What is a pharmaceutically acceptable salt?
Pharmaceutically Acceptable Salt of a compound means a salt that is pharmaceutically acceptable and that possesses the desired pharmacological activity of the parent compound.
What is difference between salt and co crystal?
LTG-NCT cocrystal is more soluble than drug at pH > 3 and reaches solubilities 18 times the drug solubility at pH ≥ 6. The cocrystal is also more soluble than the SAC salt at pH < 7, and is orders of magnitude more soluble than the salt at pH < 3.
What is the difference between crystal and Cocrystal?
The difference between a crystalline salt and a cocrystal lies merely in the transfer of a proton. The transfer of protons from one component to another in a crystal is dependent on the environment.
Is a solvate a salt?
salt: a crystal containing at least two ions. solvate: any crystal with a solvent molecule plus either a coformer or at least two ions. cocrystal: a crystal with a coformer molecule plus either another coformer or at least two ions.
Why do drugs need to be in salt form?
Without absorption, a drug cannot have a therapeutic effect, so some forms require a salt. Many medications need to be water-soluble, too. Therefore, drugs are often chemically made into their salt forms to enhance how the drug dissolves, boost its absorption into your bloodstream, and increase its effectiveness.
How does salt formation increases solubility?
Choice of the organic solvents in the salt formation leads to the formation of anhydrous salt which yields better solubility and dissolution profile than that of the hydrated form. The crystallization of the salt is achieved only when the drug concentration is adequate with a favorable pH of the solution.
What is co crystal controlled solid state synthesis?
Cocrystal-controlled solid-state synthesis (C3S3) of imides occurs via heating of cocrystals formed between anhydride and aromatic amine cocrystal formers. A series of fourteen derivatives of adamantane was synthesised.
What is the meaning of co crystal?
Co-crystals are multi-component crystals based on hydrogen bonding interactions without the transfer of hydrogen ions to form salts; this is an important feature, since Bronsted acid-base chemistry is not a requirement for the formation of a co-crystal.
What is the meaning of co Crystal?
What are hydrates and solvates give example?
Hydrates and solvates are thus multicomponent crystalline solid molecular adducts containing both the host molecule (API or excipient) and guest molecule (water (hydrate) or other solvents (solvate)) incorporated in the crystal lattice structure, commonly known as pseudopolymorphic forms.
How do you identify solvates?
Hydrates and solvates can be prepared by crystallization in water or an organic solvent or by conversion of the anhydrous material through moisture or solvent adsorption. In quality control testing, hydrates or solvates are identified by the assay of water of crystallization or solvent found in the crystal.
How does salt formation increase solubility of a drug?
The micronization and salt formation of the crystalline compound of molecule enhance the surface area. This overcome the challenges of the molecule solubilization in particular solvent. This can enhance the rate of dissolution of the drug.
What is in situ salt formation?
Processing a weak acid or base with a counterion can cause in situ salt formation, depending on the properties of the materials. Typically, counterions are small inorganic molecules (e.g., sodium, potassium, hydrochloride, or phosphate ions) or small organic molecules (e.g., citrate, tartarate, succinate, or mesylate).
How salt form of drug affect drug absorption?
Salt formation of the ionizable drug molecule is a common strategy to correct the suboptimal drug properties so as to improve physical properties, aqueous solubility, dissolution, stability, alter gastrointestinal absorption, reduce toxicity or enhance organoleptic properties [9, 10].
How does salt affect solubility?
The solubility of proteins usually increases slightly in the presence of salt, referred to as “salting in”. However, at high concentrations of salt, the solubility of the proteins drop sharply and proteins can precipitate out, referred to as “salting out”.
How do cocrystals increase solubility?
In contrast to amorphous pharmaceutical forms, cocrystals can achieve thermodynamic stability in the solid state while providing large solubility advantage over drug. Compared to polymorphs, cocrystals have the ability to increase solubility by orders of magnitude above the drug solubility.
What are solvates with example?
A solvate is a compound that forms between a solute and its solvent. Hydrates: A wide range of salts form hydrates when dissolved in water. The liquid water can then be evaporated to leave the solid hydrate. For example, ferrous chloride FeCl2 forms the hydrate FeCl2(H2O)4.
What is the definition of solvates?
Definition of solvate
(Entry 1 of 2) : an aggregate that consists of a solute ion or molecule with one or more solvent molecules also : a substance (such as a hydrate) containing such ions. solvate.
Which salt is used most widely used in pharma industry?
For basic drugs, the most common salt form is the hydrochloride; about 60% of all basic drug salt forms are hydrochlorides. Hydrochloric acid (HCl) is safe, and chlorine is abundant in the body. It is a very cheap choice, and with it being a strong acid, it will form a salt with most basic compounds.
What are 3 factors that affect drug absorption?
Several factors can affect the absorption of a drug into the body. These include: physicochemical properties (e.g. solubility)
…
the physicochemical properties of the drug, such as its:
- lipid solubility.
- molecular size.
- degree of ionization.
How does salt formation to improve drug solubility?
How does salt affect protein structure?
Salts strip off the essential layer of water molecules from the protein surface eventually denaturing the protein. Protein denaturation by urea may occur by direct or indirect mechanisms (Lindgren and Westlund, 2010).
How does salt affect dissolved oxygen?
Dissolved oxygen decreases exponentially as salt levels increase. That is why, at the same pressure and temperature, saltwater holds about 20% less dissolved oxygen than freshwater.
What is pharmaceutical Cocrystal?
Pharmaceutical cocrystals are defined as crystals that comprise two or more discrete neutral molecules at a stoichiometric ratio and bond together via noncovalent bond interactions (e.g., hydrogen bonding, van der Waals and π···π stacking interactions), in which at least one of the components is API and the others are …
What does Solvated mean in chemistry?
Solvation is the interaction of a solvent with the dissolved solute—in the case of water, solvation is often referred to as hydration.