Orodispersible dosage unit containing an estetrol component
AssigneeEstetra Srl
InventorsSéverine Francine Isabelle Jaspart, Johannes Jan Platteeuw, Denny Johan Marijn Van Den Heuvel
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Abstract
An orodispersible solid pharmaceutical dosage unit of estetrol is disclosed. The solid dosage unit is easy to manufacture and suited for sublingual, buccal or sublabial administration. The orodispersible solid pharmaceutical dosage unit can include at least 100 μg of an estetrol component and pharmaceutically acceptable excipients. Methods of manufacturing the orodispersible solid pharmaceutical dosage unit are also disclosed.
Claims16
A solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, the dosage unit comprising:
- (a) 0.1-25 wt. % of estetrol particles containing at least 90 wt. % of estetrol monohydrate, wherein the estetrol particles have a volume median diameter of from 5 μm to 15 μm;
- and
- (b) 75-99.9 wt. % of one or more pharmaceutically acceptable excipients;
- wherein the solid dosage unit contains from 10 mg to 20 mg of the estetrol monohydrate and releases at least 70% of the estetrol monohydrate within 5 minutes when subject to dissolution testing by placing one unit in 900 mL of an aqueous dissolution medium comprising KH2PO4 and NaOH at pH 6.8 and a temperature of 37±0.5° C., in a vessel of a paddle apparatus at a stirring speed of 50 rpm.
A process of preparing an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, the dosage unit comprising:
- (a) 0.1-25 wt. % of estetrol particles containing at least 90 wt. % of estetrol monohydrate;
- and
- (b) 75-99.9 wt. % of one or more pharmaceutically acceptable excipients;
- wherein the solid dosage unit contains from 10 mg to 20 mg of the estetrol monohydrate, the process comprising:
- (i) providing estetrol particles having a volume median diameter between 2 μm to 50 μm and containing at least 90 wt. % of estetrol monohydrate;
- (ii) mixing 1 part by weight of the estetrol particles with 2-1,000 parts by weight of one or more pharmaceutically acceptable excipients to obtain a dry blend;
- and
- (iii) compressing the dry blend into a solid dosage unit.
Dependencies are inferred from the claim text.