Formulation stability

Chemical Reactivity - Reactivity with Water Reacts vigorously with water to form highly flammable acetylene gas which can spontaneously ignite Reactivity with Common Materials Reacts with copper and brass to form an explosive formulation Stability During Transport Stable but in absence of water Neutralizing Agents for Acids and Caustics Not pertinent Polymerization Not pertinent Inhibitor of Polymerization Not pertinent. 

The most thermodynamically stable polymorph is usually desired for the API product to maximize its formulated stability. Selecting the thermodynamically stable form does however, have the disadvantage of minimizing the solubility and bioavailability. Although less desirable and common it is feasible to use an amorphous solid form of the API if it can be demonstrated that it is stable in the formulation. 

Drug development work also includes formulation, stability studies, and selection of drug delivery systems, as discussed in Section 5.6. Once the API has been prepared, excipients are added ... 

Intraliposomal Trapping Agents for Improving In Vivo Liposomal Drug Formulation Stability... 

Uses Rocket fuel formulations stabilizer for organic peroxide fuel additives absorbent for acid gases plant control agent photography in organic synthesis. 

After scale-up into production, it was determined that an increase in moisture content would improve the formulation stability for a high dose wet granulated product. It was decided to use the Presster to predict the results that would be obtained in production when the moisture content of the final blend was increased. Blends with three moisture levels were compressed at two forces. As shown in Figure 5, as moisture content increases, tablet hardness increased. The dissolution profiles for the tablets with different moisture levels were compared and found to be within specification, indicating that raising the moisture content in the final blend should result in acceptable tablets in production. 

The presence of polysulfonates in petroleum sulfonates used in lube formulations has a destabilizing effect on the formulation stability and function of the sulfonate in motor oils, etc. Special techniques are utilized to help reduce the carryover of residual sludge components, including the use of hydrocarbon solvents such as hexane or heptane to facilitate separation of sludge, often with centrifugation. Other desludging procedures include water wash, H2S04 wash, clay percolation, and filtration. 

Even when there are no ionizable groups present for the excipient or API, the pH of a formulation may also play an important role in the formulation stability. For example, a specific functional group or a particular resonance structure that is stabilized in a specific pH range may facilitate a reaction between the excipient and the drug. Because of additional freedom of movement and rotation in solution, these types of interactions cannot be completely ignored. 

Certain processes in a material are accelerated by increasing the temperature, such as phase separation in emulsions. A convenient way of predicting formulation stability is to run a temperature sweep and observe the response of G or tan(8). Samples that are stable will tend to show almost no major change in these parameters, whereas unstable materials will change sharply at a critical temperature. Figure H3.1.10 shows comparative data for four emulsions that are divisible into two pairs one pair that is likely to be stable and another that is... 

As a result of these unique delivery routes, there is an increased potential for toxicity to tissues at or near the injection site. Assessment of local tolerance and tissue compatibility of the clinical formulation is usually evaluated as part of the animal model of efficacy and/or general toxicity study, thus obviating the need for separate local tolerance studies. There may be additional concerns in cases where analogous products are used including potential differences in formulation, stability, and so forth. 

In order to achieve a sustained drug release and a prolonged therapeutic activity, nanoparticles must be retained in the cul-de-sac and the entrapped drug must be released from the particles at a certain rate. If the release is too fast, there is no sustained release effect. If it is too slow, the concentration of the drug in the tears might be too low to achieve penetration into the ocular tissues [208]. The major limiting issues for the development of nanoparticles include the control of particle size and drug release rate as well as the formulation stability. 

Data acquired via this system permits accurate and reproducible evaluations of relative formulation stability performance after 0.5-3 months of... 

Poor Formulation Stability for Macromolecules existing aerosol systems are not designed to protect the formulations of delicate macromolecules. 

In a metered dose inhaler, where fine drug particles are suspended in a propellent, stability and aggregation of the suspension are crucial for the performance of the inhaler. In an investigation into the aerosol formulation stability. Span 80 was added to a suspension of lactose to study the effect on deaggregation under shear.f An increase in shear stress was found to decrease aggregate size and boundary fractal dimension (Fig. 9), which was interpreted as a more compact aggregate. 

Pharmacokinetic proteomics (ADME analysis, formulation, stability studies, and pharmacokinetics). 

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