Process for the preparation of a PPI-containing pharmaceutical product
A technology for pharmaceutical preparations and pharmacy, which is used in drug combinations, pharmaceutical formulations, and devices for making drugs into special physical or taking forms, and can solve problems such as limited production methods
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Embodiment 1
[0096] Example 1: Titration Test of Omeprazole Pellet Cores with Various Base Components
[0097] In order to optimize the pellet cores, various base components were added to the formulation not containing active substances, consisting of mannitol, hydroxypropylcellulose and sodium lauryl sulfate, and they were subsequently titrated with 0.1N HCl. different amounts of Na 2 HPO 4 , MgCO 3 and meglumine for this.
[0098] The aim of the study was to select a base with good buffering effect on the pellet core to avoid degradation of omeprazole during passage through the stomach (or during testing of tolerance to gastric juices) when small amounts of acid permeate. Furthermore, after opening of the enteric polymer, a slightly alkaline pH should exist in order to avoid possible in vivo degradation of the active substance.
[0099] for Na 2 HPO 4 , the range of 0.5-1.0g was studied. Do not use larger amounts because Na 2 HPO 4 Has hygroscopic properties which may have an ad...
Embodiment 2
[0111] Embodiment 2, omeprazole pellet output as a function of process condition / production scale
[0112] Influence of various process parameters (amount of added isopropanol (granulation agent), granulation time, mixer speed) in the production of pellet cores on pellet yield on a production scale (total solids in a batch of 300 kg) research.
[0113] The results are shown in the following table:
[0114]
[0115] It can be seen that the yield of pellets in the particularly important range of 700-1250 μm can be significantly increased, especially by shortening the granulation time to less than 20 minutes (in particular to less than or equal to 8 minutes), by increasing the amount of granulating agent and at the time of granulation Period by increasing the mixer speed to greater than or equal to 50 rev / min, in particular to greater than or equal to 65 rev / min.
Embodiment 3
[0116] Embodiment 3, the production embodiment of omeprazole pill
[0117] Formulations with different ratios of active substance and excipients can be prepared by the methods described. Table 2 below provides formulation examples with reference to the composition of the pellet core, the composition of the protective layer and the composition of the enteric layer. The formulation examples provided refer to a batch size of 1 kg pellet cores.
[0118] The formula embodiment of table 2, omeprazole pill
[0119]
[0120]
[0121] The weighed components of the pellet core are transferred to a high speed mixer commonly used in pharmaceuticals and mixed. While continuously mixing / granulating, isopropanol was added to the powder mixture in the mixer until pellets of the desired mass (spherical, approximately 1 mm in diameter) were formed. The mixing time is 1 to 10 minutes, usually 5 to 8 minutes, to achieve suitable quality and yield.
[0122] The pellets moistened with iso...
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