pjs
★    

India,
2015-05-11 16:06
(3244 d 15:46 ago)

Posting: # 14783
Views: 6,668
 

 PK linearity of propranolol [PK / PD]

Dear all,

Please suggest if Propranolol Pharmacokinetics is linear or nonlinear in the dose range of 5-40mg.

Regards,
PJS
Helmut
★★★
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Vienna, Austria,
2015-05-11 16:46
(3244 d 15:06 ago)

@ pjs
Posting: # 14784
Views: 5,604
 

 Learn to google!

Hi PJS!

❝ Please suggest if Propranolol Pharmacokinetics is linear or nonlinear in the dose range of 5-40mg.


You do yourself no good posting trivial questions. Have you ever heard about [image]?
click: :google:
I’m not aware of any marketed 5 mg strength. Can you enlighten me?

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pjs
★    

India,
2015-05-11 17:06
(3244 d 14:46 ago)

@ Helmut
Posting: # 14785
Views: 5,541
 

 Learn to google!

Hi Helmut,

Thanks for the quick n brief response.

❝ I’m not aware of any marketed 5 mg strength. Can you enlighten me?


Propranolol oral solution in the streangth of 5-40mg/5ml strength is available.

If we develop oral solution in similar strength comaparing it with Innovator (tab). Data regrding PK linearity in the dose range for waiver of BE for additional strength is needed.

Regards,
PJS
Dr_Dan
★★  

Germany,
2015-05-11 19:30
(3244 d 12:22 ago)

@ pjs
Posting: # 14786
Views: 5,582
 

 PK linearity of propranolol

Dear PJS
Propranolol is almost completely absorbed after oral administration. However, it undergoes high first-pass metabolism by the liver and on average only about 25% of propranolol reaches the systemic circulation. Propranolol is a substrate for the intestinal efflux transporter, P-glycoprotein (P-gp). However, studies suggest that P-gp is not dose-limiting for intestinal absorption of propranolol in the usual therapeutic dose range.
I hope this helps
Kind regards
Dr_Dan

Kind regards and have a nice day
Dr_Dan
pjs
★    

India,
2015-05-12 10:46
(3243 d 21:06 ago)

@ Dr_Dan
Posting: # 14787
Views: 5,532
 

 PK linearity of propranolol

Dear DR Dan,

Thanks for your response.

Some of the published literature have suggested more than proportional increase at steady state in Plasma drug concentration in the dose range of 40-320mg once daily .

However, some PAR have suggested linear pharmacokinetics in the dose range. (10-80 mg).

There has been no mention regarding the linearity at the dose of 5mg.

Please suggest.

Regards,
PJS
Dr_Dan
★★  

Germany,
2015-05-12 18:58
(3243 d 12:54 ago)

@ pjs
Posting: # 14794
Views: 5,474
 

 PK linearity of propranolol

Dear PJS
The absolute BA varies between 5 and 50%, due to a high pre-systemic metabolism. As a result, the BA and plasma levels show a large inter-individual variability and the question of linear PK cannot be answered directly. The presence of an absorption window cannot be ruled out from published data but the postulated mechanism of the permeability of propranolol: passive transport driven by the strong lipophilic nature of the substance, makes the existence of such an absorption window unlikely. In a provisional classification of the WHO Essential Drugs, this API was classified to be BCS Class I. So, from a scientific point of view this API is a candidate for granting a biowaiver.
I hope this helps.
Kind regards
Dr_Dan

Kind regards and have a nice day
Dr_Dan
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