Directly compressible formulation of immediate release rosuvastatin calcium tablets stabilized with tribasic calcium phosphate
Reliable and stable tablet formulations for rosuvastatin calcium in four strengths: 5 mg, 10 mg, 20 mg and 40 mg have been developed. Rosuvastatin is a cholesterol-lowering statin drug and is known to be unstable during storage. The possibility of its stabilization with inorganic salts of multivalent metals has already been reported in the literature. In the present study, a special grade of tribasic calcium phosphate excipient was used to chemically stabilize rosuvastatin calcium in a directly compressible immediate release tablet formulation. The developed tablets exhibited good mechanical properties (breaking force ranging from 177 N to 250 N depending on tablet strength), rapid disintegration (less than 3 minutes) and fast dissolution rate (85% of the drug substance dissolved within 15 minutes) as well as satisfactory chemical stability during storage under stress conditions (50 °C/80% RH), even compared to the reference commercial product.
About this article: Daniel Zakowiecki, Tobias Hess, Krzysztof Cal, Barbara Mikolaszek, Grzegorz Garbacz & Dorota Haznar-Garbacz (2022) Directly compressible formulation of immediate release rosuvastatin calcium tablets stabilized with tribasic calcium phosphate, Pharmaceutical Development and Technology, DOI: 10.1080/10837450.2022.2073370
About Calcium Phosphates by Chemische Werke Budenheim
Budenheim offers a wide range of excipients for the production of solid oral dosage forms. DI-CAFOS® and TRI-CAFOS® excipients have been optimized for the use in efficient pharmaceutical production processes, especially for direct compression, dry and wet processes. A high batch-to-batch consistency of Budenheim s products ensures robust drug manufacturing processes, adding value to your overall productivity and efficiency.
Excellent tableting properties, particularly high tablet strength and faster disintegration, can be achieved using our excipients. The targeted use of our products also helps to overcome many typical challenges formulation developers face today: From an enhancement of the powder flow due to poor flowing active pharmaceutical ingredients (API’s) to overcoming process or equipment setup limitations, an increase of the chemical and physical stability of the formulation (e. g. when processing pH- or moisture sensitive API’s) to an improvement of re-compactability in dry granulation processes.
Budenheim excipients also are the basis for many new solution approaches: By facilitating the manufacturing of lactose-free formulations or of reduced tablet sizes, by increasing efficiency in liquid-to-solid processes and by providing a unique starting material for multiparticulate formulations.
Calcium Phosphates by Chemische Werke Budenheim
| Application | Brandname | Chemical name | Compliance to |
|---|---|---|---|
| Direct compression | DI-CAFOS® A 150 | Dicalcium phosphate anydrous | USP, Ph. Eur., JP |
| Direct compression | DI-CAFOS® D 160 | Dicalcium phosphate dihydrate | USP, Ph. Eur., JP |
| Direct compression | DI-CAFOS® A 60 | Dicalcium phosphate anydrous | USP, Ph. Eur., JP |
| Direct compression | TRI-CAFOS® 500 | Tricalcium phopshate | NF, Ph. Eur |
| Granulation | DI-CAFOS® A 12 | Dicalcium phosphate anydrous | USP, Ph. Eur., JP |
| Granulation | DI-CAFOS® D 14 | Dicalcium phosphate dihydrate | USP, Ph. Eur., JP |
| Granulation | Tri-CAFOS® 250 | Tricalcium phopshate | NF, Ph. Eur |
| Glidant | Tri-CAFOS® 200-7 | Tricalcium phopshate | NF, Ph. Eur |