Delayed release formulations for oral administration of a polypeptide therapeutic agent and methods of using same

A slow-release, therapeutic effect technology, applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, antipyretics, etc., can solve problems such as inconvenient administration, high price, and discomfort of the subjects

Inactive Publication Date: 2005-10-26
WEISS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Subcutaneous formulations must be sterile and expensive compared to other routes of administration
This line is not convenient to use, and it will cause discomfort to the subjects

Method used

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  • Delayed release formulations for oral administration of a polypeptide therapeutic agent and methods of using same
  • Delayed release formulations for oral administration of a polypeptide therapeutic agent and methods of using same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1.rhIL for compatibility of various formulation excipients and antioxidants

[0051] Compatibility studies were performed on rhIL-11 tablets containing formulation excipients and antioxidants listed in Table 1. Excipients studied included fillers, disintegrants, buffers, glidants, and lubricants. A rhIL-11 tablet containing the above-mentioned excipients was prepared by direct compression. The lyophilized rhIL-11 was collected, filtered through a #30 mesh sieve, and transferred to a suitable sized vial containing all other excipients. Mix the material by swirling the vial for 2-3 minutes. For formulations including magnesium stearate (F1, F2, F4-F8), the magnesium stearate was added at this point and mixing continued for an additional 0.5-1 minute.

[0052] Each tablet weighs 150 mg and contains 2.5 mg of rhIL-11 (addition of lyophilized powder prepared from a freeze-dried vial freeze-dried concentrate containing rhIL-11 in quantities equivalent to 5 mg alon...

Embodiment 2

[0055] Example 2: Integrity of rhIL-11 capsules during tablet preparation

[0056] Integrity of rhIL-11 under applied pressure was checked during tablet processing. Different pressures were used to evaluate the effect of tablet manufacturing pressure on rhIL-11 integrity. These tablets weigh 150 mg and contain 2.5 mg of rhIL-11 (lyophilized powder), EXPLOTAB(R), microcrystalline cellulose, NU-TAB(R), silicates and magnesium stearate. Tablets are directly compressed to a hardness of 2.4, 4.0, 7.5 or 12.5 KP. By determining the recovery %, multibody %, Met 58 Protein integrity can be determined by % oxidation, % correlation, and specific activity of rhIL-11 by T-10 bioassay. The test results in Table 4 show that for rhIL-11 tablets compressed into different hardness levels, recovery %, multibody %, Met 58 Oxidation %, correlation % did not change. Similarly, the specific activities of the different formulation mixtures and tablets were within the range stated in the label...

Embodiment 3

[0057] Example 3: Stability of enteric-coated rhIL-11 tablets

[0058] The stability of enteric-coated tablets prepared by the fluidized bed granulation method was determined using HDPE bottles at 40°C / 75%RH and room temperature. Stability experiments include Recovery %, Met 58 Determination of % Oxidation, % Correlation. The measurement results are summarized in Table 6. When stored at room temperature and 40°C / 75%RH, the strength of rhIL-11, Met 58 Oxidation %, relative % did not change.

[0059] In the micro-dissolution device, the dissolution experiment was carried out using 50 ml of glycine / phosphate dissolution medium with stirring speed at 50 or 100 rpm. The coated tablets were first placed in 0.1N HCl for 2 hours, and then placed in glycine / phosphate dissolution medium for 1 hour, and then the release of rhIL-11 from the coated tablets was detected. The dissolution results showed that less than 1% of rhIL-11 was released within two hours in 0.1 N HCl. This show...

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Abstract

The invention provides compositions containing polypeptides, including therapeutic polypeptides such as interleukin-11, that are suitable for oral administration.

Description

field of invention [0001] The present invention relates to compositions suitable for oral administration containing polypeptides, including interleukin-11. Background of the invention [0002] Recombinant human interleukin-11 (rhIL-11) is a non-glycosylated polypeptide containing 177 amino acids. The polypeptide contains no cysteine ​​residues and is highly basic (PI > 10.5). rhIL-11 is a group of human growth factors that includes human growth hormone (hGH) and granulocyte colony-stimulating factor (G-CSF). [0003] rhIL-11 can be used as a chemotherapy support agent and given in combination with other cancer treatments to increase platelet levels. It has been proven that rhIL-11 also has an inflammatory effect and can be used to treat various conditions, such as Crohn's disease and ulcerative colitis. Typically, IL-11 is administered by subcutaneous injection. Subcutaneous formulations must be sterile and are expensive compared to other routes of administration. Th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/28A61K9/36A61K9/50A61K38/20
CPCA61K9/5078A61K9/2846A61K9/2886A61K9/5026A61K38/2073A61P1/04A61P29/00A61P7/00
Inventor 尼古拉斯·W·沃内丽贝卡·科瓦尔阿温德·S·纳吉拉玛奥·S·查特拉帕利埃里克·J·本杰明
Owner WEISS INC
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