# US 2008/0187583 A1 · Tablet containing hydrogenated phospholipids

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- Number: US 2008/0187583 A1
- Document ID: US20080187583A1
- Status: Published application
- Kind: A1
- Application number: 12/009,942
- Filed: 2008-01-23
- Published: 2008-08-07
- Earliest claimed: 2007-01-23
- Assignees: Ktb Tumorforschungsgesellschaft Mbh
- Inventors: Ulrich Massing; Annette Bauer-Brandl
- Web page: https://patentgrep.com/patent/US20080187583A1

## CPC

- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- 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 present invention provides a process for preparing a tablet containing hydrogenated phospholipids and the tablet obtainable by such process.

## Claims

### Claim 1

A process for preparing a tablet containing 25 to 85% by weight of the tablet of a hydrogenated phospholipid (HPL) component and pharmaceutically acceptable carriers/excipients, said method comprises
(a) mixing an appropriate amount of a wetting agent with the pharmaceutically acceptable carriers/excipients to prepare a premixture, said carriers/excipients being stable upon contact with the wetting agent,
(b) adding said HPL component to said premixture of (a) and
(c) preparing the solid dosage form by compression.

### Claim 2 (depends on 1)

The process of claim 1, wherein the tablet is a small tablet being flat faced or concave.

### Claim 3 (depends on 2)

The process of claim 2, wherein the tablet has a diameter of 6-8 mm.

### Claim 4 (depends on 1)

The process of claim 1, wherein the tablet contains HPL as the active ingredient.

### Claim 5 (depends on 1)

The process of claim 1, wherein the tablet has a HPL content higher than 50% by weight, relative to the total weight of the tablet.

### Claim 6 (depends on 1)

The process of claim 1, wherein said HPL component comprises at least one 1,2-diacylphospholipid containing predominantly saturated acyl residues or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 6)

The process of claim 6, wherein said at least HPL has the structure of formula (I)
wherein
R1 and R2 are independently selected from H, alkylcarbonyl and arylalkylcarbonyl residues, wherein the alkyl residues are linear, branched or cyclic, saturated or unsaturated and may optionally be substituted with 1 to 3 residues R3 and one or more of the C-atoms in the alkyl residues may be substituted by O or NR4;
X is selected from H, —(CH2)n—N(4)3+, —(CH2)n—CH(N(R4)3+)—COO− and —(CH2)n—CH(OH)—CH2OH (wherein n is an integer from 1 to 5);
R3, irrespective of the occurrence of further residues R3, is selected from H, lower alkyl (wherein the lower alkyl residues may be linear, branched or cyclic, saturated or unsaturated), F, Cl, CN and OH; and
R4, irrespective of the occurrence of further residues R4, is selected from H, CH3 and CH2CH3, or a pharmacologically acceptable salt thereof.

### Claim 8 (depends on 1)

The process of claim 1, wherein the wetting agent is a polar solvent.

### Claim 9 (depends on 8)

The process of claim 8, wherein the polar solvent is selected from the group consisting of water, ethanol and acetone.

### Claim 10 (depends on 8)

The process of claim 8, wherein the polar solvent is water.

### Claim 11 (depends on 1)

The process of claim 1, wherein the wetting agent is present in an amount of 0.1 to 10% by weight, relative to the total weight of the tablet.

### Claim 12 (depends on 11)

The process of claim 11, wherein the wetting agent is present in an amount of 1 to 6% by weight, relative to the total weight of the tablet.

### Claim 13 (depends on 1)

The process of claim 1, wherein the carriers/excipients are selected from the group consisting of fillers, binders, glidants, disintegrants and lubricants.

### Claim 14 (depends on 1)

The process of claim 1, which comprises adding further carriers/excipients to the premixture in step (b) together with the HPL.

### Claim 15 (depends on 1)

The process of claim 1, which comprises adding further carriers/excipients in a separate step (b′).

### Claim 16

The process of 14, wherein said further carriers/excipients are unstable upon contact with the wetting agent.

### Claim 17 (depends on 16)

The process of claim 16, wherein said carriers/excipients unstable upon contact with the wetting agent include disintegrants.

### Claim 18 (depends on 17)

The process of claim 17, wherein said disintegrants are selected from the group consisting of croscarmellose-Na, crosslinked PVP and sodiumstarch glycolate.

### Claim 19

The process of 15, wherein said further carriers/excipients are unstable upon contact with the wetting agent.

### Claim 20 (depends on 19)

The process of claim 19, wherein said carriers/excipients unstable upon contact with the wetting agent include disintegrants.

### Claim 21 (depends on 19)

The process of claim 19, wherein said disintegrants are selected from the group consisting of croscarmellose-Na, crosslinked PVP and sodiumstarch glycolate.

### Claim 22 (depends on 1)

The process of claim 1, which further comprises adding further pharmaceutically active compounds in one or more of the reaction steps selected from the group consisting of (a), (b), and (b′).

### Claim 23 (depends on 1)

The process of claim 1, which further comprises adding compounds selected from the group consisting of flavors, colors and unsaturated phospholipids.

### Claim 24 (depends on 1)

Tablet obtainable by the process of claim 1.