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Treatment of abdominal pain associated with diarrhea-dominating irritable bowel syndrome

A technology for abdominal pain and diarrhea, which can be used in drug combinations, non-central analgesics, medical preparations without active ingredients, etc., and can solve problems such as no treatment for abdominal pain.

Pending Publication Date: 2022-03-18
硬木药品公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Additionally, there are no FDA-approved therapies specifically for the treatment of abdominal pain or discomfort associated with IBS-d
Therefore, there remains an unmet medical need for additional, well-tolerated and effective therapies to treat abdominal pain and discomfort associated with IBS-d

Method used

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  • Treatment of abdominal pain associated with diarrhea-dominating irritable bowel syndrome
  • Treatment of abdominal pain associated with diarrhea-dominating irritable bowel syndrome
  • Treatment of abdominal pain associated with diarrhea-dominating irritable bowel syndrome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0170] Delayed Release Linaclotide Tablets

[0171] Linaclotide can be formulated as a tablet for delayed drug release. Tablets have a much smaller specific surface area than beads of equal volume, making them potentially less susceptible to degradation induced by environmental factors (eg, humidity, oxidation, deamidation, etc.). Furthermore, the smaller surface area of ​​the tablet may become advantageous when an enteric coating is required since much less coating material is required to cover the surface of the dosage form.

[0172] An enteric coating can be applied in a tablet coating pan, and a coating for delayed release beads can be applied to the tablet to form a delayed release tablet. The amount of coating polymer on the tablet can vary from 5-60% (weight gain), depending on the size, shape and surface properties of the tablet. A subcoat may be applied to the tablet to separate linaclotide from the enteric or functional coating.

Embodiment 2

[0174] Enteric Coated Tablets

[0175] Table 1: Eudragit® FS30D Coated Linaclotide Delayed Release (DR) Tablet Composition

[0176]

[0177] Manufacturing method:

[0178] A. Tablets

[0179] A granulation solution can be prepared by dissolving PVP, histidine and calcium chloride in water, adjusting the pH of the solution to 2, and dissolving linaclotide. Granulation was carried out in a fluidized bed by spraying the granulation solution over the filler isomalt. At the end of granulation, the granules were dried for 30 minutes. The granules are then blended with tablet ingredients (including isomalt, crospovidone, magnesium stearate and talc) until homogeneous and compressed into tablets.

[0180] B. Enteric coating

[0181] For tablet coating, the linaclotide core tablets were placed in a pan coater and heated up to 35°C. Tablets were initially coated with Eudragit® FS 30 D suspension, the product temperature was maintained at 28°C to 32°C, and the atomizing air pres...

Embodiment 3

[0184] Delayed release compositions comprising linaclotide

[0185] Delayed release capsules comprising linaclotide can be formulated to target the ileum or colon (eg, the ileum, terminal ileum, and / or ascending colon). Compositions are formulated to include pH-triggered release based on linaclotide tablets, enteric coating of capsules, or linaclotide-coated beads contained in hard gelatin capsules. The composition can be formulated to further include stabilizing additives such as divalent cations and amino acids. PVA can be used as a binder and as a protective layer between linaclotide and the enteric coating. Linaclotide or linaclotide with a PVA outer coating (as beads, capsules or tablets) can be coated with an additional enteric coating (e.g., Eudragit® FS30D, Eudragit® S100, Eudragit® L100, Eudragit® L100- 55. Eudragit® L 30D-55) for coating, the enteric coating dissolves in a pH-dependent manner to release at a suitable pH (7) in the ileum of the GI tract. Enteric co...

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Abstract

The present invention provides methods for treating a patient having a condition, such as a GI condition or a symptom associated with a GI or non-GI condition, by administering a therapeutically effective amount of a delayed release pharmaceutical composition comprising linaclotide.

Description

[0001] Cross References to Related Applications [0002] This application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Patent Application No. 62 / 859,443, filed June 10, 2019. The entire contents of the aforementioned applications, including the figures, are hereby incorporated by reference in their entirety. technical field [0003] The present invention relates to the use of pharmaceutical compositions comprising linaclotide for the treatment of various indications including gastrointestinal (GI) disorders such as irritable bowel syndrome with diarrhea (IBS-d) and GI or non- Symptoms associated with GI disorders, such as abdominal pain. Background technique [0004] Irritable bowel syndrome (IBS) is a chronic functional gastrointestinal (GI) disorder characterized by recurrent abdominal pain associated with bowel movements and / or changes in stool frequency or pattern. IBS is often associated with abdominal distension and swelling, in addition to characteri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K38/10A61K47/32A61P1/00
CPCA61K38/10A61K9/0053A61K9/1611A61K9/1617A61K9/1623A61K9/1635A61K9/1652A61K9/1676A61K9/2009A61K9/2013A61K9/2018A61K9/2027A61K9/2813A61K9/282A61K9/284A61K9/2846A61K9/2853A61K9/2866A61K9/2886A61P1/00A61P29/00A61P1/12
Inventor W·巴托利尼
Owner 硬木药品公司