Abstract
Purpose: Interruption of oral drug administration poses a significant clinical problem for antiepileptic drugs that have no parenteral formulation. If a drug is absorbed rectally, rectal administration can be a useful alternative when the oral route of administration is not possible. The purpose of this study was to compare the single-dose pharmacokinetics of lamotrigine (LTG) compressed tablets after rectal and oral administration in healthy volunteers. Methods: A single LTG compressed tablet (100 mg) was administered orally and rectally to 12 volunteers in this single-dose, two- period, crossover study with a 2-week washout between doses. For rectal administration, tablets were crushed and suspended in 10 mL of water. Plasma samples were collected from 0 to 120 hr after each dose and analyzed for LTG by an HPLC method developed for this investigation. Results: LTG plasma concentrations were lower after rectal administration versus oral administration. The average area under the curve was 28.90 ± 9.5 μg/mL/hr after rectal administration and 51.71 ± 19.2 μg/mL/hr after oral administration. The average maximum LTG concentration was 0.53 ± 0.14 μg/mL after rectal administration and 1.45 ± 0.35 μg/mL after oral administration. The relative bioavailability for LTG compressed tablets was 0.63 ± 0.33 for rectal administration. There were no drug-related rashes or serious side effects. Conclusions: LTG suspension prepared from LTG compressed tablets is absorbed rectally, although not to the same extent or rate as when given orally.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 850-853 |
| Number of pages | 4 |
| Journal | Epilepsia |
| Volume | 41 |
| Issue number | 7 |
| DOIs | |
| State | Published - Jan 1 2000 |
Fingerprint
Keywords
- Antiepileptic
- Bioavailability
- Compressed
- Lamotrigine
- Rectal
Cite this
Rectal absorption of lamotrigine compressed tablets. / Birnbaum, Angela K.; Kriel, Robert L.; Burkhardt, R. Todd; Remmel, Rory P.
In: Epilepsia, Vol. 41, No. 7, 01.01.2000, p. 850-853.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Rectal absorption of lamotrigine compressed tablets
AU - Birnbaum, Angela K.
AU - Kriel, Robert L.
AU - Burkhardt, R. Todd
AU - Remmel, Rory P.
PY - 2000/1/1
Y1 - 2000/1/1
N2 - Purpose: Interruption of oral drug administration poses a significant clinical problem for antiepileptic drugs that have no parenteral formulation. If a drug is absorbed rectally, rectal administration can be a useful alternative when the oral route of administration is not possible. The purpose of this study was to compare the single-dose pharmacokinetics of lamotrigine (LTG) compressed tablets after rectal and oral administration in healthy volunteers. Methods: A single LTG compressed tablet (100 mg) was administered orally and rectally to 12 volunteers in this single-dose, two- period, crossover study with a 2-week washout between doses. For rectal administration, tablets were crushed and suspended in 10 mL of water. Plasma samples were collected from 0 to 120 hr after each dose and analyzed for LTG by an HPLC method developed for this investigation. Results: LTG plasma concentrations were lower after rectal administration versus oral administration. The average area under the curve was 28.90 ± 9.5 μg/mL/hr after rectal administration and 51.71 ± 19.2 μg/mL/hr after oral administration. The average maximum LTG concentration was 0.53 ± 0.14 μg/mL after rectal administration and 1.45 ± 0.35 μg/mL after oral administration. The relative bioavailability for LTG compressed tablets was 0.63 ± 0.33 for rectal administration. There were no drug-related rashes or serious side effects. Conclusions: LTG suspension prepared from LTG compressed tablets is absorbed rectally, although not to the same extent or rate as when given orally.
AB - Purpose: Interruption of oral drug administration poses a significant clinical problem for antiepileptic drugs that have no parenteral formulation. If a drug is absorbed rectally, rectal administration can be a useful alternative when the oral route of administration is not possible. The purpose of this study was to compare the single-dose pharmacokinetics of lamotrigine (LTG) compressed tablets after rectal and oral administration in healthy volunteers. Methods: A single LTG compressed tablet (100 mg) was administered orally and rectally to 12 volunteers in this single-dose, two- period, crossover study with a 2-week washout between doses. For rectal administration, tablets were crushed and suspended in 10 mL of water. Plasma samples were collected from 0 to 120 hr after each dose and analyzed for LTG by an HPLC method developed for this investigation. Results: LTG plasma concentrations were lower after rectal administration versus oral administration. The average area under the curve was 28.90 ± 9.5 μg/mL/hr after rectal administration and 51.71 ± 19.2 μg/mL/hr after oral administration. The average maximum LTG concentration was 0.53 ± 0.14 μg/mL after rectal administration and 1.45 ± 0.35 μg/mL after oral administration. The relative bioavailability for LTG compressed tablets was 0.63 ± 0.33 for rectal administration. There were no drug-related rashes or serious side effects. Conclusions: LTG suspension prepared from LTG compressed tablets is absorbed rectally, although not to the same extent or rate as when given orally.
KW - Antiepileptic
KW - Bioavailability
KW - Compressed
KW - Lamotrigine
KW - Rectal
UR - http://www.scopus.com/inward/record.url?scp=0033919212&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0033919212&partnerID=8YFLogxK
U2 - 10.1111/j.1528-1157.2000.tb00252.x
DO - 10.1111/j.1528-1157.2000.tb00252.x
M3 - Article
C2 - 10897156
AN - SCOPUS:0033919212
VL - 41
SP - 850
EP - 853
JO - Epilepsia
JF - Epilepsia
SN - 0013-9580
IS - 7
ER -