Issue 20: SEP 2010
Reduce friability and improve tablet performance during stability studies with a combination of Fujicalin® and Neusilin® Greetings! Making high quality tablets of acetaminophen can be a big challenge due to its high cohesive property. During mixing, acetaminophen tends to segregate easily causing problems of low content uniformity. Choosing an excipient which has high flowability, high compressibility, high tablet hardness, low friability with appropriate bulk density is an efficient strategy to solve the problem. Fujicalin® a directly compressible (DC) excipient which meets all above requirements is one of good choice for formulators in comparison with other DC excipients such as lactose which has poor flowability or mannitol which gives high tablet hardness but high friability. In this newsletter, we introduce a new study by Asai et al. 2009 where Fujicalin® and Neusilin® in combination reduce friability and maintain tablet hardness during accelerated stability tests of tablets with 30% of acetaminophen. As reported in the previous newsletter, Issue No. 19, June 2010, in this study, 2% of Neusilin UFL2 was used to improve hardness and protect the acetaminophen tablets from deterioration by moisture under humid conditions. Investigated formulations are shown in Table 1. The batch size of formulation was set at 1000 tablets (150 g). The materials were placed in a polyethylene bag and mixed thoroughly. Tablets were produced by single punch tabletting machine (N-30EX model, Okada Seiko Co., Ltd.; Ф7.0 mm, 700 kgf). Tablet properties including weight, thickness and hardness were measured using 10, 5, and 5 tablets respectively. The dissolution test was carried out by the paddle method (50 rpm), using 3 tablets in 900 ml of water. The dissolution rate was measured at wavelength of 244 nm. Table 1: Investigated formulations
Tablet properties and dissolution profiles are shown in Table 2. All formulations showed very good tablet properties with friability under 0.1%, and tablet hardness above 50 N. The dissolution rate of formulation #1 was 83.5% which fell slightly lower than the target range of standard pharmaceutical formulations (85% or more in 15 minutes). However, by increasing L-HPC LH-B1 from 5% to 10%, or adding 2% of SDS, dissolution rate could increase to 92.3% and 98.5% (Table 2, formulation #2 and #3). Table 2: Tablet properties and dissolution profiles
Next, the accelerated stability tests and stability test at room temperature were performed for a period of one month with 30 tablets in high-density polyethylene (HDPE) bottles (sealed or open). The tablet hardness in formulation #1, #2, and #3 slightly decreased but remained above 50 N (Fig. 1). As reported in the previous newsletter, Neusilin® UFL2 helped maintain tablet hardness of these formulations. Finally, dissolution rates remained above 85% in all test conditions by increasing disintegrant from 5% to 10% or adding 2% of SDS in formulation #2 and #3 (Fig. 1). Fig. 1 Hardness and dissolution profiles of tablets stored under humid conditions for one month
Conclusions: 1. With high API loaded tablets (30% of acetaminophen), Fujicalin® demonstrated improvement of tablet properties in formulation with 2% of Neusilin® UFL2. 2. Dissolution profiles improved by adding 2% of SDS and 5% of L-HPC LB-1 or by increasing L-HPC LB-1 to 10% in formulations with Fujicalin. Reference: Asai Y, Nohara M, Fujioka S, Isaji K, Nagira S. Application of Neusilin UFL2 on manufacturing of tablets using direct compression method, Development of core tablets containing the function of small degree of decrease of hardness at the humid conditions. Pharm Tech Japan. 2009; 25: 67-70.
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[email protected] to your address book. The information found in this publication is presented in good faith with no guarantee or obligation as to accuracy and no assumption of liability. Users should make their own tests to determine the suitability of these products for their own particular purposes. However, because of numerous factors affecting results, Fuji Chemical Industry makes no warranty of any kind, express or implied, including those of merchantability and fitness for particular purpose other than the material conforms to its applicable current standard specifications. Statements concerning the use of the products or formulations described herein are not to be construed as recommending the infringement of any patent and seller assumes no liability for the infringement arising out of such use.
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