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Parathyroid hormone (pth) containing pharmaceutical compositions for oral use

A composition and drug technology, applied in the direction of drug combination, sugar-coated pills, pharmaceutical formulations, etc., can solve the problem of slow release of active substances

Inactive Publication Date: 2006-08-09
NYCOMED DANMARK AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, known drug delivery systems for colonic delivery result in a relatively slow release of the active substance after a certain lag time

Method used

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  • Parathyroid hormone (pth) containing pharmaceutical compositions for oral use
  • Parathyroid hormone (pth) containing pharmaceutical compositions for oral use
  • Parathyroid hormone (pth) containing pharmaceutical compositions for oral use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0414] Preparation of PTH-containing tablets for intestinal delivery (jejunum)

[0415] This example illustrates the preparation of tablets for intestinal delivery (jejunum). The composition of the tablets is shown in Table 1.

[0416] Table 1

[0417] Ingredient Quantity (g)

[0418] PTH (lyophilized PTH) 120.0

[0419] insulin inhibitor 1 600.0

[0420] Sodium Lauryl Sulfate 34

[0421] Microcrystalline cellulose 560.0

[0422] Sodium carboxymethyl cellulose 560.0

[0423] Polyvinylpyrrolidone 90 26

[0424] Magnesium Stearate 10.0

[0425] Talc 90.0

[0426] Total 2000.0

[0427] 1. Assuming an effective concentration of about 0.5 mg / ml, the maximum intestinal volume of a 100 cm intestine is about 500 ml. Burst release covers 20cm of intestine, that is, the required effective dose is 0.5mg / ml×500ml×0.2m=50mg / dose.

[0428] The components are mixed in a high shear mixer and the granules are wetted and dried in a fluidized bed to an absolute...

Embodiment 2

[0448] Preparation of PTH-containing tablets for intestinal delivery (ileum)

[0449] This example illustrates the preparation of tablets for intestinal delivery (ileum). The composition of the tablet is shown in Table 4.

[0450] Table 4

[0451] Ingredient Quantity (g)

[0452] PTH (lyophilized PTH) 120.0

[0453] Amatadine 2 31.8

[0454] sodium deoxycholate 3 720.0

[0455] Microcrystalline cellulose 500.1

[0456] Sodium carboxymethylcellulose 500.1

[0457] Polyvinylpyrrolidone 90 28

[0458] Magnesium Stearate 10.0

[0459] Talc 90.0

[0460] Total 2000.0

[0461] 2. Assuming an effective concentration of about 0.0265 mg / ml (50 μΜ), the maximum intestinal volume of a 100 cm intestine is about 500 ml. Burst release covers 20cm of intestine, that is, the required effective dose is 0.0053mg / ml×532ml×0.2m=0.56mg / dose.

[0462] 3. Calculated at 3% of the solid dosage form, not in the dissolved form.

[0463] Tablets were pre...

Embodiment 3

[0476] Preparation of PTH-containing cores for colonic delivery

[0477] This example illustrates the preparation of cores for colonic delivery. The composition of the core is shown in Table 6.

[0478] Cores were prepared using extrusion / spheronization techniques.

[0479] Table 6

[0480] Ingredient Quantity (g)

[0481] PTH (lyophilized PTH) 400.0

[0482] Aprotinin 4 250.0

[0483] EDTA 1000.0

[0484] Microcrystalline cellulose 337.5

[0485] Lactose monohydrate 462.5

[0486] Sodium carboxymethyl cellulose 50.0

[0487] Purified water 775g

[0488] 4. Assuming an effective concentration of about 0.25 mg / ml, the maximum intestinal volume for 100 cm of intestine is 500 ml. Burst release covers 20cm of intestine, that is, the required effective dose is 0.25mg / ml×500ml×0.2m=25mg / dose.

[0489] The components were mixed and wetted in a Fielder high shear mixer. The wetted mass was extruded in a Nica E 140 extruder with a 0.6 mm screen. The...

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Abstract

A pharmaceutical composition for oral administration comprising PTH, wherein the in vitro release of PTH-when tested in a dissolution test of pharmacopoeia standard-is delayed with at least 2 hours and once the release starts, at least 90% w / w such as, e.g., at least 95% or at least 99% of all PTH contained in the composition is released within at the most 2 hours. The composition may also comprises a calcium containing compound and / or a vitamin, D. In particular, PTH is administered in combination with a calcium-containing compound for the treatment or prevention of bone-related diseases, so that I) an effective amount of a calcium-containing compound is administered to lower the plasma level of endogenous PTH, and II) an effective amount of PTH is administered to obtain a peak concentration of PTH once the endogeneous PTH level is lowered. This present a potential therapeutic or prophylactic regimen for bone-related disorders including osteoporosis.

Description

field of invention [0001] The present invention relates to pharmaceutical compositions containing parathyroid hormone (PTH), optionally in combination with suitable calcium- and / or vitamin D-containing compounds, for prophylaxis and / or treatment Conditions in which inhibitors of bone resorption are indicated include patients suffering from or at risk of, eg, osteoporosis. [0002] Furthermore, the present invention relates to novel pharmaceutical compositions, which are particularly suitable for the delivery of proteins / peptides such as PTH to specific parts of the gastrointestinal tract, such as the small intestine or colon. The pharmaceutical composition is designed to delay the release of the active substance by a combination of two principles, namely a combination of pH control mechanism and / or time control mechanism. Furthermore, the pharmaceutical composition is designed to release the active substance relatively quickly after a release delay in order to ensure that the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K9/50A61K38/29A61K9/16A61K31/59A61K33/06A61K45/06
CPCA61K9/5078A61K45/06A61K31/59A61K33/06A61K38/29A61K9/1652A61K9/1611A61K9/5073A61K9/2886A61K9/5084A61P19/00A61P19/10A61K2300/00A61K9/28
Inventor 利斯贝思·邦勒克卡琳·勒文施泰因·克里斯滕森吉米·希施斯普龙·施吕特汉内·阿内特·默斯格德
Owner NYCOMED DANMARK AS
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