3 7p
E ~ ~ S T IAND C VISCO-ELASTIC J o ~ .
P R O P E R T I E S OF COMPRESSED T A B L E T S
Rees and P . J . Rue, Pharmaceutics Research Group, Pharmacy Dept. of Aston, Gosta Green, Birmingham
During d i a m e t r a l compression t e s t i n g , d i f f e r e n t t a b l e t s deform by d i f f e r e n t b e f o r e f a i l u r e (Rees & Rue, 1977). S m a l l d e f o r m a t i o n u s u a l l y i n d i c a t e s b r i t t l e behaviour whereas l a r g e d e f o r m a t i o n i n d i c a t e s v i s c o u s f l o w , part of t h e Using a d i s p l a c e m e n t t r a n s d u c e r t h e t o t a l deformation b e i n g non-recoverable. non-recoverable d e f o r m a t i o n ( N R D ) w a s determined f o r t a b l e t s o f b u r d i r e c t compression m a t e r i a l s loaded t o 75% of t h e i r b r e a k i n g l o a d . P l o t t i n g t h e l o g of m ~ e,x p r e s s e d a s p e r c e n t t o t a l d e f o r m a t i o n , a g a i n s t t h e l o g of t h e r a t e of p l a t t e n movement gave l i n e a r r e l a t i o n s ( F i g . 1 ) . The b r i t t l e m a t e r i a l s , anhydrous l a c t o s e and Emcompress, show l i t t l e change i n % w i t h r a t e of p l a t t e n movement whereas t h e v i s c o - e l a s t i c materials, E l c m a and Sta-Rx show a d e c r e a s e i n % NRD a s t h e r a t e i n c r e a s e s i n d i c a t i n g t h a t h i g h e r s w a i n r a t e s produce a g r e a t e r p r o p o r t i o n of r e c o v e r a b l e e l a s t i c deformation. For l a c t o s e and Elcema t a b l e t s a t a g i v e n r a t e of t e s t i n g , i n c r e a s i n g t h e t e n s i l e T h i s i s due t o t h e l a r g e r area of i n t e r p a r t i c u l a t e d e c r e a s e s t h e % NRD. bonding c r e a t e d a t h i g h e r compaction f o r c e s because f o r a g i v e n d i a m e t r a l l o a d , t h e l a r g e r t h e t o t a l area of bonding, t h e lower t h e r e s u l t a n t stress; t h i s d e c r e a s e s t h e amount of p l a s t i c deformation and r e d u c e s t h e % NRD. The l a r g e r n e g a t i v e g r a d i e n t f o r Sta-Rx i n Fig.1, i n d i c a t e s t h a t p l a s t i c d e f o r m a t i o n i s more time-dependent t h a n f o r E l c e m a . T h i s i s confirmed by t h e e f f e c t of i n c r e a s i n g compaction d w e l l t i m e which w e f i n d h a s l i t t l e e f f e c t on t h e amount of c o n s o l i d a t i o n of Emcompress o r l a c t o s e , some e f f e c t w i t h Elcema, b u t markedly i n c r e a s e s c o n s o l i d a t i o n of Sta-Rx. I n c r e a s i n g t h e dwell time a l s o i n c r e a s e d t h e s t r e n g t h of m i c r o c r y s t a l l i n e c e l l u l o s e t a b l e t s by 37% and Sta-Rx t a b l e t s by 135% (David & Augsburger, 1977)
.
C o n s i d e r a b l e d e f o r m a t i o n of Sta-Rx t a b l e t s o c c u r s d u r i n g d i a m e t r a l l o a d i n g i n d i c a t i n g e x t e n s i v e p l a s t i c flow. However t h e t a b l e t s p o s s e s s a n unexpected low t e n s i l e swength. W e now a t t r i b u t e t h i s t o t h e i n a b i l i t y o f Sta-Rx p a r t i c l e s t o undergo e x t e n s i v e p l a s t i c d e f o r m a t i o n a t h i g h s t r a i n rates d u r i n g compaction. T h i s minimises t h e s t r e n g t h of i n t e r p a r t i c u l a t e bonds. F u r t h e r m o r e , a h i g h proT h i s w i l l r e c o v e r r a p i d l y on decompression, p o r t i o n of d e f o r m a t i o n i s e l a s t i c . r u p t u r i n g bonds and d e c r e a s i n g t h e t a b l e t s t r e n g t h .
W e propose that such measurements may p r o v i d e u s e f u l i n f o r m a t i o n r e g a r d i n g t h e compaction behaviour of m a t e r i a l s and c o u l d f a c i l i t a t e p r e d i c t i o n of t h e e f f e c t of v a r i a b l e s such a s r a t e of compaction.
-
F i g . 1 The e f f e c t of p l a t t e n movement on the % NRD of t a b l e t s when loaded to 75% of t h e i r b r e a k i n g f o r c e
10
a 2 0.01
0.1
1
10
1 Elcma G250 ( m i c r o c r y s t a l l i n e cellulose) 0 Sta-Rx 1500 ( c o m p r e s s i b l e s t a r c h ) A anhydrous l a c t o s e 0 Ekcompress ( d i b a s i c calcium phosphate1
Rate of platten movernent(rnrn rnin-1) David, S.T. Rees, J.E.
& &
Augsburger, L.L. ( 1 9 7 7 ) , J.Pharm.Sci., 66, 155-159 Rue, p.J.(1977) Drug Pevelopnent and I n d u s t r i a l Pharmacy, i n p r e s s
E ~ ~ S T IAND C VISCO-ELASTIC J o ~ .
P R O P E R T I E S OF COMPRESSED T A B L E T S
Rees and P . J . Rue, Pharmaceutics Research Group, Pharmacy Dept. of Aston, Gosta Green, Birmingham
During d i a m e t r a l compression t e s t i n g , d i f f e r e n t t a b l e t s deform by d i f f e r e n t b e f o r e f a i l u r e (Rees & Rue, 1977). S m a l l d e f o r m a t i o n u s u a l l y i n d i c a t e s b r i t t l e behaviour whereas l a r g e d e f o r m a t i o n i n d i c a t e s v i s c o u s f l o w , part of t h e Using a d i s p l a c e m e n t t r a n s d u c e r t h e t o t a l deformation b e i n g non-recoverable. non-recoverable d e f o r m a t i o n ( N R D ) w a s determined f o r t a b l e t s o f b u r d i r e c t compression m a t e r i a l s loaded t o 75% of t h e i r b r e a k i n g l o a d . P l o t t i n g t h e l o g of m ~ e,x p r e s s e d a s p e r c e n t t o t a l d e f o r m a t i o n , a g a i n s t t h e l o g of t h e r a t e of p l a t t e n movement gave l i n e a r r e l a t i o n s ( F i g . 1 ) . The b r i t t l e m a t e r i a l s , anhydrous l a c t o s e and Emcompress, show l i t t l e change i n % w i t h r a t e of p l a t t e n movement whereas t h e v i s c o - e l a s t i c materials, E l c m a and Sta-Rx show a d e c r e a s e i n % NRD a s t h e r a t e i n c r e a s e s i n d i c a t i n g t h a t h i g h e r s w a i n r a t e s produce a g r e a t e r p r o p o r t i o n of r e c o v e r a b l e e l a s t i c deformation. For l a c t o s e and Elcema t a b l e t s a t a g i v e n r a t e of t e s t i n g , i n c r e a s i n g t h e t e n s i l e T h i s i s due t o t h e l a r g e r area of i n t e r p a r t i c u l a t e d e c r e a s e s t h e % NRD. bonding c r e a t e d a t h i g h e r compaction f o r c e s because f o r a g i v e n d i a m e t r a l l o a d , t h e l a r g e r t h e t o t a l area of bonding, t h e lower t h e r e s u l t a n t stress; t h i s d e c r e a s e s t h e amount of p l a s t i c deformation and r e d u c e s t h e % NRD. The l a r g e r n e g a t i v e g r a d i e n t f o r Sta-Rx i n Fig.1, i n d i c a t e s t h a t p l a s t i c d e f o r m a t i o n i s more time-dependent t h a n f o r E l c e m a . T h i s i s confirmed by t h e e f f e c t of i n c r e a s i n g compaction d w e l l t i m e which w e f i n d h a s l i t t l e e f f e c t on t h e amount of c o n s o l i d a t i o n of Emcompress o r l a c t o s e , some e f f e c t w i t h Elcema, b u t markedly i n c r e a s e s c o n s o l i d a t i o n of Sta-Rx. I n c r e a s i n g t h e dwell time a l s o i n c r e a s e d t h e s t r e n g t h of m i c r o c r y s t a l l i n e c e l l u l o s e t a b l e t s by 37% and Sta-Rx t a b l e t s by 135% (David & Augsburger, 1977)
.
C o n s i d e r a b l e d e f o r m a t i o n of Sta-Rx t a b l e t s o c c u r s d u r i n g d i a m e t r a l l o a d i n g i n d i c a t i n g e x t e n s i v e p l a s t i c flow. However t h e t a b l e t s p o s s e s s a n unexpected low t e n s i l e swength. W e now a t t r i b u t e t h i s t o t h e i n a b i l i t y o f Sta-Rx p a r t i c l e s t o undergo e x t e n s i v e p l a s t i c d e f o r m a t i o n a t h i g h s t r a i n rates d u r i n g compaction. T h i s minimises t h e s t r e n g t h of i n t e r p a r t i c u l a t e bonds. F u r t h e r m o r e , a h i g h proT h i s w i l l r e c o v e r r a p i d l y on decompression, p o r t i o n of d e f o r m a t i o n i s e l a s t i c . r u p t u r i n g bonds and d e c r e a s i n g t h e t a b l e t s t r e n g t h .
W e propose that such measurements may p r o v i d e u s e f u l i n f o r m a t i o n r e g a r d i n g t h e compaction behaviour of m a t e r i a l s and c o u l d f a c i l i t a t e p r e d i c t i o n of t h e e f f e c t of v a r i a b l e s such a s r a t e of compaction.
-
F i g . 1 The e f f e c t of p l a t t e n movement on the % NRD of t a b l e t s when loaded to 75% of t h e i r b r e a k i n g f o r c e
10
a 2 0.01
0.1
1
10
1 Elcma G250 ( m i c r o c r y s t a l l i n e cellulose) 0 Sta-Rx 1500 ( c o m p r e s s i b l e s t a r c h ) A anhydrous l a c t o s e 0 Ekcompress ( d i b a s i c calcium phosphate1
Rate of platten movernent(rnrn rnin-1) David, S.T. Rees, J.E.
& &
Augsburger, L.L. ( 1 9 7 7 ) , J.Pharm.Sci., 66, 155-159 Rue, p.J.(1977) Drug Pevelopnent and I n d u s t r i a l Pharmacy, i n p r e s s
