CN1827095A - Pharmaceutical composition using pregabalin as active ingredient, its preparation method and use - Google Patents
Pharmaceutical composition using pregabalin as active ingredient, its preparation method and use Download PDFInfo
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- CN1827095A CN1827095A CN 200610075607 CN200610075607A CN1827095A CN 1827095 A CN1827095 A CN 1827095A CN 200610075607 CN200610075607 CN 200610075607 CN 200610075607 A CN200610075607 A CN 200610075607A CN 1827095 A CN1827095 A CN 1827095A
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- lyrica
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Abstract
This invention is about a medicine composition taking prinebalyn as active component and its preparing method and usages. It takes prinebalyn as medicine active component, and is formed by mixing acceptable finding. It is used to cure outer neuralgia and grand partly epilepsy. It uses prinebalyn as raw material and adds some findings those have specified kinds and ratios. Developing troche, capsule, dispersing tablets, granula, soft capsule, chewing tablets, buccal tablets, droplet, and other oral preparations according to the method in this invention.
Description
Technical field
The present invention relates to a kind of is Pharmaceutical composition and preparation method thereof, the purposes of active component with the lyrica, belongs to medical technical field.
Background technology
Epilepsy is the discharge of cerebral neuron paroxysmal abnormality, causes a kind of chronic disease of of short duration cerebral disorder.Owing to the related position difference of paradoxical discharge neuron, can show as motion, sensation, vegetative nerve, consciousness and the mental disorder of outbreak.It is one of clinical common symptom of causing of multiple reason.According to domestic Epidemiological study, its sickness rate is about crowd's 1 ‰, and prevalence is about crowd's 5 ‰.
The chemical name of lyrica is that (3S)-3-(Aminomethyl)-its chemical structural formula of 5-methylhexanoic acid is
Experiment finds that lyrica can combine with the α 2 γ-subunit gabapentin binding site on the calcium channel, increases neuron γ-GABA content.In the experiment of the synapse cornea of the neural cortex of rat, this medicine can suppress the activity of casein kinase, obviously strengthens with respect to gabapentin, can strengthen the activity of glutamate decarboxylase simultaneously.This chemical compound all shows antiepileptic pharmaceutically active in many animal epileptic models.Its effect is similar with gabapentin, but dosage than the low 3-10 of gabapentin doubly, and acting duration is the former 2 times.
In addition, this medicine is studies show that aspect the treatment neuropathic pain, in the mouse model of various neuropathic pains, comprise intrathecal injection P-or-NMDA neuronal acceptor, carrageenin and the inductive pain model of formalin, the lenitive effect of lyrica is 2 times of gabapentin at least, but does not have sedation.
As psychotherapeutic drugs, lyrica all has therapeutical effect preferably to generalization anxiety, social anxiety, bipolar imbalance, terrified etc., and rapid-action, safety is good, has research and development and is worth.
Summary of the invention
Having the purpose of this invention is to provide a kind of is the Pharmaceutical composition and uses thereof of active component with the lyrica.The present invention for a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that it is the active component that lyrica forms, the Pharmaceutical composition that forms with mixing acceptable accessories.
Above-mentioned a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that the consumption of described lyrica is 5mg-900mg for per unit dosage.
Above-mentioned a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that the consumption of described lyrica is preferably 10mg-600mg for per unit dosage.
Above-mentioned a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that the consumption of described lyrica is preferably 25mg-300mg more of per unit dosage.
Described a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that the Pharmaceutical composition of described lyrica is an oral formulations.
Described a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that described oral formulations can be made into tablet, capsule, dispersible tablet, soft capsule, chewable tablet, oral cavity disintegration tablet, buccal tablet, drop pill etc.
Described a kind of be the Pharmaceutical composition of active component with the lyrica, can be used for the treatment of peripheral nervous pain and epilepsy partial seizure.
The specific embodiment
Come lyrica preparation of the present invention done further specifying by following example, but be not limited in following example.
Embodiment 1 lyrica tablet
Prescription:
Amounts of components
Lyrica 25g
Microcrystalline Cellulose 60g
Pregelatinized Starch 30g
CMS-Na 5.0g
Micropowder silica gel 2.5g
Magnesium stearate 2.5g
95% ethanol is an amount of
Make 1000 altogether
Preparation method:
Guo 80 mesh sieves with lyrica, microcrystalline Cellulose, pregelatinized Starch, behind the mix homogeneously, add 95% ethanol and make soft material in right amount, 20 mesh sieves are granulated, drying, 18 mesh sieve granulate, add CMS-Na, micropowder silica gel, magnesium stearate, adopt suitable punch die compressed tablets behind the mix homogeneously, promptly.
Embodiment 2: the lyrica capsule
Prescription:
Amounts of components
Lyrica 50g
Starch 30g
Dextrin 10g
5%PVP-k 30 alcoholic solution are an amount of
PPVP 2.0g
Pulvis Talci 2.0g
Preparation method:
Lyrica, starch, dextrin are crossed 80 mesh sieves respectively, behind the mix homogeneously, add 5%PVP-k 30 alcoholic solution (about 60 milliliters) and make soft material in right amount, 24 mesh sieves are granulated, drying, 24 mesh sieve granulate, the PPVP, the Pulvis Talci that add recipe quantity, in the suitable capsule shells of packing into behind the mix homogeneously promptly.
Embodiment 3: the lyrica dispersible tablet
Prescription:
Amounts of components
Lyrica 75g
Microcrystalline Cellulose 80g
Mannitol 120
CMS-Na 18g
PPVP 3g
Fructus Citri Limoniae essence 6g
Aspartame 3g
Pulvis Talci 2.5g
50% ethanol is an amount of
Make 1000 altogether
Preparation method:
Lyrica, microcrystalline Cellulose, mannitol are crossed 80 mesh sieves respectively, behind the mix homogeneously, add 50% alcoholic solution and make soft material in right amount, 24 mesh sieves are granulated, drying, 20 mesh sieve granulate add disintegrating agent CMS-Na, PPVP, Fructus Citri Limoniae essence, aspartame, Pulvis Talci, tabletting behind the mix homogeneously, promptly.
Embodiment 4: the lyrica soft capsule
Prescription:
Amounts of components
Lyrica 100g
Soybean oil 150g
Tween 80 15g
Lecithin 5g
Cera Flava 2.5g
Make 1000 altogether
Preparation method:
Earlier lyrica is pulverized, crossed 200 mesh sieves, join in the recipe quantity soybean oil and stir, add tween 80, lecithin while stirring, evenly the back adds in 60-70 ℃ of fused Cera Flava, makes it to obtain the oil solution of even suspendible.Adjust content weight, the compacting soft capsule, promptly.
Embodiment 5: the lyrica chewable tablet
Prescription
Amounts of components
Lyrica 125g
Xylitol 140g
Sorbitol 60g
Mannitol 60g
The sweet 6g of A Siba
Flavoring orange essence 8g
The 1%PVP-K30 alcoholic solution is an amount of
Make 1000 altogether
Preparation method:
To all cross lyrica, xylitol, sorbitol, the mannitol mix homogeneously of 80 mesh sieves, with 1%PVP-K30 alcoholic solution system soft material, 16 mesh sieves are granulated, and dry, 12 mesh sieve granulate add sweet, the flavoring orange essence of A Siba, mix homogeneously, and tabletting gets final product.
Embodiment 6: the lyrica oral cavity disintegration tablet
Prescription
Amounts of components
Lyrica 150g
Microcrystalline Cellulose 158g
PPVP 24.5g
L-HPC 10.5g
Stevioside 3.5g
Fructus Citri Limoniae essence 3.5g
Dehydrated alcohol is an amount of
Make 1000 altogether
Preparation method:
After all crossing the lyrica, microcrystalline Cellulose mix homogeneously of 80 mesh sieves, with an amount of ethanol solution system soft material, the granulation of 16 mesh sieves, drying, 12 mesh sieve granulate add PPVP, L-HPC, stevioside, Fructus Citri Limoniae essence, mix homogeneously, adjust pressure, tabletting gets final product.
Embodiment 7: the lyrica buccal tablet
Prescription
Amounts of components
Lyrica 300g
Mannitol 150g
Xylitol 40g
Stevioside 5g
Mentholum 5g
Sunset yellow is an amount of
95% ethanol is an amount of
Make 1000 altogether
Preparation method:
To all cross lyrica, mannitol, the xylitol mix homogeneously of 80 mesh sieves, with the 95% alcoholic solution system soft material that is dissolved with sunset yellow, 16 mesh sieves are granulated, and dry, 12 mesh sieve granulate add recipe quantity stevioside, Mentholum, mix homogeneously, and tabletting gets final product.
Embodiment 8: the lyrica drop pill
Prescription
Amounts of components
Lyrica 100g
PEG4000 150g
S-40 40g
Make 1000 altogether
Preparation method:
Lyrica is crossed 80 mesh sieves, standby; In addition with PEG4000, S-40 mixings post-heating extremely about 60 ℃ make fusion; Lyrica is heated in the fused solution stirs, move in the dropping funnel, be incubated about 60 ℃, regulate the water dropper size, serves as the cooling phase with-20 ℃ dimethicones, the system of dripping, and ball is washed, selects in filtration, gets final product.
Claims (7)
- The present invention for a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that it is to be medicinal active ingredient with the lyrica, the Pharmaceutical composition that forms with mixing acceptable accessories.
- 2. as claimed in claim 1 a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that the consumption of described lyrica is 5mg-900mg for per unit dosage.
- 3. as claimed in claim 1 a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that the consumption of described lyrica is preferably 10mg-600mg for per unit dosage.
- 4. as claimed in claim 1 a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that the consumption of described lyrica is preferably 25mg-300mg more of per unit dosage.
- 5. as claimed in claim 1 a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that the Pharmaceutical composition of described lyrica is an oral formulations.
- 6. as claimed in claim 5 a kind of be the Pharmaceutical composition of active component with the lyrica, it is characterized in that described oral formulations can be made into tablet, capsule, dispersible tablet, granule, soft capsule, chewable tablet, oral cavity disintegration tablet, buccal tablet, drop pill etc.
- Claim 1-6 described a kind of be the Pharmaceutical composition of active component with the lyrica, can be used for the treatment of peripheral nervous pain and epilepsy partial seizure.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610075607 CN1827095A (en) | 2006-04-14 | 2006-04-14 | Pharmaceutical composition using pregabalin as active ingredient, its preparation method and use |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610075607 CN1827095A (en) | 2006-04-14 | 2006-04-14 | Pharmaceutical composition using pregabalin as active ingredient, its preparation method and use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1827095A true CN1827095A (en) | 2006-09-06 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610075607 Pending CN1827095A (en) | 2006-04-14 | 2006-04-14 | Pharmaceutical composition using pregabalin as active ingredient, its preparation method and use |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103159636A (en) * | 2013-04-05 | 2013-06-19 | 李兴惠 | Aminomethyl caproic acid derivative and use |
| CN103271888A (en) * | 2013-06-18 | 2013-09-04 | 上海奥科达生物医药科技有限公司 | Pregabalin orally disintegrating tablet and dispersible tablet and preparation method thereof |
| CN104592049A (en) * | 2013-04-05 | 2015-05-06 | 李兴惠 | Raw material medicine and preparations of pregabalin |
| CN109125287A (en) * | 2018-10-25 | 2019-01-04 | 千辉药业（安徽）有限责任公司 | A kind of Pregabalin tablet and preparation method thereof |
| JP2019052147A (en) * | 2017-09-13 | 2019-04-04 | 大原薬品工業株式会社 | Pregabalin-containing orally disintegrating tablet with improved chemical stability |
| TWI808217B (en) * | 2018-07-12 | 2023-07-11 | 大陸商四川海思科製藥有限公司 | Composition of fused tricyclic γ-amino acid derivatives and its preparation method |
-
2006
- 2006-04-14 CN CN 200610075607 patent/CN1827095A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103159636A (en) * | 2013-04-05 | 2013-06-19 | 李兴惠 | Aminomethyl caproic acid derivative and use |
| CN103159636B (en) * | 2013-04-05 | 2015-02-25 | 李兴惠 | Aminomethyl caproic acid derivative and use |
| CN104592049A (en) * | 2013-04-05 | 2015-05-06 | 李兴惠 | Raw material medicine and preparations of pregabalin |
| CN103271888A (en) * | 2013-06-18 | 2013-09-04 | 上海奥科达生物医药科技有限公司 | Pregabalin orally disintegrating tablet and dispersible tablet and preparation method thereof |
| JP2019052147A (en) * | 2017-09-13 | 2019-04-04 | 大原薬品工業株式会社 | Pregabalin-containing orally disintegrating tablet with improved chemical stability |
| TWI808217B (en) * | 2018-07-12 | 2023-07-11 | 大陸商四川海思科製藥有限公司 | Composition of fused tricyclic γ-amino acid derivatives and its preparation method |
| CN109125287A (en) * | 2018-10-25 | 2019-01-04 | 千辉药业（安徽）有限责任公司 | A kind of Pregabalin tablet and preparation method thereof |
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