Active pharmaceutical ingredient dissolution rate

Drug formulating in nanosuspension form enhances the saturable concentration of active pharmaceutical ingredients, dissolution rate as well as bioavailability of the dmg. 

The BCS is a scientific framework for classifying active pharmaceutical ingredients based upon their aqueous solubility and intestinal permeabihty. When combined with the dissolution of the pharmaceutical product, the BCS takes into account three major factors that govern the rate and extent of drug absorption (exposure) from immediate-release oral solid dosage forms dissolution, solubility, and intestinal permeability. 

Blagden, N. de Matas, M. Gavan, P.T. York, P. Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates. Adv. Drug Deliv. Rev. 2007, 59(7), 617-630. 

Nagy, Z.K. Sauceau, M. Nyul, K. Rodier, E. Vajna, B. Marosi, G. Pages, J. Use of supercritical COj-aided and conventional melt extrnsion for enhancing the dissolution rate of an active pharmaceutical ingredient. Polym. Adv. Technol. 2012, 23(5), 909-918. 

Polymorphism plays a crucial role in the preparation of active pharmaceutical ingredients (APIs), and the possibility to predict and control the crystallization of a specific polymorph is today of great interest for many applications in the pharmaceutical industry. Although identical in their chanical composition, different polymorphs often exhibit important differences in solnbility, dissolution rate, stability, melting point, density, and many other properties that significantly affect the efficacy, bioavailability, and safety of APIs (Llinas and Goodman 2008). 

The previous chapters of this book should have convinced the reader of the great potential of co-crystalhsing active pharmaceutical ingredients (APIs) with pharmaceutically acceptable co-crystal formers. The resulting pharmaceutical co-crystals potentially improve the physical properties (solubility, dissolution rate, melting point, etc.) of the final products. ... 

Another major ion chromatography application is the analysis of active ingredient counterions. Frequently, drug substances are formulated as salts in order to achieve specific pharmaceutical properties (such as improved solubility or control of dissolution rate). The analysis of... 

In the pharmaceutical industry, it is important that aU products are properly tested and vahdated prior to release for sale. One of the most important tests is the determination of tablet dissolution rate. In this procedure tablets are immersed in a suitable medium to mimic the action of the stomach and the release of the active ingredients monitored over a period of time. Automation of these procedures is obviously important for various reasons including cost, accuracy of analysis and for validation of the results according to good laboratory practice. 

Dissolution rate shall be included as a requirement for batch relecise to ensure batch to batch quality/pharmaceutical availability/bioequivalence, for all products containing one or more active ingredients where such a requirement forms part of the final product specification. Application may be made for proposed intervals of dissolution rate testing as criteria for batch release if adequate statistically processed validation data are available and submitted. This applies only to standard production lot sizes that have been validated. The proposed frequency of dissolution testing must be based on the validation results and the following factors ... 

In order to achieve appropriate levels of solubilization, dissolution rate and potentially supersaturation, excipients are required (Rowe et al., 2006 International Pharmaceutical Excipients Council 2006). Excipients are components of dosage forms which are included for a variety of reasons and are usually not directly associated with the pharmacological activity of the selected drug substance. Historically, excipients have comprised ingredients e.g., to mask or... 

Correlation of in vitro rate of dissolution with in vivo absorption is a topic of significant interest to the pharmaceutical industry because it is a means of assuring the bioavailability of active ingredient(s) from a dosage form. Once such a correlation has been established, quantitative predictions regarding the absorption of drug... 

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