The present invention provides a technetium [99Tc] methylene diphosphonate oral formulation, a preparation method therefor, and a use thereof. The oral formulation is prepared by the following raw materials, comprising, in parts by weight, a methylene diphosphonic acid, a reducing agent, a sodium [99Tc] pertechnetium, an adhesive, and a solvent. The adhesive is made of a high molecular polymer material. The oral formulation is prepared by the steps of using the methylene diphosphonic acid, the reducing agent, and the sodium [99Tc] pertechnetium to prepare technetium [99Tc] methylene diphosphonate, timely dissolving technetium [99Tc] methylene diphosphonate in the solvent, and forming a mixed solution with the adhesive for spray drying treatment, wherein the temperature of an air outlet in the spray drying treatment process does not exceed 115°C. By means of the high molecular polymer material, and the timing of spray drying and temperature control, the technetium [99Tc] methylene diphosphonate oral formulation prepared in the present application has a good bioavailability, so that the gastrointestinal irritation can be relieved and the use compliance of a patient can be improved while a same drug effect is achieved, thereby achieving an unexpected technical effect.
Disclosed are novel diphosphonate compounds, and method for preparing the novel diphosphonate compounds. The novel diphosphonate compounds provided in the present invention show an almost equivalent activity in inhibiting the activity of osteoclasts as compared to alendronate sodium and a relatively high activity in influencing the proliferation of osteoblasts as compared to positive control drugs having a relatively weak influence on the proliferation of osteoblasts. In the test examples, dosing regimens for using the diphosphonate compounds according to the present invention are provided.
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