Tablets & Capsules


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V Tablets & Capsules September 2017 33 dosage forms Hot-melt coating: A method for creating user-friendly, extended-release formulations Martin Koeberle and Detlev Haack Hermes Pharma In the treatment of many medical conditions and diseases, it is advantageous for the active pharmaceutical ingredient (API) to release gradually from the dosage form over a prolonged period. This article looks at how hot-melt coating was used to develop an effective and user-friendly extended-release formulation for vitamin C. itamin C (also known as ascorbic acid) is essential for a healthy life, yet for many individuals, the amount sup- plied in food is insufficient to meet their needs. Smokers, pregnant and nursing mothers, and people with acute infectious diseases may all have an increased risk of vita- min C deficiency. As a result, a large number of people take vitamin C supplements to boost levels in the body. But to be effec- tive, dosing must be carefully regulated. Due to its water solubility, the body cannot build reservoirs of vitamin C. If administered in a large single dose, such as in an imme- diate-release formulation at the beginning of each day, the amount that cannot be absorbed by the body will simply be excreted. During the day, the need for vitamin C may increase, resulting in a deficiency of this essential nutrient. One way to ensure the body receives a regular supply of vitamin C is by taking conventional immediate-release doses throughout the day. However, this can be inconve- nient, leading to poor patient adherence to the treatment regimen. And with people increasingly used to enjoying convenience in all areas of their lives, this option simply doesn't meet consumer expectations. So how do we develop a formulation that offers con- venience for patients and consumers yet ensures effective delivery of the active ingredient? Extended release: A product development challenge Time and again, pharmaceutical and nutraceutical companies are faced with a similar problem—the need to develop a single dosage form that produces a constant blood plasma concentration at an effective level over a prolonged period. Often, the solution is an extended- release formulation that delivers the API to the body slowly, overcoming the need for patients or consumers to take multiple doses throughout the day. In many cases, including the example in Figure 1, a single dose of an extended-release formulation taken at the start of the day successfully achieves sustained blood plasma concentrations at levels that would otherwise require several immediate-release doses. Figure 1 Plasma profiles of extended- and immediate-release formulations 500 400 300 200 100 0 0 4 8 12 16 20 24 Plasma concentration (ng/ml) Time (h) 1 st tablet 2 nd tablet 3 rd tablet Extended -release formulation, 200 mg Immediate -release formulation, 50 mg 4 th tablet

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