Self nanoprecipitating

preconcentrate of Primaquine
Phosphate

Method
PP

GMS- 20 mg
PP- 10 mg
AOT- 10 mg
DMA- 1 ml
DDW- 2 ml

EE- 35 % , PS more than 1

GMS

AOT

Batch

GMS

DMA

AOT

PP

EE (%)

20

10

10

31

20

20

10

30

20

10

10

10

10

10

10

10

10

10

20

10

62.3

10

10

29

AOT IN DMA

37.9

51.5
WITH 0.2 ml
TWEEN 80

PARTICLE SIZE WAS MORE THAN 1

10.4

Batch

GMS

DMA

AOT

PP

EE (%)

D-1

10

10

10

40

F-2

10

20

10

52

Batch

GMS

DMA

AOT

PP

EE (%)

D-1

10

10

10

35

F-2

10

20

10

61

PARTICLE SIZE WAS MORE THAN 1

By varying GMS:PP ratio

Batch

GMS

DMA

AOT

PP

EE ( %)

20

20

10

AOT IN DMA

31

10

20

10

AOT IN DMA

30

20

10

AOT IN DMA

32

Primaquine phosphate - 10 mg
AOT - 20 mg
Lutrol F 68 - 10 mg
GMS - 10 mg
DMA - 0.5 ml
EE - 0
PS 616 nm
PEG 400 - 0.5 ml
PDI 0.7

DDW - 4 ml

Batch GMS

DMA

AOT

PP

EE (%)

10

20

10

AOT, PP in aq. phase

60

10

20

10

AOT, PP in DMA

40

10

20

10

With 10 mg lutrol F 68 in
aq. phase

42.6

10

25

10

PP in aq. Phase & AOT

in DMA

63.3

PARTICLE SIZE WAS MORE THAN 1

Modified method
AOT
PP

GMS

Batch

DMA

AOT

PP

GMS

EE (%) PS / PDI

20

10

10

51

422 / 0.07

B
with lutrol F 68

20

10

10

56

433 / 0.196

Batch

DMA

AOT

PP

GMS

EE (%) PS / PDI

A 1

20

10

10

40

827/ 0.6

B2
with lutrol F 68

20

10

10

46.6

720/ 0.6

Batch

DMA : DDW AOT

PP

GMS

EE (%)

PS / PDI

0.95 : 0.05

20

10

10

48.9

>2

B
with lutrol F 68

0.95 : 0.05

20

10

10

36.3

>2

Different solvents

Pharmasolve
Transcutol
Soluphor P
Solutol HS 15

Batch

Solvent used

AOT

PP

GMS

EE (%) PS / PDI

DMA 1 ml

20

10

10

43

552 / 0.05

Pharmasolve 1 ml

20

10

10

27

472 / 0.015

By varying AOT:PP ratio

Batch

DMA

AOT

PP

GMS

EE (%)

PS / PDI

15

10

10

32

800 / 0.7

20

10

10

47.3

530 / 0.1

25

10

10

56

472 / 0.2

30

10

10

55

468 / 0.01

By increasing drugs concentration

Batch

DMA

AOT

PP

GMS

EE (%)

PS / PDI

20

15

10

33

>2

20

20

10

By increasing GMS concentration

Batch

DMA

AOT

PP

GMS

EE (%)

PS / PDI

20

10

15

27.3

>2

20

10

20

50.3

>1

Batch

DMA

AOT

PP

GMS

EE (%)

C1

25

10

10

56.6

C2

25

10

10

54

Batch

DMA

DDW

AOT

PP

GMS

EE (%)

PS / PDI

1 ml

25

10

10

20

400 / 1.1

0.5

1 ml

25

10

10

56

301 / 0.3

Batch

DMA

DDW

AOT

PP

GMS

EE (%)

PS / PDI

B1

0.5

1 ml

25

10

10

58

387 / 0.1

B2

0.5

1 ml

25

10

10

57

450 / 0.2

To improve EE,
Addition of small amount of water to DMA not stable
Change in aqueous phase pH not stable

Batch

DMA

DDW

AOT

PP

GMS

EE (%)

0.5

0.5 ml

25

10

10

17.8

A 1

0.5

0.5 ml

25

10

10

20.3

Batch

DMA

DDW

AOT

PP

GMS

EE (%)

0.5

1 ml

25

10

10

84.7

B-1

0.5

1 ml

25

10

10

83