scholarly journals Formulation and Evaluation of Liquisolid Compacts of BCS Class II Drug Ketoprofen

2021 ◽  
pp. 322-334
Author(s):  
Madhavi Kasturi ◽  
Neelesh Malviya
Keyword(s):  
Class Ii ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Dissolution Profile ◽  
Bcs Class Ii ◽  
Liquid Medication ◽  
Compact Formulation ◽  
Solubility Studies ◽  
Liquisolid Compacts

Aims: The main objective of the current research work is to develop liquisolid compacts of BCS Class II drug ketoprofen with an intention to enhance the solubility of drug by applying liquisolid technique. Place and Duration of Study: Smriti College of Pharmaceutical Education between June 2018 June 2019. Methodology: Initially liquid medication was obtained by dissolving drug in suitable solvent. Saturation solubility studies were performed in various hydrophilic non-volatile solvents to select the solvent showing highest solubility for drug. This liquid medication was admixed with calculated amounts of carrier material (Avicel PH 102) and coating material (Cab-O-Sil) using Spireas mathematical model in order to obtain liquisolid formulations. Further, this powder mass of liquisolid system was compressed to form Ketoprofen liquisolid compact formulations ranging from TK1 to TK9. They were further subjected to post compression evaluation tests such as weight variation, hardness, friability, content uniformity, disintegration and in vitro dissolution studies. Results: Based on the solubility studies, PEG 400 was selected as solvent for ketoprofen drug. Rheological properties for the prepared liquisolid powder system were performed for all the formulations and they showed acceptable flow properties. The results obtained for the post compression evaluation tests of all the prepared liquisolid compacts were present within the acceptable limits. The disintegration time observed for all formulations were within 5 minutes. The results of in vitro release of all the liquisolid compacts showed enhanced release rates compared to that of directly compressed tablet. Lquisolid compact formulation TK7 showed maximum release of 97.62% of drug within 12 minutes in pH 7.4 phosphate buffer which was much higher when compared to that of directly compressed tablet. The SEM and PXRD studies for TK7 revealed conversion of crystalline to molecularly dispersed form of drug in the obtained liquisolid formulation. DSC and FTIR studies also revealed that there was no presence of any significant interaction between drug and excipients involved in the formulation. Conclusion: Finally, it could be concluded that Liquisolid technique was successful in enhancing the solubility and further dissolution profile of BCS Class II drug Ketoprofen.

scholarly journals ENHANCEMENT OF SOLUBILITY AND BIOAVAILABILITY OF BCS CLASS-II AMBRISENTAN: IN VITRO, IN VIVO AND EX VIVO ANALYSIS

2022 ◽  
pp. 67-74
Author(s):  
RAHUL RADKE ◽  
NEETESH K. JAIN
Keyword(s):  
Solid Dispersion ◽  
Ex Vivo ◽  
Class Ii ◽  
Water Soluble ◽  
Pure Form ◽  
In Vitro Dissolution ◽  
Drug Solubility ◽  
Bcs Class Ii

Objective: The aim of this investigation was to enhance the solubility and bioavailability of the BCS class II poorly water-soluble drug ambrisentan by solid dispersion (SD) techniques using Gelucire 50/13 as a hydrophilic carrier. Methods: Solid dispersion of ambrisentan was prepared by kneading method using different dug: carrier ratios. Prepared SD was characterized for solubility, drug content, percentage yield, in vitro dissolution, ex vivo permeation and bioavailability. Solid-state characterization was performed by differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM). Results: All the SDs formulations showed increase in drug solubility and dissolution when compared with its pure form. Aqueous solubility of the drug was found to be increased 8.23 fold in SD. DSC study showed that endothermic peak of the drug was disappeared in spectra of SD, confirming its amorphous conversion, XRD study revealed the reduction to almost absence of specific high-intensity peaks of drug which confirmed the reduction of crysatallinity of ambrisentan in SD. SEM of optimized SD formulation demonstrates the complete encapsulation and solubilization drug. In vitro dissolution study showed that optimized SD formulation (ASD4) gives the faster drug release of 101.5% in 60 min, as compare to its pure form and other SD formulations. Conclusion: Solid dispersion ASD4 prepared with 1:4 drug to carrier ratio showed the highest drug solubility and in vitro dissolution. The ex vivo and in vivo studies performed on optimized formulation ASD4 showed enhancement in drug permeability and bioavailability in Gelucire 50/13 based SD formulation.

Prediction of oral absorption of griseofulvin, a BCS class II drug, based on GITA model: Utilization of a more suitable medium for in-vitro dissolution study

2007 ◽  
Vol 119 (2) ◽  
pp. 222-228 ◽  
Author(s):  
Yoshitsugu Fujioka ◽  
Keitaro Kadono ◽  
Yasuko Fujie ◽  
Yukiko Metsugi ◽  
Ken-ichi Ogawara ◽  
...  
Keyword(s):  
Oral Absorption ◽  
Class Ii ◽  
In Vitro Dissolution ◽  
Dissolution Study ◽  
Bcs Class Ii ◽  
Suitable Medium

scholarly journals STUDIES ON REFINED LIQUISOLID SYSTEM FOR SIMULTANEOUS IMPROVEMENT OF CONTENT UNIFORMITY AND DISSOLUTION PROFILE OF GLIMEPIRIDE

2019 ◽  
pp. 396-405
Author(s):  
Manish Dhall ◽  
Parmita Phaugat ◽  
Suchitra Nishal
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Xrd Analysis ◽  
Solvent System ◽  
In Vitro Dissolution ◽  
Time Interval ◽  
Content Uniformity ◽  
Dissolution Profile ◽  
Characteristic Analysis

Objective: To improve and compare dissolution contour of poorly soluble BCS Class II drug Glimepiride (GLD) by altering it to conventional solid dispersion (CSD), surface solid dispersion (SSD) and refined liquisolid system (RLS). Methods: The three formulations of GLD namely CSD, SSD and RLS were fabricated using the conventional methods by employing the suitable polymer and solvent system. These formulations were optimized on the basis of powder flow properties, FTIR, DSC and XRD analysis. All the optimized formulations were compared to the marketed formulation for content uniformity and dissolution rate. Results: The characteristic analysis of all the optimized formulations was obtained in the standard range. The average content uniformity (% age) of Marketed formulation, CSD, SSD and RLS found to be 88.28±0.721, 92.91±0.789, 95.98±0.478, 99.32±0.744 respectively. The in vitro dissolution rate  (%age at 30 min time interval) fall in the range 59.78±0.036, 75.78±0.013, 93.11±0.019, 93.99±0.062 and 98.55±0.043 for pure drug, Marketed formulation, CSD, SSD and RLS respectively. All the analytical studies exhibited improved homogeneity/distribution of the drug in RLS. Conclusion: The RLS formulation presented sheer expansion in the content uniformity and dissolution contour of GLD at a minimal cost.

scholarly journals Formulation and development of some BCS Class II drugs

2019 ◽  
Vol 9 (2) ◽  
pp. 321-329
Author(s):  
SC Marapur ◽  
Rakesh Kumar Jat ◽  
J S Patil
Keyword(s):  
Drug Release ◽  
Propylene Glycol ◽  
Class Ii ◽  
In Vitro Drug Release ◽  
Bcs Class Ii ◽  
Carrier Materials ◽  
Volatile Liquid ◽  
Liquisolid Compacts ◽  
Drug Solution

The aim of this research was to develop and evaluate liquisolid compacts of Ezetimibe a bcs class II drug. The series of formulations containing Ezetimibe drug were formulated by using aerosil a colloidal silicone dioxide and avicel PH microcrystalline cellulose in different ratios by using suitable solvent. Solubility studies were performed in propylene glycol and polyethylene glycol (PEG-200, 400, 600) for the choice of the best non volatile liquid to dissolve Ezetimibe. On the basis of the solubility data PG was chosen as a good solvent for the Ezetimibe. Ezetimibe was dissolved in solvent PG for the preparation of solution of drug. The coating and carrier materials transferred to the drug solution and added 5% of disintegrating agent (Croscarmellose) was mixed completely and the blend is compressed into compacts. Formulated compacts were evaluated for all post compression parameters and the in-vitro drug release study was carried out. All the formulations have shown a very good drug release in  15 min except compressibility problems due to higher812 loading factor of liquid vehicle for the formulations. The selected formulation F11 containing 30% of drug solution has  shown good drug release of 100.01% in 15  min compared to dissolution of  pure drug and marketed tablet which shown 45.5%  and 81.6 % respectively.No interactions were found  between drug and polymers in FITR as well as DSC. XRD of selected formulation shows that drug present in the formulation is in amorphous form. Keywords: Ezetimibe HCl, Avicel PH, Aerosil 200, Propylene glycol, liquisolid compacts

PERILAKU DISOLUSI KETOPROFEN DAN INDOMETASIN FARNESIL TERSALUT GEL KITOSAN-GOM GUAR

2012 ◽  
Vol 12 (1) ◽  
Author(s):  
Purwantiningsih Sugita ◽  
Bambang Srijanto ◽  
Budi Arifin ◽  
Fithri Amelia ◽  
Mahdi Mubarok
Keyword(s):  
Room Temperature ◽  
Guar Gum ◽  
Tween 80 ◽  
Chitosan Solution ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Magnetic Stirrer ◽  
Dissolution Behaviour ◽  
Shrimp Shell Waste

Chitosan, a modification of shrimp-shell waste, has been utilized as microcapsule. However, it’s fragile gel property needs to be strengthened by adding glutaraldehyde (glu) and natural hydrocolloid guar gum (gg). This research’s purposes were to study dissolution behaviour of ketoprofen and infar through optimum chitosan-guar gum microcapsule. Into 228.6 mL of 1.75% (w/v) chitosan solution in 1% (v/v) acetic acid,38.1 mL of gg solution was added with concentration variation of 0.35, 0.55, and 0.75% (w/v) for ketoprofen microcapsules and 0.05, 0.19, and 0.33% (w/v) for infar microcapsules, and stirred with magnetic stirrer until homogenous. Afterwards, 7.62mL of glu was added slowly under stirring, with concentrations varied: 3, 3.5, and 4% (v/v) for ketoprofen microcapsules, and 4, 4.5, and 5% (v/v) for infar microcapsules. All mixtures were shaked for 20 minutes for homogenization. All mixtures wereshaked for 20 minutes for homogenization. Into each  microcapsule mixture for ketoprofen, a solution of 2 g of ketoprofen in 250 mL of 96% ethanol was added, whereas solution of 100 mg of in 250 mL of 96% ethanol was added into each microcapsule mixture for infar. Every mixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Everymixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Conversion of suspension into fine powders/granules (microcapsules) was done by using spray dryer. The data of [gg], [glu], and medicine’s content from each microcapsule were treated with Minitab 14 software to obtain optimum [gg] and [glu] for microencapsulation. The dissolution behaviour of optimum ketoprofen and infar microcapsules were investigated. The result of optimization by using Minitab Release 14 software showed that among the microcapsule compositions of [gg] and [glu] were 0.35% (w/v) and 3.75% (v/v), respectively, optimum to coat ketoprofen, whereas [gg] and [glu] of 0.05% (w/v) and4.00% (v/v), respectively, optimum to coat infar, at constant chitosan concentration (1.75% [w/v]). In vitro dissolution profile showed that chitosan-guar gum gel microcapsule was more resistant in intestinal pH condition (rather basic) compared with that in gastric pH (very acidic).

Design, Optimization and Evaluation of Fast-Dissolving Oral Films of Ropinirole

2018 ◽  
Vol 11 (1) ◽  
pp. 3958-3967
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas A
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Good Alternative ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Peg 4000 ◽  
Oral Films

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

Biopharmaceutical and Preclinical Studies of Zaleplon as Semisolid Dispersions with Self-emulsifying Lipid Surfactants for Oral Delivery

1970 ◽  
Vol 9 (1) ◽  
pp. 3102-3111
Author(s):  
Narendar Dudhipala ◽  
Arjun Narala ◽  
Dinesh Suram ◽  
Karthik Yadav Janga
Keyword(s):  
Oral Delivery ◽  
Molecular State ◽  
In Vivo Studies ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Phase Solubility ◽  
Microscopic Studies ◽  
Pure Drug

The objective of this present study is to develop a semisolid dispersion (SSD) of zaleplon with the aid of self-emulsifying lipid based amphiphilic carriers (TPGS E or Gelucire 44/14) addressing the poor solubility of this drug. A linear relationship between the solubility of drug with respect to increase in the concentration of lipid surfactant in aqueous medium resulting in AL type phase diagram was observed from phase solubility studies. Fusion method was employed to obtain semisolid dispersions (SSD) of zaleplon which showed high content uniformity of drug. The absence of chemical interactions between the pure drug, excipients and formulations were conferred by Fourier transmission infrared spectroscopic examinations. The photographic images from polarized optical microscopic studies revealed the change in crystalline form of drug to amorphous or molecular state. The superior dissolution parameters of zaleplon from SSD over pure crystalline drug interpreted from in vitro dissolution studies envisage the ability of these lipid surfactants as solubility enhancers. Further, the caliber of TPGS E or Gelucire 44/14 in encouraging the GI absorption of drug was evident with the higher human effective permeability coefficient and fraction oral dose of drug absorbed from SSD in situ intestinal permeation study. In conclusion, in vivo studies in Wister rats demonstrated an improvement in the oral bioavailability of zaleplon from SSD over control pure drug suspension suggesting the competence of Gelucire 44/14 and TPGS E as conscientious carriers to augment the dissolution rate limited bioavailability of this active

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