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Timing pulsed release micro-pill of zolpidem salt

A zolpidem tartrate and micropellet technology, which is applied in pharmaceutical formula, drug combination, drug delivery, etc., can solve the problems of long release time, short half-life, short action time, etc., to improve permeability, regulate release, and promote water absorption. chemical effect

Inactive Publication Date: 2009-11-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Zolpidem belongs to short-acting hypnotics, its half-life is short, and its action time is short. Taking zolpidem or its salt before going to bed with ordinary preparations cannot effectively control the occurrence of early awakening
For sustained-release formulations or biphasic release formulations, early-awakening patients who do not have difficulty falling asleep do not need drugs to help them fall asleep. At the same time, sustained-release formulations prolong the effect of the drug because of their longer release time, which may cause patients to feel dizzy the next day Symptoms affecting normal work and life

Method used

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  • Timing pulsed release micro-pill of zolpidem salt
  • Timing pulsed release micro-pill of zolpidem salt
  • Timing pulsed release micro-pill of zolpidem salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Prescription: g

[0050] Blank core: sucrose and starch 51.6

[0051] Drug Layer: Zolpidem Tartrate 7.5

[0052] Polyvinylpyrrolidone K30 0.5

[0053] Organic acid layer: succinic acid 0.8

[0054] Citric acid 0.4

[0055] Polyvinylpyrrolidone K30 0.2

[0056] Lag layer: Eudragit RS30D (according to solid content) 22.9

[0057] Triethyl citrate 4.5

[0058] 1000 mesh superfine talcum powder 11.6

[0059] Preparation:

[0060] Dissolve the drug in 2% (g / ml) polyvinylpyrrolidone K30 aqueous solution as the drug application solution. Weigh blank pellet cores and place them in a fluidized bed for preheating for 10 minutes, spray the drug solution onto the blank pellet cores by bottom spraying to prepare drug-containing pellets. The drug-containing pellets were dried in an oven at 60°C for 2 hours for later use. Dissolve succinic acid and citric acid in 2% (g / ml) polyvinylpyrrolidone K30 aqueous ...

Embodiment 2

[0062] Prescription: g

[0063] Blank core: sucrose and starch 51.8

[0064] Drug Layer: Zolpidem Hemi-Tartrate 7.6

[0065] Polyvinylpyrrolidone K30 0.5

[0066] Organic acid layer: succinic acid 0.9

[0067] Citric acid 0.4

[0068] Polyvinylpyrrolidone K30 0.2

[0069] Lag layer: Eudragit RS30D (according to solid content) 22.6

[0070] Triethyl citrate 4.5

[0071] 1000 mesh superfine talcum powder 11.5

[0072] Preparation method: with embodiment 1.

Embodiment 3

[0074] Prescription: g

[0075] Blank core: sucrose and starch 52

[0076] Organic acid layer: succinic acid 2

[0077] Citric acid 0.8

[0078] Polyvinylpyrrolidone K30 0.3

[0079] Drug Layer: Zolpidem Tartrate 7.5

[0080] Polyvinylpyrrolidone K30 0.5

[0081] Lag layer: Eudragit RS30D (according to solid content) 21.7

[0082] Triethyl citrate 4.3

[0083] 1000 mesh superfine talcum powder 10.9

[0084] Preparation:

[0085]Dissolve succinic acid and citric acid in 2% (g / ml) polyvinylpyrrolidone K30 aqueous solution for later use. Weigh the blank pellet core and place it in a fluidized bed to preheat for 10 minutes, spray the organic acid solution onto the blank pellet core in the form of bottom spray to prepare organic acid-containing pellets, and dry them in an oven at 60°C for 2 hours for later use . Zolpidem tartrate was dissolved in 2% (g / ml) polyvinylpyrrolidone K30 aqueous solution, the ...

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Abstract

The invention relates to the field of pharmaceutical preparations, in particular to a timing pulsed release micro-pill of a zolpidem salt, which is characterized in that the center of the micro-pill is a blank pill core, an external time-lag layer is coated by low-permeability acrylic resin containing quaternary ammonium salt radicals, and a medicament layer and an organic acid layer are arranged between the blank pill core and the time-lag layer, wherein the organic acid layer contains a mixture of two organic acids, and the mixture of the two organic acids is prepared by mixing one of succinic acid, glutaric acid and adipic acid, and one of citric acid, malic acid and tartaric acid. Combining with sleep characteristics of early awakening crowds, the prepared micro-pill has certain release time lag and releases quickly after a period of time lag so that a patient obtains effective blood concentration on the point of awakening so as to prolong the sleep time of the patient.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a time-selected pulse-release pellet preparation of zolpidem salt. Background technique [0002] Insomnia is a common sleep disorder. With the accelerated pace of life and the aging society, sleep disorder has become a very common disease. Its symptoms generally include difficulty in falling asleep, shallow sleep, easy to wake up, early awakening, and difficulty in waking up. Falling back to sleep, and waking up tired or lacking wakefulness. Among them, early awakening refers to the phenomenon of waking up 2 to 3 hours earlier than the normal situation or more than 4 times a week, and cannot fall asleep again. Because the effective time of sleeping pills is generally 4-6 hours, taking the medicine before going to bed according to the routine will not be effective in the treatment of early awakening symptoms, which is also a blank in the treatment of sleep disorders. ...

Claims

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Application Information

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IPC IPC(8): A61K9/54A61K31/437A61K47/32A61K47/38A61P25/20
Inventor 宗莉吴瑞胡晓
Owner CHINA PHARM UNIV
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