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Agent kit containing oral insulin solid therapy

A kit and insulin technology, which can be used in medical preparations containing active ingredients, metabolic diseases, peptide/protein components, etc., and can solve problems such as interference and hypoglycemia.

Inactive Publication Date: 2008-07-16
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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  • Agent kit containing oral insulin solid therapy
  • Agent kit containing oral insulin solid therapy
  • Agent kit containing oral insulin solid therapy

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0164] Preparation of delivery agent 4-CNAB

[0165] Compounds corresponding to the following structures were prepared as described below:

[0166]

[0167] 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.

[0168] 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

[0179] Nonclinical studies of 4-CNAB and insulin / 4-CNAB

[0180] 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.

[0181] In toxicity studies, dose...

example 3

[0185] 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.

[0186] 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.

[0187] 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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Abstract

A method for protecting a mammal suffering from impaired glucose tolerance or early diabetes from developing overt diabetes or insulin-dependent diabetes comprising orally administering an effective amount of a pharmaceutical formulation comprising insulin at night (eg, at or shortly before bedtime).

Description

[0001] The patent application of the present invention is the branch of the invention patent application with the international application number PCT / US2004 / 000273, the international application date is January 6, 2004, the application number entering the Chinese national phase is 200480005261.7, and the name is "Night Oral Insulin Therapy". case application. field of invention [0002] 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 [0003] Proteins, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61P5/50A61P3/10
Inventor M·戈尔德贝格E·阿维特
Owner EMISPHERE TECH INC
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