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Melatonin orally disintegrating tablet and preparation method thereof

A technology of orally disintegrating tablets and melatonin, which is applied in pharmaceutical formulations, medical preparations containing active ingredients, drug delivery, etc., can solve problems that have not been reported yet, and achieve improved bioavailability and short production cycles , low-cost effect

Inactive Publication Date: 2008-03-19
徐贵丽 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, making melatonin into orally disintegrating tablets has extensive clinical significance and market prospects, but there are no related reports in the prior art.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Weigh 3 parts of melatonin, 6 parts of microcrystalline cellulose (SMCC), 8 parts of cross-linked polyvinylpyrrolidone (PVPP), 8.18 parts of sodium bicarbonate (NaHCO3), 9.82 parts of sodium citrate, 2.5 parts of lemon flavor, 0.75 parts of aspartame, 2 parts of magnesium stearate, 59.75 parts of mannitol for use. Grind the raw materials separately, pass through an 80-mesh sieve, and dry at 50°C. Use the equal volume addition method to mix the raw materials evenly and pass through a 60-mesh sieve; use the direct compression method to weigh the mixed powder Compression into tablets, the average tablet weight is set to 100mg, namely melatonin orally disintegrating tablets.

[0029] After testing, the hardness of the disintegrating tablet is between 14 and 16 Newtons; the disintegration time in the body is between 25 and 28 seconds; the dissolution amount in artificial gastric juice and intestinal juice at 37°C in 1 minute is 40%, and the dissolution rate in 6 minutes is up to...

Embodiment 2

[0031] Weigh 3 parts of melatonin, 3 parts of microcrystalline cellulose (SMCC), 13 parts of cross-linked polyvinylpyrrolidone (PVPP), 10 parts of sodium bicarbonate (NaHCO3), 12 parts of sodium citrate, 2.5 parts of lemon flavor, 0.75 parts of aspartame, 2 parts of magnesium stearate, 53.75 parts of mannitol for use. Grind each raw material separately, pass 80 mesh sieve, dry at 60℃, use equal volume addition method to mix the raw materials evenly, pass 60 mesh sieve; adopt direct compression method, weigh the mixed powder Compression into tablets, the average tablet weight is set to 100mg, namely melatonin orally disintegrating tablets.

[0032] After testing, the hardness of the disintegrating tablet is between 14 and 16 Newtons; the disintegration time in the body is between 28 and 30 seconds; the amount of dissolution in artificial gastric juice and intestinal juice at 37℃ in 1 minute is 30%, and the amount of dissolution in 6 minutes is up to 81%.

Embodiment 3

[0034] Weigh 3 parts of melatonin, 9 parts of microcrystalline cellulose (SMCC), 5 parts of cross-linked polyvinylpyrrolidone (PVPP), 8.18 parts of sodium bicarbonate (NaHC03), 9.82 parts of sodium citrate, 2 parts of lemon flavor, 1.25 parts of aspartame, 2 parts of magnesium stearate, 59.75 parts of mannitol for use. Grind the raw materials separately, pass through an 80 mesh sieve, and dry at 70 ℃. Use equal volume addition method to mix the raw materials uniformly and pass through a 60 mesh sieve; use the direct compression method to weigh the mixed powder Compression into tablets, the average tablet weight is set to 100mg, namely melatonin orally disintegrating tablets.

[0035] After testing, the hardness of the disintegrating tablet is between 14 and 16 Newtons; the disintegration time in vivo is between 24 and 28 seconds; the amount of dissolution in artificial gastric juice and intestinal juice at 37°C in 1 minute is 35%, and the amount of dissolution in 6 minutes is up t...

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PUM

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Abstract

The invention discloses an oral disintegrating tablet of melatonin which is made by selecting the melatonin, a disintegrator, an effervescing agent, a filling agent, an odor corrective and a lubricating agent for smashing, drying, mixing and tablet forming. The drug can be promptly disintegrated inside the mouth without water and is especially applicable to the patients with the deglutition difficulty or under the special environment, such as the elder, the children, the narcose patient etc. The drug also has good effect when used in the environment, which lacks the water, such as the outdoors, the battle field etc. The invention has simple technology and cheap cost and is provided with the advantages of short production period, simple production equipment etc. The oral disintegrating tablet which is prepared by the method of the invention has the enough rigidity to meet the requirements of the production, the packaging, the storage and the transportation, and at the same time the oral disintegrating tablet has good taste and short disintegrating time, and the inside-body disintegrating time is less than thirty seconds; the dissolved quantity inside the 37 DEG C artificial gastric juice and intestinal juice within one minute is 40 percent, and the dissolved quantity within six minutes is as high as 90 percent.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical production, and specifically relates to a melatonin orally disintegrating tablet and a preparation method thereof. Background technique [0002] Insomnia is a common sleep disorder characterized by difficulty falling asleep and maintaining sleep. Long-term insomnia will seriously affect people's normal life, work and study. At present, insomnia is caused by mental stress, busy work and study, long-term irregular rest and sleep, poor environment, family conflicts, disharmony in interpersonal relationships, various setbacks in life, and long-term psychological conflicts and negative emotional experiences caused by trauma. More and more patients. [0003] Melatonin, whose chemical name is N-acetyl-5-methoxytryptamine, is an indole hormone secreted by the pineal gland of mammals. It has the pharmacological effects of anti-stress, anti-lipid peroxidation, anti-aging, inducing sleep, enhancing immunit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/46A61K31/4045A61P25/20
Inventor 徐贵丽贺建昌顾胜华张青王慧敏
Owner 徐贵丽
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