selected from sodium carboxymethyl starch, and lubricant is selected from magnesium stearate.
In the lipase inhibitor chewable tablets preparation method of composition that the present invention is provided, as one kind side of being preferable to carry out
Case, wherein, the chewing tablet composition containing lipase inhibitor that the present invention is provided, it contains the group of following weight percents
Point：Orlistat 4%~7%, filler 50%~80%, copolyvidone S630 3%~6%, xylitol 10%~30%, sucrose palm
Acid esters 2%~4%, sodium carboxymethyl starch 2%~6%, magnesium stearate 1%~3%；The filler is selected from the SD of mannitol 200, crystallite
Cellulose pH102, Lactis Anhydrous it is a kind of and more than.Orlistat chewable tablets prepared by the present invention, after oral taking chewy, there is refrigerant
Sense, in good taste, compliance is good.
Orlistat chewable tablets of the invention and commercially available orlistat chewable tablets（Trade name：alli）Compare, it is single miscellaneous
Matter and total impurities are lower, and product stability is more preferable.Rationally, influence factor experiment and accelerated test are stable for main ingredient and each ratio of adjuvant
Property is good.
Brief description of the drawings
What Fig. 1 was represented is the preparation method of chewing tablet composition of the present invention containing lipase inhibitor.
What Fig. 2 was represented is commercially available orlistat chewable tablets（Trade name：alli）Preparation method.
Specific embodiment；
The present invention is described in further details with reference to embodiment, but not limited to this.
Embodiment 1：It is prepared with 10000 tablet recipe amounts
Product prescription：
Preparation technology：
1st, pre-process：Orlistat is crossed into 60 mesh sieves；Parteck deltaM, microcrystalline cellulose pH102, Lactis Anhydrous, xylose
Alcohol, sodium carboxymethyl starch, copolyvidone S630, sucrose palmitate cross 80 mesh sieves；Magnesium stearate crosses 160 mesh sieves, standby；
2nd, mix：The above-mentioned auxiliary material for weighing recipe quantity puts mixer, and the revolution with 18 revs/min is mixed, during mixing
Between be 15min, obtain final product intermediate products, detection level；
3rd, compressing tablet：According to intermediate products content, piece weight is determined；The loading amount for adjusting tablet press machine carries out compressing tablet, in tableting processes
Monitoring tablet weight variation（±5%）And hardness（5kg~10kg）, obtain orlistat chewable tablets.
Above-mentioned production process strict implement China drug's GMP specification, strict implement technological procedure and operational procedure, strictly hold
Row clean operation code.
To orlistat chewable tablets in embodiment 1 and European commercially available product（Trade name：alli；Specification 27mg）Carry out high temperature examination
Test carries out stability contrast with wet test high.
Above two preparation is placed 10 days under the conditions of 40 DEG C of high temperature and high humidity RH75% and sampled, to emphasis index（Proterties,
Relevant material, content）Detected, detection method is USP standards.Testing result is shown in Tables 1 and 2.
Embodiment 2：It is prepared with 10000 tablet recipe amounts
Product prescription：
Preparation technology：
1st, pre-process：Orlistat is crossed into 60 mesh sieves；Parteck deltaM, microcrystalline cellulose pH102, xylitol, carboxymethyl
Sodium starch, copolyvidone S630, sucrose palmitate cross 80 mesh sieves；Magnesium stearate crosses 160 mesh sieves, standby；
2nd, mix：The above-mentioned auxiliary material for weighing recipe quantity puts mixer, and the revolution with 15 revs/min is mixed, during mixing
Between be 30min, obtain final product intermediate products, detection level；
3rd, compressing tablet：According to intermediate products content, piece weight is determined；The loading amount for adjusting tablet press machine carries out compressing tablet, in tableting processes
Monitoring tablet weight variation（±5%）And hardness（5kg~10kg）, obtain orlistat chewable tablets.
Embodiment 3：It is prepared with 10000 tablet recipe amounts
Product prescription：
Preparation technology：
1st, pre-process：Orlistat is crossed into 60 mesh sieves；Parteck deltaM, Lactis Anhydrous, xylitol, sodium carboxymethyl starch,
Copolyvidone S630, sucrose palmitate cross 80 mesh sieves；Magnesium stearate crosses 160 mesh sieves, standby；
2nd, mix：The above-mentioned auxiliary material for weighing recipe quantity puts mixer, and the revolution with 12 revs/min is mixed, during mixing
Between be 45min, obtain final product intermediate products, detection level；
3rd, compressing tablet：According to intermediate products content, piece weight is determined；The loading amount for adjusting tablet press machine carries out compressing tablet, in tableting processes
Monitoring tablet weight variation（±5%）And hardness（5kg~10kg）, obtain orlistat chewable tablets.
Embodiment 4：It is prepared with 10000 tablet recipe amounts
Product prescription：
Preparation technology：
1st, pre-process：Orlistat is crossed into 60 mesh sieves；Parteck deltaM, xylitol, sodium carboxymethyl starch, copolyvidone
S630, sucrose palmitate cross 80 mesh sieves；Magnesium stearate crosses 160 mesh sieves, standby；
2nd, mix：The above-mentioned auxiliary material for weighing recipe quantity puts mixer, and the revolution with 15 revs/min is mixed, during mixing
Between be 45min, obtain final product intermediate products, detection level；
3rd, compressing tablet：According to intermediate products content, piece weight is determined；The loading amount for adjusting tablet press machine carries out compressing tablet, in tableting processes
Monitoring tablet weight variation（±5%）And hardness（5kg~10kg）, obtain orlistat chewable tablets.
Result above shows that the orlistat chewable tablets impurity more single than alli and total impurities of preparation of the invention are small；
High temperature and high humidity study on the stability result show that the single impurity of orlistat chewable tablets of the invention and total impurities compare alli
It is low.Illustrate steady quality of the orlistat chewable tablets than commercially available alli that composition of the invention and preparation method thereof is obtained.
Comparative example 1
European drug administration（EMA）Orlistat chewable tablets（Trade name：Alli, specification：27mg）Assessed in European Union and reported
Announcement discloses preparation technology for wet granulation technology.We are prepared investigation with reference to its prescription composition and technique, specific as follows：
Preparation technology：
1st, pre-process：Orlistat is crossed into 60 mesh sieves；Mannitol, xylitol, Lactis Anhydrous, microcrystalline cellulose, carboxymethyl
Sodium starch, sucrose palmitate, polyethylene glycol mono stearate cross 80 mesh sieves；Compritol 888 ATO and sodium stearyl fumarate mistake
160 mesh sieves, it is standby.PVP water is configured to 8% povidone solution, it is standby；
2nd, mix：Orlistat is crossed, mannitol, xylitol, Lactis Anhydrous, microcrystalline cellulose, sodium carboxymethyl starch, sugarcane
Gomuti fibre glycerin monostearate, polyethylene glycol mono stearate are put into wet granulator, are mixed 15 minutes, are well mixed；
3rd, pelletize：Povidone solution is added, softwood processed is stirred, the granulation of 20 mesh sieves is crossed；
4th, dry：Wet granular is dried 4 hours using fluid bed dryer, 20 mesh sieves is crossed and is arranged, obtain dry particl；
5th, it is total mixed：Compritol 888 ATO, sodium stearyl fumarate and dry particl are put in mixer.Revolution with 15 revs/min enters
Row mixing, incorporation time is 20min, obtains final product intermediate products, detection level；
6th, compressing tablet：According to intermediate products content, piece weight is determined；The loading amount for adjusting tablet press machine carries out compressing tablet, in tableting processes
Monitoring tablet weight variation（±5%）And hardness（5kg~10kg）, obtain orlistat chewable tablets.
40 DEG C and high humidity RH75% conditions of the embodiment 1 of table 9 and 1,2,3,4 high temperature of comparative example investigate 10 days testing results
Above result of study shows：
Comparative example 1, by drying, is influenceed using the composition and technique of commercially available product alli by temperature and humidity, produces
Certain degraded is given birth to, moisture, single impurity and total impurities are bigger than embodiment 1,2,3,4；Finished product is through high temperature and wet stability high
Investigate, single impurity and total impurities are bigger than embodiment 1,2,3,4, and amplification is very fast.The of poor quality of comparative example 1 is illustrated, quality is steady
Qualitative difference.
Chewing tablet composition containing lipase inhibitor of the invention and preparation method thereof, sharpest edges in avoiding
Orlistat meets wet and hot degraded, and the moisture of orlistat chewable tablets, single impurity and total impurities compare wet granulation technology
（Alli and comparative example 1）The orlistat chewable tablets of preparation it is small, and stability is more preferable, it is ensured that the security of product.
Claims (7)
1. the chewing tablet composition containing lipase inhibitor, it is characterised in that：Lipase inhibitor 3%~20%, filler
20%~80%, adhesive 1%~10%, flavouring 5%~40%, surfactant 0.5%~8%, disintegrant 2%~8%, lubricant 1%
~5%；The lipase inhibitor be selected from orlistat, the filler be selected from the SD of mannitol 200, microcrystalline cellulose pH102,
One kind in lactose monohydrate, cellulose milk sugar, Lactis Anhydrous, starch, pregelatinized starch, Icing Sugar and more than, adhesive is selected from hydroxyl
Third methylcellulose, PVP, copolyvidone S630, flavouring are selected from xylitol, sorbierite, and surfactant is selected from sucrose palm
Acid esters, disintegrant is received selected from cross-linked carboxymethyl cellulose, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, and lubricant is selected from hard
Fat fumaric acid sodium, magnesium stearate, superfine silica gel powder, talcum powder, Compritol 888 ATO；
Here, the preparation method of the described chewing tablet composition containing lipase inhibitor, comprises the following steps：
（1）, lipase inhibitor, filler, adhesive, flavouring, surfactant, disintegrant, lubricant sieved respectively,
Average grain diameter is 75 μm 249 μm；
（2）, by weight proportion, by lipase inhibitor, filler, adhesive, flavouring, surfactant, disintegrant, lubrication
Agent, with 8 20 revs/min of rotating speed, mixes 15 45 minutes in mixer, obtains intermediate products；
（3）, intermediate products carry out compressing tablet, the 10kg of control slice, thin piece hardness 5 obtains orlistat chewable tablets.
2. the chewing tablet composition containing lipase inhibitor according to claim 1, it is characterised in that：Lipase inhibitor
3%~10%, filler 30%~80%, adhesive 2%~8%, flavouring 10%~20%, surfactant 0.5%~5%, disintegrant
2%~6%, lubricant 1%~3%；The lipase inhibitor be selected from orlistat, the filler be selected from the SD of mannitol 200,
Microcrystalline cellulose pH102, Lactis Anhydrous it is a kind of and more than, adhesive is selected from copolyvidone S630, and flavouring is selected from xylitol, table
Face activating agent is selected from sucrose palmitate, and disintegrant is selected from sodium carboxymethyl starch, and lubricant is selected from magnesium stearate.
3. the chewing tablet composition containing lipase inhibitor according to claim 1, it is characterised in that：Orlistat 4%~
7%th, filler 50%~80%, copolyvidone S630 3%~6%, xylitol 10%~30%, sucrose palmitate 2%~4%, carboxylic first
Base sodium starch 2%~6%, magnesium stearate 1%~3%；The filler is selected from the SD of mannitol 200, microcrystalline cellulose pH102, anhydrous
Lactose it is a kind of and more than.
4. the chewing tablet composition containing lipase inhibitor according to claim 1, in terms of 10000,
Orlistat 270g
The SD 1680g of mannitol 200
Microcrystalline cellulose pH102 277g
Lactis Anhydrous 840g
Xylitol 630g
Sodium carboxymethyl starch 210g
Copolyvidone S630 126g
Sucrose palmitate 126g
Magnesium stearate 42g；
Preparation technology：
（1）, pretreatment：Orlistat is crossed into 60 mesh sieves；Parteck deltaM, microcrystalline cellulose pH102, Lactis Anhydrous, xylose
Alcohol, sodium carboxymethyl starch, copolyvidone S630, sucrose palmitate cross 80 mesh sieves；Magnesium stearate crosses 160 mesh sieves, standby；
（2）, mixing：The above-mentioned auxiliary material for weighing recipe quantity puts mixer, and the revolution with 18 revs/min is mixed, incorporation time
It is 15min, obtains final product intermediate products, detection level；
（3）Compressing tablet：According to intermediate products content, piece weight is determined；The loading amount for adjusting tablet press machine carries out compressing tablet, is monitored in tableting processes
Tablet weight variation ± 5% and hardness 5kg~10kg.
5. the chewing tablet composition containing lipase inhibitor as claimed in claim 1, in terms of 10000,
Orlistat 270g
The SD 1925g of mannitol 200
Microcrystalline cellulose pH102 350g
Xylitol 770g
Sodium carboxymethyl starch 231g
Copolyvidone S630 154g
Sucrose palmitate 77g
Magnesium stearate 77g
Preparation technology：
（1）, pretreatment：Orlistat is crossed into 60 mesh sieves；Parteck deltaM, microcrystalline cellulose pH102, xylitol, carboxymethyl form sediment
Powder sodium, copolyvidone S630, sucrose palmitate cross 80 mesh sieves；Magnesium stearate crosses 160 mesh sieves, standby；
（2）, mixing：The above-mentioned auxiliary material for weighing recipe quantity puts mixer, and the revolution with 15 revs/min is mixed, incorporation time
It is 30min, obtains final product intermediate products, detection level；
（3）, compressing tablet：According to intermediate products content, piece weight is determined；The loading amount for adjusting tablet press machine carries out compressing tablet, is supervised in tableting processes
Control tablet weight variation ± 5% and hardness 5kg~10kg.
6. the chewing tablet composition containing lipase inhibitor as claimed in claim 1, in terms of 10000,
Orlistat 270g
The SD 2200g of mannitol 200
Lactis Anhydrous 1950g
Xylitol 540g
Sodium carboxymethyl starch 108g
Copolyvidone S630 162g
Sucrose palmitate 108g
Magnesium stearate 54g
Preparation technology：
（1）, pretreatment：Orlistat is crossed into 60 mesh sieves；Parteck deltaM, Lactis Anhydrous, xylitol, sodium carboxymethyl starch, altogether
PVP S630, sucrose palmitate cross 80 mesh sieves；Magnesium stearate crosses 160 mesh sieves, standby；
（2）, mixing：The above-mentioned auxiliary material for weighing recipe quantity puts mixer, and the revolution with 12 revs/min is mixed, incorporation time
It is 45min, obtains final product intermediate products, detection level；
（3）, compressing tablet：According to intermediate products content, piece weight is determined；The loading amount for adjusting tablet press machine carries out compressing tablet, is supervised in tableting processes
Control tablet weight variation ± 5% and hardness 5kg~10kg.
7. the chewing tablet composition containing lipase inhibitor as claimed in claim 1, in terms of 10000,
Orlistat 270g
The SD 3443g of mannitol 200
Xylitol 2025g
Sodium carboxymethyl starch 135g
Copolyvidone S630 405g
Sucrose palmitate 260g
Magnesium stearate 200g
Preparation technology：
（1）, pretreatment：Orlistat is crossed into 60 mesh sieves；Parteck deltaM, xylitol, sodium carboxymethyl starch, copolyvidone
S630, sucrose palmitate cross 80 mesh sieves；Magnesium stearate crosses 160 mesh sieves, standby；
（2）, mixing：The above-mentioned auxiliary material for weighing recipe quantity puts mixer, and the revolution with 15 revs/min is mixed, incorporation time
It is 45min, obtains final product intermediate products, detection level；
（3）, compressing tablet：According to intermediate products content, piece weight is determined；The loading amount for adjusting tablet press machine carries out compressing tablet, is supervised in tableting processes
Control tablet weight variation ± 5% and hardness 5kg~10kg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410838551.5A CN104546768B (en) | 2014-12-30 | 2014-12-30 | Chewing tablet composition containing lipase inhibitor and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410838551.5A CN104546768B (en) | 2014-12-30 | 2014-12-30 | Chewing tablet composition containing lipase inhibitor and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104546768A CN104546768A (en) | 2015-04-29 |
| CN104546768B true CN104546768B (en) | 2017-06-16 |
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| Country | Link |
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Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE263558T1 (en) * | 1998-08-14 | 2004-04-15 | Hoffmann La Roche | PHARMACEUTICAL COMPOSITIONS CONTAINING LIPASE INHIBITORS AND CHITOSAN |
| JP3774118B2 (en) * | 1998-08-14 | 2006-05-10 | エフ．ホフマン−ラ ロシュ アーゲー | Pharmaceutical composition comprising a lipase inhibitor |
| US6251421B1 (en) * | 2000-09-25 | 2001-06-26 | Sarfaraz K. Niazi | Pharmaceutical composition containing psyllium fiber and a lipase inhibitor |
| US20030027786A1 (en) * | 2001-06-06 | 2003-02-06 | Karsten Maeder | Lipase inhibiting composition |
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2014
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| CN104546768A (en) | 2015-04-29 |
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Denomination of invention: Chewable tablet composition containing lipase inhibitor and preparation method thereof Effective date of registration: 20220919 Granted publication date: 20170616 Pledgee: Bank of Hankou Limited by Share Ltd. Chongqing branch Pledgor: Zhien Biotechnology Co.,Ltd. Registration number: Y2022500000071 |
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