petito et. al. v. rexall sundown

8/13/2019 Petito et. al. v. Rexall Sundown

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1 2 ) United S t a t e s PatentP e t i t o e t a l .

US006645948B2US 6 , 6 4 5 , 9 4 8 B2

* N o v . 1 1 , 2 0 0 31 0 ) P a t e n t N 0 . :4 5 ) Date o f P a t e n t :

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NUTRITIONAL COMPOSITION FOR THETREATMENT OF CONNECTIVE TISSUEI n v e n t o r s : George D . P e t i t o , 1 8 9 0 B u c k n e l l D r . ,

B e t h l e h e m , PA U S ) 1 8 0 1 5 ; A n i t a M.P e t i t o , 1 8 9 0 B u c k n e l l D r . , B e t h l e h e m ,P A U S ) 1 8 0 1 5N o t i c e : S u b j e c t t o a n y d i s c l a i m e r , t h e t e r m o f t h i s

p a t e n t i s e x t e n d e d o r a d j u s t e d u n d e r 3 5U . S . C . 1 5 4 b ) b y 0 d a y s .T h i s p a t e n t i s s u b j e c t t o a t e r m i n a l d i sc l a i m e r .

A p p l . N o . : 1 0 / 2 8 7 , 5 9 0F i l e d : N o v . 5 , 2 0 0 2

P r i o r P u b l i c a t i o n DataUS 2 0 0 3 / 0 0 6 9 1 7 1 A1 A p r . 1 0 , 2 0 0 3

R e l a t e d US. A p p l i c a t i o n DataC o n t i n u a t i o n - i n - p a r t o f a p p l i c a t i o n N o . 0 9 / 3 6 0 , 1 6 9 , ? l e d o nJ u l . 2 6 , 1 9 9 9 , n ow P a t . No. 6 , 4 7 6 , 0 0 5 , which i s a c o n t i n ua t i o n - i n - p a r t o f a p p l i c a t i o n N o . 0 9 / 0 4 6 , 7 1 0 , ? l e d o n M a r .2 4 , 1 9 9 8 , now a b a n d o n e d .I n t . Cl.7 . . . . . . . . . . . . . . . . . . . . A61K 1/7008; A61K 8/16;A61K 3 5 / 3 2US. l . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 514/62; 514/2; 514/54;

4 2 4 / 4 4 9Field o f S earch . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 514/62, 2 , 5 4 ;

4 2 4 / 4 4 9R e f e r e n c e s C i t e d

U . S . PATENT DOCUMENTS3 / 1 9 3 4 C r a n d a l l , J r .2 / 1 9 7 7 P r u d d e n8 / 1 9 8 0 R o b e r t s o n

4 , 4 5 5 , 3 0 2 A 6 / 1 9 8 4 R o b e r t so n4 , 8 3 7 , 0 2 4 A 6 / 1 9 8 9 M i c h a e l i5 , 1 4 1 , 9 2 8 A 8 / 1 9 9 2 Goldman5 , 2 5 2 , 3 3 9 A 1 0 / 1 9 9 3 C r i s t o f o r i e t a l .5 , 3 6 4 , 8 4 5 A 1 1 / 1 9 9 4 H e n d e r s o n5 , 4 4 2 , 0 5 3 A 8 / 1 9 9 5 d e l l a V a l l e e t a l .5 , 4 9 8 , 6 0 6 A 3 / 1 9 9 6 S o l l e t a l .5 , 5 8 7 , 3 6 3 A 1 2 / 1 9 9 6 H e n d e r s o n5 , 8 4 0 , 7 1 5 A 1 1 / 1 9 9 8 F l o r i o5 , 9 2 9 , 0 5 0 A 7 / 1 9 9 9 P e t i t o6,476,005 B1 * 11/2002 P e t i t o e t a l . . . . . . . . . . . . . . . . . . . 514/62

FOREIGN PATENT DOCUMENTSDE 3445324 1 2 / 1 9 8 6F R 2035781 1 2 / 1 9 7 0GB 896940 5 / 1 9 6 2

OTHER PUBLICATIONSBody Ammo u t r a c e u t i c a l s , P r o d u c t A l e r t O c t . 2 7 , 1 9 9 7 .R i c h a r d s o n L a b s , I n c . , L o o k o u t N o n F o o d s E d i t i o n ) ,S e p . 9 , 1 9 9 7 ) .* c i t e d by examinerP r i m a r y ExaminerJames O . W i l s o nA s s i s t a n t ExaminerDevesh Khare7 4 ) A t t o r n e y , A g e n t , o r FirmRichard C . L i t m a n5 7 ) ABSTRACTA u t r i t i o n a l c o m p o s i t i o n f o r t h e t r e a t m e n t o f c o n n e c t i v e

t i s s u e i n mamma ls Which i n c l u d e s a g l u c o s a m i n e s a l t ,c h o n d r o i t i n s u l f a t e , c o l l a g e n a n d s o d i u m h y a l u r o n a t e W h i c hs y n e r g i s t i c a l l y a c t a s a c h o n d r o p r o t e c t i v e a g e n t . The c o mp o s i t i o n c a n f u r t h e r i n c l u d e a d e t o x i f y i n g a g e n t , a n a n t iin?ammatory a g e n t o r a n a n a l g e s i c t o d e m o n s t r a t e a d d it i o n a l t h e r a p e u t i c a n d p h y s i o l o g i c p r o p e r t i e s . T h e n u t r i t i o n a lc o m p o s i t i o n a c t s a s a c h o n d r o - p r o t e c t i v e a g e n t Which p r ov i d e s f o u n d a t i o n a l s u p p o r t f o r t h e c r e a t i o n o f n e W bodyt i s s u e a n d c a r t i l a g e g r o W t h i n humans a n d a n i m a l s .

1 9 C l a i m s , No D r a w i n g s



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US 6 , 6 4 5 , 9 4 8 B21

NUTRITIONAL COMPOSITION FOR THETREATMENT OF CONNECTIVE TISSUE

CROSS-REFERENCE TO RELATEDAPPLICATIONS

T h i s a p p l i c a t i o n i s a c o n t i n u a t i o n - i n - p a r t o f a p p l i c a t i o nS e r . N o . 0 9 / 3 6 0 , 1 6 9 ? l e d J u l . 2 6 , 1 9 9 9 , now US. P a t . N o .6 , 4 7 6 , 0 0 5 , W h i c h i s a c o n t i n u a t i o n - i n - p a r t o f a p p l i c a t i o n S e r .N o . 0 9 / 0 4 6 , 7 1 0 ? l e d M a r . 2 4 , 1 9 9 8 , a n d n o W a b a n d o n e d .

BACKGROUND OF THE INVENTION1 . F i e l d o f t h e I n v e n t i o nT h e p r e s e n t i n v e n t i o n r e l a t e s t o t h e r a p e u t i c c o m p o s i t i o n s

Which p r o v i d e f o r t h e t r e a t m e n t o f c o n n e c t i v e t i s s u e i nmamma ls a n d , more p a r t i c u l a r l y t o n u t r i t i o n a l c o m p o s i t i o n sc a p a b l e o f a c t i n g a s c h o n d r o p r o t e c t i v e a g e n t s , a s W e l l a se x h i b i t i n g a d d e d p h a r m a c o l o g i c a l p r o p e r t i e s .

2 . D e s c r i p t i o n o f t h e R e l a t e d A r tThe r e l a t e d a r t o f i n t e r e s t d i s c l o s e s numerous pharma

c e u t i c a l c o m p o s i t i o n s a n d methods f o r t h e t r e a t m e n t o fc o n n e c t i v e t i s s u e i n humans a n d a n i m a l s . F o r e x a m p l e , US.P a t . N o . 4 , 8 3 7 , 0 2 4 i s s u e d on J u n . 6 , 1 9 8 9 , t o D o v M i c h a e l id e s c r i b e s t o p i c a l c o m p o s i t i o n s f o r i m p r o v i n g W o u n d h e a l i n gc o m p r i s i n g a s u s p e n s i o n o f p a r t i c l e s o f c o l l a g e n a n d ag l y c o s a m i n o g l y c a n . T h e c o m p o s i t i o n i s t a u g h t t o b e u s e f u lf o r t r e a t i n g s u r f a c e W o u n d s b y a p p l y i n g t h e c o m p o s i t i o n t oa g a u Z e , bandage o r t h e l i k e .

US. P a t . N o . 4 , 2 1 6 , 2 0 4 i s s u e d on A u g . 5 , 1 9 8 0 , a n d US.P a t . N o . 4 , 4 5 5 , 3 0 2 i s s u e d o n J u n . 1 9 , 1 9 8 4 , t o H a r r y J .R o b e r t s o n b o t h d i s c l o s e a m e d i c a l p r o t e i n h y d r o l y s a t e cont a i n i n g a n a c e t i c a c i d e x t r a c t o f p o l y p e p t i d e s a n d aminoa c i d s i n t h e f o r m o f poWder o r a g e l a n d p r o d u c e d f r o mp o u l t r y f e e t . An queous s o l u t i o n c a n a l s o b e i n j e c t e d i n t o aW o u nd a r e a s u c h a s b u r n e d a n i m a l r e g i o n s . The c o m p o s i t i o ni s d e s c r i b e d a s b e i n g u s e f u l f o r r e g r o W i n g m u s c l e , s k i n a n dnerve t i s s u e .

US. P a t . N o . 5 , 1 4 1 , 9 2 8 i s s u e d o n A u g . 2 5 , 1 9 9 2 , t oLaWrence G o l dman d e s c r i b e s o p h t h a l m i c m e d i c a t i o n s cont a i n i n g g l y c o s a m i n o g l y c a n p o l y s u l f a t e s (GAGPS) o r mucop o l y s a c c h a r i d e s h a v i n g a m o l e c u l a r W e i g h t i n t h e r a n g e o f5 , 0 0 0 t o 2 0 , 0 0 0 D a l t o n s combined W i t h a n t i b i o t i c s f o rt r e a t i n g e y e i n f e c t i o n s a n d a n t i m i c r o b i a l a g e n t s s u c h a sp i l o c a r p i n e o r e p i n e p h r i n e f o r g l a u c o m a . G A G P S i n c l u d ec h o n d r o i t i n s u l f a t e a n d h y a l u r o n i c a c i d t h a t c o n t a i n h e xo s a m i n e s .

U S . P a t . No. 5 , 8 4 0 , 7 1 5 i s s u e d o n Nov. 2 4 , 1998 t o V i t oF l o r i o t e a c h e s a d i e t a r y r e g i m e n o f n u t r i t i o n a l s u p p l e m e n t s

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2W o u n d s o f t h e b o d y s u r f a c e c o n t a i n i n g g l u c o s a m i n e a n d / o rN - a c e t y l g l u c o s a m i n e a n d g l u c o s a m i n e p h o s p h a t e i n a s a l i n es o l u t i o n

I t h a s f u r t h e r b e e n s u g g e s t e d b y v a r i o u s p r i o r a r t d i s c l os u r e s t o use e x c l u s i v e l y n u t r a c e u c e u t i c a l s o r compositionsc o n t a i n i n g o n l y n a t u r a l l y - o c c u r r i n g c o m p o n e n t s f o r t r e a t i n gc o n n e c t i v e t i s s u e a f f l i c t i o n s . F o r e x a m p l e , US. P a t . N o s .5 , 3 6 4 , 8 4 5 i s s u e d on N o v . 1 5 , 1 9 9 4 a n d 5 , 5 8 7 , 3 6 3 i s s u e dD e c . 2 4 , 1 9 9 6 , b o t h t o R o b e r t W . Henderson d e s c r i b et h e r a p e u t i c c o m p o s i t i o n s a d m i n i s t e r e d i n c a p s u l e s f o r m f o rt h e p r o t e c t i o n, t r e a t m e n t a n d r e p a i r o f c o n n e c t i v e t i s s u e i nmammals. T h e c o m p o s i t i o n s c o n t a i n 2 5 0 3 0 0 0 m g g l uc o s a m i n e h y d r o c h l o r i d e o r s u l f a t e , 501000 mg h o n d r o i t i ns u l f a t e , a n d c a n a d d i t i o n a l l y c o m p r i s e 1 5 9 5 0 m g manganese ascorbate.

I n o t h e r r e l a t e d a r t , Body Ammo N u t r a c e u t i c a l s i n a P r o d u c t A l e r t a r t i c l e , p u b l i s h e d O c t . 2 7 , 1 9 9 7 , d i s c l o s e sc a p s u l e s c o n t a i n i n g c u r c u m i n , h y a l u r o n i c a c i d , c h o n d r o i t i ns u l f a t e a n d g l u c o s a m i n e . T h i s p r o d u c t i s s t a t e d t o p r o v i d en u t r i t i o n a l s u p p o r t f o r c o n n e c t i v e t i s s u e . F u r t h e r , R i c h a r ds o n L a b s , I n c . i n a L o o k o u t (Non F o o d s E d i t i o n ) a b s t r a c t ,p u b l i s h e d S e p . 9 , 1 9 9 7 , d i s c l o s e s a p r o d u c t d e s c r i b e d a s af o o d s u p p l e m e n t c o n t a i n i n g h y d r o l y Z e d c o l l a g e n , g l ucosamine a n d c h o n d r o t i n s u l f a t e t h a t i s d e s c r i b e d a s b e i n gc a p a b l e o f r e c o n s t r u c t i n g b o n e c a r t i l a g e .

U S . P a t . N o . 5 , 9 2 9 , 0 5 0 i s s u e d on u l . 2 7 , 1999 t o GeorgeD . P e t i t o d i s c l o s e s a method a n d c o m p o s i t i o n f o r t r e a t i n gopen W o unds by a p p l y i n g t o t h e W o u n d a n e f f e c t i v e amounto f a n aqueous s o l u t i o n o f c h r o n d r o i t i n s u l f a t e , Which m a yo p t i o n a l l y i n c l u d e c o l l a g e n , s o d i u m h y a l u r o n a t e a n d / o r g l uc o s a m i n e h y d r o c h l o r i d eWhile a l l t h e above r e f e r e n c e s have been d e s c r i b e s a sb e i n g e f f e c t i v e f o r t h e i r i n t e n d e d u s e , t h e r e r e m a i n s a n e e di n t h e a r t f o r a t h e r a p e u t i c c o m p o s i t i o n Which d e m o n s t r a t e senhanced e f f e c t i v e n e s s i n t h e t r e a t m e n t o f c o n n e c t i v et i s s u e s , e x h i b i t o t h e r i m p r o v e d b e n e ? c i a l p r o p e r t i e s , a n dp r o v i d e e v e n W i d e r a p p l i c a t i o n s i n t h e modes o f a d m i n i st r a t i o n . The p r e s e n t i n v e n t i o n m e e t s t h e s e n e e d s .

SUMMARY OF THE INVENTIONA c c o r d i n g l y , i t i s a p r i n c i p a l o b j e c t o f t h e p r e s e n t i n v e nt i o n t o p r o v i d e t h e r a p e u t i c c o m p o s i t i o n s t h a t a r e n o t o n l y

c a p a b l e o f e f f e c t i v e l y t r e a t i n g c o n n e c t i v e t i s s u e s i nmammals, b u t d e m o n s t r a t e o t h e r b e n e ? c i a l p h y s i o l o g i c a lp r o p e r t i e s a s W e l l .

I t i s a n o t h e r o b j e c t o f t h e p r e s e n t i n v e n t i o n t o p r o v i d en u t r i t i o n a l c o m p o s i t i o n s f o r t h e t r e a t m e n t o f c o n n e c t i v e



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US 6 , 6 4 5 , 9 4 8 B23

t a b l e t f o r m f o r o r a l i n g e s t i o n . The p r e s e n t c o m p o s i t i o n s c a na l s o b e p r e p a r e d a s a g e l , p a s t e o r cream f o r t o p i c a la p p l i c a t i o n , o r i n a s o l u t i o n o r s u i t a b l e p h a r m a c e u t i c a lc a r r i e r f o r o r a l o r p a r e n t e r a l a d m i n i s t r a t i o n. P r e f e r a b l y , ad e t o x i f y i n g a g e n t , a n a n t i - i n ? a m m a t o r y a g e n t a n d / o r a na n a l g e s i c i s i n c o r p o r a t e d i n t o t h e f o r m u l a t i o n s t o p r o v i d ea d d e d b e n e ? c i a l t h e r a p e u t i c a n d p h y s i o l o g i c p r o p e r t i e s t ot h e p r e s e n t c o m p o s i t i o n s .

DETAILED DESCRIPTION OF THEPREFERRED EMBODIMENTS

The p r e s e n t i n v e n t i o n p r o v i d e s a n improvement o v e r t h ec o m p o s i t i o n s s e t f o r t h i n t h e a f o r e m e n t i o n e d a p p l i c a t i o nS e r . N o . 0 9 / 3 6 0 , 1 6 9 ? l e d J u l . 2 6 , 1 9 9 9 , t h e d i s c l o s u r e o fW h i c h i s i n c o r p o r a t e d h e r e i n b y r e f e r e n c e i n i t s e n t i r e t y .T h u s , t h e p r e s e n t i n v e n t i o n i s d i r e c t e d t o a n u t r i t i o n a lc o m p o s i t i o n c o m p r i s i n g a t h e r a p e u t i c a l l y e f f e c t i v e a m o u n to f a c h o n d r o p r o t e c t i v e a g e n t , p r e f e r a b l y i n c o m b i n a t i o nW i t h a t l e a s t o n e o t h e r p h y s i o l o g i c a l l y b e n e ? c i a l a g e n t . Thep r e s e n t n u t r i t i o n a l c o m p o s i t i o n c o m p r i s e s a b o u t 1 3 0mg/kg o f a g l u c o s a m i n e s a l t , a b o u t 1 1 5 mg/kg o f c h o nd r o i t i n s u l f a t e , a b o u t 1 3 0 m g / k g o f c o l l a g e n a n d a b o u t1 1 5 m g / k g o f s o d i u m h y a l u r o n a t e W h i c h s y n e r g i s t i c a l l y a c ta s t h e c h o n d r o p r o t e c t i v e a g e n t , W h e r e i n t h e d o s a g e o f e a c hs o l i d c o m p o n e n t p r e s e n t i n t h e c o m p o s i t i o n i s e x p r e s s e dh e r e i n i n t e r m s o f mg e r kg b o d y W e i g h t o f t h e h uman o b et r e a t e d . T h e u n i t d o s a g e s o f t h e p r e s e n t c o m p o s i t i o n s f o ra n i m a l s may b e s u b s t a n t i a l l y l a r g e r .

W h i l e t h e p r e s e n t c o m p o s i t i o n s e f f e c t i v e l y p r o v i d e f o u nd a t i o n a l s u p p o r t f o r t h e c r e a t i o n o f neW body t i s s u e a n dc a r t i l a g e g r o W t h , f a c i l i t a t e c h o n d r o c y t e s y n t h e s i s , p r o t e c ta n d m a i n t a i n h e a l t h y m u s c l e a n d t i s s u e , i n c r e a s e h y a l u r o n i ca c i d c o n c e n t r a t i o n s , a n d r e d u c e i n ? a m m a t i o n , o t h e r b e n e ?c i a l p h y s i o l o g i c a l p r o p e r t i e s o f t h e c o m p o s i t i o n s c a n b es i g n i ? c a n t l y e n h a n c e d b y t h e i n c o r p o r a t i o n o f a d d i t i o n a lc h e m i c a l a g e n t s . P r e f e r a b l y , a d e t o x i f y i n g a g e n t , a n a n t iin?ammatory a g e n t a n d / o r a n a n a l g e s i c i s a d d e d t o t h ep r e s e n t n u t r i t i o n a l c o m p o s i t i o n s f o r t h e s e i n t e n d e d p u rp o s e s .

T h e g l u c o s a m i n e s a l t c o m p o n e n t o f t h e p r e s e n t compos i t i o n s i s p r e f e r a b l y t h e h y d r o c h l o r i d e s a l t , b u t o t h e r s a l t s o fg l u c o s a m i n e s u c h a s t h e s u l f a t e , n i t r a t e o r i o d i d e o b t a i n e dfrom e i t h e r s y n t h e t i c , bovine o r p o r c i n e s o u r c e s a r e a l s os u i t a b l e . The c h o n d r o i t i n s u l f a t e component may i n c l u d eT y p e A c h o n d r o i t i n - 4 - s u l f a t e ) , T y p e B c h r o n d r o i t i n - 5s u l f a t e ) , a n d / o r T y p e C c h o n d r o i t i n - 6 - s u l f a t e ) , o b t a i n e dt h r o u g h f e r m e n t a t i o n o r e x t r a c t i o n o f b o v i n e t r a c h e a , o t h e rb o v i n e o r p o r c i n e s o u r c e s . A o l e c u l a r W e i g h t r a n g e o f2 , 0 0 0 5 0 , 0 0 0 c a n b e u s e d , W i t h a p r e f e r r e d r a n g e o f

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4i n c l u d e a manganese s a l t a n d L - m a l i c a c i d . Apreferred s a l ti s manganese a s c o r b a t e b e c a u s e i t p r o v i d e s a s c o r b i c a c i d f o rc o l l a g e n s y n t h e s i s , b u t o t h e r manganese s a l t s s u c h a s t h es u l f a t e , n i t r a t e , a n d g l u c o n a t e c a n b e u s e d . The L - m a l i c a c i da c t s a s a d e t o x i f y i n g a g e n t by r i d d i n g t h e body o f u n W a n t e dl a c t i c a c i d , o f t e n f o u n d i n c o n n e c t i v e t i s s u e . B o t h t h eL - m a l i c a c i d and manganese s a l t a r e p r e f e r a b l y o f U . S . P .f o o d g r a d e , a n d a r e p r e s e n t i n t h e n u t r i t i o n a l c o m p o s i t i o n so f t h e p r e s e n t i n v e n t i o n i n d o s a g e s r a n g i n g f r o m a b o u t 0 . 0 5t o a b o u t 8 m g / k g .

P h a r m a c o l o g i c a l a g e n t s may b e i n c o r p o r a t e d i n t o t h en u t r i t i o n a l c o m p o s i t i o n s o f t h e p r e s e n t i n v e n t i o n t o s i g n i ?c a n t l y e n h a n c e t h e p h y s i o l o g i c a l p r o p e r t i e s o f t h e compos i t i o n s . T h e a n t i - i n ? a m m a t o r y a g e n t s m e t h y s u l f o n y l m e t ha n e ( M SM ) a n d c e t y l m y r i s t o l e a t e may b e a d d e d t o r e d u c ea n in?ammatory r e s p o n s e . The MSM m a y b e added i na m o u n t s o f a b o u t 0 . 5 4 0 m g / k g , a n d c e t y l m y r i s t o l e a t e i na m o u n t s o f 1 1 0 5 m g / k g . T h e p r e s e n t c o m p o s i t i o n s maya l s o b e c o m b i n e d W i t h a s p i r i n , p r e f e r a b l y i n t h e r a n g e o fa b o u t 0 . 1 3 5 m g / k g , a n d o t h e r c o m m e r c i a l l y a v a i l a b l e a n a lg e s i c s t o r e d u c e p a i n . I n a d d i t i o n , t h e i n c o r p o r a t i o n o f s u c hv i t a m i n s a s V i t a m i n C a s c o r b i c a c i d ) a n d V i t a m i n B 1 2 i n t h ep r e s e n t c o m p o s i t i o n s p r o v i d e s a d d e d b e n e ? t s t o s o f t a n dh a r d t i s s u e s .

The n u t r i t i o n a l c o m p o s i t i o n s o f t h e p r e s e n t i n v e n t i o n a r ef o r m u l a t e d i n t o p o W d e r , c a p s u l e o r t a b l e t f o r m f o r o r a li n g e s t i o n , A l s o , t h e p r e s e n t c o m p o s i t i o n s a r e c a p a b l e o fb e i n g combined W i t h a s u i t a b l e p h a r m a c e u t i c a l c a r r i e r a n dp r e p a r e d a s a g e l , p a s t e o r cream f o r t o p i c a l a p p l i c a t i o n .A l t e r n a t i v e l y , t h e c o m p o s i t i o n s c a n b e f o r m u l a t e d i n as o l u t i o n o r s u i t a b l e pharmaceutical d i l u e n t f o r o r a l a s W e l l a sp a r e n t e r a l a d m i n i s t r a t i o n .F o r p a r e n t e r a l a d m i n i s t r a t i o n , t h e p r e s e n t c o m p o s i t i o n sa r e p r e f e r a b l y d i s s o l v e d i n s t e r i l i Z e d W a t e r and b u f f e r e d W i t hsuch b u f f e r i n g a g e n t s a s c i t r i c a c i d o r sodium c h l o r i d e t oi m p r o v e s h e l f l i f e . The p H o f t h e p r e s e n t s o l u t i o n s c a n b ea d j u s t e d W i t h c o n v e n t i o n a l a g e n t s . A l s o , p r e s e r v a t i v e s s u c ha s e t h y l e n e - d i a m i n e t e t r a a c e t i c a c i d E D T A ) , b e n Z y l a l c o h o l ,and benZalkonium c h l o r i d e can be a d d e d .

The n u t r i t i o n a l c o m p o s i t i o n s o f t h e p r e s e n t i n v e n t i o np r o v i d e a n e n h a n c e d c h o n d r o p r o t e c t i v e e f f e c t b y p r o v i d i n gf o u n d a t i o n a l s u p p o r t f o r t h e c r e a t i o n o f n e W body t i s s u e a n dc a r t i l a g e g r o W t h i n m a m m a l s . T h e c o l l a g e n c o m p o n e n t a c t sa s a t r a n s p o r t e r o r c a r r i e r f o r t h e l a r g e r molecules o f sodiumh y a l u r o n a t e a n d / o r c h o n d r o i t i n s u l f a t e b y a i d i n g i n t h ea b s o r p t i o n p r o c e s s o f t h e s e l a r g e m o l e c u l e s , t h e r e b y i n c r e a si n g t h e b i o - a v a i l a b i l i t y o f t h e s e t h e r a p e u t i c e f f e c t i v e comp o n e n t s .

I t i s t o b e u n d e r s t o o d t h a t t h e p r e s e n t i n v e n t i o n i s n o t



10/18

US 6 , 6 4 5 , 9 4 8 B25

5 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i mf u r t h e r c o m p r i s i n g a manganese s a l t .6 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i ng t o c l a i mWherein t h e manganese s a l t i s manganese a s c o r b a t e .7 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i mf u r t h e r c o m p r i s i n g a d e t o x i f y i n g a g e n t .8 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i ng t o c l a i mW h e r e i n t h e d e t o x i f y i n g a g e n t i s L - m a l i c a c i d .9 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i mf u r t h e r c o m p r i s i n g a n a n t i - i n ? a m m a t o r y a g e n t .1 0 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i mW h e r e i n t h e a n a n t i - i n ? a m m a t o r y a g e n t i s s e l e c t e d f r o m t h eg r o u p c o n s i s t i n g o f m e t h y s u l f o n y l m e t h a n e a n d c e t y l m y r i st o l e a t e .1 1 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i m 1 ,f u r t h e r c o m p r i s i n g a n a n a l g e s i c .1 2 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i m 1 1 ,W h e r e i n t h e a n a l g e s i c i s a s p i r i n .1 3 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i m 1 ,f u r t h e r comprising a v i t a m i n s e l e c t e d from t h e group cons i s t i n g o f V i t a m i n C a n d V i t a m i n B 1 2 .

1 4 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i m 1 ,W h e r e i n t h e c o m p o s i t i o n i s f o r m u l a t e d i n t o a u n i t d o s a g eform f o r o r a l a d m i n i s t r a t i o n .

1 ,

10

1 5

20

61 5 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i m 1 ,

W h e r e i n t h e c o m p o s i t i o n i s combined W i t h a s u i t a b l e p h a rm a c e u t i c a l c a r r i e r and p r e p a r e d a s a g e l , p a s t e o r cream f o rt o p i c a l a p p l i c a t i o n .1 6 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i m 1 ,Wherein t h e composition i s f o r m u l a t e d i n a s o l u t i o n o rs u i t a b l e p h a r m a c e u t i c a l d i l u e n t f o r o r a l o r p a r e n te r a l admini s t r a t i o n .1 7 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i m 1 ,W h e r e i n t h e c o m p o s i t i o n c o m p r i s e s , b a s e d o n mg/kg o fb o d y W e i g h t :

a b o u t 1 3 0 mg/kg o f a g l u c o s a m i n e s a l t ;a b o u t 1 1 5 m g / k g o f c h o n d r o i t i n s u l f a t e ;a b o u t 1 3 0 m g / k g o f c o l l a g e n ; a n da b o u t 1 1 5 m g / k g o f s o d i u m h y a l u r o n a t e .1 8 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i m 1 7 ,

f u r t h e r i n c l u d i n g a manganese s a l t r a n g i n g f r o m a b o u t 0 . 0 5t o a b o u t 8 m g / k g .1 9 . T h e n u t r i t i o n a l c o m p o s i t i o n a c c o r d i n g t o c l a i m 1 7 ,f u r t h e r i n c l u d i n g L - m a l i c a c i d r a n g i n g f r o m a b o u t 0 . 0 5 t oa b o u t 8 m g / k g .



11/18

EXHIBIT B



12/18

Part No. 22-67986

44967 07G B18617 LAB

2012

60POINTS

60POINTS

For more information visitwww.osteobiflex.com

FnL1010020

01BE5CVFkETkJUWQBEGre6

30768 034520 8

Osteo Bi-FlexMSM Formula caplets are apotent combination of highly effectiveingredients in Joint Care Science and theonly leading brand containing Joint Shieldwith 5-LOXINAdvanced.

See Bottom of Package for our

Ambassadors Clubrewards points program.

*These statements have not been evaluated by the Food and DrugAdministration. This product is not intended to diagnose, treat, cure orprevent any disease.

Osteo Bi-Flexis manufactured underthe highest standards for product

quality, purity and potency.

To learn more about Osteo Bi-Flex

visit WWW.OSTEOBIFLEX.COMor call us toll free at

1-888-VITAHELP (848-2435).

KEEP OUT OF REACH OF CHILDREN. STORE

AT ROOM TEMPERATURE AND AVOID EXCESSIVE HEAT.

TAMPER RESISTANT: DO NOT USE IF SEAL UNDER CAP

IS BROKEN OR MISSING.

CAUTION: If you are pregnant, nursing, taking any medicationsor have any medical condition, consult your doctor before use.Discontinue use and consult your doctor if any adverse reactionsoccur. Not intended for use by persons under the age of 18.

MANUFACTURED BY: REXALL SUNDOWN, INC., BOCA RATON, FL 33487 USA

Proud sponsor of the

Like calcium supplements can helpyour bones, Osteo Bi-Flexcan helpyour joints.*

The natural aging process can addexcessive stress on your joints. Annoyingflare-ups can strike at any time. Add OsteoBi-Flex MSM Formula to your joint careregimen. It contains 1,500 mg ofGlucosamine, a key building block ofcartilage.* With the addition of our Joint

Shield Proprieta ry Ble nd w hich containsChondroitin, MSM and 5-LOXINAdvanced,this revolutionary formula helps revitalize

your joints to keep them jump in.*

5-LOXIN Advanced contains highconcentrations of AKBA, which is importantfor helping with joint flare-ups.*

ADVANCED isa registeredtrademarkofP.L. Thomas-Laila NutraLLCand isused underlicense.InternationalPatentsPending.-

DIRECTIONS FOR ADULT USE: TAKE FOUR (4)CAPLETS PER DAY PREFERABLY WITH FOOD.As a reminder, discuss the supplements andmedications you take with your health care

providers.Note: You have the option of taking fourcaplets together or spread throughout the day.

Other Ingredients: Cellulose (Plant Origin),Crospovidone. Contains


13/18

EXHIBIT C



14/18

Part No. 22-52272

52272 00B B52202 AAC

2012

40POINTS

40POINTS


0

330768 03121

Osteo Bi-FlexTriple Strength caplets are apotent combination of highly effectiveingredients in Joint Care Science and is theonly leading brand containing Joint Shieldwith 5-LOXINAdvanced.


Ambassadors Clubreward points program.





visit WWW.OSTEOBIFLEX.COMor call us toll free

1-888-VITAHELP (848-2435)





CAUTION: If you are pregnant, nursing, taking any medicationsor have any medical condition, consult your doctor before use.Discontinue use and consult your doctor if any adverse reactionsoccur. Not intended for use by persons under the age of 18.




The natural aging process can add excessive

stress on your joints. Annoying flare-ups can

strike at any time. Add Osteo Bi-Flex Triple

Strength to your joint care regimen. It

contains 1,500 mg of Glucosamine, a key

building block of cartilage.* With the addition

of our Joint Shield Proprietary Blend which

contains Chondroitin, MSM and our 5-LOXIN

Advanced, this revolutionar y formula helps

revitalize your joints to keep them jumpin.*

5-LOXIN Advanced contains high

concentrations of AKBA, which is important

for helping with joint flare-ups.*

ADVANCED isa registeredtrademarkofP.L. Thomas-Laila NutraLLCand isused underlicense.InternationalPatentsPending.

-

DIRECTIONS FOR ADULT USE: TAKE TWO (2)CAPLETS PER DAY WITH FOOD.As a reminder,discuss the supplements and medications you

take with your health care providers.Note: You have the option of taking two capletstogether or spread throughout the day.

Other Ingredients: Crospovidone. Contains


15/18

EXHIBIT D



16/18

Part No. 22-52399

52399 00A B52399 MAB

2012

40POINTS

40POINTS

FnL1010020

01BE5CVFkETkJUWQBIxP1D

30768 188700 2


THE


The natural aging process can addexcessive stress on your joints. Annoying

flare-ups can strike at any time. Add Osteo

Bi-Flex Joint & Energy to your joint care

regimen. It contains 1,500 mg of

Glucosamine, a key building block of

cartilage.* With the addition of our Joint

Shield Proprietary Blend, which contains

Chondroitin, MSM and 5-LOXINAdvanced,

this revolutionary Energy Formula helps

support energy metabolism and revitalize

your joints to keep them jumpin.*

The only leading brand with 5-LOXIN

Advanced. Starts working to improvejoint comfort within 7 days.*

Based on the results of a GfK Healthcare 2011 survey among physicians who recommend abrand of Glucosamine and Chondroitin or Glucosamine supplements; and the result of aPharmacy Times Survey among pharmacists who recommend a bone/joint strengthenerdietary supplement, 2006-2012.1Basedontwo humanstudieswith5-LOXIN Advancedwheresubjectsrated theirjointhealthovertime,subjectsjointhealthimproved within 7 days, andcontinued to improvethroughoutthe durationof thestudies.**52week NielsenScanTrackdata ending8/25/12.

Osteo Bi-Flex

Joint &Energy helps to:Osteo Bi-Flex

Joint &Energy helps to:

Revitalize Joints*

Promote Mobility*

Support Energy

Metabolism*

Revitalize Joints*

Promote Mobility*

Support Energy

Metabolism*

DOCTOR & PHARMACISTRECOMMENDED BRAND

#

1

Osteo Bi-FlexJoint & Energy caplets are apotent combination of highly effectiveingredients in Joint Care Science and is theonly leading brand containing Joint Shieldwith 5-LOXINAdvanced.


Ambassadors Clubreward points program.





visit WWW.OSTEOBIFLEX.COMor call us toll free

1-888-VITAHELP (848-2435).





CAUTION:Not intended for use by pregnant or nursing women.If you are taking any medications or have any medical condition,consult your doctor before use. Discontinue use and consultyour doctor if any adverse reactions occur. Not intended for useby persons under the age of 18.



Join the millions of people who chooseOsteo Bi-Flexfor their joints everyday, and have made it the #1 brand.**

DOCTOR & PHARMACISTRECOMMENDED BRAND

#

1

ADVANCED isa registeredtrademarkofP.L. Thomas-Laila NutraLLCand isused underlicense.InternationalPatentsPending.

-

DIRECTIONS FOR ADULT USE: TAKE TWO (2) CAPLETSPER DAY PREFERABLY WITH FOOD. As a reminder,discuss the supplements and medications you takewith your health care providers.

Other Ingredients:Cellulose (Plant Origin), Crospovidone.Contains


17/18

EXHIBIT E

Case 1:13 cv 08074 PKC Document 1 Filed 11/13/13 Page 17 of 18


18/18

Part No. 22-52526

52526 00A B52514 LAB

2012

40POINTS

40POINTS


0

130768 03138

Osteo Bi-Flex Double Strengthcaplets are a potent combination ofhighly effective ingredients in JointCare Science and the only leadingbrand containing Joint Shield with5-LOXINAdvanced.



The natural aging process can addexcessive stress on your joints.

Annoying flare-ups can strike at anytime. Add Osteo Bi-Flex Double

Strength to your joint care regimen. Itcontains 1,500 mg of Glucosamine, akey building block of cartilage.* Withthe addition of our Joint ShieldProprietary Blend, which containsChondroitin, MSM and 5-LOXIN

Advanced, this revolutio nary formulahelps revitalize your joints to keepthem jumpin.*

DIRECTIONS FOR ADULT USE: TAKE THREE (3)CAPLETS PER DAY PREFERABLY WITH FOOD.As a reminder, discuss the supplements andmedications you take with your health careproviders.

Note: You have the option of taking threecaplets together or spread throughout the day.

Other Ingredients: Crospovidone.Contains

petito et. al. v. rexall sundown

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