Zolpidem tartrate time-selecting pulse sustained-release pellet and preparation method thereof

A technology of zolpidem tartrate and pellets, which is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of unsatisfactory drug release rate, technological difficulty and slow drug release rate. and other problems, to achieve the effect of easy industrial production, simple preparation process, and reduction of the amount of auxiliary materials

Inactive Publication Date: 2013-08-07
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN101269056A and CN101269059A have introduced a kind of preparation method of pulse micropill, and its basic structure is respectively from the inside to the outside the medicine-containing quick-release ball core, basic layer, hysteresis layer, wherein the hysteresis layer contains polyacrylic acid resin III, yet this technology The prepared pulse pellets released the drug completely after 3 hours of time lag, and the drug release rate was slow
However, in order to achieve the time delay, the outer layer of the pellets needs to be coated with a layer of water-insoluble polymer material, so it is difficult to obtain a pulse-like rapid release after the time delay.
The release rate of the time-lag of the usual technology is often unsatisfactory. The published data is generally >80% of the drug release within 2 hours after the time-lag, or >90% of the drug release within 3 hours after the time-lag. The purpose of the invention is to overcome the deficiencies of the above-mentioned technologies, and provide a time-selective immediate-release preparation, that is, the drug release amount >90% within 1 hour of the preparation after 4 hours

Method used

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  • Zolpidem tartrate time-selecting pulse sustained-release pellet and preparation method thereof
  • Zolpidem tartrate time-selecting pulse sustained-release pellet and preparation method thereof
  • Zolpidem tartrate time-selecting pulse sustained-release pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Drug-containing immediate-release pill core prescription:

[0041]

[0042] Preparation process: After mixing zolpidem tartrate and poloxamer 188, transfer it to a 60% ethanol solution of polyvinylpyrrolidone K30 and keep stirring. A fluidized bed is used to apply the drug by means of bottom spraying, and fluidized drying is continued at 40° C. for 2 hours after the drug application is completed, to obtain drug-containing pellets.

[0043] Swelling layer prescription:

[0044] CC-Na 8.5g

[0045] L-HPC 14.0g

[0046] Polyvinylpyrrolidone K90 3.0g

[0047] Preparation process: Disperse croscarmellose sodium and low-substituted hydroxypropyl cellulose in water, dissolve polyvinylpyrrolidone K90 in ethanol, and mix the two solutions to obtain a swelling layer coating solution. Fluidized bed coating is adopted, and a swelling layer is coated on the drug-loaded pellet core by a side spraying process.

[0048] Lag Layer Prescription:

[0049] Ethyl cellulose aqueous ...

Embodiment 2

[0052] Drug-containing immediate-release pill core prescription:

[0053]

[0054] Swelling layer prescription:

[0055] CC-Na 7.5g

[0056] L-HPC 16.0g

[0057] Polyvinylpyrrolidone K90 3.0g

[0058] Lag Layer Prescription:

[0059] Ethyl cellulose aqueous dispersion Surelease (based on solid content) 26.0g

[0060] The preparation method is the same as in Example 1.

Embodiment 3

[0062] Drug-containing immediate-release pill core prescription:

[0063]

[0064] Swelling layer prescription:

[0065] CC-Na 7.0g

[0066] L-HPC 17.0g

[0067] Polyvinylpyrrolidone K90 4.0g

[0068] Lag Layer Prescription:

[0069] Ethyl cellulose aqueous dispersion Surelease (based on solid content) 25g

[0070] Preparation process: with embodiment 1.

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Abstract

The invention relates to the field of medical preparations, in particular to a zolpidem tartrate time-selecting pulse sustained-release pellet and a preparation method thereof. The pellet sequentially comprises a blank pill core, a medicine layer, a swelling layer and a time-lag layer from inside to outside, wherein the medicine layer comprises zolpidem tartrate, a surfactant and a binder. The swelling layer consists of two swelling materials. The time-lag layer is an ethyecellulose aqueous dispersion coating. Compared with the conventional technology, the preparation method has the advantages that stable 4 hours time lag and quicker pulse release of the pellet are provided, wherein the medicine release amount within one hour after lag-time is greater than 90%, so that the early awakening patient can be effectively prevented from waking up before dawn, and meanwhile, the residual effect in the next day can be avoided. The auxiliary material used in the preparation method of the pellet is easily available, and the production process is simple and easy to operate, so that the pellet is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a preparation composition of zolpidem tartrate timed pulse controlled-release pellets and a preparation method of the preparation. Background technique [0002] Insomnia is a common psychological and physical disease that seriously affects people's daily life. Symptoms of insomnia generally include difficulty falling asleep, shallow sleep, easy awakening, and early awakening. Among them, early awakening refers to the phenomenon of waking up 2 to 3 hours earlier than normal and unable to fall asleep again. At present, there is no drug for treating early awakening in clinical practice, because the effective time of sleeping pills is generally 4-6 hours. Taking the medicine before going to bed routinely will not be effective in treating early awakening symptoms. This is also a gap in the treatment of sleep disorders. If you take hypnotics with slow-release effect to prol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K47/38A61K31/437A61P25/20
Inventor 宗莉王扣存张文晶谭震
Owner CHINA PHARM UNIV
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