Conquering Formulation Issues

How does the pharmaceutical globe meet the problem with the ever-increasing tempo in pharmaceutical item improvement? 1 quick way answer for formulators would be to use high-performing excipients. The altering landscape with the medicine industry is rising the industrial stress on R&D groups to shorten time to market for new items. Consequently, formulators are demanding more functionality and performance from their pharmaceutical excipients. These ingredients now play a critical role in achieving stability, reducing costs and improving manufacturing efficiencies. They must also produce a robust dosage form that is unaffected by variations in process parameters or other ingredients. Faced with shorter improvement cycles and more complex active pharmaceutical ingredient(APIs), formulators cannot afford the luxury of investigating new excipients. They need to make use of proven ingredients in the growth and development of new tablets or capsules, and rely heavily on the producers of these ingredients to identify new applications. Enhancing drug formulation Multi-functional excipient items have been shown to offer unique synergies with many common ingredients. For instance, combining Starch 1500 ???¡ì?C a partially pregelatinized maize starch from Colorcon? ???¡ì?C with microcrystalline cellulose leads to extremely compactable formulations with excellent dissolution. This minimizes the need for super-disintegrants that can affect stability. The flow properties and friability of lactose blends can also be greatly improved. Furthermore, incorporating specially designed pregelatinized starch items can help to eliminate the quantity of lubricants, which are known to cause over-blending problems, and affect dissolution and film coating quality. As APIs become more sophisticated, most of them are efficient at low-dose concentrations and are often micronized. But low-dose medicines can be a problem to formulate due to problems with content uniformity and physical stability. Traditionally, these drugs have been manufactured through wet granulation to assure that each tablet contains the proper quantity of active pharmaceutical ingredient material. This process can, nevertheless, be costly and time-consuming due to the many steps involved. If water has a detrimental effect on the drug, solvents should be used ?a therefore rising the cost and difficulty with the process. Pharmaceutical formulators have developed direct compression manufacturing processes for these drugs through the use of Starch 1500. Content uniformity is achieved by first preparing a pre-blend with the API and Starch 1500, followed by the addition with the remaining ingredients and tabletting. The granular morphology of this unique excipient combined with its inherent moisture content produces an ordered mix through adhesion and hydrogen bonding. Humidity control Moisture-sensitive drugs present another problem to formulators. Potential problems associated with these APIs include reduced flow properties, as well as changes in dissolution rates, chemical stability and physical stability (when it comes to color, for instance). Some methods to protect moisture sensitive items involve humidity-controlled manufacturing conditions, protective packaging, moisture barrier film coating and, most importantly, selecting excipients that minimise moisture sensitivity. In this selection process, it's important to comprehend the difference between moisture content and water activity. Total moisture content is, typically, measured by loss on drying. Nevertheless, this method does not distinguish between bound moisture (unavailable for chemical interactions) and unbound moisture (available for chemical interactions). A better measure is water activity or equilibrium relative humidity, which shows only the unbound water that is free to have an interaction with the drug. For instance, although the moisture content of Starch 1500 is higher than some other excipients', the water content is considerably lower. Therefore, it will equilibrate slower when subjected to moisture conditions and may, preferentially, bind the moisture, preventing interaction using the drug. Starch 1500 has been used to develop formulations with proven stability for many moisture-sensitive APIs, including aspirin and ranitidine. These robust formulations have helped lower costs by reducing the need for special manufacturing conditions and expensive packaging. As formulators turn to proven excipients to meet today's challenges, multi-functional excipients such as Starch 1500 offer a long history of reliability and efficacy, and still provide benefits in the growth and development of new applications. About Colorcon? Colorcon? is a globe leader in the improvement, supply and technical support of formulated coatings and excipients for the medicine industry. With Colorcon as their pharmaceutical item development" partner, corporations produce cost efficient, top quality items with superior performance and appearance. To learn more, please visit www.novachems.com