Abstract: The present disclosure provides pharmaceutical compositions comprising thiotepa and one selected from PEG, such as PEG400 or PEG600, and DMSO, and optionally water or an aqueous saline solution and thiosulfate. The composition is free or substantially free of impurities. Also provided is a method for treating cancer in a subject, or myeloablation prior to bone marrow transplantation using the composition. A method for enhancing the stability of a thiotepa formulation is also contemplated.

Abstract: The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of: 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt. % of one or more pharmaceutically acceptable ingredients; the solid dosage unit comprising at least 100 ?g of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 ?m to 50 ?m. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

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 ?g of an estetrol component and pharmaceutically acceptable excipients. Methods of manufacturing the orodispersible solid pharmaceutical dosage unit are also disclosed.

Abstract: The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of: 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt. % of one or more pharmaceutically acceptable ingredients; the solid dosage unit comprising at least 100 ?g of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 ?m to 50 ?m. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

Abstract: The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of: 0.1-25 wt.% of estetrol particles containing at least 80 wt.% of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt.% of one or more pharmaceutically acceptable ingredients; the solid dosage unit comprising at least 100 µg of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 µm to 50 µm. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

Abstract: The present disclosure provides pharmaceutical compositions comprising thiotepa and one selected from PEG, such as PEG400 or PEG600, and DMSO, and optionally water or an aqueous saline solution and thiosulfate. The composition is free or substantially free of impurities. Also provided is a method for treating cancer in a subject, or myeloablation prior to bone marrow transplantation using the composition. A method for enhancing the stability of a thiotepa formulation is also contemplated.

Abstract: The present disclosure provides pharmaceutical compositions comprising thiotepa and one selected from PEG, such as PEG400 or PEG600, and DMSO, and optionally water or an aqueous saline solution and thiosulfate. The composition is free or substantially free of impurities. Also provided is a method for treating cancer in a subject, or myeloablation prior to bone marrow transplantation using the composition. A method for enhancing the stability of a thiotepa formulation is also contemplated.

Abstract: The present invention relates to tablet dosage formulations of oleyl phosphocholine for oral administration and the processes for their preparation. Specifically, the present invention provides a process for preparing an oleyl phosphocholine containing granulate, said process comprising a blending step, a hot melt agglomeration step and a milling step. The present invention further provides a process for preparing a tablet comprising the oleyl phosphocholine containing granulate, said process comprising the step of preparing an OIPC containing granulate according to the invention, a blending step, a compression step, and optionally a coating step. The invention further provides any intermediate and/or en product resulting from these steps and processes.

Abstract: The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of: 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt. % of one or more pharmaceutically acceptable ingredients; the solid dosage unit comprising at least 100 ?g of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 ?m to 50 ?m. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

Abstract: The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit consisting of: 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt. % of one or more pharmaceutically acceptable ingredients; the solid dosage unit comprising at least 100 ?g of the estetrol component; and wherein the solid dosage unit can be obtained by a process comprising wet granulation of estetrol particles having a volume weighted average particle size of 2 ?m to 50 ?m. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

Abstract: The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit containing at least 100 ?g of an estetrol component selected from estetrol, estetrol esters and combinations thereof; wherein the solid dosage unit can be obtained by a process that comprises: providing a loading liquid comprising organic solvent; estetrol component and optionally one or more other pharmaceutically acceptable ingredients; mixing 1 part by weight of the loading liquid with 0.5-20 parts by weight of carrier particles to produce wet particles; removing organic solvent from the wet particles to produce loaded particles; optionally mixing the loaded particles with one or more tabletting excipients; and forming the loaded particles or the mixture of the loaded particles and the one or more tabletting excipients into a solid dosage unit. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

Abstract: The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit containing at least 100 ?g of an estetrol component selected from estetrol, estetrol esters and combinations thereof; wherein the solid dosage unit can be obtained by a process comprising: ?providing an aqueous liquid comprising water, estetrol component and optionally one or more other pharmaceutically acceptable ingredients; ?mixing 1 part by weight of the aqueous liquid with 0.5-20 parts by weight of the carrier particles to produce wet particles; ?removing water from the wet particles to produce loaded particles; ?optionally mixing the loaded particles with one or more tabletting excipients; and ?forming the loaded particles or the mixture of loaded particles and the one or more tabletting excipients into a solid dosage unit. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

Abstract: The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 17?-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is —Si(R2)3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10), 15-tetraen-17-one, in which A is a protecting group, via silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, and B is —Si(R2)3.

Abstract: The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit comprising: 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and 75-99.9 wt. % of one or more pharmaceutically acceptable excipients; the solid dosage unit comprising at least 100 ?g of the estetrol component; and wherein the solid dosage unit can be obtained by a process that comprises compressing a dry blend of estetrol particles and one or more pharmaceutically acceptable excipients into a solid dosage unit. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.

Abstract: An orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg is disclosed. The dosage unit comprises (a) 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and (b) 75-99.9 wt. % of one or more pharmaceutically acceptable excipients. The solid dosage unit comprises at least 100 ?g of the estetrol component and can be obtained by a process that comprises compressing a dry blend of estetrol particles and one or more pharmaceutically acceptable excipients into a solid dosage unit. The solid dosage unit is easy to manufacture and suited for sublingual, buccal or sublabial administration.

Abstract: The present invention provides an orally disintegrating solid pharmaceutical dosage unit having a weight between 50 and 1,000 mg, said dosage unit consisting of: 1-100 wt. % of particles consisting of: 0.01-10 wt. % of a partus control substance selected from oxytocin, carbetocin, atosiban and combinations thereof; 5-70 wt. % of buffering agent; 20-94 wt. % of branched glucan; 0-70 wt. % of other pharmaceutically acceptable ingredients; 0-95 wt. % of one or more pharmaceutically acceptable excipients; the solid dosage unit comprising at least 5 ?g of the partus control substance and having a pH buffer range of 3.5-5.7. The solid dosage unit of the present invention is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration. Furthermore, the dosage unit does not need to be stored and distributed under temperature controlled conditions.

Abstract: An orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg is disclosed. The dosage unit comprises (a) 0.1-25 wt. % of estetrol particles containing at least 80 wt. % of an estetrol component selected from estetrol, estetrol esters and combinations thereof; and (b) 75-99.9 wt. % of one or more pharmaceutically acceptable excipients. The solid dosage unit comprises at least 100 ?g of the estetrol component and can be obtained by a process that comprises compressing a dry blend of estetrol particles and one or more pharmaceutically acceptable excipients into a solid dosage unit. The solid dosage unit is easy to manufacture and suited for sublingual, buccal or sublabial administration.

Abstract: The present invention relates to a tablet having a weight of 30-200 mg and consisting of: 60-100 wt. % of granules consisting of: 50-90% by weight of the granules of dehydroepiandrosterone (DHEA); 6-35% by weight of the granules of microcrystalline cellulose; 0-20% by weight of the granules of one or more other pharmaceutically acceptable granule ingredients; and 0-40 wt. % of one or more other pharmaceutically acceptable tablet components. These tablets can suitably be used to orally administer DHEA in dosages of around 50 mg and are sufficiently small to be incorporated in, for instance, ordinary oral contraceptive blister packs.

Abstract: An orally disintegrating solid pharmaceutical dosage unit having a weight between 50 and 1,000 mg is disclosed. The dosage unit consists of: (a) 5-100 wt. % of coated particles comprising 50-99 wt. % of a core particle and 1-50 wt. % of a coating that envelops the core particle, said coating consisting of: 0.01-10 wt. % of a partus control substance selected from oxytocin, carbetocin, atosiban and combinations thereof; 5-50 wt. % of buffering agent; 15-80 wt. % of branched glucan; 0-78 wt. % of other pharmaceutically acceptable ingredients; and (b) 0-95 wt. % of one or more pharmaceutically acceptable excipients; the solid dosage unit comprising at least 20 ?g of the partus control substance and having a pH buffer range of 3.5-5.7.

Abstract: The invention provides an orodispersible solid pharmaceutical dosage unit having a weight between 30 and 1,000 mg, said dosage unit containing at least 100 ?g of an estetrol component selected from estetrol, estetrol esters and combinations thereof; wherein the solid dosage unit can be obtained by a process that comprises: providing a loading liquid comprising organic solvent; estetrol component and optionally one or more other pharmaceutically acceptable ingredients; mixing 1 part by weight of the loading liquid with 0.5-20 parts by weight of carrier particles to produce wet particles; removing organic solvent from the wet particles to produce loaded particles; optionally mixing the loaded particles with one or more tabletting excipients; and forming the loaded particles or the mixture of the loaded particles and the one or more tabletting excipients into a solid dosage unit. The solid dosage unit is easy to manufacture and perfectly suited for sublingual, buccal or sublabial administration.