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High bioavailability oromucosal pharmaceutical preparations based on cyclodextrin and sucralose

A technology of sucralose and availability, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of drug bioavailability, easy discoloration, and no description modification Other effects of sucralose and other issues

Active Publication Date: 2018-11-09
ALTERGON
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Sucralose in its anhydrous state tends to discolor at high temperatures; this problem has been addressed by European patent 0375122B1: it describes the complexing of crystalline sucralose with small amounts of beta-cyclodextrin (about 5-20%) , can be used to stabilize sucralose against thermal degradation; the patent does not address the difficulty of drug bioavailability and does not describe the role of modified sucralose other than sweetener

Method used

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  • High bioavailability oromucosal pharmaceutical preparations based on cyclodextrin and sucralose
  • High bioavailability oromucosal pharmaceutical preparations based on cyclodextrin and sucralose
  • High bioavailability oromucosal pharmaceutical preparations based on cyclodextrin and sucralose

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0052] Example 1: Preparation of the ternary complex testosterone / HPBCD / sucralose (molar ratio: 1.0:2.0:0.2)

[0053] Pour 278.95 g of deionized water into the dissolver at room temperature, add 279.62 g of hydroxypropyl β-cyclodextrin and dissolve with stirring at 500 rpm until completely dissolved so that the solution appears clear with no visible residue.

[0054] 6.821 g of sucralose was added to the solution and mixed at 500 rpm for 5 minutes at room temperature until fully dissolved so that the solution appeared clear with no visible residue. 26.4 g of testosterone was added to the solution with continuous stirring until completely dissolved (solution appeared clear with no visible residue). The resulting solution was diluted with the remaining aliquot of water corresponding to 172.43 g. The mixture was stirred at room temperature at 500 rpm for 10-15 minutes to homogenize the solution.

[0055] A spray-drying process is performed to obtain the final powder (spray-dr...

example 2

[0056] Example 2: Preparation of binary complex HPβCD / testosterone (molar ratio: 2.0:1.0)

[0057] Pour 278.95g of deionized water into the dissolver at room temperature, add 279.62g of hydroxypropyl β-cyclodextrin and dissolve it by stirring at 500rpm for 5 minutes until completely dissolved so that the solution appears clear and has no visible residue thing.

[0058] Under continuous stirring, 26.4 g of testosterone was added to the solution until completely dissolved (the solution appeared clear and had no visible residue. The resulting solution was diluted with the remaining aliquots of water equivalent to 172.43 g. The mixture was heated at room temperature at 500 rpm Stir for 10-15 minutes to homogenize the solution.Perform a spray drying process to obtain the final powder (spray drying mixture).

example 3

[0059] Example 3: Penetration studies through epithelial cells

[0060] The mechanism of absorption enhancement was demonstrated by testing buccal epithelial cells grown in vitro using simulated saliva at pH 6.8 (M.R.C. Marques et al., “Simulated Biological fluids with Possible application in dissolution testing”; Dissolution Technologies August 2011).

[0061] Simulated saliva at pH 6.8

[0062] Under magnetic stirring, dissolve 8.00 g of sodium chloride, 0.19 g of potassium dihydrogen phosphate and 2.38 g of disodium hydrogen phosphate in 1 L of H 2 O, after dissolution, acidify to pH 6.8 with 85% phosphoric acid.

[0063] Sample solution 1: Ternary compound of testosterone / HPβCD and spray-dried sucralose (molar ratio: 1.0:2.0:0.2)

[0064] Under slow magnetic stirring, 300 mg of the ternary complex of testosterone / HPβCD and spray-dried sucralose was dissolved in 50 mL of simulated saliva, pH 6.8. The final concentration of testosterone in solution was equal to 0.516 mg...

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Abstract

The invention relates to a new composite based on hydroxypropyl-beta-cyclodextrin, sucralose, a pharmaceutically active ingredient (API) complexed in said hydroxypropyl-beta-cyclodextrin, and optionally an aqueous vehicle. The composite is obtainable by a complexation process of the API in hydroxypropyl-beta-cyclodextrin, carried out in the presence of sucralose. The composite ensures a surprisingly high API bioavailability through buccal route of absorption, due to a high absorption rate through the oral membrane. The composite is therefore suitable for the preparation of oromucosal pharmaceutical compositions, e.g. buccal or sublingual tablets, orodispersible film, etc., having high bioavailability.

Description

technical field [0001] The present invention relates to the field of oromucosal pharmaceutical compositions, ingredients and methods for their preparation. The present invention is based on the identification of new drug complexes with high bioavailability and on the use of said complexes for the preparation of mucosal pharmaceutical compositions. Background technique [0002] The administration of active ingredients should take into account different factors, among them: the solubility of the active ingredient in the biological medium with which it comes into contact at the time of administration, the permeability of the active substance through the biomembrane in order to reach the systemic circulation, the event of elimination before the systemic circulation and patient compliance sex. The latter factor is against e.g. the parenteral route of administration, which on the one hand achieves the immediate arrival of the drug into the systemic circulation and rapidly promote...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61P13/10
CPCA61K9/0007A61K9/0056A61K9/006A61K9/0095A61K9/1617A61K9/1652A61K9/2013A61K9/205A61K31/568A61K31/57A61K47/10A61K47/32A61K47/36A61K47/38A61K47/40A61K47/6951A61P13/10A61P15/00A61K9/19A61K47/26
Inventor 洛伦佐·贝罗里尼卢卡·诺切利蒂齐亚诺·福萨蒂
Owner ALTERGON
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