# US 2010/0266702 A1 · Particles containing an active agent in the form of a co-precipitate

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- Number: US 2010/0266702 A1
- Document ID: US20100266702A1
- Status: Published application
- Kind: A1
- Application number: 12/662,370
- Filed: 2010-04-13
- Published: 2010-10-21
- Earliest claimed: 2003-07-17
- Assignees: Ethypharm
- Inventors: Gérard Cousin; Gaël Lamoureux
- Web page: https://patentgrep.com/patent/US20100266702A1

## CPC

- A61K 31/4196: 1,2,4-Triazoles
- A61K 9/1676: {having a drug-free core with discrete complete coating layer containing drug (adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921)}
- A61K 9/1682: {Processes}
- A61K 9/5078: {with drug-free core}
- A61K 31/53: having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine (melarsoprol A61K31/555 {; with four nitrogen atoms A61K31/495})
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## 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.

## Claims

### Claim at position 1

-16. (canceled)

### Claim 17

A process for the preparation of a particle composed of a coprecipitate applied as a layer around a neutral hydrophilic carrier by spraying an organic solution over said neutral hydrophilic carrier,
said organic solution comprising at least one active substance, one surface-active agent, and one hydrophilic polymer,
wherein the spraying of the whole of the solution is carried out in at least two separate stages, each of these stages being followed systematically by a stage of milling the product obtained on conclusion of the preceding stag;
wherein said process comprises the following stages:
a) preparing said organic solution comprising the active substance, the hydrophilic polymer, and the surface-active agent,
b) spraying a portion of the solution obtained in a) over the neutral hydrophilic carriers,
c) milling the particles obtained in stage b),
d) spraying the remaining amount of the organic solution over the particles milled in stage c), and
e) final milling of the particles obtained in stage d).

### Claim 18 (depends on 17)

The process as claimed in claim 17, wherein the spraying/milling sequence (stages b to d) is repeated one or more times.

### Claim 19 (depends on 17)

The process as claimed in claim 17, further comprising a drying stage either after each spraying stage, before milling, or immediately after the milling.

### Claim 20 (depends on 17)

The process as claimed in claim 17, wherein the inert hydrophilic carrier is composed of any chemically and pharmaceutically inert excipient existing in the crystalline or amorphous particulate form.

### Claim 21 (depends on 17)

The process as claimed in claim 17, wherein the hydrophilic polymer is chosen from the group consisting of polyvinylpyrrolidones, acrylic polymers, and polyethylene glycols.

### Claim 22 (depends on 17)

The process as claimed in claim 17, wherein the surface-active agent is chosen from the group consisting of cationic, anionic, nonionic, and amphoteric agents, alone or as a mixture.

### Claim 23 (depends on 17)

The process as claimed in claim 17, wherein the organic solvent is chosen from the group consisting of ethanol, isopropanol, tetrahydrofuran, isopropyl ether, acetone, methyl ethyl ketone, methylene chloride, and the mixtures of these solvents.

### Claim 24 (depends on 17)

The process as claimed in claim 17, wherein the spraying stages are carried out in a coating pan, in a perforated pan coater, or in a fluidized bed.

### Claim 25

A particle composed of a coprecipitate which is applied as a layer around a carrier and which comprises at least one active substance, one surface-active agent and one hydrophilic polymer, wherein it is capable of being obtained by spraying a solution comprising at least one active substance, one surface-active agent and one hydrophilic polymer, said spraying being carried out at least in two separate stages, said stages each being followed by a milling stage.

### Claim 26 (depends on 25)

The particle as claimed in claim 25, wherein the active substance is present in the particle in a proportion which can vary between 1 and 60% by weight.

### Claim 27 (depends on 25)

The particle as claimed in claim 25, wherein the inert hydrophilic carrier is present in a proportion which can range up to 95% by weight.

### Claim 28 (depends on 25)

The particle as claimed in claim 25, wherein the hydrophilic polymer/active principle ratio by weight is between 10/1 and 1/2.

### Claim 29 (depends on 25)

The particle as claimed in claim 25, wherein the surface-active agent is present in a proportion which can vary between 0.1 and 20% by weight, with respect to the total weight obtained.

### Claim 30 (depends on 25)

The particle as claimed in claim 25, wherein the unit particle size of the inert hydrophilic carrier can be between 50 and 500 μm.

### Claim 31 (depends on 30)

The particle as claimed in claim 30, wherein the unit particle size of the inert hydrophilic carrier can be between 90 and 200 μm.

### Claim 32 (depends on 25)

A pharmaceutical composition, comprising at least one particle as claimed in claim 25, optionally in combination with pharmaceutically acceptable excipients.

### Claim 33 (depends on 20)

The process as claimed in claim 20, wherein the inert hydrophilic carrier is composed of a chemically and pharmaceutically inert excipient chosen from the group consisting of sugar derivatives, celluloses and their mixtures.

### Claim 34 (depends on 21)

The process as claimed in claim 21, wherein the polyvinylpyrrolidones have a molecular weight of between 10,000 and 50,000 and the cellulose derivatives are selected from the group consisting of hydroxypropylmethyl cellulose, hydroxypropyl cellulose, hydroxymethyl cellulose, hydroxypropyl methylcellulose phthalate and hydroxy propylmethylcellulose acetate/succinate.