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Piperazine ferulate sustained-release tablet and its preparation method

A technology of piperazine ferulic acid and sustained-release tablets, which is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of not considering the release of the preparation and not mentioning the release results , the particle fluidity is not very good and other problems, to ensure the stability and durability, improve the bulk density and formability, maintain the effect of blood drug concentration

Active Publication Date: 2012-02-01
浙江四维医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to this, using the release point control and detection method of CN200810045251.6, although reasonable, is extremely inconvenient for detection; it is best to select a suitable release point, and the release result can be accurately detected in the same solvent
At the same time, the patent CN200810045251.6 uses the combination of quick release and sustained release to prepare sustained release preparations. This process is relatively complicated, and it puts forward high requirements for scale-up production, and it is difficult to realize
[0007] Chinese patent CN00112831.0 (name: piperazine ferulic acid slow-release preparation, patentee: Chengdu Hengda Pharmaceutical Factory, application date: April 7, 2000) has mentioned the piperazine ferulic acid slow-release preparation although it is 24 hour slow-release preparation, and did not consider the release of the preparation in the stomach; the patent application number is CN03117321.7 (name: piperazine ferulic acid slow and controlled release preparation, applicant: Li Hongjie, application date: February 21, 2003 The piperazine ferulic acid sustained and controlled release agent mentioned in the patent of Japan just simply mentioned the ratio of the main drug and the auxiliary materials. According to the inventor's observation of the examples, the release result was not mentioned, and there was no Mention the release time; at the same time, according to the literature "Central Composite Design-Response Surface Method Optimizing the Prescription of Ferulic Acid Piperazine Sustained-release Tablets" in the Chinese Journal of Pharmaceutical Sciences, Volume 7, Issue 4, etc. The direct compression method, after experimentation, the fluidity of the granules is not very good, not suitable for large-scale production

Method used

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  • Piperazine ferulate sustained-release tablet and its preparation method
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  • Piperazine ferulate sustained-release tablet and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Weigh 150 grams of piperazine ferulic acid, 60 grams of microcrystalline cellulose (PH101), 30 grams of Starch (Starch 1500, partially pregelatinized starch) and mix evenly, and use an appropriate amount of ethanol aqueous solution with a concentration of 80% or more As a binder, it is prepared into 24-30 mesh granules, dried at 50-55°C, granulated with a 24-30 mesh screen, and then 104 grams of hypromellose (K100LV), 3 grams of magnesium stearate, and micro-powdered silica gel are added. Mix 3g evenly, measure the bulk density, press into tablets, the tablet weight is 350mg / tablet, the hardness is kept at 50-100N, and the release rate is measured.

[0041] Bulk density: 0.44g / cm 3 ;Hardness: 63.5N.

Embodiment 2

[0042] Example 2: Weigh 150 grams of piperazine ferulic acid, 40 grams of microcrystalline cellulose (PH102), 20 grams of lactose, and 35 grams of Starch (Starch 1500, partially pregelatinized starch) and mix evenly, with a concentration of more than 80%. An appropriate amount of ethanol aqueous solution is used as a binder to prepare 24-30 mesh granules, dried at 50-55 ° C, and then added with 40 grams of hypromellose (K100LV) and hypromellose ( K15M) 10 grams, 2.5 grams of magnesium stearate, and 2.5 g of micropowdered silica gel were mixed uniformly, and the bulk density was measured, and pressed into tablets, with a tablet weight of 300 mg / tablet, and the hardness was maintained at 50 to 100 N to measure the release rate.

[0043] Bulk density: 0.45g / cm 3 ; Hardness: 77.0N.

Embodiment 3

[0044] Embodiment 3: Weigh 200 grams of piperazine ferulic acid, 60 grams of microcrystalline cellulose (PH102), 35 grams of Starch (Starch 1500, partially pregelatinized starch) and mix evenly, and use an appropriate amount of ethanol aqueous solution with a concentration of more than 80% as The adhesive is prepared into 24-30 mesh granules, dried at 50-55°C, granulated with a 24-30 mesh screen, and then 34 grams of hypromellose (K100LV) and 15 grams of hypromellose (K4M) are added , 4 grams of magnesium stearate, 3 grams of micro-powdered silica gel, mix evenly, measure the bulk density, press the tablet, the tablet weight is 350mg / tablet, the hardness is kept at 50-100N, and the release rate is measured.

[0045] Bulk density: 0.45g / cm 3 ; Hardness: 65.0N.

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Abstract

The invention describes a piperazine ferulate sustained-release tablet and its preparation method. The piperazine ferulate sustained-release tablet consists of piperazine ferulate, a framework material, a diluent, a lubricant, an adhesive, and optionally a coating material. In the invention, starch1500 (shanda in Chinese) is added into the diluent to improve the release of the sustained-release preparations. Meanwhile, a strict preparation process is employed so as to make the tablet of the invention reach a release result approximate to human in vivo release. With simple analysis of dissolution and release, the tablet and its preparation method are suitable for large scale production. According to a rotating basket method for in vitro drug release of sustained-release preparations in the 2010 edition of Chinese pharmacopoeia, in 900ml of water, the release rate of the tablet in the invention can be 25-35% accumulatively in 2h, 45-60% in 4h, 60-75% in 6h, and over 90% in 12h. A detailed study of the in vitro release result of the tablet indicates that the piperazine ferulate sustained-release tablet reaches good sustained-release effects and can have delayed release within 12h, so that the medicine taking time can be reduced.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a sustained-release tablet preparation and a preparation method thereof. Background technique [0002] Piperazine ferulate is white or off-white flaky crystal or crystalline powder, odorless, slightly astringent taste. This drug is slightly soluble in water, very slightly soluble in ethanol, and almost insoluble in chloroform. Piperazine ferulic acid is usually artificially obtained by separating ferulic acid from the traditional Chinese medicine Angelica and Ligusticum Chuanxiong. The structural formula is: [0003] [0004] Piperazine ferulate, also known as Baoshenkang, has the functions of anticoagulation, antiplatelet aggregation, dilating microvessels, increasing coronary flow, and relieving vasospasm. It is mainly used clinically to treat glomerular diseases caused by various causes, such as even Inflammation, chronic nephritis, nephrotic syndrome, early uremia, coronar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/495A61K31/192A61K47/36A61P13/12A61P9/10A61P7/02A61P9/00
Inventor 阮建山张存国车大庆
Owner 浙江四维医药科技有限公司
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