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High bioavailability proton pump inhibitor sustained-release technique

A proton pump inhibitor and glycoprotein inhibitor technology, applied in the field of medicine, can solve the problems of high bioavailability and long-term effect, short drug release time, low bioavailability, etc., to reduce adverse reactions and facilitate quality The effect of controlling and reducing the frequency of taking medicine

Inactive Publication Date: 2009-08-19
涂家生
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Enteric-coated preparations have the following disadvantages: (1) slow onset of action, which delays the initial inhibitory effect of the drug; (2) low bioavailability (30-40%); (3) acid breakthrough at night, and it is necessary to take the preparation before going to bed
Immediate release preparations have the following disadvantages: (1) The drug release time is short; (2) The bioavailability is not high; (3) The acid breaks through at night, and the preparation needs to be taken before going to bed
Our research found that, taking omeprazole as an example, its rapid onset of action cannot be unified with high bioavailability and long-term effect
If omeprazole wants to take effect quickly, it must be quickly dissolved in the gastric juice. At this time, it is easy to hydrolyze. It has been marketed in the United States, but long-term use has the disadvantages of producing a large amount of gas, patient discomfort, and sodium poisoning

Method used

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  • High bioavailability proton pump inhibitor sustained-release technique
  • High bioavailability proton pump inhibitor sustained-release technique
  • High bioavailability proton pump inhibitor sustained-release technique

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Preparation of omeprazole sustained-release pellets (containing TPGS)

[0047] The prescription is (per 1000 capsules):

[0048] Omeprazole 20g

[0049] Blank ball core 80g

[0050] TPGS 2g

[0051] Magnesium oxide 1.5g

[0052] Hydroxypropyl Cellulose 2g

[0053] Absolute ethanol 250mL

[0054] Titanium dioxide 0.75g

[0055] Hypromellose 3.75g

[0056] Surelease Water Dispersion (Colorcon) 60g

[0057] Distilled water 150g

[0058] Add the prescribed amount of hydroxypropyl cellulose into absolute ethanol, stir until dissolved, add magnesium oxide to disperse in the liquid, continue stirring for 2 hours, and pass through a 60-mesh sieve to obtain the adhesive. Put the pellets into the coating pan with a rotating speed of 100rpm, and apply the drug by powder layering method until the theoretical drug loading reaches 20%. The finished product is dried at 40°C, and the pellets between 700 and 900 μm are sieved to obtain drug-containing pellets.

[0059] Take t...

Embodiment 2

[0062] Preparation of omeprazole sustained-release enteric-coated pellets

[0063] The prescription is (per 1000 capsules):

[0064] Omeprazole 20g

[0065] Blank ball core 80g

[0066] Magnesium oxide 1g

[0067] TPGS 1g

[0068] Hydroxypropyl Cellulose 1g

[0069] Absolute ethanol 250mL

[0070] Titanium dioxide 0.5g

[0071] Hypromellose 2.5g

[0072] Surelease Water Dispersion (Colorcon) 50g

[0073] Distilled water 125g

[0074] Aqueous dispersion of acrylic resin: 70g

[0075] TEC: 2g

[0076] Distilled water 140g

[0077] Add the prescribed amount of hydroxypropyl cellulose into absolute ethanol, stir until dissolved, add magnesium oxide to disperse in the liquid, continue stirring for 2 hours, and pass through a 60-mesh sieve to obtain the adhesive. Put the pellets into the coating pan with a rotating speed of 100rpm, and apply the drug by powder layering method until the theoretical drug loading reaches 20%. The finished product is dried at 30°C, and the ...

Embodiment 3

[0082] Preparation of omeprazole sustained-release pellets

[0083] The prescription is (per 1000 capsules):

[0084] Omeprazole 20g

[0085] Blank ball core 80g

[0086] Magnesium oxide 3g

[0087] Hydroxypropyl Cellulose 3g

[0088] Absolute ethanol 250mL

[0089] Titanium dioxide 1.5g

[0090] Hypromellose 5g

[0091] Surelease Water Dispersion (Colorcon) 80g

[0092] Distilled water 175g

[0093] Add the prescribed amount of hydroxypropyl cellulose into absolute ethanol, stir until dissolved, add magnesium oxide to disperse in the liquid, continue stirring for 2 hours, and pass through a 60-mesh sieve to obtain the adhesive. Put the pellets into the coating pan with a rotating speed of 100rpm, and apply the drug by powder layering method until the theoretical drug loading reaches 20%. Dry at 40°C, and sieve the pellets between 700 and 900 μm to obtain drug-containing pellets.

[0094] Take the prescribed amount of Surelease aqueous dispersion coating solution, take...

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Abstract

The invention discloses proton pump inhibitor slow-release technology with high bioavailability. A micropill is prepared from a drug-containing pill core coated slow-release coating. The micropill has the advantages of higher bioavailability, good slow-release property, convenient use, low medicine taking frequency and more stable blood drug concentration, and can avoid the acid breakthrough at night and lower untoward reactions.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a digestive system medicine proton pump inhibitor slow-release pellet preparation and its preparation technology, belonging to the technical field of medicine. Background technique [0002] With the constant changes in the living environment and lifestyle, the incidence of digestive system diseases has always been among the top: peptic ulcer and Helicobacter pylori (HP) infection, gastroesophageal reflux disease (GERD), upper gastrointestinal bleeding, Zhuo-Ai Syndrome (ZES) etc. Proton pump inhibitors (PPIs) have become the main drug for the treatment of gastric acid-related diseases. Its advantage is that it can more directly inhibit the final stage of gastric acid secretion, and its curative effect is significantly better than that of other acid-suppressing agents. At the same time, it solves many problems such as tolerance. Proton pump inhibitors include omeprazole, lansopraz...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/48A61K31/4439A61K31/4184A61K47/42A61P1/04A61K47/38A61K47/34A61K47/22
Inventor 涂家生吴建梅姜斌余裕炳
Owner 涂家生
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