Citicoline sodium tablets and preparation method for directly compressing powder of citicoline sodium into tablets

Abstract

The invention provides citicoline sodium tablets and a preparation method for directly compressing powder of citicoline sodium into tablets. The citicoline sodium tablets provided by the invention are prepared from citicoline sodium, cellactose 80, sodium carboxymethyl starch, magnesium stearate and micro-powder silica gel. The tablets provided by the invention are prepared by adopting a powder direct tablet compression method and the problem that citicoline sodium granulated by a traditional wet process is easy to hydrolyze is solved; meanwhile, the conditions that the tablet weight different is relatively great and the dissolution uniformly is relatively poor, which are easily caused by direct powder compression, are solved through screening prescriptions and setting technological parameters; the quality stability and the safety of products are greatly improved.

Description

Technical field

[0001] The invention relates to a citicoline sodium tablet and a preparation method thereof, and belongs to the field of pharmacy. Background technique

[0002] Citicoline sodium was developed by Japan's Takeda Pharmaceutical Company, and was marketed under the trade name "Nicholin" in 1967, and was imported into China in 1988. The domestic marketed preparations are injections, ordinary tablets or capsules. Its molecular formula is C 14 H 25 N 4 NaO ll P 2 , Is the monosodium salt of choline cytosine diphosphate, is a nucleoside derivative, the chemical name is the monosodium salt of choline cytosine diphosphate, the dried product contains no less than citicoline sodium 98%. Citicoline sodium is mainly used to treat the sequelae of the nervous system caused by brain injury and cerebrovascular accidents, and can be used in the treatment of Parkinson's syndrome. It also has a certain effect on Alzheimer's disease; other such as delaying aging , Improve memory, et...

Examples

Embodiment 1

[0027] Example 1 The effect of different fillers and filler content on citicoline sodium tablets

[0028] In this example, the effects of different fillers and filler content on citicoline sodium tablets were tested.

[0029] Table 1. Selection prescription table of different fillers and filler content of citicoline sodium tablets

[0030]

[0031] Preparation Process:

[0032] 1) Take citicoline sodium and cross-linked polyvinylpyrrolidone XL through a 60-mesh sieve respectively, and then take lactose, spray-dried lactose Flowlac100, microcrystalline cellulose Avicel PH102, and cellactose80 through a 60-mesh sieve respectively, and set aside.

[0033] 2) Take 1 / 2 citicoline sodium and add lactose and microcrystalline cellulose Avicel PH102, spray-dried lactose Flowlac100 and microcrystalline cellulose Avicel PH102, or cellactose80 to the total mixer at 20r / min, and mix for 10 Minutes, spare.

[0034] 3) Take the above-mixed powder, add the remaining 1 / 2 citicoline sodium, cross-linked...

Embodiment 2

[0046] Example 2: The effect of different glidants / lubricants on citicoline sodium tablets

[0047] In this example, the effects of different glidants / lubricants on citicoline sodium tablets were tested.

[0048] Table 3. Citicoline sodium tablets glidant / lubricant dosage selection prescription table

[0049]

[0050] Preparation Process:

[0051] 1) Take citicoline sodium and cross-linked polyvinylpyrrolidone XL through a 60 mesh sieve, and then take cellactose 80 through a 60 mesh sieve for use.

[0052] 2) Add 1 / 2 citicoline sodium to the micro-powder silica gel and cellactose 80 in the prescription in a total mixer at 20 r / min, mix for 10 minutes, and then set aside.

[0053] 3) Take the above-mixed powder, add the remaining 1 / 2 citicoline sodium, cross-linked polyvinylpyrrolidone XL and magnesium stearate in the total mixer for 20 r / min, mix for 20 minutes, and conduct intermediate inspection.

[0054] 4) Use a die with a diameter of 6mm to press tablets with a core hardness of 5-6k...

Embodiment 3

[0060] Example 3: The effect of different disintegrants on citicoline sodium tablets

[0061] Table 5: Selection prescription table for different disintegrants of citicoline sodium tablets

[0062]

[0063]

[0064] Preparation Process:

[0065] 1) Take citicoline sodium, cross-linked polyvinylpyrrolidone XL, sodium carboxymethyl starch, and low-substituted hydroxypropyl cellulose through a 60-mesh sieve respectively, and then take cellactose 80 through a 60-mesh sieve for use.

[0066] 2) Add 1 / 2 citicoline sodium to the micro-powder silica gel and cellactose 80 in the prescription in a total mixer at 20 r / min, mix for 10 minutes, and then set aside.

[0067] 3) Take the above mixed powder, add the remaining 1 / 2 citicoline sodium, cross-linked polyvinylpyrrolidone XL (or sodium carboxymethyl starch or low-substituted hydroxypropyl cellulose) and magnesium stearate to the total 20r / min in the mixer, mixing for 20 minutes, check the intermediate.

[0068] 4) Use a die with a diameter of...

Technical field

[0001] The invention relates to a citicoline sodium tablet and a preparation method thereof, and belongs to the field of pharmacy. Background technique

[0002] Citicoline sodium was developed by Japan's Takeda Pharmaceutical Company, and was marketed under the trade name "Nicholin" in 1967, and was imported into China in 1988. The domestic marketed preparations are injections, ordinary tablets or capsules. Its molecular formula is C 14 H 25 N 4 NaO ll P 2 , Is the monosodium salt of choline cytosine diphosphate, is a nucleoside derivative, the chemical name is the monosodium salt of choline cytosine diphosphate, the dried product contains no less than citicoline sodium 98%. Citicoline sodium is mainly used to treat the sequelae of the nervous system caused by brain injury and cerebrovascular accidents, and can be used in the treatment of Parkinson's syndrome. It also has a certain effect on Alzheimer's disease; other such as delaying aging , Improve memory, et...

Examples

Embodiment 1

[0027] Example 1 The effect of different fillers and filler content on citicoline sodium tablets

[0028] In this example, the effects of different fillers and filler content on citicoline sodium tablets were tested.

[0029] Table 1. Selection prescription table of different fillers and filler content of citicoline sodium tablets

[0030]

[0031] Preparation Process:

[0032] 1) Take citicoline sodium and cross-linked polyvinylpyrrolidone XL through a 60-mesh sieve respectively, and then take lactose, spray-dried lactose Flowlac100, microcrystalline cellulose Avicel PH102, and cellactose80 through a 60-mesh sieve respectively, and set aside.

[0033] 2) Take 1 / 2 citicoline sodium and add lactose and microcrystalline cellulose Avicel PH102, spray-dried lactose Flowlac100 and microcrystalline cellulose Avicel PH102, or cellactose80 to the total mixer at 20r / min, and mix for 10 Minutes, spare.

[0034] 3) Take the above-mixed powder, add the remaining 1 / 2 citicoline sodium, cross-linked...

Embodiment 2

[0046] Example 2: The effect of different glidants / lubricants on citicoline sodium tablets

[0047] In this example, the effects of different glidants / lubricants on citicoline sodium tablets were tested.

[0048] Table 3. Citicoline sodium tablets glidant / lubricant dosage selection prescription table

[0049]

[0050] Preparation Process:

[0051] 1) Take citicoline sodium and cross-linked polyvinylpyrrolidone XL through a 60 mesh sieve, and then take cellactose 80 through a 60 mesh sieve for use.

[0052] 2) Add 1 / 2 citicoline sodium to the micro-powder silica gel and cellactose 80 in the prescription in a total mixer at 20 r / min, mix for 10 minutes, and then set aside.

[0053] 3) Take the above-mixed powder, add the remaining 1 / 2 citicoline sodium, cross-linked polyvinylpyrrolidone XL and magnesium stearate in the total mixer for 20 r / min, mix for 20 minutes, and conduct intermediate inspection.

[0054] 4) Use a die with a diameter of 6mm to press tablets with a core hardness of 5-6k...

Embodiment 3

[0060] Example 3: The effect of different disintegrants on citicoline sodium tablets

[0061] Table 5: Selection prescription table for different disintegrants of citicoline sodium tablets

[0062]

[0063]

[0064] Preparation Process:

[0065] 1) Take citicoline sodium, cross-linked polyvinylpyrrolidone XL, sodium carboxymethyl starch, and low-substituted hydroxypropyl cellulose through a 60-mesh sieve respectively, and then take cellactose 80 through a 60-mesh sieve for use.

[0066] 2) Add 1 / 2 citicoline sodium to the micro-powder silica gel and cellactose 80 in the prescription in a total mixer at 20 r / min, mix for 10 minutes, and then set aside.

[0067] 3) Take the above mixed powder, add the remaining 1 / 2 citicoline sodium, cross-linked polyvinylpyrrolidone XL (or sodium carboxymethyl starch or low-substituted hydroxypropyl cellulose) and magnesium stearate to the total 20r / min in the mixer, mixing for 20 minutes, check the intermediate.

[0068] 4) Use a die with a diameter of...

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