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Entecavir composition and preparation method thereof

A technology of entecavir and its composition, which is applied in the field of entecavir composition and its preparation, can solve the problems of material layering or compressed tablet hardness, unfavorable industrialization, uneven mixing, etc., and achieve improved content uniformity and stable dissolution rate stability, avoiding differences between single doses, avoiding the effect of uneven mixing

Pending Publication Date: 2021-03-23
SHIJIAZHUANG NO 4 PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method is very easy to cause stratification of raw materials and dispersants, and strict control is required for each parameter of the dry granulator, otherwise it is easy to cause stratification of materials in the subsequent tableting process or the hardness of the compressed tablet is low, which is not conducive to industrialization
3) Fluidized bed granulation is used to place the raw materials and auxiliary materials in the fluidized bed, and spray into the wetting agent to granulate, but it is easy to cause uneven mixing and the raw materials are blown away under the action of air flow, resulting in content loss. It is easy to cause cost increase and it is difficult to guarantee product quality

Method used

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  • Entecavir composition and preparation method thereof
  • Entecavir composition and preparation method thereof
  • Entecavir composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] To prepare 1000 entecavir tablets of 0.5 mg specification, the specific raw materials and dosage involved are as follows:

[0031] Entecavir 0.5g

[0032] Hypromellose 5.25g

[0033] Calcium hydrogen phosphate 92.25g

[0034] Self-crosslinking povidone 9g

[0035] Magnesium stearate 1g.

[0036] The preparation method comprises the following process steps:

[0037] a. Dissolve entecavir and hypromellose in 70 g of water, and heat it in a water bath to 60° C. to dissolve to obtain the main drug solution;

[0038] b. Use the single nozzle spray system on the wet granulator to atomize and spray the main drug solution onto the premix composed of calcium hydrogen phosphate, magnesium stearate and self-crosslinking povidone in the rotation, and the mist The pressure is 0.2Mpa, the rotation speed of the premix is ​​120r / min, and then dried in a vacuum oven at 50°C to remove moisture to obtain the entecavir composition, which is divided into 1000 parts and compressed into ...

Embodiment 2

[0040] To prepare 1000 entecavir tablets of 0.5 mg specification, the specific raw materials and dosage involved are as follows:

[0041] Entecavir 0.5g

[0042] Povidone 1g

[0043] Microcrystalline cellulose 73g

[0044] Croscarmellose Sodium 8.3g

[0045] Magnesium stearate 0.8g.

[0046] The preparation method comprises the following process steps:

[0047] a. Dissolve entecavir and povidone in 75g of water, and heat to 70°C in a water bath to dissolve to obtain the main drug solution;

[0048] b. Use the single nozzle spray system on the wet granulator to atomize and spray the main drug solution to the premix composed of microcrystalline cellulose, magnesium stearate and croscarmellose sodium in the rotation Above, the atomization pressure is 0.3Mpa, the rotation speed of the premix is ​​200r / min, and then dried in a vacuum oven at 55°C to remove moisture to obtain the entecavir composition, which is divided into 1000 parts and compressed into tablets to obtain 1000 ...

Embodiment 3

[0050]To prepare 1000 entecavir tablets of 1 mg specification, the specific raw materials and dosage involved are as follows:

[0051] Entecavir 1g

[0052] Hydroxypropyl cellulose 10.5g

[0053] Lactose 184.5g

[0054] Low-substituted hydroxypropyl cellulose 20g

[0055] Magnesium stearate 2g.

[0056] The preparation method comprises the following process steps:

[0057] a. Dissolve entecavir and hypromellose in 160 g of water, and heat it in a water bath to 80° C. to dissolve to obtain the main drug solution;

[0058] b. Use the single nozzle spray system on the wet granulator to atomize and spray the main drug solution onto the premix composed of calcium hydrogen phosphate, magnesium stearate and self-crosslinking povidone in the rotation, and the mist The pressure is 0.4Mpa, the rotation speed of the premix is ​​50r / min, and then dried in a vacuum oven at 60°C to remove moisture to obtain the entecavir composition, which is divided into 1000 parts and compressed into...

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Abstract

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses an entecavir composition and a preparation method thereof. The preparation method of the entecavir composition comprises the following process steps: a, dissolving entecavir and a binder in water to obtain a main drug solution; and b, spraying the main drug solution to a premix consisting of a filler and a disintegrating agent through atomization, uniformly mixing, and drying to remove moisture, thereby obtaining the entecavir composition. The entecavir composition is uniform in distributionof entecavir component and good in drug dissolution stability, and the preparation method is simple to operate and suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an entecavir composition and a preparation method thereof. Background technique [0002] The English name of Entecavir is Entecavir, and its chemical name is: 2-amino-9-[(1S,3R,4S)-4-hydroxyl-3-hydroxymethyl-2-methylenepentyl]-1,9-dihydro -6-H-purin-6-one monohydrate, the structural formula is: Molecular formula is C 12 h 15 N 5 o 3 ·H 2 O. Entecavir is an antiviral substance for the treatment of hepatitis B virus infection. It is well tolerated and has mild and reversible adverse reactions. Due to the low solubility of Enteca, the dissolution stability of its solid preparation is poor. Moreover, the current content of entecavir in a single dose is relatively small, only 0.5 mg or 1 mg, making it difficult to keep the content of active ingredients constant between single doses. Therefore, the currently prepared solid preparations of entecavir all hav...

Claims

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Application Information

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IPC IPC(8): A61K47/38A61K47/32A61K47/12A61K47/02A61K31/522A61P1/16A61P31/20
CPCA61K47/38A61K47/32A61K47/12A61K47/02A61K31/522A61P1/16A61P31/20Y02A50/30
Inventor 杨帆李彪刘芳菊程彦超董伟昌郭雅玮张伟丽李天星杨于曼赵佳琦
Owner SHIJIAZHUANG NO 4 PHARMA
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