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Lansoprazole for injecting and its preparation method

A technology for lansoprazole and injection, applied in the field of pharmaceutical dosage forms, can solve problems such as hidden safety hazards, local irritation, and short time to maintain stability

Inactive Publication Date: 2007-10-24
SHANGHAI CHENPON PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] It is reported that the injection preparation of lansoprazole is prepared in Japan, is to use the mixture of non-aqueous solvents such as alkaline solution and ethanol, propylene glycol or PEG as solvent, but, because the existence of non-aqueous solvent, these injections still can produce hemolysis, local stimulation and other adverse reactions
[0004] There are reports in my country that use disodium hydrogen phosphate as the injection lansoprazole preparation of the pH regulator, avoiding the use of non-aqueous solvents, but the consumption of disodium hydrogen phosphate is large, and the country does not have a medicinal standard for disodium hydrogen phosphate, so it is widely used There are security risks
[0005] The U.S. also usefully dissolves lansoprazole in an alkaline solution to avoid the use of non-aqueous solvents, but the prepared product remains stable for a very short time after being dissolved in water

Method used

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  • Lansoprazole for injecting and its preparation method
  • Lansoprazole for injecting and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] formulate a prescription

[0081] One, increase the solubility of lansoprazole and the technological research of stability

[0082] In this embodiment, two preparation process routes are designed and tested. One is to increase the solubility and stability of lansoprazole by adding different solubilizers; the other is to utilize the solubility of lansoprazole under alkaline conditions to increase and the more stable properties to prepare the alkali of lansoprazole neutral solution.

[0083] 1. Add solubilizer to increase solubility

[0084] The commonly used solubilizers for preparing injections have polyoxyethylene castor oil (EL), Tween 80, Prosolonic F-68 etc. at present, by adding surfactants in different proportions and different processing methods, to improve the lansoprazole in Solubility in water.

[0085] Test method: Weigh about 0.3 g of lansoprazole raw material, add 50 mL of aqueous solutions containing different concentrations of solubilizers, stir, and ...

Embodiment 2-4

[0142] * The above prescriptions are based on 1000 sticks

[0143] Weigh lansoprazole, add sodium hydroxide solution, stir, mix, add water for injection, add meglumine, stir to make the medicine dissolve completely, add mannitol, stir, dissolve and mix. Then add 0.2% activated carbon, stir for 20 minutes, filter and decarburize, then pass through 0.45 μm and 0.22 μm microporous membranes respectively, fill the filtrate into 7 mL vials, 2 mL per bottle, pre-freeze at -40 ° C for 6 h, and heat up to - Dry at 20°C for 8 hours, heat up to -10°C and dry for 4 hours, heat up to 0°C and dry for 2 hours, heat up to 25°C and dry for 2 hours, cap the treated vial stopper, crimp the cap, and seal it. Obtain the lansoprazole solid preparation for injection of the present invention.

[0144] The prepared lansoprazole solid preparation for injection is dissolved in water for injection to prepare the lansoprazole solution dosage form for injection.

Embodiment 5-7

[0146] Stability of solid dosage forms

[0147] According to the provisions of Appendix XIX C of the Chinese Pharmacopoeia in 2000, the investigation content of the stability study was selected. Accelerated tests and long-term tests were carried out on the solid preparations prepared in Examples 2-4, and the key investigation items included properties, identification, alkalinity, insoluble particles, related substances and their contents.

[0148] the result shows:

[0149] 1. Place the solid preparation prepared in Examples 2-4 for 6 months under the conditions of a temperature of 40°C ± 2°C and a relative humidity of 75% ± 5% according to the package to be marketed, and there is no significant change in each index.

[0150] 2. The solid preparations prepared in Examples 2-4 were placed in commercially available packages at a temperature of 25°C±2°C and a relative humidity of 60%±10% for 6 months, and all indicators had no significant changes.

[0151] 3. Place the solid pr...

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Abstract

The invention discloses a Lansoprazole preparation for injection comprising (1) Lansoprazole 10-50 weigh parts, (2) meglumine 2-20 weight parts, (3) sodium hydroxide 1-5 weight parts, (4) mannitol 20-100 weight parts. The invention also discloses the process for preparing the preparation.

Description

technical field [0001] The invention relates to a pharmaceutical dosage form, in particular to a lansoprazole preparation for injection. Background technique [0002] The mechanism of action of the second-generation proton pump inhibitor lansoprazole is the same as that of omeprazole, and it also acts by inhibiting the last link of gastric acid secretion, H+ / K+-ATPase (proton pump). Since this product is a weakly alkaline drug, the original drug has very little activity. After being absorbed into the blood, it is transported to the gastric mucosal cells, and finally reaches the secretory duct and the acidic cavity. It is continuously enriched and converted into biologically active sulfenic acid and sulfenic acid amines in the form of sulfenic acid catalyzed by acid. The active drug interacts with the H+ / K+-ATPase transport mechanism to inhibit acid secretion. Therefore, this product can completely block the secretion of gastric acid stimulated by chemical media such as acet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K9/19A61P1/04
Inventor 杜狄峥陈虎林吴波峰张磊
Owner SHANGHAI CHENPON PHARM TECH CO LTD
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