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Oral instant preparation of proton pump inhibitor and preparation method thereof

The technology of an alkalizing agent and a supporting agent is applied in the preparation and preparation fields of esomeprazole, and achieves the effects of improving stability, high bioavailability, and increasing controllability of safety and quality.

Inactive Publication Date: 2013-11-13
CHONGQING LUMMY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

"Paragraph 0012" of the description in the application defines alkaline substances, which include inorganic bases and organic bases (such as amine compound alkalizing agents), but this application points out that: magnesium oxide in inorganic bases or Magnesium hydroxide performs better in ensuring the stability of esomeprazole free base; the present invention aims at the better stability of magnesium oxide or magnesium hydroxide in inorganic bases than other alkaline substances (amine compound alkalizing agent) "This technical bias has been studied
In addition, it is well known that patients with stomach problems, especially patients with gastric ulcers, should be cautious in using medicines containing magnesium ions or other metal ions; for the stability of the medicine, other ingredients are introduced, and some of them lose sight of the other.

Method used

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  • Oral instant preparation of proton pump inhibitor and preparation method thereof
  • Oral instant preparation of proton pump inhibitor and preparation method thereof
  • Oral instant preparation of proton pump inhibitor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The water system of embodiment one amine compound alkalizing agent is applied in the stabilizer of preparation esomeprazole free base

[0030] Investigate the influence of amine compound alkalizing agent on the solubility of esomeprazole in the preparation method of injection process and freeze-drying process. According to the prescriptions of each batch number in the following table 20-001-055, weigh the prescribed amount of amine compound alkalizing agent, dissolve them in purified water, then add the corresponding prescribed amount of esomeprazole, and stir until completely dissolved. Combined with the actual production situation, place it at room temperature for 8 hours, observe, and record the results, as shown in Tables 1-7 below.

[0031] Table 1 Effects of meglumine

[0032]

[0033] Table 2 Effect of arginine

[0034]

[0035] Table 3 Effect of Lysine

[0036]

[0037] Table 4 Effect of ornithine

[0038]

[0039]

[0040] Table 5 Effect of his...

Embodiment 2

[0055] Esomeprazole

[0056] purified water

[0057] Weigh the prescribed amount of lysine and dissolve in purified water, then add esomeprazole and stir until completely dissolved. Then add sodium chloride and glycyrrhizin, stir to dissolve, add apple essence after filtering, constant volume, degassing, divide into molds or special bottles, and put into freeze-drying box. Set the pre-freezing temperature to -40°C, keep it for 3 hours, raise the temperature to 20°C at a heating rate of 2°C / h (drying time is 30 hours), and the vacuum degree is 0.05-0.1mbar. Control moisture to 1-3% and seal out the box.

Embodiment 3

[0059] Esomeprazole

[0060] Weigh the prescribed amount of ornithine and dissolve in purified water, add esomeprazole and stir to dissolve until completely dissolved. Then add mannitol and aspartame to dissolve in purified water, filter and add apple essence to constant volume. Degas, divide into molds or special bottles, and put into freeze-drying boxes. Set the pre-freezing temperature to -40°C, keep it for 5 hours, and raise the temperature to 20°C at a rate of 5°C / h (drying time 12 hours) (vacuum degree 0.02-0.06mbar). Control moisture to 1-3% and seal out the box.

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PUM

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Abstract

The invention belongs to the field of drug preparation, provides a proton pump inhibitor and a preparation method thereof, and especially relates to an application of a water system of amine compound alkalizer in the preparation of stabilizer of esomeprazole free alkali. Besides, the invention provides a stable water system of esomeprazole free alkali, and the system is composed of amine compound alkalizer, esomeprazole free alkali and water medium. On the basis of the water system, an oral instant preparation of esomeprazole is prepared. The preparation has the advantages of stable quality, good taste, rapid absorption, quick effect and user-friendliness, can improve the compliance of the patients, and is especially suitable for the patients when the disease attacks with no water available. The preparation effectively solves the problem that esomeprazole is decomposed by acid, relieves the stimulation to the digestive tract, and increases the stability of the esomeprazole preparation and the safety of clinical application.

Description

technical field [0001] The invention belongs to the field of pharmacy, in particular to a preparation of esomeprazole and a preparation method thereof. Background technique [0002] Proton pump inhibitor (proton pump inhibitor PPI) is the drug of choice for the treatment of peptic ulcer. + / K + -ATPase active compound sulfenamide, rapidly reacts with H + / K + - The sulfhydryl group of cysteine ​​on the ATPase binds to form a disulfhydryl bond, thereby inactivating the enzyme and specifically inhibiting gastric parietal cell H + / K + -ATPase activity thereby inhibiting gastric acid secretion. Esomeprazole (esomeprazole, (S)-5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridyl)methylsulfinyl]-3H- Benzimidazole) is the first optical isomer among proton pump inhibitors. As a relatively new proton pump inhibitor, it has been widely used clinically in recent years, and a large number of studies and clinical trials have shown that it is effective in the treatment of peptic ulcer I...

Claims

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Application Information

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IPC IPC(8): A61K47/18A61K31/4439A61P1/04
Inventor 胡显刚
Owner CHONGQING LUMMY PHARMA
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