Oral sustained-release preparation of hydroxypiperidone

A technology for hydroxypiperidine and sustained-release preparations, which is applied in the field of medicine, can solve the problems of long interval between taking medicines at night, cannot maintain blood drug concentration, and treat blind spots, etc., and can meet the slow-release release effect, reduce the number of times of taking medicines, and be convenient to take. Effect

Active Publication Date: 2019-09-20
普霖贝利生物医药研发(上海)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The number of daily oral administration by patients is more troublesome, and it is prone to missed doses and too long intervals between doses taken at night, which cannot maintain effective blood drug concentration and exert a sustained therapeutic effect, resulting in blind spots in treatment

Method used

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  • Oral sustained-release preparation of hydroxypiperidone
  • Oral sustained-release preparation of hydroxypiperidone
  • Oral sustained-release preparation of hydroxypiperidone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Embodiment 1 (single-layer matrix sustained-release tablet)

[0072] This embodiment is a common single-layer matrix sustained-release tablet of piperaperone, and the composition and content of its drug layer are as shown in Table 1:

[0073] Table 1

[0074]

[0075]

[0076] Preparation Process:

[0077] 1. Take the prescribed amount of piperidone hydrochloride, hydroxypropyl methylcellulose, sodium carmellose, microcrystalline cellulose and pregelatinized starch and mix evenly;

[0078] 2. Use 5% PVPK30 aqueous solution to make soft materials, and pass through a 2.0mm screen to make wet granules;

[0079] 3. The obtained wet granules are dried in a fluidized bed until the water content is less than 2%.

[0080] 4. After passing the dry granules through a 1.2mm sieve for granulation, mix them with the prescribed amount of magnesium stearate, and compress them into tablets. The theoretical tablet weight is 150mg.

[0081] Release test, adopt Chinese Pharmacop...

Embodiment 2

[0083] Embodiment 2 (double-layer matrix sustained-release tablet)

[0084] The present embodiment is a double-layer matrix sustained-release tablet of piperidone, and the composition and content of the drug layer are as shown in Table 2:

[0085] Table 2

[0086]

[0087]

[0088] The composition and content of the barrier layer of the dipiprone double-layer matrix sustained-release tablet are as shown in Table 3:

[0089] table 3

[0090] components Dosage (mg) lactose monohydrate 47.7 yellow iron oxide 0.3 Hydroxypropyl Methyl Cellulose (HPMC, K4M) 60 Glyceryl behenate 37.5 Polyvinylpyrrolidone (PVP, K30) 3 Magnesium stearate 1.5 Total 150

[0091] The preparation process of the drug layer of the bilayer matrix sustained-release tablet of piperidone:

[0092] 1. Take the prescribed amount of piperidone hydrochloride, hydroxypropyl methylcellulose, sodium carmellose, lactose monohydrate and glyceryl behenate ...

Embodiment 3

[0105] Embodiment 3 (three-layer matrix sustained-release tablet)

[0106] This example is a three-layer matrix sustained-release tablet of piperaperone with different hydroxypropylmethylcellulose contents, and the composition and content of the drug layer are as shown in Table 4:

[0107] Table 4

[0108]

[0109] The preparation process of the drug layer of the three-layer matrix sustained-release tablet of piperidone: the same as in Example 2.

[0110] The composition and preparation process of the barrier layer of the three-layer matrix sustained-release tablet of piperaperone: the same as in Example 2.

[0111] Tablets:

[0112] The above-prepared drug layer granules and barrier layer granules were pressed into a three-layer tablet. The first layer was composed of a 150 mg barrier layer, the second layer was composed of a 150 mg drug layer, and contained 20 mg of piperapidone, and the third layer was composed of 150 mg of barrier layer composition.

[0113] Coating...

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Abstract

The invention discloses an oral sustained-release preparation of hydroxypiperidone. The sustained-release preparation comprises the following components: hydroxypiperidone or a pharmaceutically acceptable salt thereof, one or more pharmaceutically acceptable excipients, and at least one polymer with a sustained-release effect. According to the invention, the medicinal high-molecular material is selected as the sustained-release material, and an in-vitro release test result shows that the provided sustained-release hydroxypiperidone tablet gradually releases drugs within 8-24 hours, so that the peak-valley phenomenon of drug absorption is reduced, the blood concentration required by treatment is maintained, compared with a common tablet, the oral sustained-release preparation of the hydroxypiperidone has the advantages that purposes of reduction of the administration times, lasting effect and convenience in administration can be achieved, and the sustained-release preparation is beneficial to treatment of diseases.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to oral sustained-release preparations of piperidone. Background technique [0002] Depression is a syndrome caused by various reasons with persistent low mood, loss of interest, and slow thinking as the main clinical features. The characteristics of poor identification, low medical visits, and low treatment rates seriously endanger human physical and mental health. With the continuous acceleration of the pace of life, people's mental pressure is gradually increasing. Depression has become a common and frequently-occurring disease in modern society, and its incidence is increasing year by year. [0003] Currently, drug therapy is one of the main means of depression treatment. Clinically commonly used antidepressants, including 5-HT reuptake inhibitors (SSRIs, such as fluoxetine), 5-HT / NE dual reuptake inhibitors (SNRIs, such as duloxetine), etc., all have delayed ons...

Claims

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Application Information

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IPC IPC(8): A61K9/24A61K47/38A61K47/14A61K31/4545A61P25/24
CPCA61K9/2013A61K9/2054A61K9/2086A61K31/4545A61P25/24
Inventor 郑珊珊邱宏春龚欢谢媛媛包圆圆姜孟寅郭晓迪谭丽阮舒恬
Owner 普霖贝利生物医药研发(上海)有限公司
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