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Pharmaceutical composition comprising an androgen receptor inhibitor

a technology of androgen receptor antagonists and compositions, applied in the field of pharmaceuticals, can solve the problems of not always improving the bioavailability of low-solubility drugs combining drugs with solubilizing polymers, and unable to suppress ar when cancer becomes hormone refractory, etc., to achieve high patient compliance, mask bitter taste, and pleasant taste

Inactive Publication Date: 2019-07-11
FTF PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a liquid pharmaceutical composition that includes an androgen receptor inhibitor and several other excipients such as fillers, solvents, and preservatives. The composition has improved stability and taste, and can be adjusted for different patient needs. The liquid composition also has a better dissolution profile. This makes it easier for patients to swallow the medication. Additionally, the composition includes a sweetening and flavoring agent to mask the bitter taste of the medication.

Problems solved by technology

Although initially effective, these treatments quickly fail and the cancer becomes hormone refractory.
While it has an inhibitory effect on AR in hormone sensitive prostate cancer, it fails to suppress AR when cancer becomes hormone refractory.
Two weaknesses of current antiandrogens are blamed for the failure to prevent prostate cancer progression from the hormone sensitive stage to the hormone refractory disease and to effectively treat hormone refractory prostate cancer.
Combining drugs with solubilizing polymers does not always improve bioavailability for a low-solubility drugs, however.
Solubilization of a specific drug depends on its chemical structure and physical properties; therefore, whether any particular polymer will solubilize a specific drug is not necessarily predictable.
It is often difficult and time-consuming to select polymers which achieve improved solubilization, because the drug-polymer interaction is poorly understood.
For example, addition of polymers may actually speed dissolution of a drug, rather than provide enhanced concentration.
These preparations have their own disadvantages and limitations, for example they are not suitable for all types of patient populations.
Oral solid dosage forms may not be convenient for all types of patient populations (e.g. paediatric patients) to take because of swallowing problems.

Method used

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  • Pharmaceutical composition comprising an androgen receptor inhibitor

Examples

Experimental program
Comparison scheme
Effect test

example 1

A Liquid Oral Pharmaceutical Composition Comprising Enzalutamide

[0066]

TABLE 2Enzalutamide liquid composition (Example-1)Sr.No.Ingredientmg / 5 ml1Enzalutamide1602Labrasol / Labrasol ALF / PEG2600300 / PEG 400 or combination ofsolubilizer3ButylatedHydroxyanisole (BHA)2.04Butylatedhydroxytoluene (BHT)0.45Sucralose256Mint flavour2.07Ethanol982.58Medium chain triglycerideQ.S. to 5 ml(Kollisolv ® MCT 70)

[0067]Method of Preparation:

[0068]A liquid oral pharmaceutical composition comprising Enzalutamide as active ingredient and Labrasol, ButylatedHydroxyanisole (BHA), Butylatedhydroxytoluene (BHT), Sucralose, Mint flavour, Ethanol and Kollisolv® MCT 70 was prepared following below mentioned process comprising steps of: (a) Mix the required quantity of Labrasol / Labrasol ALF / PEG 300 / PEG 400 or combination of solubilizer and Ethanol under stirring;[0069](b) Dissolve required quantity of Enzalutamide in the mixture obtained in Step (a);[0070](c) Add required quantity of Sucralose to the mixture obtaine...

example 2

A Liquid Oral Pharmaceutical Composition Comprising Enzalutamide

[0075]

TABLE 3Enzalutamide liquid composition (Example-2)Sr. No.Name of Ingredientsmg / 5 ml1Enzalutamide1602Labrasol / / Labrasol ALF / PEG3500300 / PEG 400 or combination ofsolubilizer3ButylatedHydroxyanisol(BHA)3.54ButylatedHydroxytoluene(BHT)0.355Sucralose106Mint flavour107Propylene GlycolQ.S. up to 5 ml

[0076]Method of Preparation:

[0077]A liquid oral pharmaceutical composition comprising Enzalutamide as active ingredient and Labrasol, ButylatedHydroxyanisole (BHA), Butylatedhydroxytoluene (BHT), Sucralose, Mint flavour, Ethanol and Propylene glycol was prepared following below mentioned process comprising steps of:[0078](a) Dissolve the required quantity of Labrasol / Labrasol ALF / PEG 300 / PEG 400 or combination of solubilizer in Ethanol. The mixture can be heated at 50-55° C. to get clear solution;[0079](b) Add required quantity of ButylatedHydroxyanisole (BHA and Butylatedhydroxytoluene (BHT) in the pre-heated mixture obtained...

example 3

Stability Studies of the Pharmaceutical Composition Prepared in Example 1

[0084]The oral liquid pharmaceutical composition prepared according to Example 1 exhibits unexpected stability profile when tested after three (3) months under the conditions 40° C. / 75 RH and 250C / 60 RH. The liquid composition according to the present invention possess very less amount of impurities and highest degree of purity. The results of the stability tests conducted are summarized in the table below.

TABLE 4Stability study results of Enzalutamide liquid composition of Example-1ResultsAfter 3 After 3 months atmonths atName of ImpurityLimitInitial40° C. / 75RH25° C. / 60 RHAmine amideNMT 0.2%NDNDNDimpurityTrifluoromethylNMT 0.2%NDNDNDimpurityDioxoimidazolidineNMT 0.2%0.1%0.2%0.1%impurityDesfluoro impurityNMT 0.2%NDNDNDHighest individualNMT 0.2%0.1%0.1%0.1%unspecified impurityTotal amount ofNMT 1.5%0.2%0.4%0.3%impuritiesNMT = Not More Than;ND = Not Detected

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Abstract

The present invention relates to the oral pharmaceutical composition comprising an androgen receptor inhibitor and one or more pharmaceutically acceptable excipients selected from the group comprising of fillers / vehicles, solvents / co-solvents, preservatives / antioxidants, surfactants, buffering agents, chelating agents, sweetening agents, flavouring agents, sweetness / flavour enhancing agents, or combinations thereof. The present invention also relates to the processes for the preparation of the oral pharmaceutical composition comprising androgen receptor inhibitor and one or more pharmaceutically acceptable excipients.

Description

FIELD OF THE INVENTION[0001]The present invention relates, in general, to the pharmaceutical field, and more precisely it relates to a pharmaceutical composition for the oral administration of Androgen Receptor Antagonists and to the process for the preparation thereof. In particular, the present invention relates to the oral liquid composition comprising Enzalutamide.BACKGROUND OF THE INVENTION[0002]The Androgen Receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding either of the androgenic hormones, testosterone, or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor.[0003]The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression; however, the androgen receptor has other f...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4166A61K47/14A61K47/10A61K47/26A61K9/08
CPCA61K9/0053A61K31/4166A61K47/14A61K47/10A61K47/26A61K9/08
Inventor PATEL, NILESHKUMAR BHIKHABHAIGURJAR, LALCHAND DATARAMMANDAL, JAYANTA KUMAR
Owner FTF PHARMA
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