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1011 Exhibit: Ex 1011 Wells

Document IPR2021-01132, No. 1011 Exhibit - Ex 1011 Wells (P.T.A.B. Jun. 17, 2021)
Nonethelessit is usually better to formulate with a salt since it will control the pH of the diffusion layer — the saturated, highly concentrated solution immediately adjacentto the dissolving surface.
Thus, although the concept of 7 substitutent constants is simple, care must be exercised in its application since a numberof anomalies arise which will give misleading estimates of log P. Nonetheless good estimates are possible and ...
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1022 Exhibit: Ex 1022 Stahl

Document IPR2021-01132, No. 1022 Exhibit - Ex 1022 Stahl (P.T.A.B. Jun. 17, 2021)
It is recommendedto search for the latest safety records in the RTECSin- ventory and in literature at the time when a Class 3 acid or base would be considered for salt formation with an NCE.
GRAS and ADI While there is a chance to change unfavorable drug properties to the bet- ter by selecting less commonly used salt formers, there may be limitations with respect to the acceptability.
This is indi- cated by an ADI (=Acceptable Daily Intake) assigned to them (WHO); in the: USA, the FDA grants the GRAS (= ‘Generally Regarded As Safe’) status to food additives and processing aids [3][4].
The ADJ for man, expressed on a body weight basis, is the amountof a | food additive that can be taken daily in the diet, even overa lifetime, with- out risk.
An ADIis assigned by the Joint FAO/WHO Expert Committee on Food Additives only to those substances for which the available data include either the results of adequate short-term and long-term toxicological investigations, or satisfactory information on the biochemistry and metabolic fate of the compound,or both.
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1013 Exhibit: Ex 1013 Paulekuhn

Document IPR2021-01132, No. 1013 Exhibit - Ex 1013 Paulekuhn (P.T.A.B. Jun. 17, 2021)
6665 _ Trends in Active Pharmaceutical Ingredient SaltSelection based on Analysis of the Orange Book Database G. Steffen Paulekuhn,’* Jennifer B. Dressman,* and Christoph Saal** .. Merck KGaA, Frankfurter Strasse 250, 64293 Darmstadt,Germany, and Institute of Pharmaceutical Technology, Biocenter, Johann Wolfgang Goethe University, Max von Laue Street 9, 60438 Frankfurt (Main), Germany Received August 20, 2007 The Orange Bookdatabase published by the US.
Properties such as solubil- ity, dissolution rate, hygroscopicity, stability, impurity profiles, and crystal habit canbe influenced by using a variety of pharmaceutically acceptable counterions.8 Even polymorphism issues can be resolved in many cases by formation ofsalts.
'°"° Owing to dramatic changes in the techniques applied in pharmaceutical discovery programs over the past 20 years, the physical chemical properties of development candidates have changedsubstantially.’ Drug design based on high-throughput screening has in general led to more lipophilic compounds exhibiting/low aqueoussolubility.
On the other hand, publications giving an overview of approved salt forms are very few.”3 All publica- tions known to the authors dealing with occurrence of coun- terions for formation of pharmaceuticalsalts list the counterions and their distribution in the respective data set only at a given point in time.
Relative incidencesof all anions used in FDA- approved oral formulations are presented in Table 4, The anion Silver Procaine Benzathine (1) mma Calcium (12) Piperazine ~ Potassium C= Cholinate (1) Megiumine gama Diethanolamine (1) ~~ Magnesium Diethylamine (1) .--- LYSINE Diethylamine mmm Lysine (1) Diethanolamine Magnesium (2) Cholinate mage MVeglumine (5) fe Calcium => Piperazine (1) wmzas Potassium (11) sq Procaine(1) wm Silver (1) saa Sodium (131) tama Tromethamine (3) = Zine @) fo
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