Amlodipine Besylate

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Cat Number

API111470996

CAS Number

111470-99-6

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Product Detail Description Scientific Support Advanced Innovations Customer Q&A

CAS Number

111470-99-6

EINECS

1312995-182-4

Storage

2-8℃

Synonyms

2-[(2-Aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester benzenesulfonate

Molecular Formula

C26H31ClN2O8S

Molecular Weight

567.1

Smiles

CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2Cl)C(=O)OC)C)COCCN.C1=CC=C(C=C1)S(=O)(=O)O

Appearance

White powder

Melting Point

199-201℃

pKa

8.6

General Description

Amlodipine Besylate is a long-acting calcium channel blocker (dihydropyridine class) used as a first-line agent in the treatment of hypertension, stable angina, and Prinzmetal's (vasospastic) angina. Its unique pharmacokinetic profile includes a slow absorption phase and prolonged half-life, providing sustained calcium channel blockade and a gradual, extended reduction in blood pressure over 24 hours with once-daily dosing.

Mechanism of Action

Amlodipine Besylate selectively blocks L-type voltage-gated calcium channels in vascular smooth muscle cells and cardiac myocytes. In vascular smooth muscle, calcium channel blockade causes vasodilation of peripheral arterioles, reducing systemic vascular resistance (afterload) and lowering blood pressure. In cardiac tissue, it causes a modest negative inotropic effect. The gradual, sustained onset of action is attributed to its slow dissociation from calcium channels.

Application

Amlodipine Besylate is indicated for the treatment of hypertension (as monotherapy or in combination with other antihypertensives) and for the treatment of stable angina and vasospastic angina.

Amlodipine besylate (AML), an antihypertensive drug, was repurposed as an antibacterial agent and formulated into zein nanoparticles (ZNs) for ocular delivery. AML-ZNs were prepared by anti-solvent precipitation and optimized using Box-Behnken design. The optimal formulation (2.068% zein, 0.75% Labrafac, 1% Poloxamer 407) had particle size 185 nm, PDI 0.157, zeta potential +17.6 mV, and entrapment efficiency 59.25%. To improve stability and viscosity, ZNs were coated with sodium alginate, producing 349.9 nm particles with -55.45 mV zeta potential and 81.3% entrapment efficiency. Coating provided controlled drug release (40% over 48 hours) and enhanced corneal permeation (37% permeated vs. 17% for uncoated).
Assays showed AML-ZNs-Alg inhibited MRSA with lower MIC than free AML. Studies in rabbits demonstrated antibacterial efficacy against MRSA keratitis, reducing microbial counts significantly, with no ocular irritation. Alginate-coated zein nanoparticles represent a promising topical antibacterial system for ocular infections.

Fig. 1 Evaluation of the optimal Amlodipine Besylate-ZNs. (Eita A S.; et al. 2025)

References

Eita A S, et al. Coated Zein Polymeric Nanoparticles Loaded with Amlodipine as a Repurposed Antibacterial Ocular Cure for MRSA-Induced Infection: Optimization, In vitro, Ex Vivo, and In Vivo Assessments. Pharmaceutics, 2025, 17(10): 1314.

Mouth dissolving films (MDFs) of amlodipine besylate (AMLO) were developed to improve patient compliance, especially for elderly and pediatric populations. Film formers included HPMC E3, E5, E15, and methyl cellulose (MC), with PVP K30 or sodium lauryl sulfate (SLS) as solubilizers. Films were prepared by solvent casting and evaluated for drug content, thickness, mechanical properties, disintegration time, and in vitro dissolution. All films showed good uniformity and mechanical strength. FTIR, SEM, and X-RD confirmed drug-excipient compatibility and amorphous drug dispersion. HPMC E3-based formulations exhibited faster disintegration and dissolution than E5, E15, or MC. Formulation F3 (7.5% HPMC E3 with 0.04% PVP K30) achieved complete drug release within 60 seconds, significantly faster than other formulations. Dissolution followed Higuchi kinetics, indicating diffusion-controlled release. PVP-containing films performed better than those with SLS. The developed MDFs offer rapid onset, potential for improved bioavailability, and enhanced therapeutic efficacy for hypertension and angina management.

Fig. 2 Physicomechanical properties of different Amlodipine Besylate MDFs. (Maheswari K M.; et al. 2014)

References

Maheswari K M, et al. Development and evaluation of mouth dissolving films of amlodipine besylate for enhanced therapeutic efficacy. Journal of pharmaceutics, 2014, 2014(1): 520949.

What is the recommended storage condition for Amlodipine Besylate?

It should be stored at 2-8°C in a well-sealed container, protected from moisture and direct light, to maintain its chemical integrity throughout the shelf life.

Can we obtain batch-specific analytical data for Amlodipine Besylate?

Batch-specific COA documents are standard with every shipment. Additional analytical reports, including HPLC chromatograms or spectral data, may be provided upon request.

Does your company offer custom packaging for Amlodipine Besylate?

Yes, custom pack sizes are available. Specific quantity requirements can be discussed directly with our team to align with your production or research scale.

Is Amlodipine Besylate available in multiple salt forms?

The standard commercial salt form is supplied; for inquiries about alternative salt forms or polymorphs, please contact our technical team.

Is Amlodipine Besylate suitable for use in regulated pharmaceutical processes?

Yes, it is manufactured under quality standards consistent with regulated pharmaceutical applications, including in-process controls and release testing aligned with industry requirements.