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Oral medication path of somatostatin analogue polypeptide drug

A technology of somatostatin and drug delivery route, which is applied in the field of medicine, can solve the problems of short half-life and instability of somatostatin, and achieve the effect of increasing the application range

Inactive Publication Date: 2015-12-23
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Natural somatostatin is unstable in vivo and has a short half-life (2-3min)

Method used

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  • Oral medication path of somatostatin analogue polypeptide drug
  • Oral medication path of somatostatin analogue polypeptide drug
  • Oral medication path of somatostatin analogue polypeptide drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1 Stability of three kinds of somatostatin analogue polypeptides octreotide, vapreotide, and lanreotide in artificial gastric juice:

[0016] Step 1: Prepare artificial gastric juice according to the formula of the United States Pharmacopoeia. The specific formula is as follows: In 1000 mL of artificial gastric juice, 2.0 g of NaCl, 3.2 g of pepsin, and HCl were added to adjust the pH value to 1.2, and incubated at 37° C. for 30 minutes before use.

[0017] The second step: use the artificial gastric juice in the first step to prepare 1 mL of octreotide, vapreotide, and lanreotide solutions with a concentration of 100 μg / mL, and make 3 copies in parallel, and incubate at 37°C for a certain period of time (0, 10, 30, After 60, 120, and 180 minutes), the reaction was terminated with 3 mL of glacial acetonitrile, centrifuged at 30,000 g for 10 minutes, and the supernatant was taken for detection by LC-MS / MS.

[0018] Step 3: Calculate the residual amount. Taki...

Embodiment 2

[0019] Example 2 Stability of three kinds of somatostatin analog polypeptides octreotide, vapreotide, and lanreotide in artificial intestinal juice:

[0020] Step 1: Prepare artificial intestinal juice according to the formula of the United States Pharmacopoeia. The specific formula is as follows: in 1000mL artificial intestinal juice, trypsin 10.0g, KH 2 PO 4 6.8g, adjust the pH value to 7.5±0.1 with NaOH, and incubate at 37°C for 30 minutes before use.

[0021] The second step: use the artificial intestinal juice in the first step to prepare 1 mL of octreotide, vapreotide, and lanreotide solutions with a concentration of 100 μg / mL, and make 3 copies in parallel, and incubate at 37°C for a certain period of time (0, 10, 30, After 60, 120, and 180 minutes), the reaction was terminated with 3 mL of glacial acetonitrile, centrifuged at 30,000 g for 10 minutes, and the supernatant was taken for detection by LC-MS / MS.

[0022] Step 3: Calculate the residual amount. Taking the ...

Embodiment 3

[0023] Example 3 Blood drug concentration over time after intravenous injection and intragastric administration of three somatostatin analogue polypeptides in rats:

[0024] The first step: 30 male SD rats, 180-200g, were randomly divided into 6 groups, 5 rats in each group, respectively octreotide intravenous injection group, octreotide intragastric administration group, vapreotide intravenous injection group, vapreotide infusion group Stomach group, lanreotide intravenous injection group, lanreotide intragastric administration group.

[0025] Step 2: Before administration, all rats were fasted without water for 12 hours. In the intravenous injection group of the three polypeptides, the rats were injected into the tail vein at a dose of 0.1 mg / kg, and blood was collected in heparinized EP tubes at 2, 5, 10, 20, 40, 60, 90, 120, and 240 minutes; In the gavage group, the dosage of 15, 30, and 60 mg / kg was gavaged with the aqueous solution of the three polypeptides, and the blo...

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Abstract

The invention provides an oral medication path of a somatostatin analogue polypeptide drug, and in particularly relates to an oral medication path of three somatostatin analogue polypeptides, including octreotide, vapreotide and lanreotide, belonging to the field of medicine. The invention provides the stability of the three somatostatin analogues in in-vitro artificial gastric juice and artificial intestinal juice, and the experiments prove that the three somatostatin analogue polypeptides are stable in the artificial gastric juice and can not be degraded; in the artificial intestinal juice, the three polypeptides are gradually degraded along with time, the sequences of the stabilities of the three polypeptides from high to low are as follows: octreotide, vapreotide and lanreotide. The invention further provides the absorbing states of the three polypeptides after the three polypeptides are given to a rat through intragastric administration, and describes the oral pharmacokinetic behaviors of the three polypeptides. According to the invention, on the basis of the original injection paths of the three polypeptides, the oral medication path of the three polypeptides is increased, so that the compliance of a patient is improved.

Description

technical field [0001] The present invention relates to the change of the administration route of somatostatin analog polypeptide octreotide (octreotide), lanreotide (lanreotide), vapreotide (vapreotide), specifically on the basis of its conventional injection administration route, increase The route of oral administration thereof improves the safety and compliance of drug use, and belongs to the field of drugs. Background technique [0002] With the development of life sciences, active peptide drugs have become a key research field in the pharmaceutical industry, and the research and development and marketing of peptide drugs have gradually accelerated. At present, more than 50 peptide drugs have been approved for marketing in the world, about 140 peptide drugs are in clinical research, and 500 to 600 peptide drugs are in the preclinical research and development stage. However, peptide drugs are limited by their physical and chemical properties when taken orally, such as b...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K38/08A61P5/00A61P35/00
Inventor 王广基梁艳饶泰王谦
Owner CHINA PHARM UNIV
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