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Phosphatidylcholine-containing pharmaceutical preparation for the treatment of ulcerative colitis

A technology for ulcerative colitis and phosphatidylcholine, which is applied in the field of pharmaceutical preparations containing phosphatidylcholine for the treatment of ulcerative colitis, and can solve problems such as adverse side effects of steroids and ineffective improvement of symptoms of ulcerative colitis

Inactive Publication Date: 2019-04-26
LIPID THERAPEUTICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

While steroids are often effective in reducing inflammatory episodes, long-term steroid use is associated with unwanted side effects
ASA-refractory within the scope of the present invention means that the use of the above-mentioned 5-ASA-compounds, especially 5-amino-2-hydroxy-benzoic acid, has not been effective in improving the symptoms of ulcerative colitis disease

Method used

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  • Phosphatidylcholine-containing pharmaceutical preparation for the treatment of ulcerative colitis
  • Phosphatidylcholine-containing pharmaceutical preparation for the treatment of ulcerative colitis
  • Phosphatidylcholine-containing pharmaceutical preparation for the treatment of ulcerative colitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1a

[0152] Embodiment 1a (is the PC preparation of pill)

[0153] A pharmaceutical formulation was prepared in the form of pellets (0.5-1.8 mm in diameter) comprising 27% by weight of the specific phosphatidylcholine product (PC) of formula (I), comprising the following amounts of fatty acids (% of the total amount of fatty acids in PC) % by weight):

[0154] 64 linoleic acid

[0155] 14 palmitic acid

[0156] 11 Oleic acid

[0157] 06 Linolenic acid

[0158] 04 stearic acid

[0159] 01 Other C-14 to C-22 fatty acids.

[0160] The phosphatidylcholine product (PC) has high purity and contains less than 0.1% of (PE) and (PI). This PC product can be obtained by chemical preparation or the process described earlier starting from soybean lecithin and formulated together with the following excipients in the following proportions (% by weight), wherein the component named A) is used to prepare the PC-pellets (core) and excipients named B) for delayed release layer:

[0161] A) Fo...

Embodiment 1b

[0175] Embodiment 1b (batch preparation of test sample pill (C103) and placebo pill (C104))

[0176] For example, the formulation can be prepared as follows within the technical scope:

[0177]

[0178] Batch formulation for film coating pre-isolated with barrier lacquer (quantities stated include 10% overproduction of all excipients required for film coating)

[0179]

[0180] Batch formulation of film coating with gastric juice resistant slippery layer (see above)

[0181]

[0182] 1) Water is removed during the preparation process and no water is contained in the final formulation.

Embodiment 2

[0183] Embodiment 2 (release and stability of PC)

[0184] The stability of pellets containing the specific phosphatidylcholine product (PC) according to Example 1 was determined under various conditions. Under acidic conditions (pH 1.0; 0.1 N HCl), the release of PC was less than 10% by weight after 120 minutes. After a further 60 minutes at pH 6.0 and after a further 60 minutes at pH 7.2, the release of all three media tested exceeded 75% by weight.

[0185] The enteric coated pills of Example 1 were packed into sachets and tested by classic stability test. Acceptance criteria were defined as 90%-110% analytical grade PC (relative to nominal value) and up to 5% hemolytic PC (relative to PC).

[0186] The first batch of the resulting formulation was tested after 36 months storage in cold storage (5°C, ±3°C) and the pellets were found to be stable. The test results were found to be as follows: (Analytical PC (relative to nominal) = 96% and Hemolytic-PC (relative to PC) = 3....

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Abstract

A pharmaceutical preparation comprising a phosphatidylcholine product of formula (I), wherein R 1 is the residue of a saturated or unsaturated fatty acid having 12‑24 carbon atoms, and R 2 is the residue of a saturated or unsaturated fatty acid having 12-24 carbon atoms, and wherein the phosphatidylcholine product (PC) contains the following amounts of fatty acids: 55-72 linoleic acid, 10-18 palmitic acid, 07 -15 oleic acid, 02-08 linolenic acid, 02-08 stearic acid, and at least one excipient for delayed release, which can be used for the improved treatment of ulcerative colitis.

Description

technical field [0001] The present invention relates to pharmaceutical formulations comprising phosphatidylcholine for the treatment of chronic inflammatory diseases such as ulcerative colitis, especially ulcerative colitis in ASA-refractory individuals. Background technique [0002] Phosphatidylcholine (PC) is a known class of naturally occurring products. In animal and plant tissues, they are found together with other lipid compounds as a component of lecithin. A typical phosphatidylcholine consists of the following structural components: phosphoric acid, choline, fatty acids, and glycerol. The composition of fatty acid residues in PC has an important influence on the properties of phosphatidylcholine. The phosphatidylcholine can be synthesized or chemically or mechanically extracted from natural sources such as soybeans, other plants or eggs. Phosphatidylcholine generally has low solubility in water but is dispersible in water. They are not particularly stable in acid...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/01A61P1/00
CPCA61K9/5026A61K9/5073A61K31/685A61P1/00A61P1/04A61P29/00A61K9/284
Inventor 哥哈德·谢豪尔
Owner LIPID THERAPEUTICS