Stable lenalidomide oral solid preparation

A technology of lenalidomide and solid preparations, which is applied in the field of pharmaceutical preparations, can solve the problems of changing appearance and color, affecting the stability of preparations, and increasing the impurity content of solid oral preparations, achieving improved stability, low impurity content, and high solubility Effect

Active Publication Date: 2010-08-04

NANJING CAVENDISH BIO ENG TECH +1

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AI-Extracted Technical Summary

Problems solved by technology

[0009] Because lenalidomide is insoluble in water, it affects the dissolution rate of its oral solid preparation and then directly affects the bioavailability of the drug. The prior art solves this problem by micronization or strong salt; in addition, the oral solid preparation auxiliary material The type may affect the stability of the preparation. For example, due to the...

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Abstract

The invention discloses a lenalidomide oral solid preparation which is based on 10000 solid preparation units and is prepared by the following components: 10-500g of lenalidomide, 300-1200g of premixed powder, 50-200g of cross-linked sodium carboxymethyl cellulose, 1-50g of magnesium stearate and 100-500ml of 10% (percent weight in volume) povidone absolute ethyl alcohol solution, wherein the premixed powder is the mixture of lactose and microcrystalline cellulose which have the weight ratio of 2:3. In addition, the invention also discloses a preparation method of the lenalidomide oral solid preparation and usage thereof. The lenalidomide oral solid preparation has the advantages that a sample can be reserved for a long time with stable quality; and the lenalidomide oral solid preparation can be released within a short time so as to be easily absorbed by the human body completely.

Application Domain

Organic active ingredientsPharmaceutical delivery mechanism +3

Technology Topic

ChemistrySodium carboxymethylcellulose +8

Image

Examples

Experimental program(4)
Comparison scheme(2)
Effect test(1)

Example Embodiment

[0082] Example 1

[0083] 5mg lenalidomide capsules

[0084] Premix powder prescription

[0085] Lactose 3000g

[0086] Microcrystalline cellulose 2000g

[0087] 5000g in total

[0088] Attachment: Preparation of adhesive (10% povidone ethanol solution):

[0089] Povidone K30 200g

[0090] Add absolute ethanol to 2000ml

[0091] Capsule prescription

[0092] Lenalidomide 50g

[0093] Premixed accessories 800g

[0094] Croscarmellose Sodium 100g

[0095] 10% povidone ethanol solution 350ml

[0096] Magnesium stearate 10g

[0097] Filled with 10,000 grains

[0098] Preparation:

[0099] (1) Preparation of adhesive Weigh 100g of povidone K30, put it in a 1000ml beaker, add an appropriate amount of absolute ethanol, stir to dissolve, add absolute ethanol to 1000ml, stir well, and set aside.

[0100] (2) Take lactose and microcrystalline cellulose, crush them and pass through a 100-mesh sieve, and mix them evenly according to the prescription of premixed auxiliary materials to obtain premixed auxiliary materials for use.

[0101] (3) Take croscarmellose sodium, crush it and pass it through a 100-mesh sieve for use.

[0102] (4) Take Nalidomide, smash it and pass it through a 100-mesh sieve for use.

[0103] (5) Weigh the pre-mixed excipients, croscarmellose sodium and lenalidomide according to the capsule prescription, and mix them evenly to obtain the drug-containing mixed powder for use.

[0104] (6) Add a binder to the medicine-containing mixed powder to prepare 16 mesh wet granules, and dry them at 40°C to obtain dry granules.

[0105] (7) After the dry granules are sized through an 18-mesh sieve, magnesium stearate is added and mixed with the dry granules to obtain intermediate granules.

[0106] (8) Determination of the intermediate particle content, and calculate the amount based on the content.

[0107] (9) Adjust the volume and fill the capsule.

[0108] (10) Packing to get finished product.

Example Embodiment

[0109] Example 2

[0110] 10mg lenalidomide capsules

[0111] The premixed powder prescription is the same as in Example 1

[0112] Capsule prescription

[0113] Lenalidomide 100g

[0114] Premixed accessories 750g

[0115] Croscarmellose Sodium 100g

[0116] 10% povidone ethanol solution 350ml

[0117] Magnesium stearate 10g

[0118] Filled with 10,000 grains

[0119] Preparation method: the same as in Example 1.

Example Embodiment

[0120] Example 3

[0121] 25mg lenalidomide capsules

[0122] The premixed powder prescription is the same as in Example 1

[0123] Capsule prescription

[0124] Lenalidomide 250g

[0125] Premixed accessories 600g

[0126] Croscarmellose Sodium 100g

[0127] 10% povidone ethanol solution 350ml

[0128] Magnesium stearate 10g

[0129] Filled with 10,000 grains

[0130] Preparation method: the same as in Example 1.

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Description & Claims & Application Information

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Classification and recommendation of technical efficacy words

Low impurity content
Improve solubility

Stable lenalidomide oral solid preparation

AI-Extracted Technical Summary

Problems solved by technology

Abstract

Image

Examples

Example Embodiment

Example Embodiment

Example Embodiment

PUM

Description & Claims & Application Information

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