كتاب  Comparative pharmacokinetics of ivermectin after its subcutaneous administration in healthy sheep and sheep infected with mangeكتب الطب

كتاب Comparative pharmacokinetics of ivermectin after its subcutaneous administration in healthy sheep and sheep infected with mange

Comparative pharmacokinetics of ivermectin after its subcutaneous administration in healthy sheep and sheep infected with mange من كتب طب بيطرى Comparative pharmacokinetics of ivermectin after its subcutaneous administration in healthy sheep and sheep infected with mange J. ECHEVERRI ́ A* , N. MESTORINO* , & J. O. ERRECALDE* , *Ca ́ tedra de Farmacologı ́ a, Farmacotecnia y Terape ́ utica, Facultad de Ciencias Veterinarias, Universidad Nacional de La Plata, La Plata, Argentina; INCAM, Vero ́ nica Experimental Station, La Plata, Argentina; (Paper received: 21 March 2001; accepted for publication 19 November 2001) Correspondence (e-mail: [email protected]) It is well established that the efficacy of any anthelmintic drug depends not only on its affinity for specific parasite target sites but also on its ability to reach high and sustained drug concentrations where the parasites are located. Ivermectin is one of the most useful anti-parasitic agents. It belongs to the family of avermectins that are highly lipophilic macrocyclic lactones. It is a fermentation product of Streptomyces avermitilis . One of the most important characteristics of iver- mectin is its wide spectrum of activity involving endo- and ectoparasites. Ivermectin is effective when it is applied orally, parenterally or topically. Its absorption is rapid by any of these routes of administration (Campbell, 1989, 1993). Mange is an ectoparasitic disease produced by the mite Psoroptes ovis . It has major economic importance in South America, especially Argentina, Chile and Uruguay. It is antici- pated that in the diseased animal there are kinetic modifications largely dependent on the change of body condition. The objective of the present paper was to determine the pharmacokinetic changes of ivermectin when applied subcutaneously to healthy animals and animals carrying natural mange infections. Six adult and healthy sheep (weighing 50 ± 6 kg) and five sheep naturally infested with psoroptic mites and showing mange lesions on at least 30% of their body surface (weighing 43 ± 6 kg) received 200 l g/kg ivermectin subcutaneously, the sampling times being at the following post-administration days: 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 15, 18, 20, 25 and 30. Plasma was separated by centrifugation and kept frozen at ) 20 ° C until assayed. Assay was performed by high-performance liquid chromatography (HPLC). The recovery was 85% and the quantitation limit was 0.1 ng/mL. Variability was lower than 8%. The HPLC system was a Shimadzu LC-10 AS pump and TM III 1311 model fluoromonitor. The column was a C8 reverse phase lichrospher and the mobile phase was glacial acetic acid/ methanol/acetonitrile (9:200:291 mL) at a flow rate of 1.5 mL/ min. Reagents were HPLC grade. Extraction was accomplished by the solid–liquid method with C18 cartridges. The eluate was evaporated, derivatizated and injected into the HPLC system (Alvinerie et al ., 1987). Pharmacokinetic analysis wa
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وصف الكتاب : Comparative pharmacokinetics of ivermectin after its subcutaneous administration in healthy sheep and sheep infected with mange من كتب طب بيطرى

Comparative pharmacokinetics of ivermectin after its subcutaneous
administration in healthy sheep and sheep infected with mange
J. ECHEVERRI
́
A*
,
N. MESTORINO*
,
&
J. O. ERRECALDE*
,
*Ca
́
tedra de Farmacologı
́
a, Farmacotecnia y Terape
́
utica, Facultad de Ciencias Veterinarias, Universidad Nacional de La Plata, La Plata,
Argentina;
INCAM, Vero
́
nica Experimental Station, La Plata, Argentina;
(Paper received: 21 March 2001; accepted for publication 19 November 2001)
Correspondence (e-mail: [email protected])
It is well established that the efficacy of any anthelmintic drug
depends not only on its affinity for specific parasite target sites
but also on its ability to reach high and sustained drug
concentrations where the parasites are located.
Ivermectin is one of the most useful anti-parasitic agents. It
belongs to the family of avermectins that are highly lipophilic
macrocyclic lactones. It is a fermentation product of
Streptomyces
avermitilis
. One of the most important characteristics of iver-
mectin is its wide spectrum of activity involving endo- and
ectoparasites.
Ivermectin is effective when it is applied orally, parenterally or
topically. Its absorption is rapid by any of these routes of
administration (Campbell, 1989, 1993).
Mange is an ectoparasitic disease produced by the mite
Psoroptes ovis
. It has major economic importance in South
America, especially Argentina, Chile and Uruguay. It is antici-
pated that in the diseased animal there are kinetic modifications
largely dependent on the change of body condition. The objective
of the present paper was to determine the pharmacokinetic
changes of ivermectin when applied subcutaneously to healthy
animals and animals carrying natural mange infections.
Six adult and healthy sheep (weighing 50 ± 6 kg) and five
sheep naturally infested with psoroptic mites and showing
mange lesions on at least 30% of their body surface (weighing
43 ± 6 kg) received 200
l
g/kg ivermectin subcutaneously, the
sampling times being at the following post-administration days:
0.5, 1, 2, 3, 4, 6, 8, 10, 12, 15, 18, 20, 25 and 30. Plasma was
separated by centrifugation and kept frozen at
)
20
°
C until
assayed. Assay was performed by high-performance liquid
chromatography (HPLC). The recovery was 85% and the
quantitation limit was 0.1 ng/mL. Variability was lower than
8%. The HPLC system was a Shimadzu LC-10 AS pump and TM
III 1311 model fluoromonitor. The column was a C8 reverse
phase lichrospher and the mobile phase was glacial acetic acid/
methanol/acetonitrile (9:200:291 mL) at a flow rate of 1.5 mL/
min. Reagents were HPLC grade. Extraction was accomplished
by the solid–liquid method with C18 cartridges. The eluate was
evaporated, derivatizated and injected into the HPLC system
(Alvinerie
et al
., 1987). Pharmacokinetic analysis wa

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Comparative pharmacokinetics of ivermectin after its subcutaneous administration in healthy sheep and sheep infected with mange من كتب طب بيطرى

Comparative  pharmacokinetics  of  ivermectin  after  its  subcutaneous
administration  in  healthy  sheep  and  sheep  infected  with  mange
J.  ECHEVERRI
 ́
A*
,
N.  MESTORINO*
,
&
J.  O.  ERRECALDE*
,
*Ca
 ́
tedra  de  Farmacologı
 ́
a,  Farmacotecnia  y  Terape
 ́
utica,  Facultad  de  Ciencias  Veterinarias,  Universidad  Nacional  de  La  Plata,  La  Plata,
Argentina;
INCAM,  Vero
 ́
nica  Experimental  Station,  La  Plata,  Argentina;
(Paper  received:  21  March  2001;  accepted  for  publication  19  November  2001)
Correspondence  (e-mail:  [email protected])
It  is  well  established  that  the  efficacy  of  any  anthelmintic  drug
depends  not  only  on  its  affinity  for  specific  parasite  target  sites
but   also   on   its   ability   to   reach   high   and   sustained   drug
concentrations  where  the  parasites  are  located.
Ivermectin  is  one  of  the  most  useful  anti-parasitic  agents.  It
belongs  to  the  family  of  avermectins  that  are  highly  lipophilic
macrocyclic lactones. It is a fermentation product of
Streptomyces
avermitilis
.  One  of  the  most  important  characteristics  of  iver-
mectin   is   its   wide   spectrum   of   activity   involving   endo-   and
ectoparasites.
Ivermectin is effective when it is applied orally, parenterally or
topically.   Its   absorption   is   rapid   by   any   of   these   routes   of
administration  (Campbell,  1989,  1993).
Mange   is   an   ectoparasitic   disease   produced   by   the   mite
Psoroptes   ovis
.   It   has   major   economic   importance   in   South
America,  especially  Argentina,  Chile  and  Uruguay.  It  is  antici-
pated that in the diseased animal there are kinetic modifications
largely dependent on the change of body condition. The objective
of   the   present   paper   was   to   determine   the   pharmacokinetic
changes  of  ivermectin  when  applied  subcutaneously  to  healthy
animals  and  animals  carrying  natural  mange  infections.
Six  adult  and  healthy  sheep  (weighing  50  ±  6  kg)  and  five
sheep   naturally   infested   with   psoroptic   mites   and   showing
mange  lesions  on  at  least  30%  of  their  body  surface  (weighing
43  ±  6  kg)  received  200
l
g/kg  ivermectin  subcutaneously,  the
sampling  times  being  at  the  following  post-administration  days:
0.5, 1, 2, 3, 4, 6, 8, 10, 12, 15, 18, 20, 25 and 30. Plasma was
separated   by   centrifugation   and   kept   frozen   at
)
20
°
C   until
assayed.    Assay   was    performed    by    high-performance    liquid
chromatography    (HPLC).    The    recovery    was    85%    and    the
quantitation  limit  was  0.1  ng/mL.  Variability  was  lower  than
8%. The HPLC system was a Shimadzu LC-10 AS pump and TM
III  1311  model  fluoromonitor.  The  column  was  a  C8  reverse
phase  lichrospher  and  the  mobile  phase  was  glacial  acetic  acid/
methanol/acetonitrile  (9:200:291  mL) at  a flow  rate of 1.5  mL/
min.  Reagents  were  HPLC  grade.  Extraction  was  accomplished
by  the  solid–liquid  method  with  C18  cartridges.  The  eluate  was
evaporated,   derivatizated   and   injected   into   the   HPLC   system
(Alvinerie
et  al
., 1987). Pharmacokinetic analysis wa



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