The combination was stirred at room temperature for about hrs. According to the present invention, a liquid composition can also contain a buffer such as gluconic acid, lactic acid, citric acid or acetic acid, sodium gluconate, sodium lactate, sodium citrate or sodium acetate. Renin Angiotensin Aldosterone Syst. This suggests that the medoxomil-ester prodrug is rapidly and completely converted to its pharmacologically active form in the gastrointestinal mucosa, portal blood, and liver before it comes into systemic circulation.
Acetone is especially preferred. Furthermore, as shown in Fig. Angiotensin II antagosist 1-biphenylmethylimidazole compounds and their therapeutic use. Direct compression produces a more uniform tablet without granules. Trityl olmesartan medoxomil g, mmol Separating the triphenyl carbinol from the solution can be performed by any means known in the art, such as filtration or centrifugation. In another embodiment, the present invention provides a process for preparing olmesartan medoxomil including the steps of: Preferably, the trityl olmesartan medoxomil is contacted with a mixture of a water miscible organic solvent and water.
The protein expression was localized in cytosolic fractions rather than in microsomal fractions in these two tissues, consistent with the higher subcellular distribution of the OM-hydrolyzing activity in the cytosolic fraction than in the microsomal fraction in both the liver and intestine Fig. Historically, many ester-based prodrugs have been developed with the aim of overcoming a number of barriers to drug-like properties 2—4.
The process of claim 15, wherein the purified olmesartan medoxomil contains less than about 0. Diluents increase the bulk of a solid pharmaceutical composition, and can make a pharmaceutical dosage form containing the composition easier for the patient and care giver to handle.
The standard solutions were injected with a stop time of 20 minutes. The process of claim 4, wherein the amount of the C ketone is at least about 10 volumes to about 1 gram of solid olmesartan medoxomil. An adjuvant assists the action of an active ingredient.
B13 30with its gene was encoded on a plasmid. A method of treating hypertension comprising administering a hypertension treating effective amount of the pharmaceutical composition of claim 13 to a subject in need thereof.
Esterases, which are involved in the prodrug bioactivation, as typically represented by carboxylesterases 56cholinesterases 78and paraoxonases 9are widely distributed in the blood, liver, intestine, and many other biological fluids and tissues.
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The process of claim 21, wherein the first solution further comprises water, and the ratio of water to acetone in the first solution is about 1: The sample solutions were injected continuing the chromatogram up to the end of gradient. Preservatives and chelating agents such as alcohol, sodium benzoate, butylated hydroxy toluene, butylated hydroxyanisole, and ethylenediamine tetraacetic acid can be added at levels safe for ingestion to improve storage stability.
The process can further include the step of heating the solution. Excipients that are particularly well suited for direct compression tableting include microcrystalline cellulose, spray dried lactose, dicalcium phosphate dihydrate, and colloidal silica.