This document discusses homogeneous systems and methods for adjusting tonicity, including Class I and Class II methods. Class I methods use sodium chloride or other substances to lower the freezing point of a drug solution to make it isotonic. Class II methods add water and then an isotonic or buffered diluting solution to form an isotonic preparation. Specific Class II methods discussed are the White-Vincent method and Sprowls method. The importance of isotonic solutions for ophthalmic and parenteral preparations is also summarized.
This document discusses homogeneous systems and methods for adjusting tonicity, including Class I and Class II methods. Class I methods use sodium chloride or other substances to lower the freezing point of a drug solution to make it isotonic. Class II methods add water and then an isotonic or buffered diluting solution to form an isotonic preparation. Specific Class II methods discussed are the White-Vincent method and Sprowls method. The importance of isotonic solutions for ophthalmic and parenteral preparations is also summarized.
This document discusses homogeneous systems and methods for adjusting tonicity, including Class I and Class II methods. Class I methods use sodium chloride or other substances to lower the freezing point of a drug solution to make it isotonic. Class II methods add water and then an isotonic or buffered diluting solution to form an isotonic preparation. Specific Class II methods discussed are the White-Vincent method and Sprowls method. The importance of isotonic solutions for ophthalmic and parenteral preparations is also summarized.
is added to the drug in a MODULE 1: HOMEGENEOUS SYSTEMS sufficient amount to form an isotonic solution. The preparation is then made up to its final In aqueous solution, volume with an isotonic or a - an ACID increases the buffered isotonic dilution solution. concentration of hydronium ions These include; [H3O+], sometimes represented as 1. White–Vincent method hydrogen ions [H+] 2. Sprowls method. - a BASE increases the concentration of hydroxide ions Sodium chloride equivalent method [OH-]. - This method is based on calculating the E-value. - BUFFERS are included in the - the sodium chloride equivalent or dosage form to impart sufficient tonicity equivalent of a drug. It is stability to enable the the amount of sodium chloride formulation. that has the same osmotic effect - BUFFERS are substances or a (is equivalent to) as 1 g of the combination of substances that, drug. by their presence in solution, resist White–Vincent method changes in pH upon the addition - This method involves the addition of small quantities of acid or alkali. of water to the drugs to prepare an isotonic solution, followed by Body fluids (blood and lacrimal fluid) the addition of an isotonic or have an osmotic pressure corresponding isotonic-buffered diluting vehicle to that of 0.9% (w/v) sodium chloride. to make up the solution up to the final volume. hydronium and hydroxide ions are Application of Tonicity present both in pure water and in all - It is generally accepted that for aqueous solutions, and their ophthalmic and parenteral concentrations are inversely administration, isotonic solutions proportional as determined by the ion are better tolerated by the product of water. patient than those at the extremes of hypo- or B. Methods of Adjusting Tonicity hypertonicity. The methods for adjusting tonicity - Isotonic solutions cause no subdivided into two classes: swelling or contraction of the → Class I methods, which employ tissues with which they come in sodium chloride or some other contact and produce no substance to the drug solution to discomfort when instilled in the lower the freezing point of the eye, nasal tract, blood or other solution to – 0.52° and thus make body tissues. it isotonic with body fluids. Ophthalmic medication 1. Cryoscopic method - It is generally accepted that 2. Sodium chloride equivalent ophthalmic preparations method intended for instillation into the PHYSICAL PHARMACY LABORATORY (REVIEWER – THEORETICAL) cul-desac of the eye should, if The influence of substituents on the solubility possible, be approximately of molecules in water can be due to their isotonic to avoid irritation. The effect on the properties of the solid or isotonic preparation duplicates liquid or to the effect of the substituent on its interaction with water molecules. ophthalmic tears for the comfort of the patient. • Polar groups such as –OH capable of Parenteral medication hydrogen bonding with water - Injections that are not isotonic molecules impart high solubility. should be administered slowly • Non-polar groups such as –CH3 and – and in small quantities to Cl are hydrophobic and impart low minimize tissue irritation, pain and solubility. cell fluid imbalance. - When parenteral solutions are formulated, the tonicity of OTHER NOTES FOR LECTURE: hypotonic solutions is adjusted by SOLIDS – Amorphous powder (ionic, the addition of dextrose or covalent) sodium chloride. This is true for LIQUIDS – Water bonds parenterally administered GASES – Free to move around medicines and total parenteral - Inhaler (high kinetic energy) nutrition (TPN), which is an Polyphasic – adjusting phases integral part of therapeutic Eutexia – absorb heat (liquefy) options available to hospitalized patients. SUBLIMATION – solid to gas MELTING – solid to liquid A. SOLUBILITY OF SOLIDS IN WATER FREEZING – liquid to solid Liquid crystalline state – in between - Solubility is defined liquid in quantitative terms as the concentration of solute in a Solvates – pseudomolymorphs saturated solution at a certain Enantiotropic – reverse direction temperature, and in a qualitative Monotropic – one direction only way, it can be defined as the spontaneous interaction of two or more substances to form a homogeneous molecular dispersion. The boiling point of liquids and the melting point of solids both reflect the strengths of interactions between the molecules in the pure liquid or the solid state.
- In general, aqueous solubility decreases with increasing boiling point and melting point.