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Enteric-coated gastro-retentive oral dosage form in tablet form, and application and pharmaceutical composition thereof

An enteric coating, gastric retention technology, used in the treatment of upper gastrointestinal and throat diseases

Pending Publication Date: 2018-05-22
IRONWOOD PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0025] Despite strong evidence of efficacy, PPIs have significant limitations
For example, patients who do not respond to PPI inhibitor therapy alone may not respond because although PPIs reduce acid reflux from the stomach, bile acids from the duodenum remain

Method used

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  • Enteric-coated gastro-retentive oral dosage form in tablet form, and application and pharmaceutical composition thereof
  • Enteric-coated gastro-retentive oral dosage form in tablet form, and application and pharmaceutical composition thereof
  • Enteric-coated gastro-retentive oral dosage form in tablet form, and application and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0164] Embodiment 1: the production process of large-scale batch

[0165] 1. Intragranular mixing

[0166] The intragranular components (except magnesium stearate) were dispersed and passed through a 20 mesh screen. The components were added to the V-blender and mixed at 25 RPM for 10 minutes. Then, the intragranular magnesium stearate was dispersed and passed through a 20 mesh screen. Magnesium stearate was added to the V-blender and mixed at 25 RPM for 2 minutes. Remove the resulting intragranular blend from the V-blender.

[0167] 2. heavy pressure

[0168] A 24-station Fette tablet press was equipped with eight 0.6250" disc, flat B-shaped die elements. The intragranular blend obtained above was added to the feed hopper of the tablet press. Using Tablet press turret speed of 15-25RPM to compress the blend into a pre-compaction body with a target weight of 1200-1400mg and a hardness of 9-15kp. Appearance, weight, hardness and thickness are checked during re-pressing in...

Embodiment 2

[0185] Example 2: Large-Scale Batches Produced

[0186] Following the procedure described in Example 1 the following large scale batches were produced. Table 1 below summarizes the amounts of excipients used during the production of each of the 6 batches.

[0187] Table 1

[0188]

[0189] Microcrystalline cellulose (MCC) was used as a filler / compression aid in the formulation. Two types of MCC have been evaluated. One manufacturer has shown that Prosolv SMCC90, a siliconized microcrystalline cellulose, has better powder flow than non-siliconized MCC.

[0190] KG-100 is another MCC used as a substitute for SMCC90. According to one manufacturer: KG-1000 has the lowest bulk density among the MCC grades. Compared to other standard MCC grades, KG-100 exhibits superior firmness. KG-1000 particles have a very large L / D value. The particles are easily aligned upright against the force of the compacting body; thus, the contact area of ​​the MCC particles is increased. Entan...

Embodiment 3A

[0196] Example 3A: In Vitro Dissolution / Drug Release

[0197] The drug release rates of six dosage forms produced on a large scale were determined using an indirect method, considering that colesevelam and colesevelam HCl are insoluble polymers and their concentrations could not be determined by standard direct HPLC methods for soluble drugs.

[0198] The drug release rate from the tablets was determined in vitro in acetate buffer at pH 4.5 (100 mM) containing a known bile acid (glycocholic acid) at a concentration of 2 mg / mL. The bile acid consumption of the tablets during swelling and erosion was determined and compared with values ​​obtained from a series of standard solutions of known bile acid concentrations. The rate of bile acid consumption corresponds to the rate of drug release. These drug release rate results were obtained using a USPI Type II (paddle) apparatus with tablets placed in a settler. The results are summarized in figure 1 middle.

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Abstract

The invention relates to the field of medicine, and specifically discloses an enteric-coated gastro-retentive oral dosage form in tablet form, and applications and a pharmaceutical composition thereof. The oral dosage form includes: a. a bile acid chelating agent selected from colesevelam and colesevelam hydrochloride; b. a polymeric matrix comprising a poly(alkylene), the bile acid chelating agent being dispersed in the polymeric matrix; c. one or more fillers or compression agents selected from microcrystalline cellulose, lactose, starch, maltodextrin, and dicalcium phosphate, wherein the oral dosage form slowly releases the bile acid chelating agent into a stomach. The dosage form is capable of providing the bile acid chelating agent to the stomach in long-lasting and stable level, theconcentration of the bile acid chelating agent permitting the bile acid chelating agent to optimally combine with bile acids refluxing from a small intestine to the stomach, thereby avoiding damages of a gastric mucosa caused by bile acids, and preventing the bile acids in the stomach from refluxing to an esophagus and other parts of an upper digestive tract and a throat, to prevent further damage.

Description

[0001] This application is a Chinese invention patent application with an application date of January 14, 2014, a priority date of January 15, 2013, an application number of 201480015783.9, and a Chinese invention patent application titled "Gastric Retention and Slow Release Oral Formulation of Bile Acid Sequestrants" divisional application. [0002] Cross References to Related Applications [0003] This application claims priority to US Provisional Patent Application 61 / 752,726, filed January 15, 2013, and US Provisional Application 61 / 914,804, filed December 11, 2013. The entire disclosures of these patent applications are hereby incorporated by reference. technical field [0004] The present disclosure relates broadly to sustained-release dosage forms for gastric retention containing bile acid sequestrants. It also relates to methods for the treatment of diseases of the upper gastrointestinal tract and throat by administration of said dosage forms. Background technique ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/785A61K45/06A61P1/00A61P11/04A61P35/00A61P11/00
CPCA61K9/0065A61K9/2031A61K9/2866A61K31/785A61K45/06A61K38/10A61K31/197A61K31/4439A61K31/506A61K9/2054A61P1/00A61P1/04A61P1/14A61P1/16A61P11/00A61P11/04A61P35/00A61P43/00A61K2300/00A61K9/2013
Inventor V·塞瑟拉曼D·B·赫登K·M·莱斯科
Owner IRONWOOD PHARMA
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