CN104546817A - Pregabalin sustained release preparation - Google Patents
Pregabalin sustained release preparation Download PDFInfo
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- CN104546817A CN104546817A CN201410826607.5A CN201410826607A CN104546817A CN 104546817 A CN104546817 A CN 104546817A CN 201410826607 A CN201410826607 A CN 201410826607A CN 104546817 A CN104546817 A CN 104546817A
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Abstract
The invention relates to a pregabalin sustained release preparation. The preparation comprises pregabalin or a pharmaceutically acceptable salt and at least a sustained release drug composition made from a release rate controlled material.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, particularly relate to a kind of slow released pregabalin medicine composition for the treatment of neuronal pain.
Background technology
Lyrica is a kind of new antiepileptic drugs, its molecular structure has gamma aminobutyric acid structure, thus has spasmolytic effect, is usually used in treating peripheral neuralgia, or auxiliary treatment partial seizures.In December, 2008, food and drug administration (FDA) ratifies lyrica (trade name " Le Ruika ") and is used for the treatment of diabetic peripheral neuralgia (DPN) and these two kinds of modal neuropathic pains of postherpetic neuralgia (PHN).
Neuropathic pain is one of the most refractory chronic pain syndrome, with dull pain, scorching hot, twinge for principal character, neuralgic inducement is a lot, diabetes, infection (as herpes zoster), cancer and AIDS etc. all can cause neuralgia, and in Europe, the crowd of about 3% suffer from neuralgic torment.
Drug therapy is the common method for the treatment of of neuropathic pain, along with going deep into of a large amount of basis and clinical research, has had one, two, the three line medicines comparing and determine.At present, the conventional medicine of neuropathic pain mainly comprises agents of calcium ion channel modulators (lyrica), antidepressants, opiates and external preparation for skin medicine etc.
Lyrica treatment PHN, quick, potent, curative effect is dose dependent, pain relief degree can be significantly improved and improve pain relevant sleep obstacle, absorb linearly relevant to dosage, and in dose dependent, untoward reaction major part is light moderate, and dizzy, drowsiness is common adverse reactions.Lyrica is widely used in treatment periphery and central sexual nerves pathological pain in the world, and obtaining the high praise of numerous experts and scholars, is the first-line treatment medicine of neuropathic pain by multiple internal authority Guidelines recommend.
Lyrica chemical name: (S)-3-(aminomethyl)-5-methylhexanoic acid.Structural formula:
Current domestic listing have lyrica capsule, be mainly used in treatment neuralgia and auxiliary treatment epilepsy, its listing specification is 25mg, 50mg, 75mg, 100mg, 150mg, 200mg, 300mg, and daily dosage is 150-600mg.
Lyrica has the shorter half-life (being about 6 hours), and every day, multiple dosing, can cause the blood drug level of medicine to produce obviously fluctuation.Must frequent drug administration to keep the blood drug level of quite stable.The effective dose of lyrica is 150 ~ 600mg/ days, give with divided doses, every day taken 3 times by lyrica capsule, and after this Therapeutic mode causes administration, blood drug concentration raises rapidly, then due to drug distribution, metabolism and excretion, drug level reduces rapidly.The difference of the highest and minimum blood drug level is greatly the major defect of conventional dosage forms, for overcoming these shortcomings of lyrica, the present inventor is through repeatedly studying, lyrica is made slow releasing preparation, the problem of the fluctuation of fluctuation effective blood drug concentration and multiple dosing can be solved well, reduce administration number of times, improve the compliance of patient, reduce side effect.
Summary of the invention
The invention provides a kind of sustained release pharmaceutical composition, control material comprising lyrica or its pharmaceutically acceptable salt or hydrate and at least one rate of release.The lyrica of this pharmaceutical composition reaches at least 10 ~ 24 hours release time, is preferably 14 ~ 18 hours.
The weight that the rate of release existed in sustained release pharmaceutical composition of the present invention controls material is 10% ~ 70% (weighing scale by compositions), preferably 30% ~ 50% (weighing scale by compositions).It can be that one or more are selected from following material: cellulose family, castor oil hydrogenated, Glyceryl Behenate, sodium carboxymethyl cellulose that rate of release controls material.
Slow releasing composition of the present invention may further include one or more excipient, and this excipient can be diluent (filler), binding agent, fluidizer, one or more in lubricant.Diluent can be in mannitol, microcrystalline Cellulose, lactose, starch in one or more.Binding agent can be one or more in polyvidone, hydroxypropyl cellulose, hypromellose.Disintegrating agent can be one or more in cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone, pregelatinized Starch, carboxymethyl starch sodium.Lubricant can be one or more in Pulvis Talci, silicon dioxide, magnesium stearate, sodium stearyl fumarate.
The dosage form of the sustained release pharmaceutical composition of lyrica of the present invention can be tablet, capsule, granule or piller, preferred tablet or capsule.
Accompanying drawing explanation
Fig. 1 is each embodiment release profiles.
Detailed description of the invention
Embodiment 1: prepare 1000 slow released pregabalin sheets, prescription is as follows:
Preparation technology is as follows:
1. lyrica is crossed 80 mesh sieve pretreatment, 60 mesh sieves crossed by microcrystalline Cellulose, hypromellose, castor oil hydrogenated, and magnesium stearate crosses 100 mesh sieves, for subsequent use;
2. polyvidone is made into the aqueous solution of 10%, makes binding agent;
3., by lyrica, microcrystalline Cellulose, hypromellose, castor oil hydrogenated mix homogeneously, add binding agent and granulate, dry, granulate, additional magnesium stearate mix homogeneously;
4. according to intermediate testing result tabletting.
Embodiment 2: prepare 1000 slow released pregabalin sheets, prescription is as follows:
Preparation technology is as follows:
1. lyrica is crossed 80 mesh sieve pretreatment, microcrystalline Cellulose, hypromellose, sodium carboxymethyl cellulose cross 60 mesh sieves, and magnesium stearate crosses 100 mesh sieves, for subsequent use;
2. by lyrica, microcrystalline Cellulose, hypromellose, sodium carboxymethyl cellulose mix homogeneously, add water granulation, dry, granulate, additional magnesium stearate mix homogeneously;
3. according to intermediate testing result tabletting.
Embodiment 3: prepare 1000 slow released pregabalin sheets, prescription is as follows:
Preparation technology is as follows:
1. lyrica is crossed 80 mesh sieve pretreatment, microcrystalline Cellulose, hypromellose, Glyceryl Behenate cross 60 mesh sieves, and magnesium stearate crosses 100 mesh sieves, for subsequent use;
2. by lyrica, microcrystalline Cellulose, hypromellose, Glyceryl Behenate mix homogeneously, add water granulation, dry, granulate, additional magnesium stearate mix homogeneously;
3. according to intermediate testing result tabletting.
Embodiment 4: prepare 1000 slow released pregabalin sheets, prescription is as follows:
Preparation technology is as follows:
1. lyrica is crossed 80 mesh sieve pretreatment, microcrystalline Cellulose, hypromellose, sodium carboxymethyl cellulose cross 60 mesh sieves, and magnesium stearate crosses 100 mesh sieves, for subsequent use;
2. by lyrica, microcrystalline Cellulose, hypromellose, sodium carboxymethyl cellulose mix homogeneously, add water granulation, dry, granulate, additional silicon dioxide, magnesium stearate mix homogeneously;
3. according to intermediate testing result tabletting.
The release method of each embodiment sees the following form:
Each embodiment release profiles Fig. 1.According to Fig. 1 release profiles, embodiment 1,2,3,4 all can reach slow release effect.
Claims (4)
1. a slow released pregabalin preparation, comprises the slow-release material of acceptable salt or hydrate and its rate of release of control on lyrica or its materia medica.
2. slow released pregabalin preparation according to claim 1, the slow-release material that it is characterized in that controlling its rate of release be selected from cellulose family, castor oil hydrogenated, Glyceryl Behenate, sodium carboxymethyl cellulose one or more.
3. pregabaline formulation slow-release material according to claim 2, cellulose family be wherein selected from hypromellose 1000mPa.s-100000mPa.s, ethyl cellulose or methylcellulose one or more.
4. slow released pregabalin preparation according to claim 2, it is characterized in that one or more conbined usage in slow-release material cellulose family and castor oil hydrogenated or Glyceryl Behenate or sodium carboxymethyl cellulose, cellulose family consumption 20-40%, castor oil hydrogenated consumption 1-10%, Glyceryl Behenate consumption 1-10%, sodium carboxymethyl cellulose consumption 1-10%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410826607.5A CN104546817A (en) | 2014-12-25 | 2014-12-25 | Pregabalin sustained release preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410826607.5A CN104546817A (en) | 2014-12-25 | 2014-12-25 | Pregabalin sustained release preparation |
Publications (1)
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| CN104546817A true CN104546817A (en) | 2015-04-29 |
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| CN201410826607.5A Pending CN104546817A (en) | 2014-12-25 | 2014-12-25 | Pregabalin sustained release preparation |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111803467A (en) * | 2019-12-17 | 2020-10-23 | 山东则正医药技术有限公司 | Solid medicine composition for controlling medicine release and method for preparing solid medicine composition into granules |
| CN112957337A (en) * | 2021-02-08 | 2021-06-15 | 浙江诺得药业有限公司 | Pregabalin composition and preparation method thereof |
| US11938222B2 (en) | 2018-06-13 | 2024-03-26 | Beijing Tide Pharmaceutical Co., Ltd. | Pregabalin sustained release composition and method for preparing the same |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1857244A (en) * | 2006-03-06 | 2006-11-08 | 重庆医药工业研究院有限责任公司 | Slow released pregabalin medicine composition |
| WO2010143052A1 (en) * | 2009-06-12 | 2010-12-16 | Micro Labs Limited | Novel pharmaceutical compositions containing pregabalin |
| CN102743357A (en) * | 2012-06-26 | 2012-10-24 | 严轶东 | Pregabalin sustained release preparation effervescent and floating in stomach and preparation method thereof |
-
2014
- 2014-12-25 CN CN201410826607.5A patent/CN104546817A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1857244A (en) * | 2006-03-06 | 2006-11-08 | 重庆医药工业研究院有限责任公司 | Slow released pregabalin medicine composition |
| WO2010143052A1 (en) * | 2009-06-12 | 2010-12-16 | Micro Labs Limited | Novel pharmaceutical compositions containing pregabalin |
| CN102743357A (en) * | 2012-06-26 | 2012-10-24 | 严轶东 | Pregabalin sustained release preparation effervescent and floating in stomach and preparation method thereof |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11938222B2 (en) | 2018-06-13 | 2024-03-26 | Beijing Tide Pharmaceutical Co., Ltd. | Pregabalin sustained release composition and method for preparing the same |
| CN111803467A (en) * | 2019-12-17 | 2020-10-23 | 山东则正医药技术有限公司 | Solid medicine composition for controlling medicine release and method for preparing solid medicine composition into granules |
| CN112957337A (en) * | 2021-02-08 | 2021-06-15 | 浙江诺得药业有限公司 | Pregabalin composition and preparation method thereof |
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Application publication date: 20150429 |
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