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 is the difference between Cocrystal and salt?

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.

How are Cocrystals formed?

Cocrystals are typically generated through slow evaporation of solutions of the two components. This approach has been successful with molecules of complementary hydrogen bonding properties, in which case cocrystallization is likely to be thermodynamically favored.

Which drug shows Rapa dissolution rate?

Which form of a drug has greater solubility? Explanation: Anhydrous form of a drug has a greater aqueous solubility than the hydrates.

Which other cocrystal preparation technique can be considered as green approach?

5. Melting crystallization. Melting crystallization is an alternative green approach for preparing pharmaceutical cocrystals38. Although solvents are not involved in this approach, the thermal stability of drug and coformer should be carefully evaluated in advance82.

What is cocrystal 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.

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 …

Which form of drug shows higher solubility stable or unstable?

Generally, metastable forms are more soluble than the corresponding stable polymorphic forms, but they transform to the more thermodynamically stable form in a relatively short time [14], and thus it is necessary to monitor the polymorphic transformation during formulation, manufacturing, and storage of dosage forms to …

What is the effect of crystallization on the solubility of drug?

The mechanism of increased dissolution rate of drugs by solid dispersion crystallization technique has been attributed to a number of factors such as drug amorphization, increased drug solubility, reduction in particle size, a higher degree of surface area and porosity [14-17].

What is difference between API and formulation?

APIs denote the dosage in a drug, or in other words the key chemicals that make the drug work, while finished formulation is the process in which different chemicals, including the active ingredient, are mixed in specified ratios to produce a specific drug.

How do I choose a Coformer for my cocrystal?

A general approach to coformer selection is by “tactless” cocrystal screening, whereby a predetermined library of pharmaceutically acceptable/approved compounds is used to attempt cocrystallization. In cocrystal development one of the approach of coformer selection is based on trial and error.

Which form of drug has greater stability?

Pharmaceutical dosage forms: solid dosage forms are more stable than liquid dosage forms for presence of water.

What factors affect the stability of a drug?

Stability of drugs depends on both environmental factors such as light, temperature, humidity, air, and drug-related factors such as the active ingredient itself, the dosage form (tablet, 1 suspension, etc.) and the manufacturing process .

How can you increase the solubility of a drug?

There are various techniques to enhance the drug solubility such as particle size reduction, nanosuspension, use of surfactants, salt formation, solid dispersion, etc. From this article it may be concluded that solid dispersion is an important approach for improvement of bioavailability of poor water-soluble drugs.

Is amorphous or crystalline more soluble?

Conclusions: Amorphous pharmaceuticals are markedly more soluble than their crystalline counterparts, however, their experimental solubility advantage is typically less than that predicted from simple thermodynamic considerations.

What is the difference between API and intermediates?

an API is not made from raw material by just one reaction, but by a variety of compounds that become API. the compounds that are being transformed from raw materials into APIs are called intermediates. Some APIs go through more than ten intermediates in the process of going from raw material to API.