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Particles containing an acitve agent in the form of a co-precipitate

A technology of co-precipitating agents, surfactants, applied in the field of a method and dosage forms comprising these particles

Active Publication Date: 2012-07-25
ETHYPHARM SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The first difficulty lies in obtaining the particles with the fastest dissolution rate and highest dissolution ratio to ensure satisfactory bioavailability of the molecule
[0009] A second difficulty lies in obtaining particles with a narrow size distribution, of a size suitable for placement in formulations for oral administration and capable of maintaining a high content of active substance
[0010] A third difficulty lies in obtaining formulations that are consistently stable under unfavorable temperature and humidity conditions such as 30°C / 60% RH (relative humidity) or 40°C / 75% RH (relative humidity) used in stability studies. %RH

Method used

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  • Particles containing an acitve agent in the form of a co-precipitate
  • Particles containing an acitve agent in the form of a co-precipitate
  • Particles containing an acitve agent in the form of a co-precipitate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] 1. Preparation of particles including surfactants

[0103] Manufacturing is performed on a GPCG1 fluidized bed using bottom spray mode.

[0104] The spray solution was prepared by dissolving itraconazole (supplied by Wickoff) in a solvent mixture, 96° alcohol / methylene chloride weight ratio of 41.6 / 58.4, and HPMC29105cPs (supplied by Dow Chemical) and polysorbate 20 (Montanox 20, provided by Seppic).

[0105] EFK Lactose (supplied by HMS) was introduced into the fluid bed and the solution was sprayed in bottom spray mode; 4 steps of spraying the solution were carried out in succession; after each spraying step the granules were milled on the fluid bed with a Forplex mill equipped with a 630 μm sieve Dry and grind.

[0106] After the fourth step, the granules obtained are dried in a fluidized bed.

[0107] The coating parameters are shown in Table 1:

[0108] Table 1

[0109]

[0110] The total weight of the sprayed solution was 11 kg and the total milling time...

Embodiment 2

[0131] 1. Preparation of Surfactant-Free Granules

[0132] Granules were prepared according to the procedure described in Example 1. The formulations produced are shown in Table 3.

[0133] table 3

[0134] starting material

Quantity (g)

％

EFK Lactose

600

40.68

Itraconazole

350

23.73

HMPC 29105cPs

525

35.59

Polysorbate 20

0

0

96° alcohol

4200

/

Dichloromethane

5900

/

Spray solution volume

10975

/

Theoretical dry capacity

1475

/

theoretical test

237.3mg / g

/

[0135] 2. result

[0136] 2.1 particle size distribution

[0137] as attached image 3 shown. The particle size distribution has the following results:

[0138] -D 10％ : 88μm

[0139] -D 50％ : 239μm

[0140] -D 90％ : 435μm

[0141] 2.2 Dissolution kinetics The study was carried out under the same conditions as ...

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Abstract

The invention relates to particles containing an active agent in the form of a co-precipitate, to a method for producing said particles and to pharmaceutical forms containing said particles.

Description

technical field [0001] The present invention relates to granules containing active substances in co-precipitated form, as well as processes for the preparation of said granules and dosage forms comprising these granules. Background technique [0002] The preparation of oral medicines is limited by increasingly complex synthetic molecules that often exhibit physicochemical characteristics unfavorable for the absorption of said molecules in the gastrointestinal tract and have low solubility in aqueous media. [0003] This is often manifested in the low bioavailability of these molecules and the need to administer high doses of the active substance to the patient in order to achieve an effective concentration. [0004] The above situation becomes more serious when the effective concentration to be achieved is higher, or when the amount of tablets or capsules to be taken at one time is larger, or when they are taken more times a day. [0005] The preparation of solid dispersion...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/50A61K31/4196A61K31/53
CPCA61K9/5078A61K31/4196A61K31/53A61K9/1682A61K9/1676
Inventor G·库赞G·拉穆勒
Owner ETHYPHARM SA