scholarly journals Comparative Evaluation of Amorphous Polymers in Solubility and Bioavailability Enhancement of Famotidine Through Solid Dispersion

2021 ◽  
Author(s):  
Ankit Mishra ◽  
Priyanka Chaturvedi ◽  
Pranali Mishra ◽  
MS Sudheesh
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Milk Powder ◽  
Amorphous Polymers ◽  
Dissolution Enhancement ◽  
Study Results ◽  
Xrd Studies

The present study aimed to enhance the dissolution rate, therefore bioavailability, of famotidine (FMT) using its solid dispersions (SDs) with polyvinyl pyrrolidone (PVP)-K 30, milk powder, and inulin, both in-vitro and in-vivo. The study was also aimed to compare the effect of different amorphous polymers in enhancing the dissolution rate of FMT. The SDs were prepared with a 1:4 weight ratio by a solvent evaporation technique. Evaluation of the properties of the SDs was performed using dissolution, Fourier-transform infrared (FTIR) spectroscopy, and X-ray diffraction (XRD) studies. The SDs of FMT exhibited an enhanced dissolution rate. The FTIR spectroscopic studies showed the stability of FMT and the absence of well-defined drug excipient interaction. The XRD studies indicated the amorphous state of FMT in SDs. The drug release rate of all SDs formulation was found to be greater than the pure drug. Within one hour of dissolution studies, 99.43%, 92.5%, and 58.93% drug release were obtained, respectively, for PVP K-30, milk powder, and inulin. The first two were showing significantly higher release. SDs were also studied for bioavailability studies in-vivo in rats, which confirms that the SDs prepared by PVP K-30 and milk powder significantly enhancing the bioavailability of FMT. The maximum concentration of 15.05±2.45 μg/ml was achieved in 2 hours, and the area under the curve was found to be 33.78±7.3 μg. hour/ml. Therefore, the study results conclude that SDs of the FMT prepared by PVP K-30 successfully increases the dissolution and in-vivo bioavailability. Keywords – Solid dispersion, Second generation solid dispersions, Famotidine, In-vivo bioavailability, amorphous polymers, dissolution enhancement, solubility enhancement.

scholarly journals Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

scholarly journals EFFECT OF CARRIER TYPES ON THE PHYSICOCHEMICAL AND DISSOLUTION CHARACTERISTICS OF OFLOXACIN SOLID DISPERSION

2002 ◽  
Vol 70 (3) ◽  
pp. 309-316
Author(s):  
Okonogi S ◽  
Sirithunyalung J ◽  
Sirithunyalig B ◽  
Wolschann P ◽  
Viernstein H
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Weight Fraction ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Water Soluble Polymers ◽  
Dissolution Properties ◽  
Peg 4000

Solid dispersions of ofloxacin (OFX) and of a number of carriers including chitosan and the water soluble polymers polyethylene glycol (PEG) 4000, PEG 20000, and polyvinylpyrrolidone K- 90 were prepared by solvent evaporation method in order to increase the dissolution of the drug. The solid dispersions were subjected to X-ray diffraction, DSC, and dissolution to characterize their physicochemical and dissolution properties. The results demonstrated a decrease in drug crystallinity at higher amounts of carrier. Dissolution studies indicated that the dissolution rate of OFX was markedly increased in these solid dispersion systems compared with the pure drug. The results also showed that the increase in dissolution rate was higher when the weight fraction of carriers increased. An influence of molecular weight of PEG on OFX dissolution could also be observed. In solid dispersion with 1:9 ratio drug to carrier, PEG 4000 gave highest drug dissolution rate, whereas in 1:1 ratio, chitosan seems to be the best carrier for drug release. It was concluded that chitosan might be the carrier of choice for dissolution enhancement in solid dispersions with high content of drug.

scholarly journals Effect of Amphiphilic Graft Co-Polymer Carrier on Solubility and Dissolution Enhancement of Ambrisentan

2021 ◽  
pp. 329-338
Author(s):  
Rahul Radke ◽  
Neetesh K. Jain
Keyword(s):  
Ftir Spectroscopy ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Polymer Carrier ◽  
Dissolution Study

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.

scholarly journals Design expert assisted mathematical optimization of solubility and study of fast disintegrating tablets of Lercanidipine Hydrochloride

2019 ◽  
Vol 9 (1-s) ◽  
pp. 172-180
Author(s):  
Seema Saini ◽  
Rajeev Garg
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Mathematical Optimization ◽  
Statistical Design ◽  
In Vivo Studies ◽  
Dissolution Profile ◽  
Fast Disintegrating Tablets ◽  
Lercanidipine Hydrochloride

90% of drugs being researched today, posses poor solubility setback which inturn renders  the drug with slower rate of absorption from the buccal route; hence dissolution is the rate limiting step for such lipophilic drugs. So, there is a need to keep a check on the dissolution profile of these drugs to ensure maximum therapeutic utilization. The dissolution rate therefore becomes a primary factor which governs the rate and extent of its absorption. Enormous work is being performed in the field of enhancement of solubility and dissolution behaviour of such drugs. Advancements and innovations have developed solid dispersion (SD) technique as the novel method for the solubility enhancement. Precision of dosing and patient's compliance is a crucial prerequisite for the management of chronic Antihypertensive treatment, So there arised a need to formulate a system which should resolve the difficulties associated with conventional tablets. This issue can be better tackled with the formulation of orally fast disintegrating tablets. The aim of the present study was to improve the solubility and dissolution rate of Lercanidipine hydrochloride (LRH) by formulating a solid dispersion with Polyvinyl pyrollidine (PVP-K30) and Guargum. Full Factorial designs are exploited to learn and research the effects of different variables on the quality determinant parameters. An appropriate statistical model was selected for the scrutiny of the enhanced dissolution pattern. Finally, these solid dispersions were incorporated into fast disintegrating tablets. Keywords: Lercanidipine Hydrochloride, Solid dispersion, Statistical design approach, Melt fusion method, Fast disintegrating tablet, In vivo studies

Optimization and Evaluation of Orodispersible Solid Dispersion Tablet of Ketotifen Fumarate

2021 ◽  
pp. 3610-3616
Author(s):  
Zeina D Salman
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Fusion Method ◽  
Disintegration Time ◽  
Solubility Study ◽  
Ketotifen Fumarate ◽  
Orodispersible Tablets

The present study was aimed to integrate the developed and optimized ketotifen fumarate dispersion into Orodispersible tablets formulations, to enhance the dissolution rate and bioavailability aspects of the drug. Ketotifen fumarate solid dispersion was prepared using different concentrations of poloxamer 407via solvent evaporation and fusion method. Solubility study, x-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR) and other investigations were done. Ten formulations of the optimum dispersed ketotifen fumarate Orodispersible tablets were prepared with various superdisintegrants, the results of in vitro - in vivo tests revealed that, the dispersion of the drug in the polymer considerably enhanced the solubility, the batch (Fsd 3) prepared by fusion method showed increased the solubility as ~2-fold compared with a pure drug. FTIR spectra, SEM and XRD data, showed amorphrization of ketotifen fumarate, which explains the better dissolution rate of the drug from its solid dispersions. Formulation F1 containing 15%w/w of crospovidone was showed in vitro- in vivo disintegration time (17 sec., 15 sec. respectively) and percent of drug dissolved in 2 min. was 90.04%, proved to be the optimum formulation, which is required for obtaining rapidly disintegrating tablets. The solubility of the drug had increased, and the resultant orodispersible tablets can be considered as a promising dosage form to achieve better patient compliance.

scholarly journals Formulation and Physicochemical Characterization of Cyclosporine Microfiber by Electrospinning

2019 ◽  
Vol 9 (2) ◽  
pp. 249-254
Author(s):  
Shahla Mirzaeei ◽  
Ghobad Mohammadi ◽  
Navid Fattahi ◽  
Pardis Mohammadi ◽  
Ali Fattahi ◽  
...  
Keyword(s):  
Drug Release ◽  
Physicochemical Properties ◽  
Dissolution Rate ◽  
Water Soluble ◽  
Crystalline Lattice ◽  
Drug Dissolution ◽  
Absolute Bioavailability ◽  
Study Results ◽  
Pure Drug

Purpose: The objective of this study was to improve the permeability and water solubility rate of a poor water soluble drug, cyclosporine A (CsA). Methods: In order to improve the drug dissolution rate and oral bioavailability, electrospinning method was used as an approach to prepare. The fibers were evaluated for surface morphology, thermal characterizations, drug crystallinity, in vitro drug release and in vivo bioavailability studies. Results: Scanning electron microscope (SEM) results confirmed that the fibers were in microsize range and the size of the fibers was in the rang of 0.2 to 2 micron. Differential scanning calorimetry (DSC) and powder X-ray diffractometry (XRPD) analysis ensured that the crystalline lattice of drug were weakened or destroyed in the fibers. The drug release was 15.28%, 20.67%, and 32.84% from pure drug, fibers of formulation B, and formulation A, respectively. In vivo study results indicated that the bioavailability parameters of the optimized fiber formulation were improved and the maximum concentration (Cmax) were significantly higher for fibers (3001 ng/mL) than for pure drug (2550 ng/mL). The dissolution rate of the formulations was dependent on the nature and ratio of drug to carriers. Conclusion: The physicochemical properties showed that the optimized mixture of polyethylene glycol (PEG) and povidone (PVP) fibers could be an effective carrier for CsA delivery. PEG and PVP fibers improved the absolute bioavailability and drug dissolution rate with appropriate physicochemical properties.

It is Possible to Achieve Tablets with Good Tabletability from Solid Dispersions – the Case of the High Dose Drug Gemfibrozil

2020 ◽  
Vol 17 ◽  
Author(s):  
Eduarda Rocha Bigogno ◽  
Luciano Soares ◽  
Matheus Henrique Ruela Mews ◽  
Melissa Zétola ◽  
Giovana Carolina Bazzo ◽  
...  
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Croscarmellose Sodium ◽  
Poorly Water Soluble

Background: Solid dispersions (SDs) have been extensively used to increase dissolution of poorly water-soluble drugs. However, there are few studies exploring SDs properties that must be considered during tablet development, like tabletability. Poorly water-soluble drugs with poor compression properties and high therapeutic doses, like gemfibrozil, are an additional challenge in the production of SDs-based tablets. Objective: This study evaluates the applicability of SDs to improve both tabletability and dissolution rate of gemfibrozil. A SD-based tablet formulation was also proposed. Method: SDs were prepared by ball milling, using hydroxypropyl methylcellulose (HPMC) as carrier, according to a 23 factorial design. The formulation variables were: gemfibrozil:HPMC ratio, milling speed, and milling time. The response in the factorial analysis was the tensile strength of the compacted SDs. Dissolution rate and solid-state characterization of SDs were also performed. Results: SDs showed simultaneous drug dissolution enhancement and improved tabletability when compared to corresponding physical mixtures and gemfibrozil. The main variable influencing drug dissolution and tabletability was the gemfibrozil:HPMC ratio. Tablets containing gemfibrozil-HPMC-SD (1:0.250 w/w) and croscarmellose sodium showed fast and complete drug release while those containing the same SD and sodium starch glycolate exhibited poor drug release due to their prolonged disintegration time. Conclusion: SDs proved to be effective for simultaneously improving tabletability and dissolution profile of gemfibrozil. Tablets containing gemfibrozil-HPMC-SD and croscarmellose sodium as disintegrating agent showed improved drug release and good mechanical strength, demonstrating the potential of HPMC-based SDs to simultaneously overcome the poor dissolution and tabletability properties of this drug.

Development and Evaluation of Fast Disintegrating Tablets of Lornoxicam Solid Dispersions

2019 ◽  
Vol 12 (4) ◽  
pp. 4585-4592
Author(s):  
Hafsa Mohammadi ◽  
Hemanath Kumar V ◽  
Roshan S ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Statistical Significance ◽  
Solid Dispersions ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Weight Variation ◽  
Fast Disintegrating Tablets

Lornoxicam is a nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class. It belongs to BCS class II substance with low solubility and high permeability. The aim of current research is to formulate solid dispersion incorporated Fast disintegrating tablets of Lornoxicam to enhance the dissolution rate and aqueous solubility and to enable faster onset of action. Solid dispersions are prepared with polymers like Kolliwax GMS, Soluplus and HPMC in three different ratios 1:1:1, 1:2:1 and 1:3:1. Formulations were characterized for drug content studies, drug release studies, and drug-polymer interactions using Fourier transform infrared spectroscopy (FTIR) spectrum. The solid dispersions can be evaluated by in-vitro dissolution studies. The optimized solid dispersion SD9 was further used to prepare fast disintegrating tablet by direct compression method using 33 Response surface method (3 variables and 3 levels of superdisintegrants) by using Design of experiment software with superdisintegrants like locust bean gum, gum karaya, Plantago ovata. The values of pre-compression parameters evaluated were within prescribed limits that indicated good free flowing properties. The data obtained of post-compression parameters such as weight variation, hardness, friability, content uniformity, disintegration time (33 sec) and percentage drug release was maximum in LF24 (99.21±1.87%) within 10 minutes and was found to superior over Marketed formulation i.e., 87.27±0.27 %. From in vivo bioavailability studies the best formulation has shown Tmax of 1.0 h which was highly significant (P < 0.05) when compared with marketed formulation 2.5 h. The statistical significance was assessed by one-way analysis of variance. Therefore, the solid dispersions incorporated fast disintegrating tablets of Lornoxicam can be successfully used for improvement of dissolution, resulted in faster onset of action as indicated by in vivo studies. It can be concluded that fast disintegrating tablets using Lornoxicam solid dispersion could be used to improve better patient compliance with immediate action in the effective management of pain and inflammation.

scholarly journals Dissolution enhancement of poorly soluble drug by solvent evaporation method using hydrophilic polymer: a solid dispersion technique

2012 ◽  
Vol 1 (2) ◽  
Author(s):  
Md Armin Minhaz ◽  
Md Mofizur Rahman ◽  
Md Qamnul Ahsan ◽  
Abul Bashar Ripon Khalipha ◽  
Mohammed Raihan Chowdhury
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Dissolution Enhancement ◽  
Solvent Evaporation Method ◽  
Peg 6000 ◽  
Evaporation Method ◽  
Poorly Soluble ◽  
Pure Drug

In order to investigate the effect of polymers on release mechanism of poorly soluble drugs from solid dispersions, Clonazepam was used as a model drug for these purposes. Five types of solid dispersions were prepared using polyethylene glycol 6000 (PEG- 6000), Kollicoat IR, Kollidon VA 64 and Poloxomer in different drug-tocarrier ratios (1:2, 1:4, 1:6, 1:8, 1:10). The solvent evaporation method was used for preparation of solid dispersions. The in-vitro dissolution study with temperature of 37° C and a paddle method, 100 rpm was used in 1000 ml of distilled water as dissolution medium in each dissolution basket for the pure drug and solid dispersions. For pure Clonazepam showed very slow dissolution rate and the solid dispersion considerably enhanced the dissolution rate. Decreased crystalline and increased amorphous fraction of the drug was probably done by wettability and dispersibility. The highest improvement in wettability and dissolution rate of Clonazepam was observed in PEG-6000, Poloxomer and Kollidon VA 64 (1:10 ratio). Solid dispersions containing polymer (1:10 ratio) prepared by solvent method showed significant improvement in the release profile as compared to pure drug, Clonazepam. DOI: http://dx.doi.org/10.3329/ijpls.v1i2.12952 International Journal of Pharmaceutical and Life Sciences Vol.1(2) 2012

Formulation and Evaluation of Flurbiprofen Solid Dispersions Incorporated Buccal Patches

2020 ◽  
pp. 674-681
Author(s):  
Mohammed Jaffer Sadik ◽  
Abdulla Khan
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Release ◽  
Solid Dispersion ◽  
Release Kinetics ◽  
Solid Dispersions ◽  
Methyl Cellulose ◽  
Sustained Drug Release ◽  
Casting Technique ◽  
Zero Order Release

Flurbiprofen is an anti-inflammatory drug used in treating rheumatoid arthritis and ankylosing spondylitis. The present work is aimed at overcoming the deprived solubility of flurbiprofen by solid dispersion (SD) technique. The current paper is  the continuance of the published solid dispersion by considering the best final optimized formulation containing flurbiprofen drug: AQOAT AS: SLS as drug: polymer: surfactant in 1:5:2 ratios, and incorporating it into buccal patches to overcome the gastric side effect and attaining  sustained drug release. In this study 15 buccal patches  were formulated  by adopting  solvent casting technique  using polymers like polyvinyl hydroxyethylcellulose (HEC), hydroxypropryl methyl cellulose E15 (HPMC E15), polyvinyl pyrrolidone (PVP), carbopol and analyzed  for the drug content, drug  diffusion, in-vivo dissolution  and stability studies. All SD loaded patches displayed superior drug release (95% to 99.96%) over 12 h. The formulation BP14 showed excellent drug release extended over 12 h with drug release of 99.96% whereas marketed formulation which is sustained release Tablet showed 96.86% drug release within 6 h. The drug release kinetics show that the buccal patches follow zero order release kinetics with correlation coefficient (R2) ranging between 0.905-0.971 and BP14 formulation shown best R2 value. All the formulations exhibited best fit to Higuchi model with R2 ranging between 0.9911 – 0.9962 indicating drug release by diffusion process. The results conclude that buccal patches are superior alternatives for flurbiprofen that facilitates enhanced drug release for prolonged period of time in the effective management of rheumatoid arthritis.

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