| How does the pharmaceutical world meet the | | | | drug, solvents must be used — thus increasing |
| challenge of the ever-increasing pace in | | | | the cost and difficulty of the process. |
| pharmaceutical product development? One | | | | Pharmaceutical formulators have developed direct |
| shortcut solution for formulators is to use | | | | compression manufacturing processes for these |
| high-performing excipients. | | | | drugs through the use of Starch 1500. Content |
| The changing landscape of the pharmaceutical | | | | uniformity is achieved by first preparing a |
| industry is increasing the commercial pressure on | | | | pre-blend of the API and Starch 1500, followed by |
| R&D groups to shorten time to market for new | | | | the addition of the remaining ingredients and |
| products. As a result, formulators are demanding | | | | tabletting. The granular morphology of this unique |
| more functionality and performance from their | | | | excipient combined with its inherent moisture |
| pharmaceutical excipients. These ingredients now | | | | content produces an ordered mix through |
| play a critical role in achieving stability, reducing | | | | adhesion and hydrogen bonding. |
| costs and improving manufacturing efficiencies. | | | | Humidity control |
| They must also produce a robust dosage form | | | | Moisture-sensitive drugs present another challenge |
| that is unaffected by variations in process | | | | to formulators. Potential problems associated with |
| parameters or other ingredients. | | | | these APIs include reduced flow properties, as |
| Faced with shorter development cycles and more | | | | well as changes in dissolution rates, chemical |
| complex active pharmaceutical ingredients (APIs), | | | | stability and physical stability (in terms of color, for |
| formulators cannot afford the luxury of | | | | example). Some ways to protect moisture |
| investigating new excipients. They need to use | | | | sensitive products involve humidity-controlled |
| proven ingredients in the development of new | | | | manufacturing conditions, protective packaging, |
| tablets or capsules, and rely heavily on the | | | | moisture barrier film coating and, most |
| producers of these ingredients to identify new | | | | importantly, selecting excipients that minimize |
| applications. | | | | moisture sensitivity. In this selection process, it is |
| Enhancing drug formulation | | | | important to understand the difference between |
| Multi-functional excipient products have been | | | | moisture content and water activity. |
| shown to offer unique synergies with many | | | | Total moisture content is, typically, measured by |
| common ingredients. For example, combining | | | | loss on drying. However, this method does not |
| Starch 1500 – a partially pregelatinized maize | | | | distinguish between bound moisture (unavailable |
| starch from Colorcon® – with | | | | for chemical interactions) and unbound moisture |
| microcrystalline cellulose results in very | | | | (available for chemical interactions). A better |
| compactable formulations with excellent dissolution. | | | | measure is water activity or equilibrium relative |
| This minimizes the need for super-disintegrants | | | | humidity, which shows only the unbound water |
| that can affect stability. The flow properties and | | | | that is free to interact with the drug. |
| friability of lactose blends can also be greatly | | | | For example, although the moisture content of |
| improved. Moreover, incorporating specially | | | | Starch 1500 is higher than some other excipients', |
| designed pregelatinized starch products can | | | | the water content is considerably lower. |
| reduce the amount of lubricants, which are known | | | | Therefore, it will equilibrate slower when exposed |
| to cause over-blending problems, and affect | | | | to moisture conditions and may, preferentially, |
| dissolution and film coating quality. | | | | bind the moisture, preventing interaction with the |
| As APIs become more sophisticated, many of | | | | drug. Starch 1500 has been used to develop |
| them are effective at low-dose concentrations | | | | formulations with proven stability for many |
| and are often micronized. But low-dose medicines | | | | moisture-sensitive APIs, including aspirin and |
| can be a challenge to formulate due to problems | | | | ranitidine. These robust formulations have helped |
| with content uniformity and physical stability. | | | | lower costs by reducing the need for special |
| Traditionally, these drugs have been manufactured | | | | manufacturing conditions and expensive packaging. |
| through wet granulation to assure that each tablet | | | | As formulators turn to proven excipients to meet |
| contains the proper amount of active material. | | | | today's challenges, multi-functional excipients such |
| This process can, however, be costly and | | | | as Starch 1500 offer a long history of reliability |
| time-consuming because of the many steps | | | | and efficacy, and continue to provide benefits in |
| involved. If water has a detrimental effect on the | | | | the development of new applications. |