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Slow release preparation of ranitidine

A sustained-release preparation, the technology of ranitidine, which is applied to the sustained-release preparation of ranitidine and the field of preparation thereof, can solve the problems of affecting drug efficacy, inconvenient use of patients, affecting drug blood concentration, etc. The effect of improving adaptability and reducing the frequency of medication

Inactive Publication Date: 2007-07-25
刘凤鸣
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After oral administration, it is rapidly absorbed from the gastrointestinal tract. The time to peak plasma concentration (tmax) is 1 to 2 hours, and the half-life (t1 / 2) is 2 to 3 hours. Ranitidine is a drug with a short biological half-life. The dose is 150mg, and it is generally necessary to give the medicine every 8 hours or so, which brings inconvenience to the patient. At the same time, due to the influence of factors such as sleep time, the steady-state blood drug concentration of the drug is affected, thereby affecting the efficacy of the drug.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] The preparation of embodiment 1-ranitidine sustained-release tablet (1)

[0050] Method: Take 150 grams of ranitidine, 50 grams of hydroxypropyl cellulose, 15 grams of hypromellose, 10 grams of lactose, 10 grams of microcrystalline cellulose, 1 gram of carbomer, and 30 grams of polyethylene glycol 4000 gram, mixed evenly, dry granulated, mixed with magnesium stearate, compressed into tablets to obtain finished product, the drug-containing amount is 150mg / tablet. Then the dissolution rate of the ranitidine sustained-release tablet (1) in 900 ml of water at 37° C. was measured. After release measurement, the results are shown in Table 1, which meets the requirements.

[0051] The dissolution rate of table 1 ranitidine sustained-release tablet (1)

[0052] Sampling time (hours)

Embodiment 2

[0053] The preparation of embodiment 2-ranitidine sustained-release tablet (2)

[0054] Method: Take 150 grams of ranitidine, 10 grams of hydroxypropyl cellulose, 20 grams of stearyl alcohol, 15 grams of hypromellose, 1 gram of carbomer, and 10 grams of lactose, pass through 80-mesh sieves, and grind Mix evenly, add 95% ethanol solution of 10% polyvinylpyrrolidone as a binder and stir to make a soft material, granulate through a 16-mesh sieve, dry the granules at room temperature for 2 hours, granulate with a 16-mesh sieve, and then add hard Magnesium fatty acid 4.5 grams, micropowder silica gel 2 grams, mix evenly, compress tablet to obtain the finished product, containing medicine amount is 150mg / tablet. Then measure the dissolution rate of ranitidine sustained-release tablet (2) in 900ml water at 37°C. After release measurement, the results are shown in Table 2, which meets the requirements.

[0055] The dissolution rate of table 2 ranitidine sustained-rel...

Embodiment 3

[0057] The preparation of embodiment 3-ranitidine sustained-release tablet (3)

[0058] Method: Take 150g of ranitidine, 35g of hypromellose, 5g of microcrystalline cellulose, and 1g of carbomer respectively, pass through 80 mesh sieves, mix well, add 95% ethanol with a concentration of 10% polyvinylpyrrolidone The solution is used as a binder and stirred to make a soft material, granulated through a 16-mesh sieve, dried at 60°C for 1 hour, granulated with a 16-mesh sieve, then added with 2.5 grams of magnesium stearate, mixed evenly, and compressed to obtain a finished product, containing Drug dosage is 150mg / tablet. Then the dissolution rate of the ranitidine sustained-release tablet (3) in 900 ml of water at 37° C. was measured. After release measurement, the results are shown in Table 3, meeting the requirements.

[0059] The dissolution rate of table 3 ranitidine sustained-release tablet (3)

[0060] Sampling time (hours)

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PUM

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Abstract

A slowly-released medicine of ranitidine in the form of dispersing solid is prepared from ranitidine and slow-releasing skeleton.

Description

[0001] [Technical field] The present invention relates to a sustained release formulation of ranitidine and a preparation method thereof. [Background technique] [0002] The research and development of sustained-release preparations has a history of more than 40 years. It releases slowly and at a non-constant rate as required in a prescribed environment. Prolonged formulation. This kind of preparation can make the human body maintain this kind of blood drug concentration for a long time, instead of dropping rapidly like ordinary preparations, so as to avoid the "peak and valley" phenomenon that occurs when common preparations are frequently administered, and ensure the safety of the drug. Sexuality, effectiveness or adaptability have been improved, thereby reducing the number of medications, which greatly facilitates patients, especially patients who have been taking medication for a long time. Commonly used oral dosage forms include matrix tablets, microporous coated surface...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/48A61K47/02A61K47/12A61K47/34A61K47/38A61K47/42A61K47/44A61K31/341A61P1/04A61K47/10
Inventor 刘凤鸣
Owner 刘凤鸣
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