Antimalarial drugs are used to prevent and cure malaria. Artemisinins are rapid acting blood schizonticidal antimalarials against chloroquinine resistant malaria.

1. Market Survey of ArtemisininsMarket Survey of Artemisinins
( Antimalarial Drugs)( Antimalarial Drugs)
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2. IntroductionIntroduction
 To carry out market survey of ArtemisininsTo carry out market survey of Artemisinins
used as Antimalarials.used as Antimalarials.
- Artemether- Artemether
- Artesunate- Artesunate
- Arteether- Arteether
 Study of Pharmacokinetic parametersStudy of Pharmacokinetic parameters
 Proposal for a new formulation with improvedProposal for a new formulation with improved
bioavailabilitybioavailability

3. AntimalarialsAntimalarials
 Antimalarial drugsAntimalarial drugs are used to prevent andare used to prevent and
cure cure malariamalaria..
 Artemisinins are rapid acting bloodArtemisinins are rapid acting blood
schizonticidal antimalarials againstschizonticidal antimalarials against
chloroquinine resistant malaria.chloroquinine resistant malaria.

4. Artemisinin Derivatives used asArtemisinin Derivatives used as
AntimalarialsAntimalarials
 ArtemetherArtemether
 ArteetherArteether
 ArtesunateArtesunate

5. ArtemetherArtemether
 It is an antimalarial drug used for the treatmentIt is an antimalarial drug used for the treatment
of multiple drug-resistant strains ofof multiple drug-resistant strains of PlasmodiumPlasmodium
falciparumfalciparum..
 Chemically, it is a semi-synthetic derivative ofChemically, it is a semi-synthetic derivative of
artemisininartemisinin

6. ArteetherArteether
 ArteetherArteether is a fast acting blood schizonticideis a fast acting blood schizonticide
specifically indicated for the treatment ofspecifically indicated for the treatment of
chloroquinine resistantchloroquinine resistant Plasmodium falciparumPlasmodium falciparum
malaria and cerebral malaria cases.malaria and cerebral malaria cases.

7. ArtesunateArtesunate
 ArtesunateArtesunate is used in treatment of malaria. It isis used in treatment of malaria. It is
water-soluble and can be given by parenteralwater-soluble and can be given by parenteral
route. It is a semi-synthetic derivative ofroute. It is a semi-synthetic derivative of
artemisinin.artemisinin.

8. Plan of WorkPlan of Work
 Market survey of artemisinin derivatives forMarket survey of artemisinin derivatives for
available formulationsavailable formulations
 Comparative studyComparative study
 Study of pharmacokinetics and relatedStudy of pharmacokinetics and related
parameters from literatureparameters from literature
 Exploration of possible strategies forExploration of possible strategies for
development of oral formulation withdevelopment of oral formulation with
improved bioavailability.improved bioavailability.

9. Market formulation: ArtemetherMarket formulation: Artemether
S.NoS.No BrandBrand Mfg byMfg by FormulationFormulation PotencyPotency M.R.PM.R.P
1.1. AarmetAarmet Alpha aromaticAlpha aromatic InjectionInjection 150mg/ml150mg/ml 150/-150/-
2.2. AbtherAbther
AbAb
Mac organicsMac organics InjectionInjection 150mg/ml150mg/ml 105/-105/-
3.3. AlbaretAlbaret Pink healthPink health InjectionInjection 75mg/ml75mg/ml 70/-70/-
4.4. ArtimisaArtimisa RehvinaRehvina
PharmaceutcalPharmaceutcal
CapsuleCapsule 40mg40mg 80/-80/-

10. Market formulation: ArteetherMarket formulation: Arteether
S.NoS.No BrandBrand Mfg byMfg by FormulationFormulation PotencyPotency M.R.PM.R.P
1.1. AdthecAdthec AdleyAdley AMPAMP 150mg/2ml150mg/2ml 99.60/-99.60/-
2.2. AldaAlda AvyuketAvyuket InjectionInjection 150mg150mg 102.00/-102.00/-
3.3. AarteeAartee SiennaSienna InjectionInjection 150mg/2ml150mg/2ml 125.00/-125.00/-
4.4. AbterAbter ZytrasZytras I.VI.V 150mg150mg 255/-255/-

11. Market Formulation: ArtesunateMarket Formulation: Artesunate
S. NoS. No BrandBrand Mfg byMfg by FormulationFormulation PotencyPotency M.R.PM.R.P
1.1. AssonateAssonate AdlayAdlay
FormForm
InjectionInjection 60mg/ml60mg/ml 115/-115/-
2.2. DuranteDurante SamarthSamarth
PharmaPharma
TabletTablet 50mg50mg 225/-225/-
3.3. FalcateFalcate GeneticGenetic
PharmaPharma
InjectionInjection 60mg/ml60mg/ml 180/-180/-
4.4. FalchionFalchion ZydusZydus
CadilaCadila
InjectionInjection 60mg/ml60mg/ml 171/-171/-

12. Study of Pharmacokinetic ParameterStudy of Pharmacokinetic Parameter
PropertiesProperties ArtemetherArtemether ArteetherArteether ArtesunateArtesunate
SolubilitySolubility Soluble inSoluble in
AcetoneAcetone
EthanolEthanol
Partly in water,Partly in water,
Chloroform &Chloroform &
Ethyl acetateEthyl acetate
freely soluble infreely soluble in
Dichloromethane,Dichloromethane,
EthanolEthanol
AqueousAqueous
SolubilitySolubility
InsolubleInsoluble Partly solublePartly soluble Slightly solubleSlightly soluble
OralOral
Bio-availabiltyBio-availabilty
43%43% 19-35%19-35% 61%61%
tt ½½ 40 minutes40 minutes 50-55 minutes50-55 minutes 60 minutes60 minutes
MICMIC 5050 5050 µg/mlµg/ml 0.25-10.25-1 µgµg/ml/ml 4mg/kg4mg/kg

13. Merits & Therapeutic Uses :Merits & Therapeutic Uses :
Side effects
- Headache , Nausea, abdominal pain, vomiting, Diarrhoea
- Safe and effective in treatment of severe malaria
- Artemisinins are well tolerated and toxicity of artemisinins
derivatives is much less than chloroquinine.
- Artemether is effective against the blood schizonts of
Plasmodium falciparum & Plasmodium vivax
- Arteether is used in Acute malaria. It gets accumulated in
brain tissue and thus used in treatment of cereberal malaria.

14. ConclusionsConclusions
Absorption of orally administered artemisinins or its derivativesAbsorption of orally administered artemisinins or its derivatives
seems to be rapid but isseems to be rapid but is incompleteincomplete (Hepatic elimination).(Hepatic elimination).
Substantial hydrolysis of artemisinins into dihydroartemisininsSubstantial hydrolysis of artemisinins into dihydroartemisinins
occurs before absorption which is subsequently converted intooccurs before absorption which is subsequently converted into
metabolites which aremetabolites which are inactiveinactive (Less therapeutic efficacy).(Less therapeutic efficacy).
Therefore artemisininsTherefore artemisinins are used as anti-malarial via parenteralare used as anti-malarial via parenteral
route as in case of oral administration bioavailability is very less.route as in case of oral administration bioavailability is very less.
Use of variousUse of various Bioavailability enhancerBioavailability enhancer such as Piperine orsuch as Piperine or
SyntheticSynthetic Solubility enhancerSolubility enhancer such as Dextran or cyclodextrinssuch as Dextran or cyclodextrins
may result in improved solubility and bioavailability in case of oralmay result in improved solubility and bioavailability in case of oral
dosage form.dosage form.
This will be explored in next phase of the project.This will be explored in next phase of the project.

15. ThankThank
you !!!....you !!!....
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