Stability-indicating assay method for determination of actarit, its process related impurities and degradation products: Insight into stability profile and degradation pathways ☆

Abiramasundari, A.; Joshi, Rahul; Sharma, Jayesh A.; Pandya, Dhaivat H.; Pandya, Amit N.; Sudarsanam, V.; Vasu, Kamala K.

doi:10.1016/j.jpha.2014.01.002

Cited by 8 publications

(5 citation statements)

References 14 publications

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“…Despite substantial research on actarit, e.g., exploring its clinical phenotype [ 15 , 17 ], improving its administration [ 18 , 19 ] or enhancing its stability within the organism [ 20 , 21 ], no molecular target of this drug has previously been found. MolTarPred v1 was hence able to discover the first target for actarit where SEA could not [ 7 ].…”

Section: Discussionmentioning

confidence: 99%

Identification and Validation of Carbonic Anhydrase II as the First Target of the Anti-Inflammatory Drug Actarit

2020

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Background and purpose: Identifying the macromolecular targets of drug molecules is a fundamental aspect of drug discovery and pharmacology. Several drugs remain without known targets (orphan) despite large-scale in silico and in vitro target prediction efforts. Ligand-centric chemical-similarity-based methods for in silico target prediction have been found to be particularly powerful, but the question remains of whether they are able to discover targets for target-orphan drugs. Experimental Approach: We used one of these in silico methods to carry out a target prediction analysis for two orphan drugs: actarit and malotilate. The top target predicted for each drug was carbonic anhydrase II (CAII). Each drug was therefore quantitatively evaluated for CAII inhibition to validate these two prospective predictions. Key Results: Actarit showed in vitro concentration-dependent inhibition of CAII activity with submicromolar potency (IC50 = 422 nM) whilst no consistent inhibition was observed for malotilate. Among the other 25 targets predicted for actarit, RORγ (RAR-related orphan receptor-gamma) is promising in that it is strongly related to actarit’s indication, rheumatoid arthritis (RA). Conclusion and Implications: This study is a proof-of-concept of the utility of MolTarPred for the fast and cost-effective identification of targets of orphan drugs. Furthermore, the mechanism of action of actarit as an anti-RA agent can now be re-examined from a CAII-inhibitor perspective, given existing relationships between this target and RA. Moreover, the confirmed CAII-actarit association supports investigating the repositioning of actarit on other CAII-linked indications (e.g., hypertension, epilepsy, migraine, anemia and bone, eye and cardiac disorders).

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Section: Discussionmentioning

confidence: 99%

Identification and Validation of Carbonic Anhydrase II as the First Target of the Anti-Inflammatory Drug Actarit

2020

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“…In other words, there was no interference from coeluting analytes. This result confirms that the HPLC method has the ability to determine the α-mangostin even in the presence of other compounds (Abiramasundari et al, 2014). 8.…”

Section: Analytical Methods Validationsupporting

confidence: 82%

Development of Sunscreen Cream Containing Mangosteen Pericarp Extract Encapsulated in Solid Lipid Nanoparticles

Diniyanti

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The aim of this study was to develop cream containing mangosteen pericarp extract (MPE) encapsulated in solid lipid nanoparticles (SLNs) in order to achieve enhanced photoprotection and to be an alternative for synthetic sunscreens in the market. The MPE was prepared by maceration method and evaluated for SPF value by UV-Vis spectrophotometer. SLNs were prepared by ultrasonication method. Blank SLNs were formulated using stearic acid (SA) or palmitic acid (PA) as a solid lipid at a concentration of 3%. Tween? 80 or PVA was employed as a surfactant with concentrations ranging from 1 to 2%. The obtained blank-SLNs were investigated for its physical characteristics, i.e., morphology, particle size, polydispersity index (PDI), and zeta potential value. The blank SLNs with suitable physical characteristics were selected to encapsulate MPE and evaluated for the physical characteristics. Finally, the cream containing MPE encapsulated in SLNs (MPE-SLNs) were formulated and evaluated for their physical properties, chemical stabilities, and SPF values during storage at 4-8oC for 3 months. The obtained MPE was a dark brown powder with an SPF value ranged from 3.09?0.01 to 27.20?0.05 at concentrations ranging from 0.02 to 0.1 mg/ml. Based on the physical characteristics, the blank SLNs employing PA or SA with 1% of PVA were selected. MPE-SLNs were successfully loaded into cream at the MPE concentration of 3%. The SLNs enhanced the SPF values of cream containing MPE-SLNs by two-fold compared with cream containing 3% MPE. The cream containing MPE-PA-SLNs and MPE-SA-SLNs displayed good physical appearances, and was chemically stable, without any significant difference of SPF values after storage at 4-8 oC for 3 months. The results indicated that the cream containing MPE-SLNs had a promising potential to be used as an alternative UVB photoprotector to the synthetic sunscreens.

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“…Drug at a concentration of 1mg ml -1 was used in all degradation studies. Conditions employed for stability studies were as follows [20][21][22] .…”

Section: Forced Degradation Studiesmentioning

confidence: 99%

Development and Validation of Stability Indicating Assay Method of Doxycycline Hyclate by using UV-Spectrophotometer

Sahoo¹,

Sahoo²,

Mohapatra³

et al. 2023

J. Drug Delivery Ther.

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In the present study a simple, rapid, sensitive, and cost-effective stability indicating UV- spectrophotometric method was developed of doxycycline hyclate in bulk form and validated as per ICH guidelines. The stability-indicating study of doxycycline hyclate was based on the forced degradation reactions of the drug under different ICH-prescribed stress conditions like acid, alkali, neutral, oxidation, thermal, and photolysis. The absorption maximum of the drug was shown at 270nm and methanol was selected as solvent on the basis of the solubility of the drug. A linear relation with a regression coefficient value (R2) of 0.999 indicates that the method follows Beer’s- Lambert’s law within the concentrations range of 5 - 50µg/ml. The detection limit and quantitation limit were found to be 0.53 µg/ml and 1.55 µg/ml respectively. The % of recoveries was found to be within the range of 98.87 -99.88 with a low % of RSD indicating the accuracy of the method for estimation of the drug. Under stressed conditions, significant degradation was found in alkali, neutral and oxidation conditions and found to be sensitive under thermal and photolytic conditions but stable to acidic hydrolytic conditions. The developed method was validated according to ICH guidelines and found accurate, precise, and specific, suggesting that the developed stability-indicating spectroscopic method could be successfully adopted to estimate doxycycline hyclate. Keywords: Doxycycline Hyclate; Stability Indicating method; UV spectrophotometer; Validation; Stress degradation.

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Stability-indicating assay method for determination of actarit, its process related impurities and degradation products: Insight into stability profile and degradation pathways ☆

Cited by 8 publications

References 14 publications

Identification and Validation of Carbonic Anhydrase II as the First Target of the Anti-Inflammatory Drug Actarit

Identification and Validation of Carbonic Anhydrase II as the First Target of the Anti-Inflammatory Drug Actarit

Development of Sunscreen Cream Containing Mangosteen Pericarp Extract Encapsulated in Solid Lipid Nanoparticles

Development and Validation of Stability Indicating Assay Method of Doxycycline Hyclate by using UV-Spectrophotometer

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