INTRODUCTION:

Oral drug delivery system achieved nice success and terribly common route of drug administration. The reason behind this quality could be by its "ease of administration" however one issue could have an effect on its quality and use of administration, i.e., in depth first-pass metabolism. The drug degrades by first-pass metabolism leads to short length of therapeutic action and low general bioavailability. In these route, a drug is run by the mouth in such approach that the drug is quickly absorbed by the blood vessels rather than interesting through gastrointestinal tract. This class of medication releases their drug content directly into tissue layer lining of the mouth below the tongue. Tenofovir alafenamide is a ester polymerase substance and used in the treatment of HIV infection. Tenofovir alafenamide is poorly soluble drug. Its having binary compound solubility Tenofovir alafenamide comes beneath BCS Class-II drug.

Tenofovir alafenamide undergoes in depth internal organ first-pass metabolism. it's having a dose 25mg. The analysis targeted on the preparation and analysis of the tablets of Tenofovir alafenamide exploitation superdisintegrants.

MATERIALS AND METHODS:

Materials:

Tenofovir alafenamide was obtained as a present sample from Cipla R&D, Mumbai. Sodium starch glycolate and disaccharide were obtained from HiMedia Laboratories, Mumbai. Crospovidone was obtained from Loba chemicals. crystalline from Loba chemicals. Talc, sucrose, mannitol, magnesium stearate (Loba chemicals).

Method:

Preparation of solid dispersion by kneading methodology:

During this methodology, drug and compound² were taken to cut back the dimensions of the mixture. water was extra within the physical mixture, and suspension mass was then dried in hot air oven at 45°C. The dried product was capable sieve no. 36. Preparation of these tablets of Tenofovir alafenamide. The active ingredient and all the excepients was weighed and sieved singly through #44 mesh size. After sieving all the ingredients were mixed in geometrical order. Talc was weighed and capable an equivalent sieve and was extra to the formulation and mixed for two min to induce free-flowing powder and eventually, the blend was compressed in the pill punching machine. Formulation, all the six batches of sublingual tablets³, was ready by dynamical the concentration of sodium starch glycolate and crospovidone. (Table 1).

Analysis of Ready tablets:

Weight variation:

It had been distributed to confirm the right quantity of drug in every pill⁴. twenty tablets were weighed singly with the assistance of chemical balance. the common weight was calculated and also the % weight variation was calculated with the assistance formula.

% Weight Variation = (Individual weight – Average weight)/ Average weight ^{x 100}

Hardness:

The hardness of the pill is decided with the assistance of Monsanto hardness tester and it's expressed in kg/cm².

Diameter and thickness:

The diameter and also the thickness of the pill is measured with the assistance of calipers and it's expressed in mm.

Friability:

10 tablets square measure weighed and placed into the equipment wherever they're exposed to rolling and recurrent shocks as they fall half-dozen inches in every flip among the equipment. when four minutes of this treatment or one hundred revolutions, the tablets square measure weighed and also the weight compared with the initial weight. The loss because of abrasion could be a live of the pill breakableness. No more than 1 Chronicles of the burden of the tablets is appropriate.

Friability = (W1-W2) / W1 x one hundred.

Here, W1 is that the initial weight of pill and W2 is that the final weight of pill.

Drug content:

Tablets were at random chosen and crushed into mortar pestle. an acceptable amount of powder was extracted with 900ml of phosphate buffer (Ph6.8). This was filtered and analyzed by UV photometer (Shimadzu 1800) at 259nm.

In-vitro drug release:

The drug unleash from the Tenofovir alafenamide tablets was investigated in a very USP-II (paddle) equipment. At preset time intervals of two minutes, samples were withdrawn and filtered with Whatman paper and diluted ten times and so analyzed with ultraviolet illumination photometer at wavelength at 259nm.

Table 1: Composition of formulated Tablet:

Ingredients	Fl(mg)	F2(mg)	F3(mg)	F4(mg)	F5(mg)	F6(mg)
Tenofovir alafenamide (solid dispersion)	25	25	25	25	25	25
Sod. starch glycolate	-	5(2%)	-	10(4%)	7(3%)	-
Crospovidone	5(2%)	-	10(4%)	-	-	7(3%)
Sucrose	10	10	10	10	10	10
MCC	40	40	40	40	40	40
Talc	20	20	20	20	20	20
starch	25	25	25	25	25	25
Lactose	q.s.	q.s.	q.s.	q.s.	q.s.	q.s.

Table 2:Pre-compression studies of formulated tablets

Formulation Code	Bulk density (gm/mL) ±SD	Tapped Density (gm/mL) ±SD	Carr’s Index (%) ±SD	Hausner’s Ratio	Angle of repose (Ɵ) ±SD
F1	0.316±0.008	0.336±0.017	7.71±0.08	1.20	24.12±0.55
F2	0.317±0.01	0.357±0.02	6.26±0.13	1.21	25.43±0.89
F3	0.341±0.007	0.382±0.019	6.80±0.18	1.34	25.55±0.86
F4	0.295±0.03	0.321±0.04	7.14±0.06	1.08	26.33±0.90
F5	0.292±0.03	0.353±0.07	6.24±0.04	1.32	24.21±0.44
F6	0.326±0.05	0.368±0.04	7.25±0.04	1.31	25.07±0.44

Table 3: Post-compression studies of formulated tablets

Batch Code	Thickness (mm) ± SD	Hardness (Kg/cm2) ± SD	Friability (%)	Weight Variation (mg)	wetting time (sec)	Drug Content (%) ± SD	Disintegration Time(s)
F1	3.42±0.76	4.32±0.844	0.71±0.011	151±0.913	113.66±3.5	93.24±1.77	123.66±2.08
F2	3.32±0.41	4.14±1.21	0.55±0.014	148±0.661	103±1.52	95.15±1.57	117.33±1.52
F3	3.26±0.449	4±0.894	0.67±0.026	147±0.776	98.76±1.15	95.22±0.92	110.66±1.15
F4	3.53±0.28	3.82±1.329	0.79±0.022	154±0.564	156.33±2.51	96.17±2.77	158.66±2.22
F5	3.52±0.41	3.15±0.983	0.69±0.020	156±0.852	132±3.05	97.45±2.32	145.33±2.51
F6	3.31±0.406	4.15±2.56	0.77±0.012	150±0.987	99±1.73	96.27±0.83	118.33±2.51

In Vitro drug release profile Study of formulated batches:

The in vitro dissolution study of the tablets were performed in phosphate buffer (6.8 pH) and discovered results are mentioned in Figure two.

Figure 1: In-vitro drug release study

CONCLUSION:

During this analysis work, the sublingual tablets of Tenofovir alafenamide were ready, and solubility of Tenofovir alafenamide was found to be exaggerated exploitation solid dispersion ready by kneading techniques. The identification tests of tenofovir alafenamide sample was through with the assistance of ultraviolet illumination analysis, melting point determination, solubility studies, IR and DSC tests. From the current study, it are often over that the use of solid dispersion⁵ and super disintegrates exaggerated solubility and in vitro drug unleash of Tenofovir alafenamide. By making ready sublingual formulation (tablets) the bioavailability of Tenofovir alafenamide was exaggerated and stop them from in depth first-pass impact. The optimized batch gave the best lead to terms of in-vitro drug unleash rate and bioavailibility.

CONFLICT OF INTEREST:

The authors declare no conflict of interest.

REFERENCES:

1. Liberman H, Lachman L, The Theory and Practice of Industrial Pharmacy. 3rd Ed. Bombay: Verghese Publication House, 1991, 171-193.

2. Lolisson T. Duchene, cyclodextrins and their pharmaceutical application. Int J Pharm 2007; 329:1-11

3. Richman MD, Fox D. Shangraw RE'. Preparation and stability of glyceryl trinitrate sublingual tablets prepared by direct compression. J Pharm Sci 1965; 54: 447-51.

4. Rameshwari S, Anandi J. Formulation and evaluation of nifedipine sublingual tablets. Asian J Pharm Clin Res 2009; 2: 41-8.

5. Dhere M, Majumdar A and Malviya N: Formulation and evaluation of hydrotropic solid dispersion of eluxadoline. Int J Pharm Sci and Res 2019; 10(12): 5450-54.

Received on 27.05.2020 Modified on 26.06.2020

Research J. Pharm. and Tech 2021; 14(3):1716-1718.

DOI: 10.5958/0974-360X.2021.00305.X