Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A kind of bremelanotide oral pharmaceutical composition and application thereof

A composition and drug technology, applied in the field of bremelanotide oral pharmaceutical composition and its application, and polypeptide drug oral pharmaceutical composition, can solve the complex preparation process, unexplained influence, unexplained gastric absorption, etc. problems, to achieve the effect of improving the degree of absorption, avoiding potential dangers, and solving poor compliance

Active Publication Date: 2022-05-13
北京汇诚瑞祥医药生物科技有限公司
View PDF9 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] U.S. patent application US20180185440A1 discloses oral capsules containing bremelanotide and SNAC. The preparation process is complicated, and the situation of gastric absorption in experimental animals is not described, nor is the effect of in vitro dissolution on the time to peak plasma concentration in animals Influence, did not explain the particle size of bremelanotide raw material and the influence of various excipients on drug dissolution and drug time curve, did not explain the ratio relationship between bremelanotide and SNAC with in vivo pharmacokinetic characteristics comparable to subcutaneous injection preparations and formulation composition

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of bremelanotide oral pharmaceutical composition and application thereof
  • A kind of bremelanotide oral pharmaceutical composition and application thereof
  • A kind of bremelanotide oral pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] Rats were fasted for 16 hours before administration, but had free access to water. After intraperitoneal injection of anesthesia, the rats were placed under a heating lamp to keep the body temperature at about 37°C, and the intestine was exposed through a midline abdominal incision. After the bile duct was ligated, the intestinal tract was flushed with phosphate buffer (pH 7.4), and the remaining buffer was vented with air. Both ends of the small intestine were cannulated with polyethylene tubing. Perfuse the drug solution containing the absorption enhancer or the solution containing only the drug, the volume is 200ml, the solution is Krebs-Ringer solution, and the preparation method is to weigh 7.8g of NaCl, 0.35g of KCl, and 0.35g of CaCl 2 0.37g, NaHCO3 1.37g, NaH 2 PO 4 0.32g, MgCl 2 0.02g, glucose 1.4g, dissolved in a small amount of water, in which CaCl 2 Add dropwise after dissolving separately, add glucose immediately after use, dilute to 1L with purifie...

Embodiment 2

[0108] Rats were fasted for 16 hours before administration, but had free access to water. After intraperitoneal injection of anesthesia, the rats were placed under a heating lamp to keep the body temperature at about 37°C, and the stomach was exposed through a midline abdominal incision. Incision was made at both ends of the stomach, polyethylene tubes were inserted at both ends of the stomach, the stomach was flushed with phosphate buffer (pH 7.4), and the remaining buffer was vented with air. Perfuse the drug solution containing the absorption enhancer or the solution containing only the drug, the volume is 200ml, the solution is Krebs-Ringer solution, and the preparation method is the same as in Example 1. The perfusion solution was maintained at 37°C and the solution administered through the catheter was warmed and circulated. The jugular vein was exposed, and 0.3 ml blood samples were collected by direct puncture of a heparin syringe at 20, 40, 60, 90, and 120 minutes af...

Embodiment 3

[0116] Prepare artificial gastric juice (refer to the preparation method of the United States Pharmacopoeia) and artificial intestinal juice (refer to the preparation method of phosphate buffer solution with a pH value of 6.8 containing trypsin included in the Chinese Pharmacopoeia 2020 edition). Weigh an appropriate amount of bremelanotide, dissolve it with artificial gastric juice and artificial intestinal juice respectively to form a 0.1 mg / ml solution, and place it in a 37°C water bath. The content of bremelanotide in artificial gastric juice and artificial intestinal juice was detected by high performance liquid chromatography. Detection method: high performance liquid chromatography, C 18 Column, detection wavelength 215nm; column temperature 30°C; flow rate 1.0ml / min; injection volume: 20ul; sample concentration 0.1mg / ml; mobile phase A contains 1% trifluoroacetic acid in acetonitrile solution, mobile phase B contains 1% Aqueous solution of fluoroacetic acid; see Table...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention relates to the field of oral pharmaceutical compositions of polypeptide drugs, in particular to an oral pharmaceutical composition of bremelanotide and its application field. The present invention provides a kind of oral pharmaceutical composition and application thereof, and its pharmaceutical composition comprises at least bremelanotide and 8-(2-hydroxybenzamido) octanoic acid sodium, wherein bremelanotide and The weight ratio of 8-(2-hydroxybenzamido) sodium octanoate is 3.2~12:12~18. Compared with the hypodermic injections on the market, the oral pharmaceutical composition of the present invention has a simpler preparation process, avoids the potential danger of microorganisms and bacterial endotoxins in the injections, solves the problem of poor compliance of many patients with injections, and can significantly improve the oral administration of bremerol. In vivo absorption and utilization of Tango.

Description

technical field [0001] The invention relates to the field of oral pharmaceutical compositions of polypeptide drugs, in particular to an oral pharmaceutical composition of bremelanotide and its application field. Background technique [0002] The vast majority of peptide and protein drugs are administered through intramuscular injection, intravenous injection or subcutaneous injection in clinical practice, and pharmacologists have been working on the research of oral formulations of such drugs. Existing studies believe that the digestion products of proteins or polypeptides in the gastrointestinal tract are mainly polypeptides such as dipeptides and tripeptides. For polypeptides consisting of less than 12 amino acids, the possibility of oral administration is relatively high, but for proteins, it is difficult to predict. Currently known mechanisms and pathways for oral absorption of polypeptide and protein drugs include: 1) carrier transport, mainly for small molecule drugs;...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/12A61K9/16A61K9/48A61K47/18A61K47/32A61K47/38A61P15/00
CPCA61K38/12A61K9/1617A61K9/1652A61K9/1635A61K9/4866A61K9/4858A61K9/0053A61P15/00
Inventor 吴涛卢骏冯岩胡建平姜艳崔宏亮
Owner 北京汇诚瑞祥医药生物科技有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com