Pharmaceutical Bulk Atorvastatin Calcium Powder

CAS:134523-03-8

MF: C33H37CaFN2O5

MW: 600.74

EINECS: 200-659-6

Specification​: 99% min Atorvastatin Calcium Powder

Sample: Atorvastatin Calcium Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Atorvastatin Calcium Powder Usage and Synthesis.

Atorvastatin calcium tablets are used in two main ways: to treat hypercholesterolemia; Reduce the risk of myocardial infarction, stroke and revascularization in patients with coronary heart disease (such as acute coronary syndrome, stable coronary heart disease, coronary revascularization, etc.) or other atherosclerotic cardiovascular diseases (such as ischemic cardiomyopathy, ischemic stroke, transient ischemic attack, peripheral atherosclerosis, etc.).

Uses and functions of Bulk Atorvastatin Calcium Powder.

Patients with hypercholesterolaemia primary hypercholesterolaemia. This includes patients with familial hypercholesterolaemia (heterozygous type) or mixed hyperlipidaemia (equivalent to types IIa and IIb of Fredrickson's classification) in whom the application of this product is indicated for the treatment of elevated total cholesterol (TC), elevated low-density lipoprotein cholesterol (LDL-C), elevated apolipoprotein B (Apo B) and elevated triglycerides (TG).

In patients with pure familial hypercholesterolaemia, atorvastatin may be used in combination with other lipid-lowering therapies (e.g., LDL plasma dialysis) or alone (when no other treatment is available) to lower TC and LDL-C. Patients with coronary artery disease coronary artery disease or coronary heart disease and other critical conditions (e.g., diabetes mellitus, symptomatic atherosclerotic disease, etc.) combined with hypercholesterolaemia or mixed dyslipidaemia.

Pharmacological Effects of Bulk Atorvastatin Calcium Powder.

1. The risk of myalgia is increased when combined with cyclosporine, beta-lipid-lowering agents, erythromycins, nicotinic acid and pyrrole antifungal agents.

2. When combined with antacids such as MaaloxTc suspension (containing aluminium hydroxide and magnesium hydroxide), the blood concentration of this product can be reduced by 30%, but the effect of lowering LDL-C is unchanged.

3. In combination with digoxin, the steady-state blood concentration of digoxin increased by approximately 20% after multiple administrations.

4. In combination with erythromycin (cytochrome P4503A4 inhibitor), the blood concentration of this product increased by approximately 40%.
5. In combination with the oral contraceptives norethindrone or ethinyl estradiol, the area under the concentration-time curve (AUC) of norethindrone and ethinyl estradiol increased by 30% and 20%, respectively. 

Production method of Atorvastatin Calcium.

Paal-Knorr synthesisThe core of the Paal-Knorr synthesis is the synthesis of the important intermediates M-4[4-fluoro-α-(2-methyl-1-oxopropyl)-γ-oxo-N,β-diphenylphenylbutyramide] and atorvastatin intermediates ATS (atorvastatinintermediates), in this paper ATS is taken as ATS ATS-9 [(4R-cis)-6-aminoethyl-2,2-dimethyl-1,3-dioxane-4-acetic acid tert-butyl ester] was used as an example.ATS-9 was reacted with M-4 by Paal-Knorr reaction to obtain atorvastatin lactone, and then hydrolysed to obtain atorvastatin calcium.

The synthesis of intermediate M-4 was based on isobutyrylacetanilide 2, which was condensed to obtain α,β-unsaturated ketone 3, which underwent the Stetter reaction to obtain intermediate M-4. Because of the relatively mild reaction conditions, simple raw materials, and high yields, this method has become an important one for the synthesis of intermediate M-4