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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: 2015-06-03
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] Example 1: Preparation of Fentanyl Bilayer Buccal Tablets

[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 Eddie Su Croscarmellose sodium (CMC-Na) (6mg / tab), magnesium stearate (4mg / tab), polyethylene glycol PEG4000 (5mg / tab), red iron oxide (1mg / tab), stevia glycosides (5mg / tab), total 200mg / tab.

[0045] Inner sustained-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), red iron oxide (1mg / tab), stevioside (5mg / tab), total 200mg / tab.

[0046] Among the above components, red iron oxide can be replaced by carotene or limonin; stevioside can be replaced by asparagine phenylalanine methyl ester, apple essence, orange essence or banana essence.

[0047] Each component is pulverized and...

Embodiment 2

[0048] Example 2: Preparation of Fentanyl Bilayer Buccal Tablets

[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 complex STARLAC (3mg / tab), magnesium stearate (2mg / tab), carbopol 934NF (3mg / tab), red iron oxide (0.5mg / tab), stevioside (2mg / tab), total 100mg / tab.

[0051] Inner slow-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), red iron oxide (0.5mg / tab), stevioside (2mg / tab), total 100mg / tab.

[0053] Using dry powder or wet tableting, pre-compress the slow-release granules first, and adjust the tablet weight and pre-compression pressure to 1-10kg / cm 2 , and then adding the immediate-release layer granules for compression to obtain a double-layer oral buccal tablet ...

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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 analgesic drugs, 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 that is 100 times that of morphine. It is less addictive, has rapid onset of action, and is easy to pass through 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 the effective blood drug concentration; while the skin patch releases the drug slowly and takes effect after 20-48 hours, which is suitable for the treatment of chronic dull pain . [0003] The oral and mucosal fentanyl preparations (trade name: ACTIQ) marke...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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