CN104983714A - Celecoxib capsule and preparing method thereof - Google Patents

Abstract

The invention relates to a celecoxib capsule and a preparing method thereof. The celecoxib capsule is composed of celecoxib, lactose, croscarmellose sodium, povidone K30, lauryl sodium sulfate, a 2% sodium dodecyl sulfate solution and magnesium stearate. By means of the celecoxib capsule, the dissolution rate of the celecoxib is greatly increased, the stability of preparations is good, equipment is simple, and the celecoxib capsule is very suitable for industrial production.

Description

A kind of Celebret and preparation method thereof

Technical field

The present invention relates to pharmaceutical field, be specifically related to a kind of Celebret and preparation method.

Background technology

Celecoxib (celecoxib) is first specificity COX-2 (COX-2) inhibitor of Xi Er company of U.S. exploitation, for the treatment of osteoarthritis and rheumatoid arthritis, is the maximum non_steroidal anti_inflammatory drug of current global recipe quantity.

Celecoxib is white to off-white color crystalline powder, almost insoluble in water, belongs to insoluble drug.In order to improve the stripping of celecoxib, technical staff have employed different solutions, raw material is made undefined structure or solid dispersion is conventional method.But due to crystal structure, make the physicochemical property of celecoxib show as the preparation processability of extreme difference.This characteristic shows as: the first, almost insoluble in water, if directly by without the medicine filled capsules pulverized, Oral drug absorption will be caused very slow, affect bioavailability; Second, quality is light, bulk density is low, easy cohesion in bulk, causes the method adopting micromill process to improve dissolubility and bioavailability to become very difficult, when it mixes with adjuvant, also easy coalescent in bulk, be separated with adjuvant, not only cause preparation medicine uniformity of dosage units defective, and impact absorbs.

Have capsule at the celecoxib preparation of China list marketing at present, specification is 0.1g, 0.2g.The wet granulation that the many employings of capsule are traditional, production process is more, mainly through supplementary material mixing, prepare soft material, granulation, drying, arrangement, total mixed, filling, polishing, bubble-cap, operation is relatively loaded down with trivial details, consuming time longer.Make celecoxib in process of production variable color deterioration happen occasionally, it is large that medicine quality homogeneity controls difficulty, and between batch, quality fluctuation is remarkable, is unfavorable for patient safety medication.

Summary of the invention

In order to solve the problem of celecoxib preparation difficulty in prior art, the invention provides a kind of new Celebret and preparation method thereof.

First aspect, the present invention relates to a kind of Celebret, consists of the following composition:

Be preferably:

Or consist of:

Be preferably:

On the other hand, the present invention relates to a kind of preparation method of Celebret:

(1) celecoxib raw material pulverizer is crushed to D90≤15 μm, for subsequent use;

(2) take lactose, cross-linking sodium carboxymethyl cellulose, sodium lauryl sulphate and polyvidone k30 by recipe quantity, join mix homogeneously in Fastmixinggranulator;

(3) wet method soft material is carried out with 2% sodium dodecyl sulfate solution;

(4) oscillating granulator 30 order carries out wet granular granulate;

Dry in (5) 60 DEG C of air dry ovens, control moisture <2%;

(6) oscillating granulator carries out 30 mesh sieve granulate;

(7) dry granule and recipe quantity magnesium stearate are joined in LSD-50 moulding mixture bucket mixer, mixing;

(8) fill capsule.

Celebret of the present invention not only substantially increases the dissolution of celecoxib, and better stability of preparation, and equipment is simple, is very applicable to commercial production.

Accompanying drawing explanation

Fig. 1 is the process chart of the Celebret in the present invention

Detailed description of the invention

embodiment 1the preparation of 100mg specification Celebret

Table 1,100mg specification Celebret prescription

Supplementary material is taken according to the prescription proportioning of table 1; Celecoxib raw material pulverizer is crushed to D90≤15 μm, for subsequent use; Take lactose, cross-linking sodium carboxymethyl cellulose, sodium lauryl sulphate and polyvidone k30, to join in Fastmixinggranulator mix homogeneously in mixer; Wet method soft material is carried out with 2% sodium dodecyl sulfate solution; Oscillating granulator 30 order carries out wet granular granulate; Dry in 60 DEG C of air dry ovens, control moisture <2%; Oscillating granulator carries out 30 mesh sieve granulate; Dry granule and recipe quantity magnesium stearate are joined in LSD-50 moulding mixture bucket mixer, mixing; Intermediate detects; Fill capsule, packaging; Quan Jian, warehouse-in.

Table 2,100mg specification Celebret preparation technology parameter

embodiment 2specification is 200mg

Table 3,200mg specification Celebret prescription

Preparation method is with reference to embodiment 1.

embodiment 3inspection

Table 4, inspection item

Result shows that this preparation technology favorable reproducibility, method are feasible, with laboratory indices no significant difference, made sample passes, stable yield, can realize workshop and amplify production.

Claims (5)

1. a Celebret, it consists of:

。

2. Celebret as claimed in claim 1, its composition is preferably:

。

3. a Celebret, it consists of:

。

4. Celebret as claimed in claim 3, its composition is preferably:

。

5. the preparation method of the Celebret described in any one of claim 1-4, it comprises the steps:

Celecoxib raw material pulverizer is crushed to D90≤15 μm, for subsequent use;

Take lactose, cross-linking sodium carboxymethyl cellulose, sodium lauryl sulphate and polyvidone k30 by recipe quantity, join mix homogeneously in Fastmixinggranulator;

Wet method soft material is carried out with 2% sodium dodecyl sulfate solution;

Oscillating granulator 30 order carries out wet granular granulate;

Dry in 60 DEG C of air dry ovens, control moisture <2%;

Oscillating granulator carries out 30 mesh sieve granulate;

Dry granule and recipe quantity magnesium stearate are joined in LSD-50 moulding mixture bucket mixer, mixing;

Fill capsule.