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Night-time oral insulin therapy

A technology for insulin and diabetes, applied in the field of oral delivery of effective doses of insulin into the blood, which can solve problems such as interference and hypoglycemia

Inactive Publication Date: 2006-03-29
EMISPHERE TECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, interfering events can occur between meal and insulin administration, and food intake can affect the expected glucose excursion
Furthermore, hypoglycemia is also possible if insulin is administered at an inappropriate time (for example, after the elevated glucose level due to eating has decreased) to provide efficacy

Method used

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  • Night-time oral insulin therapy
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  • Night-time oral insulin therapy

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0163] Preparation of delivery agent 4-CNAB

[0164] Compounds corresponding to the following structures were prepared as described below:

[0165]

[0166] 4-Chlorosalicylic acid (10.0 grams, 0.0579 moles) was added to a 250 ml single necked round bottom flask containing about 50 ml of dichloromethane. Stirring was started and continued for the remainder of the reaction. The coupling agent 1,1-carbonyldiimidazole (9.39 g, 0.0579 mol) was added to the flask as a solid portion. After adding all the coupler, stir at room temperature for about 20 minutes, then add ethyl-4-aminobutyric acid hydrochloride (9.7 g, 0.0579 mol) with stirring. Then, triethylamine (10.49 ml, 0.0752 mol) was added dropwise through a funnel. The funnel was rinsed with dichloromethane. The reaction was stirred overnight at room temperature.

[0167] The reactant was poured into a separatory funnel and washed with 2 N hydrochloric acid to form an emulsion. The emulsion was allowed to stand for 2 da...

example 2

[0178] Nonclinical studies of 4-CNAB and insulin / 4-CNAB

[0179] For the composition of the present invention comprising insulin and delivery agent 4-CNAB, the safety and toxicity in non-clinical programs were evaluated, including pharmacological screening, pharmacokinetic distribution and toxicity evaluation in mice and monkeys. In general, the physiological responses of animals to 4-CNAB alone were comparable to those to insulin / 4-CNAB. Pharmacokinetic studies in mice, rats and monkeys have shown that 4-CNAB is rapidly absorbed after oral administration and then cleared from the body. In receptor binding screening assays, 4-CNAB did not show potential activity at any of the primary molecular targets. Four genotoxicity studies conducted with 4-CNAB were not positive. Based on a 14-day oral repeated dose toxicity study, the NOAEL (No Adverse Effect Level) was estimated to be 500 mg / kg in Sprague-Dawley rats and 400 mg / kg in rhesus monkeys.

[0180] In toxicity studies, dose...

example 3

[0184] This example describes the method for preparing insulin / 4-CNAB capsules. 4-CNAB prepared as above was first screened through a 35 mesh. Weigh the desired amount of screened 4-CNAB and place in a covered weighing pan. Weigh the required amount of insulin into the covered weighing pan.

[0185] The above insulin was sifted through a 35 mesh onto the same mortar and approximately 2.0 grams of 4-CNAB was sifted through the same 35 mesh onto the insulin. Gently grind the contents of the mixing mortar with a glass mortar and pestle for 3 minutes, scraping with a spatula if necessary. The above 4-CNAB was continued through a 35 mesh screen in a small fraction corresponding to the volume of the material in the mortar. The contents of the mortar were mixed for approximately 3 minutes after each addition.

[0186] After the final addition, gently grind the contents of the mixing mortar with a glass mortar and pestle for 3 minutes, scraping with a spatula if necessary. The fi...

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PUM

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Abstract

A method for protection of a mammal that has impaired glucose tolerance or early stage diabetes mellitus from developing overt or insulin dependent diabetes comprises administering an orally effective dose of a pharmaceutical formulation comprising insulin at nighttime, e.g., at or shortly before bedtime.

Description

field of invention [0001] The present invention relates to the oral delivery of a therapeutically effective dose of insulin into the bloodstream as part of a regimen for the treatment of diabetes. The present invention further relates to a composition of an oral delivery agent and insulin to facilitate the delivery of a therapeutically effective dose of insulin into the blood for the treatment of diabetes. The present invention further relates to oral administration of insulin preparations and a delivery agent at or shortly before bedtime for the treatment of diabetes. Background of the invention [0002] Proteins, polypeptides and other biomolecules ("biomacromolecules", ie biopolymers such as proteins and polypeptides) are increasingly used in many fields of science and technology. For example, proteins are used as active agents in the field of pharmaceuticals, vaccines and veterinary products. Unfortunately, the presence of natural absorption barriers of channels where ...

Claims

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Application Information

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IPC IPC(8): A61K38/28
Inventor M·戈尔德贝格E·阿维特
Owner EMISPHERE TECH INC
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