Freeze-dried (R)-lansoprazole powder injection, and preparation method and application thereof

A technology of dexlansoprazole and freeze-dried powder injection, which is applied in the field of medicine and can solve problems such as bleeding, dysphagia, and inappropriate oral medication

Active Publication Date: 2019-02-26
南京博德生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for the above-mentioned patients, there are usually dysphagia and gastrointestinal bleeding, especially for patients with severe bleeding, it is not suitable for oral administration. Later, Takeda developed lansoprazole for injection to overcome the drug defects of lansoprazole

Method used

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  • Freeze-dried (R)-lansoprazole powder injection, and preparation method and application thereof
  • Freeze-dried (R)-lansoprazole powder injection, and preparation method and application thereof
  • Freeze-dried (R)-lansoprazole powder injection, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The preparation of embodiment 1 freeze-dried powder injection

[0033] Prepare respectively 10mg, 20mg, 30mg, 60mg and 90mg dexlansoprazole freeze-dried powder injection according to the prescription in Table 3.

[0034] Table 3 prescription composition

[0035]

[0036] The preparation process is as follows:

[0037] (1) Dosing: add mannitol, meglumine, dexlansoprazole and sodium hydroxide in the prescribed amount to the water for injection, stir until completely dissolved, and adjust the pH to between 11.8-12.3;

[0038] (2) Filtration: add 0.1% activated carbon for needles, stir at room temperature for 15min-30min, coarsely filter out carbon with a titanium rod, filter with a 0.45μm filter membrane, and finely filter with a 0.22μm filter membrane.

[0039] (3) Filling and freeze-drying in a freeze dryer.

[0040] (4) Freeze-drying: Pre-freeze the product to below -35°C and keep it for 2 hours; raise the temperature of the heat transfer oil to -15°C and keep it ...

Embodiment 2

[0041] Embodiment 2 Rat acute toxicity test

[0042]The quantitative determination of toxicity is to introduce different doses of the test substances into the experimental animals, and the dose sufficient to make 50% of the total number of individuals under the test conditions is called LD50 (half lethal dose), generally used per kilogram of body weight expressed in milligrams of toxicant.

[0043] Give test product dexlansoprazole for injection and reference substance lansoprazole for injection by disposable intravenous injection, observe the acute toxic reaction produced to tested animal SD rats, compare dexlansoprazole and lansoprazole The safety of Soprazole, toxicity test result are shown in Table 4 and Table 5.

[0044] The rat acute toxicity test result of table 4 dexlansoprazole

[0045] dose

250.0mg / kg

225.0mg / kg

202.5mg / kg

182.3mg / kg

164.0mg / kg

LD50

mortality rate

80％

60％

20％

10％

0％

221.5mg / kg

[0046]...

Embodiment 3

[0052] The tolerance of embodiment 3 Dexlansoprazole for injection

[0053] The tolerance test is a dose-escalation clinical tolerance test carried out in healthy subjects, the purpose is to observe the tolerance and safety of normal people after administration of dexlansoprazole for injection.

[0054] Subjects: healthy volunteers aged 18-45;

[0055] Drug source:

[0056] Dexlansoprazole for injection is prepared according to Example 1;

[0057] Lansoprazole for injection, purchased from Shandong Luoxin Pharmaceutical Co., Ltd., specification: 30mg, batch number: 513093217;

[0058] "For injection" means that the pharmaceutical dosage form is freeze-dried powder injection.

[0059] Drug preparation: constant-speed intravenous injection for 60 minutes, twice a day. When using this product, dilute it with 100mL of 0.9% Sodium Chloride Injection. Injection was filtered using an in-line filter with a pore size of 1.2 μm.

[0060] Clinical Observation Index

[0061] During...

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Abstract

The invention discloses a freeze-dried (R)-lansoprazole powder injection. The freeze-dried (R)-lansoprazole powder injection contains (R)-lansoprazole, mannitol, meglumine and sodium hydroxide, wherein the content of (R)-lansoprazole is 10-30 mg. Through research on the dosage of a prescription and a freeze-drying process, a sample with good appearance, qualified water residue content and good resolubility is obtained. The results of experiments on rats about acute toxicity, tolerability and safety verify that the freeze-dried (R)-lansoprazole powder injection of the invention has good tolerability and safety and few adverse reactions, and is more applicable to preparation of drugs used for treating upper gastrointestinal hemorrhage caused by peptic ulcers.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a freeze-dried powder injection of dexlansoprazole, its preparation method and application. Background technique [0002] Lansoprazole is the second proton pump preparation on the market. It belongs to the benzimidazole class like other proton pump inhibitors, but because of the trifluoroethoxy substituent, its bioavailability is 30% higher than that of omeprazole. Strong lipid, can quickly pass through the parietal cell membrane into sulfenic acid and sulfenyl derivatives to play a role. Takeda Pharmaceutical Company developed oral dexlansoprazole controlled-release capsules, which were first launched in Japan in 1992 for the treatment of gastric ulcer, duodenal ulcer, reflux esophagitis, Zoller-Ellison syndrome, anastomotic stoma ulcer. But usually there is dysphagia for above-mentioned patient, gastrointestinal hemorrhage, especially for the patient with severe hemorrhage...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/4439A61K47/26A61K47/02A61K47/10A61P1/04A61P7/04
CPCA61K9/0019A61K9/19A61K31/4439A61K47/02A61K47/10A61K47/26A61P1/04A61P7/04
Inventor 张峰江雁钟元元朱素华薛峪泉刘春猛
Owner 南京博德生物制药有限公司
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