Camostat mesilate orally disintegrating tablet, and preparation method and new application thereof

A technology of camostat mesylate and orally disintegrating tablets, which is applied in the field of camostat mesylate orally disintegrating tablets and its preparation, and can solve problems such as difficulty in swallowing tablets, burning pain in the digestive tract, and high incidence of stomatitis , to achieve the effects of good promotion prospects, easy swallowing, and simple and easy preparation process

Active Publication Date: 2015-04-08
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Because patients with acute exacerbation of chronic pancreatitis often have different degrees of abdominal pain and vomiting, patients with postoperative reflux esophagitis may easily cause burning pain in the digestive tract when swallowing tablets orally, and patients with stomatitis caused by chemotherapy have difficulty swallowing tablets due to oral ulcers , and the incidence of stomatitis in chemotherapy patients is extremely high, so it is necessary to develop an orally disintegrating camostat mesylate tablet that is more easily accepted by patients with the above diseases. Sestat orally disintegrating tablet, its preparation method, and its new application in oral mucositis have no published literature reports

Method used

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  • Camostat mesilate orally disintegrating tablet, and preparation method and new application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] prescription:

[0032] Camostat Mesylate 20% Mannitol (Pearlitol 200 SD) 45% Sorbitol 5% Optimized Microcrystalline Cellulose (Prosolv 50) 17% Cross-linked polyvinylpyrrolidone (PVPP) 5% aspartame 2% lemon zest 2% Micropowder silica gel 3% Magnesium stearate 1%

[0033] Preparation: Grind cross-linked polyvinylpyrrolidone, aspartame, and lemon essence separately and pass through a 80-mesh sieve, and camostat mesylate pass through a 100-mesh sieve, and mix the three evenly; microcrystalline cellulose, sorbitol and mannitol Pass through a 40-mesh sieve, weigh them according to the amount, and add them to the mixed drug in step 1 in the above order and mix them evenly; then add the prescribed amount of micropowder silica gel and magnesium stearate and mix evenly, and measure the content of the intermediates to determine the content of the tablets. After re-weighting, use direct compression technology to compress...

Embodiment 2

[0035] prescription:

[0036] Camostat Mesylate 10% Mannitol (Pearlitol 50 C) 70% Sorbitol 10% Povidone (PVP-K30) 1% Cross-linked polyvinylpyrrolidone (PVPP) 6% aspartame 1% lemon zest 1% Magnesium stearate 1%

[0037] Preparation: Grind camostat mesylate, mannitol, sorbitol, cross-linked polyvinylpyrrolidone, aspartame, and lemon flavor in half of the prescription amount, respectively, and pass through a 100-mesh sieve, and mix evenly; add 2% povidone in 50% ethanol aqueous solution to prepare soft material, pass through 20 mesh sieve to granulate, dry in an oven at 40-60°C until the water content of the granules is between 2% and 4%, and the dry granules pass through 24 mesh Sieve for granulation; add magnesium stearate and the remaining amount of cross-linked polyvinylpyrrolidone to the obtained dry granules, after mixing, carry out intermediate content determination, determine the weight of the tablet, and then press ...

Embodiment 3

[0039] prescription:

[0040] Camostat Mesylate 15% Mannitol (Pearlitol 50 C) 57.2% Lactose (Granulac200) 14.3% Hydroxypropyl Cellulose (HPC-L) 2% Croscarmellose Sodium (CMC-Na) 8% aspartame 2% lemon zest 1% Magnesium stearate 0.5%

[0041] Preparation: Grind camostat mesylate, mannitol, lactose, croscarmellose sodium, aspartame, and lemon flavor in half of the prescription amount, respectively, and pass through a 100-mesh sieve, and mix evenly; the obtained mixed drug Add 2% hydroxypropyl cellulose and 25% ethanol aqueous solution to prepare soft material, pass through a 20 mesh sieve to granulate, and dry in an oven at 40-60°C until the water content of the granules is between 2% and 4%. The granules are passed through a 24-mesh sieve for granulation; magnesium stearate and the remaining amount of croscarmellose sodium are added to the obtained dry granules, after mixing, the content of intermediates is determined, and ...

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Abstract

The invention discloses an orally disintegrating camostat mesylate tablet, a preparation method thereof and a new application thereof. The orally disintegrating tablet contains 10% to 30% of the main drug camostat mesylate, 40% to 70% of a filler, 0% to 20% of a binder, and 2% to 10% of a disintegrant in parts by weight. %, flavoring agent 2%-8%, glidant 0%-5%, lubricant 0.5%-2.5%; the preparation can be prepared by wet granulation or powder direct compression. The present invention provides an orally disintegrating tablet of camostat mesylate, which is convenient to take, has a good taste, and has a rapid effect on indications. Improve the patient's medication compliance. Meanwhile, the product prepared by the present invention can be used for the existing indications such as acute exacerbation of chronic pancreatitis and postoperative reflux esophagitis. Research has found that it also has anti-inflammatory effects on oral mucositis caused by chemotherapy. New therapeutic uses.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an orally disintegrating camostat mesylate tablet, a preparation method thereof and a new application thereof. Background technique [0002] Camostat mesilate (Camostat Mesilate) chemical name is dimethylcarbamoylmethyl 4-(4-guanidinobenzyloxy) phenylacetic acid mesylate, which is a synthetic non-peptide protease inhibitor. It can relieve the acute attack of chronic pancreatitis and improve the symptoms of postoperative reflux esophagitis. After oral administration, this product quickly acts on the body's kinin system, fibrinolytic system, coagulation system and complement system, immediately blocks the activity of related enzymes and inhibits their abnormal hyperactivity, thereby relieving the symptoms and pain of chronic pancreatitis and improving amylase. value. In addition, it can improve postoperative reflux esophagitis by inhibiting trypsin in the re...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/245A61K47/26A61P1/02A61P1/18A61P1/04
Inventor 王志钢胡延臣刘莱刘玉静杨青松张伟强
Owner BEIJING TIDE PHARMA
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