scholarly journals FORMULATION AND DEVELOPMENT OF EFAVIRENZ TABLETS BY PAPER TECHNIQUE USING CO-SOLVENCY METHOD

Author(s):  
CH. DHANA SUBRAHMANYESWARI ◽  
Y. PRASANTH ◽  
SAMEEDA RUBEEN

Objective: The present study is to formulate and development of efavirenz tablets by paper technique using the co-solvency method, the drug is antiviral drug used for the treatment of HIV. Methods: In this 7 formulation (F1-F7) were prepared by using different tissue papers like kitchen roll paper, hand kercheif paper, facial tissue paper, with different weights. The prepared tablets were evaluated for hardness, friability, thickness, content uniformity, disintegration time and in vitro dissolution study. Results: Among all the formulations, F2 (kicthen roll paper with weight 250 mg) was consired to be the best formulation, which release up to 98.02% drug in 3 h. The results of stability studies of formulation F2 after a period of 2 mo indicated that the formulation was stable. Conclusion: It was concluted that a paper tablet of efavirenz shows better results and it does not contain any excipient and increase the dissolution rate.

Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas A

The main objective of this study was to develop fast dissolving oral films of ropinirole HCl to attain quick onset of action for the better management of Parkinson’s disease. Twenty-seven formulations (F1-F27) of ropinirole oral dissolving films by solvent-casting method using 33 response surface method by using HPMC E15, Maltodextrin PEG 4000 by using Design of experiment software. Formulations were evaluated for their physical characteristics, thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and drug release characteristics and found to be within the limits. Among the prepared formulations F4 showed minimum disintegration time 11 sec, maximum drug was released i.e. 99.68 ± 1.52% of drug within 10 min when compared to the other formulations and finalized as optimized formulation. FTIR data revealed that no interactions takes place between the drug and polymers used in the optimized formulation. The in vitro dissolution profiles of marketed product and optimized formulation was compared and found to be the drug released was 92.77 ± 1.52 after 50 min. Therefore, it can be a good alternative to conventional ropinirole for immediate action. In vitro evaluation of the ropinirole fast dissolving films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of ropinirole. The oral dissolving film is considered to be potentially useful for the treatment of Parkinson’s disease where quick onset of action is desired


Author(s):  
R. SANTOSH KUMAR ◽  
ANNU KUMARI ◽  
B. KUSUMA LATHA ◽  
PRUDHVI RAJ

Objective: The aim of the current research is optimization, preparation and evaluation of starch tartrate (novel super disintegrant) and preparation of fast dissolving oral films of cetirizine dihydrochloride by employing starch tartrate. Methods: To check the drug excipient compatibility studies of the selected drug (Cetrizine dihydrochloride) and the prepared excipient i. e starch tartrate, different studies like FTIR (Fourier-transform infrared spectroscopy), DSC (Differential scanning calorimetry) and thin-layer chromatography (TLC) were carried out to find out whether there is any interaction between cetirizine dihydrochloride and starch tartrate. The solvent casting method was used for the preparation of fast dissolving films. The prepared films were then evaluated for thickness, folding endurance, content uniformity, tensile strength, percent elongation, in vitro disintegration time and in-vitro dissolution studies. Response surface plots and contour plots were also plotted to know the individual and combined effect of starch tartrate (A), croscarmellose sodium (B) and crospovidone (C) on disintegration time and drug dissolution efficiency in 10 min (dependent variables). Results: Films of all the formulations are of good quality, smooth and elegant by appearance. Drug content (100±5%), thickness (0.059 mm to 0.061 mm), the weight of films varies from 51.33 to 58.06 mg, folding endurance (52 to 67 times), tensile strength (10.25 to 12.08 N/mm2). Fast dissolving films were found to disintegrate between 34 to 69 sec. Percent dissolved in 5 min were found to be more in F1 formulation which confirms that starch tartrate was effective at 1%. Conclusion: From the research conducted, it was proved that starch tartrate can be used in the formulation of fast dissolving films of cetirizine dihydrochloride. The disintegration time of the films was increased with increase in concentration of super disintegrant.


2017 ◽  
Vol 9 (6) ◽  
pp. 39
Author(s):  
Zainab E. Jassim

Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) studies.Results: The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion: The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.


Author(s):  
S. Jyothi Sri ◽  
D.V. R.N Bhikshapathi

The present investigation was aimed with the objective of developing fast dissolving oral films of Aripiprazole to attain quick onset of action for the better management of Schizophrenia. Fourteen formulations (F1-F14) of Aripiprazole mouth dissolving films by solvent-casting method using HPMC E5, HPMC E15, Maltodextrin, PG and PVA. Formulations were evaluated for their physical characteristics, thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and drug release characteristics and found to be within the limits. Among the prepared formulations F13 showed minimum disintegration time 10 sec, maximum drug was released i.e. 99.49 ± 0.36% of drug within 8 min when compared to the other formulations and finalized as optimized formulation. FTIR data revealed that no interactions take place between the drug and polymers used in the optimized formulation. The in vitro dissolution profiles of marketed product and optimized formulation was compared and found to be the drug released was 20.73 ± 0.25 after 8 min. Therefore, it can be a good alternative to conventional Aripiprazole for immediate action. In vitro evaluation of the Aripiprazole fast dissolving oral films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Aripiprazole. The mouth dissolving film is potentially useful for the treatment of Schizophrenia where the quick onset of action is desired.


Author(s):  
Rahul Radke ◽  
Neetesh K. Jain

Aim: Ambrisentan is a endothelin type A selective receptor antagonist used in the management of pulmonary arterial hypertension. Ambrisentan is BCS Class II drug haves very poor solubility in water and shows incomplete absorption after oral administration. The present work was aimed to study the effect of amphiphilic graft co-polymer carrier on enhancement of solubility and dissolution rate of poorly water soluble drug ambrisentan. To improve the aqueous solubility of ambrisentan solid dispersion was formulated by using novel carrier amphiphilic graft co-polymer (Soluplus® ). Materials and Methods: Solid dispersion was prepared by kneading technique by utilizing various ratios of carrier. Obtained solid dispersions ware evaluated for solubility, percentage yield, drug content and in vitro dissolution study. Powder characterization was performed by infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD). Results: FTIR spectroscopy shows no interaction between drug and polymer. DSC study showed that endothermic peak of drug was completely disappeared in Solid dispersion suggesting complete miscibility of drug in Soluplus®. XRD study suggest the conversion of crystalline ambrisentan in to amorphous form. All solid dispersions prepared with Soluplus® as a carrier showed increase in solubility. Solubility of ambrisentan was found to be increased 7.17 fold in optimized SD formulation ASD5. In vitro dissolution study showed the faster drug release from SD formulation compare to its pure form. All solid dispersion formulation’s release more than 50% of drug in first 10 min. Conclusion: This study conclude that the preparation of amphiphilic graft co-polymer based solid dispersion prepared by kneading technique is found to be useful in enhancement the solubility and dissolution rate of ambrisentan.


2018 ◽  
Vol 6 (3) ◽  
pp. 5-16 ◽  
Author(s):  
ABRAHAM LINKU ◽  
JOSEPH SIJIMOL

The aim of present work was the development of fast dissolving oral film of Loratadine to overcome the limitations of current routes of administration, to provide immediate action and increase the patient compliance. To improve the bioavailability of the drug, fast dissolving oral film were formulated using different grades of Hydroxy Propyl Methyl Cellulose(HPMC) and various plasticizers like Polyethylene Glycol(PEG) 400, glycerol, Propylene glycol(PG) by solvent casting method. The formulated films were evaluated for film thickness, surface pH, folding endurance, weight variation, % moisture loss, exvivo permeation study, tensile strength, % elongation, drug content uniformity, in vitro dissolution studies,in vitro disintegration test and in vivo study. The optimized formulation (F9) containing HPMC E5 and glycerol showed minimum disintegration time (10.5 s), highest in vitrodissolution (92.5%) and satisfactory stability. Ex vivo permeation study of optimized formulation showed a drug release of 80.6% within 10 min. The milk induced leucocytosis inrat proved that fast dissolving oral films of Loratadine produced a faster onset of action compared to the conventional tablets. These findings suggest that fast dissolving oral film of Loratadine could be potentially useful for treatment of allergy where quick onset of action is required.


Author(s):  
Vedanshu Malviya ◽  
Srikant Pande

The intention of the present study was to formulate the oral dispersible film of Fluoxetine hydrochloride using pullulan as a polymer and to evaluate it with the different parameters. The drug-excipients studies were carried out in order to determine any type of incompatibilities by using Fourier transmission infrared spectroscopy (FT-IR). The oral dispersible films were prepared using solvent casting method using pullulan as a polymer. Glycerin was used as a plasticizer. The prepared films were evaluated for the parameters like physical appearance, thickness, folding endurance, In-vitro disintegration, mechanical properties, surface pH, drug content uniformity, taste evaluation, In-vitro dissolution test and stability study. The X5 formulation was found to be stable and appropriate in its evaluation parameters than compared to other formulations. The folding endurance was found to be 259±2.53, disintegration time was found to be 04±0.69, thickness was found to be 0.081±0.003, tensile strength was found to be 5.55, the % elongation was found to be 27.50, the maximum percentage drug release was found to be 95.80% in 30 minutes. The drug content was found to be 99.86 with surface pH of 6.8. In the stability studies of the formulation the product was found to be stable for 90 days. The oral dispersible film is simple to administer and very much effective for the patients and the prepared film of fluoxetine hydrochloride proves to be potential candidate for safe and effective oral dispersible drug delivery.


2021 ◽  
Vol 3 (2) ◽  
Author(s):  
Km. Roshani ◽  
Mangla Nand Singh ◽  
D. Sasmal ◽  
P. D. Panda ◽  
Jai Narayan Mishra ◽  
...  

Etoricoxib belongs to a class of drugs called non-steroidal anti-inflammatory drugs (NSAIDs). Etoricoxib acts by reducing the pain and swelling (inflammation) in the joints and muscles of people older than 16 years of age and older patients with osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and gout. The present study was aimed to formulate fast dissolving oral films to enhance bioavailability, avoid presystemic metabolism and fast onset of action. The Preformulation studies such as Micromeritics, melting point, partition coefficients, UV spectroscopy, thin layer chromatography, loss on drying were carried out. The fast dissolving oral film was successfully fabricated by solvent casting method. Oral film was fabricated using PVA and PVP polymer. The prepared films were evaluated for Organoleptic evaluations, film weight, thickness, folding endurance, tensile strength, drug content uniformity of films, surface pH, disintegration time and in-vitro dissolution studies and SEM study. The formulation F8 has shown disintegration time of 22±1 seconds and is more promising, showed drug release in phosphate buffer 6.8 pH 86.33% in 10 min. Hence formulation F8 was selected as best formulation. In the stability testing all films stored at elevated temperature showed slight change in pH, other parameters were found to be unchanged.


Author(s):  
N. G. Rao ◽  
Upendra Kulkarni ◽  
Hari Prassanna C. ◽  
Basawaraj Patil ◽  
Rabbani G.

Felodipine which is used in the present study is a dihydropyridine derivative, that is chemically described as ethyl methyl-4-(2, 3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate, widely accepted for its excellent antihypertensive and anti-anginal properties since it is calcium antagonist compound (calcium channel blocker). Felodipine is practically insoluble in water and its dissolution rate is limited by its physicochemical properties. In the present study fast disintegrating tablets of felodipine were prepared by adopting vacuum drying technique to study the effect of different subliming agents with various concentrations on disintegrating time. The powder blend was examined for the pre-compressional parameters. The prepared formulations were evaluated for post-compressional analysis for the parameters like hardness, friability, thickness, wetting time, water absorption ratio, weight variation, in-vitro disintegration time, in- vitro dispersion time, in-vitro dissolution study. Drug compatibility with excipients was checked by FTIR studies. The results obtained showed that quantity of ammonium bicarbonate, urea and menthol significantly affect the response variables (P> 0.05). No chemical interaction between drug and excipients was confirmed by FTIR studies. Stability studies carried out as per ICH guidelines for three months and results revealed that upon storage disintegration time of tablets decreased significantly (P> 0.05). The results concluded that fast disintegrating tablets of felodipine showing enhanced dissolution rate with increasing the concentrations of subliming agents. Among all the formulations A3 and M3 shows the improved dissolution rate which lead to improved bioavailability and effective therapy by using vacuum drying technique.


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