Fentanyl double-layer buccal tablet and preparation method thereof

A buccal tablet and fentanyl citrate technology, applied in the field of fentanyl double-layered buccal tablet and its preparation, can solve the problems of short analgesic effect, can not fully meet the needs of analgesia and the like, and achieve convenient use Effect

Inactive Publication Date: 2013-10-09
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Fentora has a rapid onset of action, and the effective blood concentration can be reached within 10-15 minutes, but its analgesic effect is short-lived and cannot fully meet the needs of analgesia

Method used

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  • Fentanyl double-layer buccal tablet and preparation method thereof
  • Fentanyl double-layer buccal tablet and preparation method thereof
  • Fentanyl double-layer buccal tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1: the preparation of fentanyl bilayer buccal tablet

[0043] Outer immediate release layer formula:

[0044] Fentanyl citrate (1.5mg / tab), mannitol (90.5mg / tab), sodium bicarbonate (42mg / tab), sodium carbonate (20mg / tab), citric acid (30mg / tab), Ac- Di-Sol Addison Croscarmellose Sodium (CMC-Na) (6mg / tab), Magnesium Stearate (4mg / tab), Macrogol PEG4000 (5mg / tab), Iron Oxide Red (1mg / tab), Stevia Glycosides (5mg / tab), the total amount is 200mg / tab.

[0045] Inner slow-release layer formula: fentanyl citrate (3.0mg / tab), mannitol (90mg / tab), hypromellose HPMC K4M (42mg / tab), HPMC K15M (20mg / tab), lactose (30mg / tab), magnesium stearate (4mg / tab), iron oxide red (1mg / tab), stevioside (5mg / tab), the total amount is 200mg / tab.

[0046] Among the above components, iron oxide red can be replaced by carotene or limonene; stevioside can be replaced by aspartame, apple essence, orange essence or banana essence.

[0047] Each component was crushed through a 100-m...

Embodiment 2

[0048] Embodiment 2: the preparation of fentanyl bilayer buccal tablet

[0049] Outer immediate release layer formula:

[0050] Fentanyl citrate (1.5mg / tab), mannitol (45mg / tab), sodium bicarbonate (21mg / tab), citric acid (15mg / tab), sodium carbonate (10mg / tab), starch lactose compound STARLAC (3mg / tab), magnesium stearate (2mg / tab), carbopol 934NF (3mg / tab), iron oxide red (0.5mg / tab), stevioside (2mg / tab), total 100mg / tab.

[0051] Inner sustained-release layer formula:

[0052] Fentanyl citrate (3.0mg / tab), mannitol (45mg / tab), hypromellose HPMC K15M (20mg / tab), HPMC K4M (11mg / tab), lactose (15mg / tab), hard Magnesium fatty acid (2mg / tab), iron oxide red (0.5mg / tab), stevioside (2mg / tab), total 100mg / tab.

[0053] Use dry powder or wet compression method, firstly pre-compress the sustained-release granules, adjust the tablet weight and pre-compression pressure at 1-10kg / cm 2 , and then add immediate-release layer particles for compression to obtain a double-layer buc...

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PUM

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Abstract

The invention discloses a fentanyl double-layer buccal tablet and a preparation method thereof. The buccal tablet is composed by a quick release layer (an outer layer) and a sustained release layer (an inner layer) which form a biphasic drug release system. The quick release layer is prepared by effervescence and cyclodextrin inclusion technologies, a transient change of a pH value happens around the tablet by utilizing an effervescence reaction, and the quick release layer rapidly disintegrates and releases fentanyl in a few minutes; the sustained release layer slowly releases drugs to maintain an effective plasma concentration for up to a few hours. The buccal tablet releases the drugs from fast to slow, maintains the effective plasma concentration for a long time, is easy to use, is safe and reliable, and has the characteristics of rapid and continuous analgesia.

Description

technical field [0001] The invention belongs to the technical field of analgesics, and relates to a fentanyl double-layer buccal tablet and a preparation method thereof. Background technique [0002] Pain is one of the most common and direct body damages caused by injuries and weapons of war, which seriously affects the quality of life of patients. As a highly selective μ opioid receptor agonist, fentanyl has an analgesic effect 100 times that of morphine. It is less addictive, has a fast onset of action, and easily penetrates the blood-brain barrier. Pain and other sharp pains. About 80% of fentanyl is metabolized within 30 minutes after injection, and repeated administration is required to maintain effective blood drug concentration; while skin patches release slowly and take effect after 20-48 hours, suitable for chronic dull pain treatment . [0003] The fentanyl oromucosal administration preparation (trade name: ACTIQ) launched by Cephalon Corporation of the United S...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/4468A61P29/00A61P25/04
Inventor 吴红罗晓星范黎乔友备
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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