Lactose for injection and preparation method thereof

Abstract

The invention discloses lactose for injection and a preparation method thereof. The method includes the following steps of ultrafiltration, concentration and crystallization, drying and pulverization.It is shown through studies that the lactose prepared by means of the process can control the levels of residual protein (including alpha-whey protein, beta-lactoglobulin and whole milk protein), endotoxin and other colored impurities to be in accordance with quality standards for injection, and the prepared lactose is still lactose monohydrate and is available for injection products.

Description

technical field

[0001] The invention belongs to the field of medicine, and in particular relates to lactose for injection and a preparation method thereof.

[0002] technical background

[0003] Lactose is a disaccharide, the English name is Lactose; it is connected by a molecule of β-D-galactose and a molecule of α-D-glucose at the β-1,4-position to form a glycosidic bond. Molecular formula C 12 h 22 o 11 , Molar mass 342.3. There are two anomers: α-lactose and β-lactose, which can be converted into each other in aqueous solution, and α-lactose is easy to combine with a molecule of crystal water. The structural formula is as follows:

[0004]

[0005] Lactose is a commonly used pharmaceutical excipient. It is rarely used in injections. It is mainly used as a filler in oral solid preparations or as a diluent in inhalants, but it is also used in some freeze-dried preparations and injections. The biggest difference between lactose as a freeze-drying excipient and other...

Examples

Embodiment 1

[0022] (1) Weigh 100g of commercially available common lactose monohydrate or medicinal lactose, dissolve in purified water and set the volume to 1000mL, heat to 50°C to dissolve for 100min, and use 10KD membrane bag for ultrafiltration after cooling down to room temperature;

[0023] (2) Concentrated crystallization: Concentrate the ultra-filtered lactose solution at 80°C, heat and stir the concentrated solution at 18°C ​​for 13 hours, then stand at 8°C for 1 hour to crystallize;

[0024] (3) Drying: filter the lactose solution after static crystallization, and then vacuum dry at 90°C for 10 hours;

[0025] (4) Pulverization: After drying, the lactose is pulverized to obtain the product; the yield is 78.5%.

Embodiment 2

[0027] (1) Weigh 5Kg of commercially available common lactose monohydrate or medicinal lactose, dissolve in purified water and set the volume to 16.2L, heat to 90°C to dissolve for 20min, and use a 30KD membrane bag for ultrafiltration after cooling down to room temperature;

[0028] (2) Concentrated crystallization: Concentrate the ultra-filtered lactose solution at 70°C, heat and stir the concentrated solution at 28°C for 18 hours, then stand at 5°C for 6 hours;

[0029] (3) Drying: filter the lactose solution after static crystallization, and then vacuum dry at 70°C for 32 hours;

[0030] (4) Pulverization: After drying, the lactose is pulverized to obtain the product; the yield is 75.3%.

Embodiment 3

[0032] (1) Weigh 10Kg of commercially available common lactose monohydrate or medicinal lactose, dissolve it in purified water and set the volume to 24.4L, heat to 80°C to dissolve for 60min, and use 3KD membrane bag for ultrafiltration after cooling down to room temperature;

[0033] (2) Concentrated crystallization: Concentrate the ultra-filtered lactose solution at 80°C, heat and stir the concentrated solution at 20°C for 26 hours, and then stand at 2°C for 8 hours;

[0034] (3) Drying: filter the lactose solution after static crystallization, and then vacuum dry at 80°C for 24 hours;

[0035] (4) Pulverization: After drying, the lactose was pulverized to obtain the product; the yield was 82.1%.

technical field

[0001] The invention belongs to the field of medicine, and in particular relates to lactose for injection and a preparation method thereof.

[0002] technical background

[0003] Lactose is a disaccharide, the English name is Lactose; it is connected by a molecule of β-D-galactose and a molecule of α-D-glucose at the β-1,4-position to form a glycosidic bond. Molecular formula C 12 h 22 o 11 , Molar mass 342.3. There are two anomers: α-lactose and β-lactose, which can be converted into each other in aqueous solution, and α-lactose is easy to combine with a molecule of crystal water. The structural formula is as follows:

[0004]

[0005] Lactose is a commonly used pharmaceutical excipient. It is rarely used in injections. It is mainly used as a filler in oral solid preparations or as a diluent in inhalants, but it is also used in some freeze-dried preparations and injections. The biggest difference between lactose as a freeze-drying excipient and other...

Examples

Embodiment 1

[0022] (1) Weigh 100g of commercially available common lactose monohydrate or medicinal lactose, dissolve in purified water and set the volume to 1000mL, heat to 50°C to dissolve for 100min, and use 10KD membrane bag for ultrafiltration after cooling down to room temperature;

[0023] (2) Concentrated crystallization: Concentrate the ultra-filtered lactose solution at 80°C, heat and stir the concentrated solution at 18°C ​​for 13 hours, then stand at 8°C for 1 hour to crystallize;

[0024] (3) Drying: filter the lactose solution after static crystallization, and then vacuum dry at 90°C for 10 hours;

[0025] (4) Pulverization: After drying, the lactose is pulverized to obtain the product; the yield is 78.5%.

Embodiment 2

[0027] (1) Weigh 5Kg of commercially available common lactose monohydrate or medicinal lactose, dissolve in purified water and set the volume to 16.2L, heat to 90°C to dissolve for 20min, and use a 30KD membrane bag for ultrafiltration after cooling down to room temperature;

[0028] (2) Concentrated crystallization: Concentrate the ultra-filtered lactose solution at 70°C, heat and stir the concentrated solution at 28°C for 18 hours, then stand at 5°C for 6 hours;

[0029] (3) Drying: filter the lactose solution after static crystallization, and then vacuum dry at 70°C for 32 hours;

[0030] (4) Pulverization: After drying, the lactose is pulverized to obtain the product; the yield is 75.3%.

Embodiment 3

[0032] (1) Weigh 10Kg of commercially available common lactose monohydrate or medicinal lactose, dissolve it in purified water and set the volume to 24.4L, heat to 80°C to dissolve for 60min, and use 3KD membrane bag for ultrafiltration after cooling down to room temperature;

[0033] (2) Concentrated crystallization: Concentrate the ultra-filtered lactose solution at 80°C, heat and stir the concentrated solution at 20°C for 26 hours, and then stand at 2°C for 8 hours;

[0034] (3) Drying: filter the lactose solution after static crystallization, and then vacuum dry at 80°C for 24 hours;

[0035] (4) Pulverization: After drying, the lactose was pulverized to obtain the product; the yield was 82.1%.

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