What are some ways to alter pharmacokinetics of an insoluble drug?

18 April 2022 1 5K Report

For a drug that is practically insoluble in water and sparingly soluble in ethanol and DMSO, how may each of the following factors be manipulated to maximize the drug exposure when applied into a sustained-release injection (parenteral or IV) formulation?

particle size distribution
API crystal form (anhydrous/monohydrate) -> any effect?
suspension solution (aqueous/oil)
route of administration (SC/IV/IM)
metabolizing enzyme induction/inhibition (CYP/UGT)

James Demers

There's probably no one recipe for all drugs. I think it's pretty consistent that an amorphous form, if you can obtain it, is more rapidly soluble, and that smaller particles dissolve more quickly (due to the larger surface area), but the other factors will vary from one drug to the next. You don't specify if you're relying on low (slow) solubility for the sustained release effect.

Badges
Science topic

More Min Gui Jang's questions See All

Difference between assessing EC50 in presence of physiological levels of human serum albumin and alpha1 acid glycoprotein vs. % human serum?

01 February 2021 1,825 1 View

How would you assess protein binding adjusted EC50 for a drug that has a binding rate of over 95%?

I'm in need of a reference or a method to come up with a protocol that allows one to get the protein-adjusted EC50 for an antiviral drug in presence of human serum albumin and acid glycoprotein.

27 January 2021 1,402 1 View

What factors may contribute to the PK differences in rats and mice?

I can fathom the idea of PK being different b/w dogs and rodents, but why would I be seeing a significantly different PK profile for the same drug tested on rats and mice?

10 September 2020 8,697 5 View

error in running a model in Abaqus

Excessive rotation of nodes in node set ErrNodeExcessRotation-Step1

17 August 2021 0 0 View

error in modelling model in Abaqus

Excessive rotation of nodes in node set ErrNodeExcessRotation-Step1

17 August 2021 0 0 View

MGL tools

20 June 2021 0 0 View

How climate change will influences human and animal behavioral change?

The role of climate change influencing the human behavior as well as economics interest

01 June 2021 0 0 View

flexibility of polymers chain

effect of double bond on the flexibility of polymers

07 April 2021 0 0 View

i have some problem with chtMultiRegionSimpleFoam

--> FOAM FATAL ERROR: Maximum number of iterations exceeded From function Foam::scalar Foam::species::thermo::T(Foam::scalar, Foam::scalar, Foam::scalar, Foam::scalar (Foam::species::thermo::*)(Foam::scalar, Foam::scalar) const, Foam::scalar (Foam::species::thermo::*)(Foam::scalar, Foam::scalar) const, Foam::scalar (Foam::species::thermo::*)(Foam::scalar) const) const [with Thermo = Foam::hConstThermo >; Type = Foam::sensibleEnthalpy; Foam::scalar = double; Foam::species::thermo = Foam::species::thermo >, Foam::sensibleEnthalpy>] in file /home/ubuntu/OpenFOAM/OpenFOAM-4.1/src/thermophysicalModels/specie/lnInclude/thermoI.H at line 66. FOAM aborting #0 Foam::error::printStack(Foam::Ostream&) at ??:? #1 Foam::error::abort() at ??:? #2 Foam::heRhoThermo >, Foam::sensibleEnthalpy> > > >::calculate() at ??:? #3 Foam::heRhoThermo >, Foam::sensibleEnthalpy> > > >::correct() at ??:? #4 ? at ??:? #5 __libc_start_main in "/lib/x86_64-linux-gnu/libc.so.6" #6 ? at ??:?

24 March 2021 0 0 View

Formulation of polymer color flakes

I am writing to request some information for making polymer color flakes. I would appreciate the help.

17 March 2021 0 0 View

Can we classify HV and LV lines based on line length?

I have dataset which shows the length of power lines. I need to classify the lines based on the line length. Is there a rule to classify the High voltage (HV) and low voltage (LV) lines based on...

03 March 2021 4,116 4 View

What's the best way to measure growth rates in House sparrow chicks from day 2 to day 10?

What's the best way to measure growth rates in House sparrow chicks from day 2 to day 10? Since, the growth curve from day 2 to 10 won't be like the "Logistic curve" it might not follow logistic...

03 March 2021 1,401 3 View

How two melting peaks in DSC of polypropylene can be merged into one crystallization peak?

The figure shows DSC cooling (blue) and 2nd heating (green) curves (step: 10 K/min) for a commercial sample supplied as Atactic Polypropylene (APP). The heating curve illustrates two major...

03 March 2021 5,857 3 View