3.5
After a drug is administered, the amount of administered drug that enters the systemic circulation and is available for distribution to its site of action is called bioavailability.
The bioavailability of an orally administered drug is affected by GI absorption and biotransformation by the liver.
In the case of a drug that is intravenously administered, the drug directly enters the systemic circulation, and the bioavailability is assumed to be 100%, by definition.
For an orally administered drug, a comparison of the plasma concentration of the drug administered through the IV route helps to determine the bioavailability of that drug.
A plot of the drug's plasma concentration versus time for the same drug administered in equivalent doses, both orally and intravenously, can be generated.
The total area under the curve for each route of administration represents the extent of drug absorption for that route.
The ratio of the areas calculated gives an estimate of the bioavailable fraction of the orally administered drug.
生物利用性とは、投与後に全く変化していない薬物のうち、全身循環に入り、望ましい作用部位に配布される割合を指します。薬物の生物利用性は、胃腸管(GI)吸収や肝臓の生理学的変換などの要因に影響を受けます。薬物が静注されると、それは直接全身循環に入ります。定義上、その生物利用性は100%とされます。経口投与薬物の生物利用性は、その薬物のそれと同じを静脈内投与した場合の血漿濃度と比較することで判断できます。経口と静脈内の両方で、等価量の薬物を時間に沿って血漿濃度で表したグラフを作成することができます。このグラフの下の総面積は、各投与方法による薬物吸収の度合いを示します。これらの面積の比を計算することで、経口投与された薬物の生物利用可能な部分の推定値を得ることができます。
After a drug is administered, the amount of administered drug that enters the systemic circulation and is available for distribution to its site of action is called bioavailability.
The bioavailability of an orally administered drug is affected by GI absorption and biotransformation by the liver.
In the case of a drug that is intravenously administered, the drug directly enters the systemic circulation, and the bioavailability is assumed to be 100%, by definition.
For an orally administered drug, a comparison of the plasma concentration of the drug administered through the IV route helps to determine the bioavailability of that drug.
A plot of the drug's plasma concentration versus time for the same drug administered in equivalent doses, both orally and intravenously, can be generated.
The total area under the curve for each route of administration represents the extent of drug absorption for that route.
The ratio of the areas calculated gives an estimate of the bioavailable fraction of the orally administered drug.
From Chapter 3:
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