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Therapeutic formulations and uses thereof

A technology of crystallization inhibitors and tablets, which can be used in pill delivery, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems affecting API activity and bioavailability

Pending Publication Date: 2022-06-03
BONOMICS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such formulation studies take into account factors such as pH, solubility, particle size, polymorphism, etc., which ultimately affect bioavailability and thus the activity of the API at the time of formulation

Method used

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  • Therapeutic formulations and uses thereof
  • Therapeutic formulations and uses thereof
  • Therapeutic formulations and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0228] Example 1 (Ex1): Preparation of a representative spray-dried dispersion (SDD) composition of the present invention

[0229] Approximately 150g of the compound (I) (also referred to as "BNC210") is dissolved in a mixture of 4kg of dichloromethane and methanol (80:20% w / w). An appropriate amount of polymer (Table 1) was added to the solution, the mixture was stirred to give a homogeneous solution. Alternatively, additional excipients such as SLS sodium lauryl sulfate are added. Spray dry the solution using a Büchi B290 spray dryer with two fluid nozzles. The representative composition and physical appearance of the spray-dried dispersion powder are given in Table 1.

[0230]

[0231]

Embodiment 2

[0232] Example 2 (Ex2): Preparation of a representative hot melt extrusion (HME) dispersion composition of the present invention

[0233]Using Turbula Blender, about 6g of compound (I) (also known as "BNC210") and HPMCAS-H polymers were mixed, the blend was de-blocked through 25 meshes and blended again. The blended mixture is fed down at a screw speed of 200 rpm into a HAAKE Mini CTW extruder with a reverse screw rotation configuration of 165 °C or 175 °C or 180 °C and pressed by a mold. Optionally, use a dry cold but roller to quench the extrudate to cool. Grind the extrudate through a 60 mesh sieve.

[0234] The representative composition of the hot melt extruded extrusion and its physical appearance are given in Table 2.

[0235]

[0236]

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Abstract

The present invention relates to formulations of Compound (I) (BNC210), compound (I) (BNC210) being an allosteric modulator of the alpha7-nicotinic receptor, having a non-sedative anti-anxiety effect; specifically, the invention relates to solid dispersions, methods of manufacture thereof, and methods of treatment and uses thereof in the treatment of central nervous system diseases.

Description

Technical field [0001] The present invention relates in general to a therapeutic formulation comprising a therapeutic compound exhibiting a non-sedative anxiolytic effect, the preparation of the formulation, and the method and use of the formulation in the treatment of anxiety and related central nervous system diseases. Background [0002] Formulation science is a complex but very important aspect of creating physiologically effective drugs, which ensure that active pharmaceutical ingredients (APIs) are delivered to the desired parts of the body at the correct concentration and rate, thus achieving an effective therapeutic response while also avoiding any undesirable side effects. There are actually thousands of excipients / ingredients for the formulator to choose in order to promote the desired effect, which largely depends on the physical properties of the API and the desired pharmacokinetics (PK). [0003] In addition to the above, the specific form of the formulation is oral ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4375A61P25/22A61K9/20A61P25/24
CPCA61K31/5377A61P25/22A61K9/2054A61K9/2027A61K9/2095A61K9/146A61K9/1652A61K31/405A61K9/1635A61K9/2013A61K9/1617A61K47/20A61K47/12
Inventor 达拉姆·保罗茱莉亚·克罗斯曼伊丽莎白·杜林汤姆·雷诺兹吴向明杰夫·米兰托马斯·斯塔普菲格克里斯蒂·当宁
Owner BONOMICS LTD
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