Oleanolic acid dispersible tablet and preparation method thereof

Abstract

The invention provides an oleanolic acid dispersible tablet and a preparation method thereof, a new oleanolic acid preparation-the oleanolic acid dispersible tablet is provided to solve the problem of low bioavailability of the oleanolic acid in the prior art; the oleanolic acid is carried out the micronizing, a filling agent, a disintegrant with 42 percent, a surfactant, a corrective and a lubricant are added for even mixing, an adhesive is added, the screening by a 20-mesh sieve and the granulation are carried out, the drying is carried out at 45 DEG C, the screening by a 24-mesh sieve and the size stabilization are carried out, the disintegrant with 58 percent is added and evenly mixed, the tablet pressing is carried out to obtain the oleanolic acid dispersible tablet, and the oleanolic acid dispersible tablet can meet the demands of the people for using the tablet on the different formulations and enrich the market. The dissolution rate of the oleanolic acid dispersible tablet of the invention can achieve more than 93 percent at 60 minutes, thus effectively utilizing the biological activity of the oleanolic acid and improving the efficacy of the oleanolic acid dispersible tablet; furthermore, the preparation method is simple and easy to realize the industrial large-scale production, thus laying a foundation for the industrial application of the dispersible tablet of the invention.

Description

technical field

[0001] The invention relates to an oleanolic acid preparation and a preparation method thereof, in particular to an oleanolic acid dispersible tablet and a preparation method thereof. Background technique

[0002] Oleanolic acid (OA) is a pentacyclic three-mushroom compound widely distributed in the plant kingdom. For example, in plants such as Pleurotus chinensis, Ligustrum lucidum, and cypress, oleanoic acid is free or combined into glycosides. The form exists, and its structural formula is:

[0003]

[0004] Molecular formula: C 30 h 48 o 3 Molecular weight: 456.71

[0005] Since the drug was used to treat hepatitis in the 1970s, its new pharmacological effects have been continuously discovered, widely used clinically, attracted widespread attention, and conducted in-depth research. However, due to the extremely strong fat solubility of oleanolic acid, the dissolution rate of its pharmaceutical preparations is not ideal at present, a...

Examples

Embodiment 1

[0043] Embodiment 1: oleanolic acid 20g, calcium hydrogen phosphate 100g, lactose 100g, 10% povidone K 30 9g of ethanol solution, 24g of crospovidone, 2.5g of sodium lauryl sulfate, 0.5g of sucralose, 2g of magnesium stearate, 95% ethanol

[0044] Take oleanolic acid and micronize it so that the particle size is below 10 μm, add calcium hydrogen phosphate, lactose, 10 g of crospovidone, sodium lauryl sulfate, sucralose and magnesium stearate, and mix well , adding 10% povidone K 30 The ethanol solution was passed through a 20-mesh sieve, granulated, dried at 45° C., passed through a 24-mesh sieve for granulation, added the remaining 14 g of crospovidone, mixed evenly, compressed into tablets, and made into 1000 tablets.

[0045] Usage and dosage: take orally. 1-4 tablets each time, 3 times a day.

Embodiment 2

[0046] Embodiment 2: oleanolic acid 15g, calcium hydrogen phosphate 100g, lactose 90g, 10% povidone K 30 10g of ethanol solution, 26g of crospovidone, 2g of sodium lauryl sulfate, 0.6g of sucralose, 1.5g of magnesium stearate, 95% ethanol

[0047]Take oleanolic acid and micronize it so that the particle size is below 10 μm, add calcium hydrogen phosphate, lactose, 11 g of crospovidone, sodium lauryl sulfate, sucralose and magnesium stearate, and mix well , adding 10% povidone K 30 The ethanol solution was passed through a 20 mesh sieve, granulated, dried at 45°C, passed through a 24 mesh sieve for granulation, added the remaining 15g of crospovidone, mixed evenly, compressed into tablets, and made into 1000 pieces.

[0048] Usage and dosage: take orally. 1-4 tablets each time, 3 times a day.

Embodiment 3

[0049] Embodiment 3: oleanolic acid 25g, calcium hydrogen phosphate 90g, lactose 120g, 10% povidone K 30 8g of ethanol solution, 22g of crospovidone, 3g of sodium lauryl sulfate, 0.4g of sucralose, 2.5g of magnesium stearate, 95% ethanol

[0050] Take oleanolic acid and take oleanolic acid and carry out micronization treatment to make its particle size below 10 μm, add calcium hydrogen phosphate, lactose, 11g crospovidone, sodium lauryl sulfate, sucralose and hard Magnesium fatty acid, mix well, add 10% Povidone K 30 The ethanol solution was passed through a 20 mesh sieve, granulated, dried at 45°C, passed through a 24 mesh sieve for granulation, added the remaining 15g of crospovidone, mixed evenly, compressed into tablets, and made into 1000 pieces.

[0051] Usage and dosage: take orally. 1-4 tablets each time, 3 times a day.

technical field

[0001] The invention relates to an oleanolic acid preparation and a preparation method thereof, in particular to an oleanolic acid dispersible tablet and a preparation method thereof. Background technique

[0002] Oleanolic acid (OA) is a pentacyclic three-mushroom compound widely distributed in the plant kingdom. For example, in plants such as Pleurotus chinensis, Ligustrum lucidum, and cypress, oleanoic acid is free or combined into glycosides. The form exists, and its structural formula is:

[0003]

[0004] Molecular formula: C 30 h 48 o 3 Molecular weight: 456.71

[0005] Since the drug was used to treat hepatitis in the 1970s, its new pharmacological effects have been continuously discovered, widely used clinically, attracted widespread attention, and conducted in-depth research. However, due to the extremely strong fat solubility of oleanolic acid, the dissolution rate of its pharmaceutical preparations is not ideal at present, a...

Examples

Embodiment 1

[0043] Embodiment 1: oleanolic acid 20g, calcium hydrogen phosphate 100g, lactose 100g, 10% povidone K 30 9g of ethanol solution, 24g of crospovidone, 2.5g of sodium lauryl sulfate, 0.5g of sucralose, 2g of magnesium stearate, 95% ethanol

[0044] Take oleanolic acid and micronize it so that the particle size is below 10 μm, add calcium hydrogen phosphate, lactose, 10 g of crospovidone, sodium lauryl sulfate, sucralose and magnesium stearate, and mix well , adding 10% povidone K 30 The ethanol solution was passed through a 20-mesh sieve, granulated, dried at 45° C., passed through a 24-mesh sieve for granulation, added the remaining 14 g of crospovidone, mixed evenly, compressed into tablets, and made into 1000 tablets.

[0045] Usage and dosage: take orally. 1-4 tablets each time, 3 times a day.

Embodiment 2

[0046] Embodiment 2: oleanolic acid 15g, calcium hydrogen phosphate 100g, lactose 90g, 10% povidone K 30 10g of ethanol solution, 26g of crospovidone, 2g of sodium lauryl sulfate, 0.6g of sucralose, 1.5g of magnesium stearate, 95% ethanol

[0047]Take oleanolic acid and micronize it so that the particle size is below 10 μm, add calcium hydrogen phosphate, lactose, 11 g of crospovidone, sodium lauryl sulfate, sucralose and magnesium stearate, and mix well , adding 10% povidone K 30 The ethanol solution was passed through a 20 mesh sieve, granulated, dried at 45°C, passed through a 24 mesh sieve for granulation, added the remaining 15g of crospovidone, mixed evenly, compressed into tablets, and made into 1000 pieces.

[0048] Usage and dosage: take orally. 1-4 tablets each time, 3 times a day.

Embodiment 3

[0049] Embodiment 3: oleanolic acid 25g, calcium hydrogen phosphate 90g, lactose 120g, 10% povidone K 30 8g of ethanol solution, 22g of crospovidone, 3g of sodium lauryl sulfate, 0.4g of sucralose, 2.5g of magnesium stearate, 95% ethanol

[0050] Take oleanolic acid and take oleanolic acid and carry out micronization treatment to make its particle size below 10 μm, add calcium hydrogen phosphate, lactose, 11g crospovidone, sodium lauryl sulfate, sucralose and hard Magnesium fatty acid, mix well, add 10% Povidone K 30 The ethanol solution was passed through a 20 mesh sieve, granulated, dried at 45°C, passed through a 24 mesh sieve for granulation, added the remaining 15g of crospovidone, mixed evenly, compressed into tablets, and made into 1000 pieces.

[0051] Usage and dosage: take orally. 1-4 tablets each time, 3 times a day.

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