Atorvastatin

To be considered a quality drug, a pharmaceutical tablet must meet specific standards. Key quality criteria for any drug in dosage form include safety, potency, efficacy, stability, patient acceptability, and regulatory compliance. These quality aspects must be established during the product development stage, where physical, chemical, and biological specifications are determined to ensure the product meets quality requirements. Our study aimed to determine and compare the percentage labeled claim, quality, and physicochemical characteristics of different brands of atorvastatin tablets using official and unofficial quality control tests. Atorvastatin, an HMG- CoA reductase inhibitor (statin), is essential for preventing hypercholesterolemia and related diseases. Although cholesterol is crucial in daily bodily functions, it can contribute to atherosclerosis development. We selected five brands of atorvastatin tablets (Atorva 40mg, Aztor 40mg, Lipicure 40mg, Lipikind 40mg, Lipvas 40mg) for analysis. Each sample underwent tests for hardness, friability, weight variation, disintegration, dissolution, and assay according to Indian Pharmacopoeia (IP) standards. All brands met the IP limits for hardness (4-8 kg/m2) and also complied with the requirements for weight variation and friability. The disintegration time for all brands was within the 30-minute IP recommendation for film-coated tablets. Each brand exhibited over 85% drug release within 30 minutes, and the content ranged from 90% to 110% of the labeled claim. These findings indicate that all tested atorvastatin brands available in Kerala (Kanjirappally) meet IP quality requirements.

Atorvastatin calcium is a HMG-CoA reductase inhibitor used in the treatment of hyperlipidaemia. It has oral bioavailability of less than 12%. It also undergoes high first pass metabolism. The objective of the present work was to formulate, optimize and in vivo evaluation of the potential novel proniosomal gel containing atorvastatin for transdermal delivery. On the basis of the preliminary trials a 3-factor, 3-level Box–Behnken design was employed to study the effect of Cholesterol, soya lecithin and Span 60 independent variable on dependent variables (particle size and % entrapment efficiency). Atorvastatin optimized proniosomal formulation F2 shown better particle size and % entrapment efficiency and also the drug release was 99.72% within 24h in slow and controlled manner when compared with control. The particle size and Zeta potential of the optimized atorvastatin proniosomal gel was found to be 65.72 and -10.5 respectively. Optimized batch of Proniosomes was used for the preparation of Atorvastatin - based proniosomal hydrogel by incorporating hydrated Proniosomes to Carbopol matrix to enhance the stability and viscosity of the system. The enhanced skin permeation for prolonged period of time, may lead to improved efficacy and better patient compliance. From in vivo studies the maximal concentrations (Cmax) of drug was significantly reduced while the areas under the plasma concentration–time curve (AUC) and t1/2 were evidently increased and extended. This study suggests that proniosomal gel of atorvastatin would be a promising alternative to improve the bioavailability problems of atorvastatin.

The studies were intended to investigate the possible antihyperlipidemic effect of tulsi and cinnamon oil in high cholesterol diet induced hyperlipidemic rats. Tulsi and cinnamon oil were evaluated for antihyperlipidemic activity using high cholesterol diet induced hyperlipidemia model in male Wistar albino rats(200-250g). A comparison was also made between the action of tulsi(0.5 mg/kg b.w) and cinnamon oil extracts(1.8mg/200g b.w) and antihyperlipidemic drug atorvastatin (0.18mg/200g). Parameters assessed were body weight, total cholesterol, triglyceride, HDL-C, LDL-C.  The results of the study are represented by mean ± SEM. Statistical significance of data was assessed by one way analysis of variance (ANOVA) followed by a comparison between different groups using “Tukey - Kramer” test. Oral administration of 0.5 mg/kg of tulsi oil with dist. water and Cinnamon oil of 1.8 mg/200g suspended in tween80 solution exhibited significant reduction (p ˂ 0.01) in serum biochemical parameters total cholesterol, triglycerides, low density lipoprotein (LDL), very low density lipoprotein (VLDL)  and increase in high density lipoprotein (HDL) levels in hyperlipidemic rats of HC diet model  compared to hyperlipidemic positive control. The results demonstrated that tulsi and cinnamon oil extracts possessed significant antihyperlipidemic activity.

Cyclodextrin nanosponges are solid, porous, bio-compatible, nano-particulate three dimensional structures which form inclusion complexes with different types of lipophilic or hydrophilic drug molecules and have been used as drug carrier for different drugs. In this present work, new cyclodextrin-based nanosponges of atorvastatin were prepared by condensation polymerization and interfacial polymerization to release Atorvastatin in expected manner in the treatment of dyslipidaemia as novel carriers. Results of encapsulation efficiencies of all formulation trials revealed that condensation polymerization is the best method for nanosponges formation and that is considered as best selected method for preparation. For the selected condensation polymerization, encapsulation efficiencies of atorvastatin in nanosponge formulations were found to be 72 to 86%. SEM images revealed their porous nature and cavity was of β-cyclodextrin. The mean particle size of nanosponges was about 328 nm and Zeta potentials of the nanosponges were sufficient enough (-10 to -15mv) due to presence of carboxylic group and inclusion complex formation which assured stability of formulations. The results of FTIR and DSC confirmed that atorvastatin was compatible with β-cyclodextrin and completely encapsulated in nanosponges structure respectively. The selected formulation produces good dissolution profile (release more than 75% atorvastatin within 60 mins in 0.1 N HCL) which indicated that the solubility of atorvastatin was improved by forming nanosponges. In accelerated stability studies, no significant changes occurred in physical appearance and drug content of atorvastatin nanopsonges formulation during 3 months stability studies. Atorvastatin nanosponges confirmed by insolubility in water and organic solvents like dimethyl formamide, dichloromethane.

5-Hydroxytryptamine (serotonin) (5-HT) and norepinephrine (NE) are implicated in modulating descending inhibitory pain pathways in the central nervous system. Milnacipran (MLN) is a selective and potent dual 5-HT and NE reuptake inhibitor (SNRI). In the present study, the effects of HMG-CoA reductase inhibitor atorvastatin (ATR) on antidepressant- induced anti-nociception have been investigated. Anti-nociceptive effects were evaluated using formalin test in rats after administration of atorvastatin and milnacipran alone as well as in combination. Fifty microlitre of 2.5% formalin solution was injected subcutaneously into the plantar surface of the right hind paw and nociceptive behavior was observed up to 45 min in the blocks of 5 min. Milnacipran induced a dose-dependent anti-nociception in the first phase as well as in the second phase of the formalin test at the dose levels of 10, 20, 40 and 60 mg/kg, p.o.. Milnacipran significantly attenuated the duration of licking and licking frequency both in second phase. Atorvastatin (1, 5, 10 and 20 mg/kg, p.o.) did not inhibit the nociceptive behavior of formalin significantly when treated alone. A combination of sub-therapeutic doses of the milnacipran (20 and 40 mg/kg, p.o.) with atorvastatin (10 and 20 mg/kg, p.o.) potentiate anti-nociception induced by antidepressant significantly. It is concluded that the atorvastatin modulate the antidepressant-induced anti-nociception in formalin induced inflammatory pain model. However, studies in chronic models of neuropathic pain are required to evaluate the efficacy of milnacipran and atorvastatin combination in rats.

A simple, rapid, and precise RP-HPLC method for simultaneous analysis of Losartan potassium and Atorvastatin calcium in bulk and its pharmaceutical formulations has been developed and validated. Atorvastatin was separated from losartan by using Grace Smart Altima C-18 column (25 cm × 4.6 mm, 5-μm) with a mobile phase consisting of acetonitrile: 10mM phosphate buffer (55:45 %v/v, pH 3.0) a flow rate of 1mL/min and detection wavelength at 240 nm. Aceclofenac was used as an internal standard in this method. Losartan, atorvastatin and aceclofenac were eluted with retention times of 4.85 min, 8.31min and 9.51 min respectively. The method was validated for accuracy, precision, linearity and sensitivity in accordance with ICH (Q2B) guidelines and the results of all the validation parameters were found to be within the acceptable limits. The calibration plots were linear over the concentration ranges from 200-30000ng/mL (r2 = 0.999) for both the drugs. Accuracy and precision were determined by QC sample covering low, medium, and high concentration levels. Intra and inert-day accuracy were found to be 97.16-102.57% for losartan and 97.01-103.05% for atorvastatin. The limit of quantification was found to be166ng/mL and 179ng/mL for losartan and atorvastain respectively. The method was successfully applied for the assay of the dosage form, recovery of the individual drugs from the combined tablet dosage was found to be >97% for both the drugs. From the results it is suggested that the proposed method is simple, reproducible, accurate and precise.