Thotakura Sai Pavan*, Naresh Panigrahi and Mukthinuthalapati Mathrusri Annapurna
GITAM Institute of Pharmacy, GITAM (Deemed to be University), Visakhapatnam, India
*Corresponding Author: Thotakura Sai Pavan, GITAM Institute of Pharmacy, GITAM (Deemed to be University), Visakhapatnam, India.
Received: January 30, 2021; Published: February 17, 2021
Citation: Thotakura Sai Pavan and Naresh Panigrahi. “Newer Conventional and Nonconventional Treatment Strategy of Chikungunya Fever along with a Review of its Virology and Epidemiology”. Acta Scientific Pharmaceutical Sciences 5.3 (2021): 10-12.
Dolutegravir is a novel integrase stand transfer inhibitor active against human immunodeficiency virus. Dolutegravir is an integrase strand transfer inhibitor which preferentially blocks the strand transfer step of integration of the viral genome into the host cell's DNA mediated by the viral integrase enzyme. The authors have reviewed the analytical methods developed for the estimation of Dolutegravir in pharmaceutical dosage forms and in biological samples in the present paper.
Keywords: Dolutegravir; Integrase Strand Transfer Inhibitor; DNA
Dolutegravir is chemically (4R,12aS)-N-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3 4,6, 8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide (C20H18F2N3NaO5). Dolutegravir is an integrase strand transfer inhibitor [1]. Dolutegravir sodium is a white to light yellow powder and is slightly soluble in water and methanol and is rapidly absorbed after oral administration and it was approved by FDA. Dolutegravir is active against HIV type 1 and also has some in vitro activity against HIV type 2 [2].
Figure 1: Structure of Dolutegravir.
Dolutegravir blocks the strand transfer step of the integration of the viral genome into the host cell and prevents HIV from replicating and lowers the amount of HIV in the blood. Dolutegravir will not cure or prevent HIV infection or AIDS, however, it helps keep HIV from reproducing and appears to slow down the destruction of the immune system.
Dolutegravir is available as tablets with brand name Instgra (Labelled claim 50 mg) from Avalon Pharma Pvt Ltd (India). Dolutegravir is also available in combination with Rilpivirine (Juluca) (Labelled claim: Dolutegravir: 50 mg and Rilpivirine: 25 mg) as film coated tablets; Lamivudine (Dovato) (Labelled claim: Dolutegravir: 50 mg and Lamivudine: 300 mg); Lamivudine and Tenofovir Disoproxil Fumarate (Viropil) (Labelled claim: Dolutegravir: 50 mg, Lamivudine: 300 mg and Tenofovir Disoproxil Fumarate: 300 mg).
The authors have summarised the analytical methods so far developed in the literature for the determination of Dolutegravir in the present review article. The methods include are spectrophotometry [4-7], HPLC [8,9], HPTLC [10] (Table 1) for the pharmaceutical formulations. Liquid chromatographic methods were also developed for the separation of optical isomers of Dolutegravir [11,12] and for the estimation of Dolutegravir in human plasma using HPLC [13], UPLC [14] and LC-MS/MS [15].
Reagent |
Linearity (µg/ml) |
lmax (nm) |
Comment |
Ref |
Spectrophotometric methods |
||||
Water |
5 - 40 |
259.8 |
- |
3 |
Ferric chloride and 1,10- Phenanthroline reagent |
40 - 140 |
520
|
Visible spectrophotometry Orange red complex |
4
|
0.8 M aq. Urea |
2.5 - 20 |
258 248 - 268 256 |
Absorption maxima method AUC method First derivative method |
5 |
Water |
2 - 18 |
259 |
- |
6 |
Water |
5 - 40 |
259.8 |
- |
7 |
Liquid chromatographic methods |
||||
0.1% Aq. Trifluoro acetic acid: Methanol |
0.076 - 1.5 |
240 |
HPLC (Gradient mode) |
8 |
Dipotassium hydrogen orthophosphate: Methanol (70:30), |
50 - 150 |
260 |
HPLC |
9 |
Acetonitrile: water (pH 7.5) (80:20) Methanol: Chloroform: Formic acid (8: 2: 0.5) |
5 - 35 200 - 900 ng/spot |
260 265 |
HPLC HPTLC |
10 |
Table 1: Review of analytical methods for the determination of Dolutegravir.
The present review article helps the readers to do research in a new field apart from the presenting existing analytical techniques for the anti-viral drug Dolutegravir.
Copyright: © 2021 Thotakura Sai Pavan and Naresh Panigrahi. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.