Esomeprazole sodium enteric-coated tablet and preparation method thereof

A technology of esomeprazole sodium and enteric-coated tablets, which is applied in pill delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve problems such as increasing gastrointestinal irritation and increasing operation complexity, and achieve increased drug use Safety, improved drug stability, improved release effect

CN103006610AInactive Publication Date: 2013-04-03QINGDAO UNIV
6 Cites 6 Cited by

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
Publication Date
2013-04-03
Estimated Expiration
Not applicable · inactive patent

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention discloses an esomeprazole sodium enteric-coated tablet, which is obtained by coating a tablet core with an isolation coating and an enteric coating in sequence. The tablet core is composed of esomeprazole sodium, sodium hydroxide, a filler, a disintegrating agent and a lubricating agent, wherein the weight ratio of the esomeprazole sodium to the sodium hydroxide is 1: (0.05-0.45). According to a preparation method, through dissolving an alkaline material in a solvent, the esomeprazole sodium and a pharmaceutic adjuvant mixture are used for granulating; not only is the addition amount of the alkaline material greatly reduced, but also consistency of an alkaline environment in the tablet core is guaranteed; and the stability of medicine is improved.
Need to check novelty before this filing date? Find Prior Art

Description

Background technique

[0001] Esomeprazole is the S-isomer of omeprazole, which has metabolic advantages. Compared with omeprazole, it has higher bioavailability and more consistent pharmacokinetics. Esomeprazole has been listed Magnesium oral preparation, the chemical name of its active ingredient is S-5-methoxy-2-{[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfinyl}- 1H-Benzimidazole Magnesium, the structural formula is as follows:

[0002]

[0003] The raw material of esomeprazole magnesium has poor stability and poor water solubility, is easily destroyed in gastric acid, and is easily degraded when exposed to light. The raw material of esomeprazole sodium is less stable than esomeprazole magnesium, which is also the main reason why no esomeprazole sodium oral preparations have been listed in any country in the world so far. The prior art also only discloses the enteric-coated preparation of esomeprazole magnesium, such as:

[0004] CN102100671A discloses a preparation m...

Examples

Embodiment 1

[0026] Tablet core prescription

[0027]

[0028] Barrier Formulation

[0029]

[0030] Enteric layer formula

[0031]

[0032] Preparation Process

[0033] Mix esomeprazole sodium with lactose, sodium carboxymethyl starch, and microcrystalline cellulose evenly, add aqueous sodium hydroxide solution, granulate, dry, add magnesium stearate, mix evenly, and compress to obtain the product.

[0034] The compressed tablet is coated with an isolation coat with a weight gain of 5%, and then with an enteric coating with a weight gain of 15%.

Embodiment 2

[0036] Tablet core prescription

[0037]

[0038] Barrier Formulation

[0039]

[0040] Enteric layer formula

[0041]

[0042] Preparation Process

[0043] Mix esomeprazole sodium, sodium carboxymethyl starch and microcrystalline cellulose evenly, add sodium carbonate aqueous solution, granulate, dry, add magnesium stearate, mix evenly, and tablet to obtain.

[0044] The compressed tablet was coated with an isolation coat with a weight gain of 6%, and then with an enteric coating with a weight gain of 18%.

Embodiment 3

[0046] Tablet core prescription

[0047]

[0048] Barrier Formulation

[0049]

[0050]

[0051] Enteric layer formula

[0052]

[0053] Preparation Process

[0054] Mix esomeprazole sodium with lactose and crospovidone evenly, add sodium hydroxide aqueous solution, granulate, dry, add magnesium stearate, mix evenly, and compress into tablets to obtain the product.

[0055] The compressed tablet is coated with an isolation coat with a weight gain of 5%, and then with an enteric coating with a weight gain of 15%.