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

Oil based formulations for sublingual and buccal delivery

A delivery system and agonist technology, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, pill delivery, etc., can solve problems such as discomfort, inconvenience, pain, etc.

Inactive Publication Date: 2019-10-22
BIOLINGUS IP LLC
View PDF10 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, many people find such applicators daunting, uncomfortable, painful and / or generally inconvenient
Due to these issues, patient compliance can be an ongoing challenge

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
  • Oil based formulations for sublingual and buccal delivery
  • Oil based formulations for sublingual and buccal delivery
  • Oil based formulations for sublingual and buccal delivery

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Example 1 - Sublingual Insulin Aspart Study

[0099] Dissolve insulin aspart (a rapid-acting insulin analog), exenatide, or a mixture of insulin aspart and exenatide in a solution containing 20% ​​vitamin E oil, 20% polyethylene glycol 200, 20% chlorobutanol, and 40% peppermint alcohol / eucalyptol diluent / flavored oil (TPMCEu) and swirl the mixture until homogeneous.

[0100] Male diabetic mice (C57 / BL6 strain) were from Shanghai SLAC Laboratory Animal Co. Ltd. (Shanghai, China). For the experiments described below, mice of approximately 60 g were used. 5 μL of the resulting oil mixture containing insulin aspart was placed under the tongue of an anesthetized diabetic mouse. Blood glucose was measured at -30 minutes, 0 minutes, 30 minutes, 60 minutes, 120 minutes and 240 minutes.

[0101] Five groups of five mice each were treated. The treatment groups were administered as follows: 1) 5 μg sublingually administered exenatide (SL-exenatide); 2) 100 U / kg sublingually ad...

Embodiment 2

[0104] Example 2 - Sublingual insulin glargine study

[0105] Insulin glargine (a long-acting insulin analog) was dissolved in an oil containing 20% ​​vitamin E oil, 20% polyethylene glycol 200, 20% chlorobutanol, and 40% menthol / eucalyptol diluent / flavor oil ( TPMCEu), the mixture is swirled until homogeneous and absorbed into the solid dosage formulation.

[0106] Male diabetic mice (C57 / BL6 strain) were from Shanghai SLAC Experimental Animal Co., Ltd. (Shanghai, China). One solid dose formulation was placed under the tongue of an anesthetized diabetic mouse. Blood glucose was measured at 0 hours, 1 hour, 2 hours, 4 hours, 8 hours, 20 hours and 24 hours.

[0107] Four groups of five mice each were treated. Treatment groups were administered as follows: 1) Sublingual solid dose formulation placebo (Group 1: SL-CSSR 4; where "CSSR-4" means a solid formulation comprising vitamin E, PEG 200 and flavor oil). 2) 1 IU / kg subcutaneous insulin glargine (group 2: SC-insulin glargi...

Embodiment 3

[0110] Example 3 - "InsulinPlus" Sublingual Insulin Aspart / Insulin Glargine / Exenatide Study 1

[0111] Dissolve insulin aspart, exenatide, and / or insulin glargine in diluent / flavored oil containing 20% ​​vitamin E oil, 20% polyethylene glycol 200, 20% chlorobutanol, and 40% menthol / eucalyptol oil ("CSSR6b") and swirl the mixture until homogeneous.

[0112] Male diabetic mice (C57 / BL6 strain) were from Shanghai SLAC Experimental Animal Co., Ltd. (Shanghai, China). For the experiments described below, mice of approximately 50 g were used. 5 μL of the resulting oil mixture containing the active agents was placed under the tongue of an anesthetized diabetic mouse. Blood glucose was measured at -30 minutes, 0 minutes, 30 minutes, 60 minutes, 120 minutes, 240 minutes, 480 minutes and 720 minutes. Mice were allowed to eat 4 hours later.

[0113] Four groups of five mice each were treated. The treatment groups were administered as follows: 1) Sublingual oil formulation placebo (G...

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

No PUM Login to View More

Abstract

The present invention is a delivery system for sublingual and / or buccal delivery comprising at least one functional oil (i.e. acting as an oil delivery base); at least one surfactant; and at least onepharmaceutically active agent. The invention also includes a method for treating diabetes, for regulating blood glucose levels and / or for treating hyperglycaemia by sublingual or buccal administration of the delivery system where the pharmaceutical agent is insulin and / or an insulin analogue or mimetic, and / or a glucagon-like peptide-1 agonist.

Description

technical field [0001] The present disclosure generally relates to oil-based delivery systems and compositions formulated for sublingual and buccal mucosal delivery of pharmaceutically active agents, and uses thereof. Background technique [0002] Oral formulations for the delivery of active pharmaceutical ingredients such as proteins and peptides include tablets, capsules (hard and soft shells), lozenges, powders, emulsions and liquids. To benefit from such formulations, the active pharmaceutical ingredient must remain bioavailable after passing through acid digestion in the stomach and enzymatic digestion in the gastrointestinal tract. Daily food consumption also affects the bioavailability of active pharmaceutical ingredients, and subjects must have a well-functioning gastrointestinal system to ensure adequate absorption via the gastrointestinal tract. [0003] To avoid these problems with oral administration, many active pharmaceutical ingredients, such as insulin, are ...

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 Applications(China)
IPC IPC(8): A61K9/107A61K9/10A61K38/28A61K31/04A61P5/48
CPCA61K9/006A61K9/06A61K9/08A61K9/107A61K9/2013A61K9/2031A61K31/05A61K38/26A61K38/28A61K47/10A61K47/26A61K47/44A61P3/10A61P5/48A61K38/2278A61K47/22A61K47/34
Inventor 萨伊英·克
Owner BIOLINGUS IP LLC
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