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LOGO LOGO LOGO Preformulation study Physical and Chemical Properties Biopharmaceutical Properties Pharmacological?andToxicological properties Ⅰ Physical and Chemical Properties Description of the products Description of the business hygrooscopicity Solubility and Pka Text in here Text in here Text in here Text in here stability micromeritics hygroscopicity Compatibility of excipient MP and polymorphism Text in here Partition coefficient solubility Pka/Dissociation constants drug must possess aqueous solubility for threaepeutic efficacy. If the solubility of drug is less than desirable,consideration must be given to improve its solubility The extent of dissociation in many cases is highly dependent on the Ph of the medium containing the drug In formulation often the vehicleis adjusted to certain Ph to abtain a certain level of ionization Or dissociation for solubility or stability Partition coefficient the oil-water partition coefficient( P ) is a measure of a molecule’ lipophilic character. Drugs which have bigger P can be easily absorbed when they have the similiar Pka value. P = (Conc. Of drug in octanol )/(Conc. Drug in water) while octanol is the most common used s solvent during the measurement of the P, and when drug exist as a monomer P = (Conc. Of drug in octanol )n/(Conc. Drug in water) while the drug exists as polymer Text in here Relation between P of barbiturates and absorption in stomach of rats Barbiturates Pka p absorption rate(%) Barbital 7.9 0.72 6.2 Phenobarbital 7.41 4.44 12.6 Pentobarbital 8.11 24.1 17.6 Amobarbital 7.49 33.8 17.7 Polymorphic forms
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