Steroid hormone products and methods for preparing them
a technology of steroid hormone and products, applied in the field of steroid hormone products, can solve the problems of regulatory authorities objecting to the use of such solvents, environmental objectionable organic solvents are generally required, solvents often pose safety hazards, etc., and achieves the effects of improving the dissolution profile, high dissolution properties, and sufficient mechanical energy
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example 1
Amorphous Lactose / Norgestimate Dry Ground Mixture
[0041]Amorphous norgestimate was prepared by dissolving norgestimate (200 mg) in 5 ml of (DCM) dichloromethane and 0.26 ml ethanol (EtOH). The solution was filtered through a 0.2 μm filter, and solvent was evaporated under reduced pressure to afford amorphous solid.
[0042]Mixtures of norgestimate and lactose, in amorphous and crystalline forms, were milled for 20 minutes. The amorphous state of each ingredient and of the mixture was confirmed by powder x-ray pattern diffraction (PXRD). The results are described below and summarized in Table 5.
[0043]A mixture of crystalline norgestimate:crystalline lactose (1:9) was milled in a Wig-I-Bug mill. A small mill containing a ball afforded amorphous norgestimate with mostly crystalline lactose, whereas a larger mill containing a bar yielded both as crystalline materials. Milling a 1:1 mixture of crystalline norgestimate:crystalline lactose afforded partially crystalline norgestimate with mostl...
example 2
Stability Studies of Amorphous Materials
[0045]This study shows that amorphous norgestimate is stabilized by lactose in a number of norgestimate: lactose preparations. Stress studies as well as thermal analyses (Example 3) showed the stabilization of norgestimate in norgestimate: latose mixtures.
[0046]Amorphous norgestimate was prepared from DCM:EtOH solution, and its stability was studied under various humidity conditions to establish a baseline of norgestimate stability. In order to simulate drug products, non-crystalline norgestimate: lactose mixtures were obtained from one of the following four methods: co-precipitation from EtOH:H2O, or 2-BuOH:H20, spray drying onto amorphous lactose, milling of crystalline mixtures, or milling of amorphous mixtures. The physical stability of non-crystalline norgestimate to resist recrystallization was also studied in the absence of and with an equal amount of lactose.
[0047]The materials for each sample were prepared as follows:
Amorphous Norgest...
example 3
[0060]The lactose / norgestimate mixtures made as in Example 2 were subjected to thermal analysis, according to conventional Differential Scanning calorimetry (DSC).
Glass-Transition Temperature and Crystallization Exotherm Measurements
[0061]Amorphous materials exhibit glass-transition temperatures (Tg) that reflect the physical stability of the amorphous form. The stabilized mixtures, norgestimate:lactose (1:9) mixtures, were examined along with individual amorphous materials to obtain Tg values that might give insight to the stability of each mixture compared to a single-component system. Glass-transition temperature measurements generally entail trial runs on a DSC to obtain an optimal method for observing glass-transition events. Amorphous lactose exhibits a very strong Tg event at 114-115° C. However, amorphous norgestimate does not produce consistent Tg events. Some amorphous norgestimate samples produce a weak Tg event at 122-123° C., while other samples shown an exothermic even...
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