Preparation of Vitamin E tablets with Fujicalin® and Comparison with other commercially available DCPA's

Welcome. This issue of Fuji's newsletter presents preparation of vitamin E tablets with Fujicalin® and comparison with other commercially available DCPA's.

Vitamin E is a fat soluble vitamin like A, D and K. It is oily in physical appearance and exists either in the form of tocopherols or tocotreinols. Vitamin E is primarily found in vegetable oils and is a powerful antioxidant that have been associated with many health benefits from prevention of cardiovascular disease to cancer. The recommended daily allowance (RDA) is 10-15 mg for adults and to ensure we obtain them, supplementation is recommended.

Converting vegetable oils rich in vitamin E into a free flowing powder which can be processed into capsules or tablets provides advantages to both manufacturers and consumers alike. However, the amount of oily materials that can be adsorbed on to a carrier is generally low making it difficult to produce directly compressible tablets with optimum load. Silicates and other ingredients such as microcrystalline cellulose, maltodextrin have been recommended for oil adsorption. The oil loading capacities of these excipients are comparatively low, affecting flowability, compactability and compressibility of tablets.

Fuji Chemical offers a unique excipient, Fujicalin®, an anhydrous form of dibasic calcium phosphate (DCPA), to develop free flowing powders of oily actives that has excellent tablettability. Fujicalin® is ideal for both pharmaceutical and nutraceutical applications and it is categorized as a Generally Recognized as Safe (GRAS) material. In this newsletter, we compare the vitamin E adsorbent properties and tablettability of Fujicalin® to that of other available DCPA's.

Figure 1. SEM Photomicrographs of Fujicalin® and other DCPA's from USA, Europe and Japan

Thanks to spray dry technology, Fujicalin® particles have a very smooth surface leading to less abrasion (wear and tear) and longer life of tabletting equipment.

Oil to Powder- Vitamin E example:
Fig2

12.5 g of tocopherol acetate (Vitamin E) was diluted with the same amount of ethanol and mixed well before loading on to 83.5 g Fujicalin® or other available grades of DCPA. The mixture was dried in an oven at 50°C overnight. Three grams of Croscarmellose Sodium (disintegrant) and 1 g Mg-stearate (lubricant) was added to the formulation and the mixture was sieved through a 30 mesh screen. Tabletting was carried out in a single punch tabletting machine (Sankyo Piotech) at 5, 10 and 15 kN.

High quality vitamin E tablets with sufficient hardness (80-100N) were possible with Fujicalin® at compression forces as low as 2-5 kN. On the other hand, other DCPA's produced softer tablets at compression forces up to 15 kN. The maximum hardness achieved with a vitamin E load for DCPA1 (US Grade) was 79 N while other DCPA's tested showed much lower values (Figure 2). Fujicalin® has a distinct advantage over other DCPA's in converting oily actives into free flowing powders. This is further established by examining the Carr index after loading vitamin E at 12.5% (Table 1). Sticking to dies and punches and oil extrusions were additional problems observed during tabletting with DCPA's other than Fujicalin®.

Table 1. Physical parameters including Carr index of DCPA powders after 12.5% vitamin E load

Values in parenthesis () shows initial value
DCPA 2 (JP Grade) could not be measured after vitamin E loading.

Conclusions:
Fujicalin® is spherically granulated, has lower mean particle size and extremely high specific surface area when compared to other available DCPA and Dibasic Calcium Phosphate Dihydrate (DCPD). Among the DCPA's tested, Fujicalin® showed superior tabletting properties after vitamin E adsorption. Fujicalin® was the best performer giving highest tablet hardness at low compression forces. Superior Carr index values validate the efficiency of Fujicalin® in converting oily actives into a free flowing powder with excellent tabletting properties. Compact, thin vitamin E tablets with recommended daily allowance are clearly possible when Fujicalin® is used as an excipient.

Dosage and Safety:
Fujicalin® is manufactured under strict quality control at our FDA-GMP certified facilities. Dibasic calcium phosphate anhydrous is widely used in oral pharmaceutical products and food products. It is generally regarded as relatively nontoxic and nonirritant material.

Fujicalin®:

Chemical formula : CaHPO4
Chemical Abstract Service (CAS) Number: 7757-93-9
U.S. Patent No. 5,486,365, Jan 1996
U.S. Drug Master File (DMF) filed, Conforms to USP/NF, EP and JP; and listed as GRAS

Fujicalin is a trademark or registered trademark of Fuji Chemical Industry Co., Ltd in Japan, United States of America, Europe and/or other countries.

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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.