Thought would reactivate this old thread I found seeing something recent just occurred re propofol
Excuse any format issues as on ph doing this but will provide links end of post.
The patent for PARENTERAL AQUEOUS PHARMACEUTICAL COMPOSITION has just been published as per below copy - date emphasis by me.
Pub. No.: WO/2018/225229 International Application No.: PCT/JP2017/021392
Publication Date: 13.12.2018 International Filing Date: 08.06.2017
IPC:
A61K 9/00 (2006.01) ,A61K 47/22 (2006.01) ,A61K 47/26 (2006.01) ,A61K 9/08 (2006.01) ,A61K 31/05 (2006.01)
Applicants:
TERUMO KABUSHIKI KAISHA [JP/JP]; 44-1, Hatagaya 2-chome, Shibuya-ku, Tokyo 1510072, JP
PHOSPHAGENICS LIMITED [AU/AU]; Unit A8, 2A Westall Road, Clayton VIC 3168, AU
Inventors:
IWAKIRI, Chisato; JP
EL-TAMIMY, Mahmoud; AU
GAVIN, Paul; AU
Now, we know there was an original filing way back and this WIPO publication phase is described as follows:
International Publication: as soon as possible after the expiration of 18 months from the earliest filing date,
the content of your international application is disclosed to the world.
So...a couple of snips of what it's about.
Can read further details and technical info from links obviously.
I underlined a couple of findings last couple paragraphs re timings on administration time frame and stability of the composition.
And yes, we know that patents don't gtee $ before "someone" says it, however, they do provide the opportunity to protect potential $ if something goes commercial and the data and claims at the least appear quite positive at this juncture
Also found a couple of other smaller items that appear to have been getting dealt with in the background this year but will try get to that tomoz.
Summary of Invention
Technical Problem
[0005]
Similar to Patent Literature 1, the inventors of the present invention conducted intensive studies under the purpose of obtaining a parenteral aqueous pharmaceutical composition containing propofol. During that process, the inventors attempted to prepare a parenteral aqueous pharmaceutical composition by adopting particular substances as a solubilizing agent. As a result of this attempt, it was found that white cloudiness or precipitation of a solution occurs after the composition is stored at a room temperature. The occurrence of white cloudiness in the parenteral aqueous pharmaceutical composition is not desirable from the viewpoint of not only the quality but also the outer appearance of a pharmaceutical product. As such, the current state is that development of a parenteral aqueous pharmaceutical composition containing propofol, which has suppressed occurrence of white cloudiness or precipitation even after the composition is stored at a room temperature, is needed.
Solution to Problem
[0007]
The inventors of the present invention conducted intensive studies to solve the above problems. As a result, it was surprisingly found that, by using polysorbate 20 in combination with polysorbate 80 as a solubilizing agent, controlling their total content and content mass ratio within a specific range, controlling the total content of TPM in a composition within a specific range, and controlling pH of a composition within a specific range,
the above problems can be solved, and the present invention is completed accordingly.
Advantageous Effects of Invention
[0009]
According to the present invention, a parenteral aqueous pharmaceutical composition containing propofol which has suppressed occurrence of white cloudiness or precipitation even after the composition is stored at a room temperature can be provided.
(TPM)
Furthermore, the parenteral aqueous pharmaceutical composition according to this embodiment also contains a mixture (i.e., TPM) of mono(tocopheryl) phosphate (also referred to as "TP") and di(tocopheryl) phosphate (also referred to as "T2P") as a solubilizing agent. According to the determination by the inventors of the present invention, controlling the blending amount of TPM is also effective for suppressing the white cloudiness or precipitation after the composition is stored at a room temperature described above.
Summary and purpose of experiment)
In the attached document relating to Diprivan, it is described as a caution for application that "the preparation should not be admixed with other pharmaceutical preparation before administration (except 5% glucose solution for injection). The dilution ratio for diluting the preparation with 5% Dextrose injection (glass container) should not be greater than 5 times (i.e., propofol concentration is 2 mg/mL or higher).
The dilution needs to be carried out aseptically right before administration, and use thereof should be made within 6 hours". Furthermore, it is also described that "this preparation may be administered together with 5% Dextrose Injection, USP, Lactated Ringers Injection, USP, Lactated Ringers and 5% Dextrose Injection and 5% Dextrose and 0.45% Sodium Chloride Injection, USP".
[0058]
Accordingly, determination was made to see whether or not the clear propofol solution of the present invention satisfies the above conditions.
As shown in Fig.1 and Tables 20 to 23, stability was shown for every item without having any change over 24hours. Thus, it was found that the preparation can be diluted by 5 times with 5% glucose solution for injection, lactic acid Ringers solution, lactic acid Ringers solution added with glucose, and physiological saline added with glucose,
and it can be used over 24 hours after dilution.
The parenteral aqueous pharmaceutical composition according to any one of claims 1 to 6,
wherein the parenteral aqueous pharmaceutical composition is a composition for injection.
https://patentscope.wipo.int/search...FP:(Phosphagenics)&recNum=1&maxRec=70
https://www.wipo.int/pct/en/faqs/faqs.htmlhttp://manuals.ipaustralia.gov.au/p...se/2.20.1.3A_National_Phase_Preliminaries.htm
http://manuals.ipaustralia.gov.au/p...se/2.20.1.3A_National_Phase_Preliminaries.htm
(20min delay)
