Quiz
MD4 How drugs dissolve
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1Pharmaceutical examples of release of drug (API) from dosage forms:
- release from conventional tablets that [blank_start]disintegrate[blank_end]
- release from normal capsules containing [blank_start]solid drug[blank_end]
- release from matrix tablets or pellets: lipid matrix ([blank_start]nonhydrating[blank_end]) and swellable ([blank_start]hydrating[blank_end]) matrix
- release from a coated tablet or coated granules/pellets, where the coat remains [blank_start]intact[blank_end]; liquid & dissolved drug may [blank_start]permeate[blank_end] the film coat- Adisintegrate
- Bsolid drug
- Cnonhydrating
- Dhydrating
- Eintact
- Fpermeate
2There are two steps of the dissolution of a solid dosage form:
1. [blank_start]Detachment[blank_end] of molecules [blank_start]from the solid surface[blank_end] to form solvated molecules at the solid liquid interface ([blank_start]liberation[blank_end])
2. [blank_start]Transport[blank_end] from this interface [blank_start]to the bulk solution[blank_end] ([blank_start]diffusion[blank_end])
Depending on whether step 1 or step 2 is rate limiting, the dissolution process is either [blank_start]reaction-rate controlled[blank_end] or [blank_start]transport-rate controlled[blank_end]; it may be a combination of both.- ADetachment
- Bfrom the solid surface
- Cliberation
- DTransport
- Eto the bulk solution
- Fdiffusion
- Greaction-rate controlled
- Htransport-rate controlled
3The Noyes-Whitney Equation states that:
- Awhen surface area is constant, the dissolution rate (dW/dt or dm/dt) of a drug is proportional to the difference between its solubility — Cs, and its bulk solution concentration — Cb
- Bindependent of surface area, the dissolution rate (dW/dt or dm/dt) of a drug is proportional to the difference between its solubility — Cs, and its bulk solution concentration — Cb
- Cwhen surface area is constant, the dissolution rate (dW/dt or dm/dt) of a drug is proportional to the difference between its solid remaining concentration — Ct, and its bulk solution concentration — Cb
4The Noyes-Whitney equation defines the rate of dissolution of a solid when the process is diffusion controlled and involves no chemical reaction.
- ARichtig
- BFalsch
5Nernst and Brunner suggested that diffusion occurs across a thin [blank_start]stagnant[blank_end] layer of [blank_start]saturated[blank_end] solution, called the [blank_start]diffusion layer[blank_end] (or hydrodynamic boundary layer) into the bulk solution. This layer experiences [blank_start]no convection[blank_end] and is analogous to a membrane.
The Nernst-Brunner equation states that the rate of diffusion (dW/dt) is equal to the [blank_start]diffusion constant[blank_end] (D) multiplied by the [blank_start]surface area[blank_end] (A) divided by the [blank_start]thickness[blank_end] of the diffusion layer (h), all multiplied by the [blank_start]difference[blank_end] in saturated concentration (Cs) and concentration of the bulk solution(Cbulk).
Therefore dW/dt = DA/h * (Cs - Cbulk)- Astagnant
- Bsaturated
- Cdiffusion layer
- Dno convection
- Ediffusion constant
- Fsurface area
- Gthickness
- Hdifference
6Assumptions made by the Nernst-Brunner equation:
1. Drug dissolves [blank_start]uniformly from all surfaces[blank_end]
2. Particles are [blank_start]spherical[blank_end]
3. Particles are uniform [blank_start]size[blank_end]
4. Thickness of the diffusion layer is [blank_start]constant[blank_end]
5. Both h and Cs are assumed to be [blank_start]independent of particle size[blank_end]- Auniformly from all surfaces
- Bspherical
- Csize
- Dconstant
- Eindependent of particle size
7Mathematical models of release:
1. Zero order release model
[blank_start]Constant amount of drug is released[blank_end] per unit time. Minimizes potential peak/trough [blank_start]fluctuations[blank_end] and [blank_start]side effects[blank_end], while [blank_start]maximizing[blank_end] the time the drug concentration remains within the therapeutic window.
2. First order release model
Drug release [blank_start]depends on concentration[blank_end]. Release obeys the Noyes-Whitney (Nernst-Brunner) equation.
3. Hixson-Crowell release model
Describes drug release by dissolution in which the [blank_start]dimensions[blank_end] of the dosage form [blank_start]diminish proportionally[blank_end] but the [blank_start]geometric shape[blank_end] remains constant.
4. Higuchi release model
If drug is dispersed in a [blank_start]homogeneous granular polymer matrix[blank_end] that is non-erodible. If the first 60% of release occurs in accordance with the Higuchi equation (i.e. % cumulative drug release is [blank_start]linearly[blank_end] proportional to the [blank_start]square root[blank_end] of time) then it suggests release occurs by diffusion of the drug from the surface of the device.
5. Korsmeyer-Peppas release model
Semi-empirical equation (the so-called power law) to describe drug release from [blank_start]polymeric[blank_end] devices. Linear if [blank_start]log % drug release[blank_end] plotted against [blank_start]log of time[blank_end].- AConstant amount of drug is released
- Bfluctuations
- Cside effects
- Dmaximizing
- Edepends on concentration
- Fdimensions
- Gdiminish proportionally
- Hgeometric shape
- Ihomogeneous granular polymer matrix
- Jlinearly
- Ksquare root
- Lpolymeric
- Mlog % drug release
- Nlog of time
8Empirical dissolution models have many inherent drawbacks, namely that the elucidation of the [blank_start]underlying mass transport mechanisms[blank_end] is not possible and [blank_start]not a single characteristic parameter[blank_end] of the dosage form is related to the intrinsic dissolution rate of the drug. Therefore, these studies do result in [blank_start]incomplete[blank_end] process and product understanding.
- Aunderlying mass transport mechanisms
- Bnot a single characteristic parameter
- Cincomplete
Informationen
- Beschreibung
- PHCY211 (Medicines) Quiz am MD4 How drugs dissolve, erstellt von Mer Scott am 12/05/2018.
- Autor
- Mer Scott
- Sprache
- English
- Aufrufe
- 7
- Schlagwörter
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