scholarly journals Formulation and in vitro Evaluation of Spherical Crystal Agglomerates of Ebastine by Quasi Emulsion Solvent Diffusion Method

2018 ◽  
pp. 77-92
Author(s):  
Marwah Mohammed Hareeja ◽  
Eman B.H.Al-Khedairy
Keyword(s):  
Polyethylene Glycol ◽  
Dissolution Rate ◽  
Water Soluble ◽  
Crystal Habit ◽  
Diffusion Method ◽  
Scanning Calorimetry ◽  
Solvent Diffusion ◽  
Peg 4000 ◽  
Spherical Crystal

Ebastine (EBS) is a poorly water-soluble antihistaminic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS). The aim of the present work was to enhance the solubility, dissolution rate and micromeritic properties of the drug, by formulating it as spherical crystal agglomerates by Quasi Emulsion Solvent Diffusion (QESD) method. Spherical crystal agglomerates (SCAs) were prepared in presence of three solvents dichloromethane (DCM), water and chloroform as a good solvent, poor solvent and bridging solvent respectively.  Agglomeration of EBS involved the use of some hydrophilic polymers like polyethylene glycol 4000 (PEG 4000), polyvinyl pyrrolidine K30 (PVP K30), D-?-tocopheryl polyethylene glycol 1000 succinate (TPGS) and ?. cyclodextrin. The pure drug (EBS) and its agglomerates with and without polymers were characterized for their drug content, percentage yield, solubility, in vitro drug release study and micromeritic property as well as by optical microscope, Scanning Electron Microscopy (SEM), FTIR spectroscopic studies, Differential Scanning Calorimetry (DSC) and X-ray Diffraction (XRD). The results of this work showed that there was a   marketed enhancement in the solubility with improvement in dissolution rate, physiochemical properties, decrease in crystallinity and alteration in the crystal habit of the drug especially in presence of polymers. The best results were obtained with formula prepared by the combination of PEG 4000 and ?. cyclodextrin in the agglomeration process of (EBS).

scholarly journals Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate

2016 ◽  
Vol 52 (1) ◽  
pp. 1-13 ◽  
Author(s):  
Ehsan Adeli
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Polyethylene Glycols ◽  
X Ray Diffraction ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Peg 4000 ◽  
Poorly Soluble

ABSTRACT Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical mixtures of azithromycin were made using PEG 4000, 6000, 8000, 12000 and 20000 in various ratios, based on the solvent evaporation method. From the studied drug release profile, it was discovered that the dissolution rate of the physical mixture, as the well as the solid dispersions, were higher than those of the drug alone. There was no chemical incompatibility between the drug and polymer from the observed Infrared (IR) spectra. Drug-polymer interactions were also investigated using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Election Microscopy (SEM). In conclusion, the dissolution rate and solubility of azithromycin were found to improve significantly, using hydrophilic carriers, especially PEG 6000.

scholarly journals DEVELOPMENT AND IN VITRO DISSOLUTION STUDY OF BINARY AND TERNARY SOLID DISPERSIONS OF ACECLOFENAC

2019 ◽  
Author(s):  
Md. Shahidul Islam ◽  
Rasheda Akter Lucky
Keyword(s):  
Polyethylene Glycol ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Peg 6000

The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.

scholarly journals Development and Characterization of Metronidazole Loaded Microsponges for the Management of Diabetic Foot

2021 ◽  
Vol 8 (10) ◽  
pp. 440-457
Author(s):  
Ponni Sujathan ◽  
Umesh Kumar Sharma
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Diabetic Foot ◽  
Particle Size Analysis ◽  
Diffusion Method ◽  
Size Analysis ◽  
Poly Vinyl Alcohol ◽  
Scanning Calorimetry ◽  
Solvent Diffusion

The objective of present work was formulation and evaluation of Metronidazole loaded microsponges for the management of diabetic foot ulcer via topical application and to reduce side effects. The microsponges were prepared by quasi-emulsion solvent diffusion method using different concentrations of Ethyl cellulose and Poly vinyl alcohol. The prepared microsponges were evaluated for particle size analysis, SEM, % production yield, % drug entrapment efficiency, in-vitro drug release studies, DSC and antimicrobial studies. FTIR studies shown that there was no interaction between drug and polymers. The optimum sustained release of drug around a period of 12hrs was shown by formulation F8. The n value of optimized formulation indicated that the drug release followed zero order kinetics. It was confirmed from the stability studies that the optimized formulation remained stable at 45±2℃ and 70±5% relative humidity. Keywords: Microsponges, Metronidazole, Diabetic Foot, Quasi-emulsion solvent diffusion, Sustained release, Scanning electron microscopy, Differential scanning calorimetry.

DEVELOPMENT OF SOLID DISPERSION TABLET OF CARVEDILOL TO IMPROVE SOLUBILITY

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 54-59
Author(s):  
S. S Shelake ◽  
◽  
R. G Gaikwad ◽  
S Patil ◽  
F. I. Mevekari ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Media ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Water Soluble Drugs ◽  
Ft Ir

Crystalline state compounds are typically dissolution rate limited and dissolution rate is directly proportional to the solubility for BCS class II or class IV compounds. Solid dispersions are one of the most promising strategies to improve the oral bioavailability poorly water soluble drugs. The purpose of this study was to increase solubility of carvedilol by solid dispersion (SDs) technique with Poloxamer (PXM) 407 in aqueous media. The carvedilol- PXM 407 solid dispersion was prepared by solvent evaporation, kneading and melting method. It was characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), Fourier transformation infra-red spectroscopy (FT-IR), scanning electron microscopy (SEM) and in vitro dissolution studies. The prepared solid dispersion were found to have higher dissolution rates as compared to intact carvedilol. During formulation of solid dispersion crystalline to amorphous transition has been observed.

scholarly journals THE DEVELOPMENT OF GLIBENCLAMIDE-SACCHARIN COCRYSTAL TABLET FORMULATIONS TO INCREASE THE DISSOLUTION RATE OF THE DRUG

2019 ◽  
pp. 359-364 ◽  
Author(s):  
ARIF BUDIMAN ◽  
PATIHUL HUSNI ◽  
SHAFIRA ◽  
Tazyinul Q. Alfauziah
Keyword(s):  
Dissolution Rate ◽  
Dosage Form ◽  
Water Soluble ◽  
Crystal Habit ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Grinding Method ◽  
Water Soluble Drugs ◽  
Rate Test ◽  
Tablet Dosage

Objective: Cocrystallisation is a promising method in order to increase the solubility and dissolution of poorly water-soluble drugs. The aim of this study was to prepare, formulate and evaluate glibenclamide (GCM) cocrystal in direct compress tablet dosage form using saccharin (SAC) as the coformer. Methods: GCM cocrystal with various stoichiometric ratios were prepared by the solvent drop grinding method. The co-crystal was characterized by a saturated solubility test and dissolution rate test, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Powder X-Ray Diffraction (PXRD). The tablet dosage form of GCM was formulated and evaluated compare with the conventional dosage form. Results: The solubility and disso­lution rate of GCM-SAC cocrystals increased significantly compared with pure GCM, especially for 1:2 of ratio. The dissolution rate of cocrystal with ratio 1:2 increased by almost 91.9% compared with pure GCM. Based on the FTIR analysis, it showed the shifting of characteristic bands of GCM in the spectrum and there was no chemical reaction in GCM cocrystal. In PXRD measurement, the new crystalline peak was detected in the crystal habit of cocrystal compared with pure GCM and coformer. The new single melting of GCM-SAC cocrystal also was detected in DSC measurement. The tablets of GCM-SAC cocrystal were successfully prepared by direct compression method which rapidly disintegrated (1 min) and has higher dissolution compared with its pure form (32.36% greater than glibenclamide after 45 min). Conclusion: The tablet dosage form of GCM cocrystal with SAC as coformer was successfully prepared, formulated and improved its solubility and dissolution rate.

scholarly journals PREPARATION AND IN VITRO EVALUATION OF LACIDIPINE ORAL LIQUID SOLID TABLET AS AN APPROACH OF SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT

2018 ◽  
Vol 10 (1) ◽  
pp. 145
Author(s):  
Nawal Ayash Rajab
Keyword(s):  
Dissolution Rate ◽  
Chemical Interaction ◽  
Liquid Paraffin ◽  
Physical Mixture ◽  
Water Soluble ◽  
Tween 20 ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Volatile Solvents

Objective: The aim of the present study was to prepare a new liquid-solid tablet to enhance the dissolution and bioavailability of a poor water soluble calcium channel blocker lacidipine.Methods: Firstly, solubility study of lacidipine in different media of water-miscible non-volatile solvents as tween 20, tween 80, propylene glycol, liquid paraffin, PEG200, PEG400, and PEG600 was investigated to select the most suitable solvent. A mathematical model was applied to calculate the appropriate amount of carrier and coating material.Four liquid-solid tablets of 6 mg lacidipine were prepared by dissolving the drug in the previously chosen water miscible non-volatile solvents, then a binary mixture of the carrier (Avicel PH 102) and coating material (Aerosil 200) at a ratio of 45:1 was used in all preparation since it gave the optimal flow property. Croscarmellose and magnesium stearate were incorporated in all prepared formulas as super disintegrant and lubricant respectively. On the other hand, directly compressed lacidipine tablet of the same previous composition without the addition of any non-volatile solvent was prepared for comparism study. Both characterizations of powder mixture and post-compression tablet evaluations were done. Differential scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FTIR) were investigated for the pure drug, physical mixture, and selected liquid-solid tablet to exclude any drug-excipients interaction.Results: The obtained results indicated that PEG 200 was the most suitable solvent with lacidipine solubility of 2.81 mg/ml. Flowability of all the prepared formulas was found to be within the specification limits. The liquid-solid tablet formula with PEG 200 at 10% w/w lacidipine was the most suitable one in the term of disintegration time (21±0.2 second), 100% of drug release within 10 min, and with accepted other tablet properties.DSC thermograms for both physical mixture of selected liquisolid system and its tablets illustrated the formation of lacidipine amorphous solid solution. The absence of chemical interaction between drug and other formula components was confirmed by remaining all characteristic peaks of lacidipine in all investigated FTIR spectra.Conclusion: Liquid-solid tablet was considered as a promising system to enhance solubility and dissolution rate of poor-water soluble lacidipine. 

scholarly journals FORMULATION AND EVALUATION OF LIQUISOLID COMPACTS OF LORNOXICAM

2019 ◽  
pp. 33-37
Author(s):  
Asma Azaruddin Mokashi ◽  
SNEHALATA L. GAIKWAD
Keyword(s):  
Dissolution Rate ◽  
Drug Concentration ◽  
In Vitro Release ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Spectra Analysis ◽  
X Ray ◽  
Liquisolid Compacts

Objective: Objective of the present investigation was to enhance the solubility and dissolution rate of poorly water-soluble drug lornoxicam using liquisolid technique with comparative determination of in vitro release profile of liquisolid compacts and conventional formulation of lornoxicam. Methods: Formulation was prepared by a liquisolid technique using different drug concentration in a liquid vehicle and different carrier/coating ratio. Prepared liquisolid compact was evaluated for Fourier transform infrared (FTIR) spectra analysis, differential scanning calorimetry (DSC), X-ray diffraction (P-XRD), scanning electron microscopy (SEM) and in vitro dissolution study. Results: The result showed that liquisolid compacts of lornoxicam displayed significantly higher drug release rate as compared to pure drug and conventional tablet prepared. The results of both DSC and X-ray crystallography indicated loss of crystallinity of the drug upon formulated into the liquisolid compact. Conclusion: Dissolution rate of the drug from liquisolid compacts was affected by changing the drug concentration and excipient ratio. The liquisolid technique appeared to be a promising approach for improving the dissolution of poorly soluble drug lornoxicam.

scholarly journals IN VITRO DISSOLUTION STUDY OF GLIMEPIRIDE FROM BINARY AND TERNARY SOLID DISPERSION FORMULATION

2019 ◽  
Author(s):  
Sharmin Akhter ◽  
Md. Sajjad Hossen ◽  
Md. Salahuddin ◽  
Muazzem Ahmed Sunny ◽  
Farzana Akther Sathi ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Peer Review ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Peg 4000 ◽  
Ternary Solid Dispersion ◽  
E Mail

Glimepiride (GMP) is poorly water soluble drug, so solubility is the main constraint for its oral bioavailability. Because, poor aqueous solubility and slow dissolution rate of the glimepiride lead to irreproducible clinical response or therapeutic failure in some cases due to sub therapeutic plasma drug levels. In this study, binary and ternary solid dispersion of glimepiride were prepared with polyethylene glycol 6000 (PEG 6000) and polyethylene glycol 4000 (PEG 4000) at different weight ratios using the solvent evaporation and melting method. It was found the drug was released 0.46% after 5 minutes and only 15.83% within 60 minutes from active glimepiride on the other hand the release pattern of glimepiride from the binary formulation containing PEG 4000 in 1:5 (Formulation coding: G5) showed the best result. It was found that the ternary different SD formulation containing(PEG4000:Glimepiride:Povidone) In ratio 1:1:0.25 (Formulation coding were : G13) showed the best result. The drug was changed to amorphous form after solid dispersion. Itwas also evident that solid dispersions improve solubility of drug particles thus enhancing dissolution characteristics of drugs they increase the oral bioavailability. Peer Review History: UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file Average Peer review marks at initial stage: 4.5/10 Average Peer review marks at publication stage: 7.5/10 Reviewer(s) detail: Name: Dr. Mohammed Abdel-Wahab Sayed Abourehab  Affiliation: Umm Al-Qura University;  Makkah Al-Mukarramah, Saudi Arabia E-mail: [email protected]   Name: Dr. Evren Alğin Yapar Affiliation: Turkish Medicines and Medical Devices Agency, Turkiye E-mail: [email protected] Comments of reviewer(s):

scholarly journals ENHANCEMENT OF THE SOLUBILITY AND THE DISSOLUTION RATE OF CANDESARTAN CILEXETIL USING MICROSPONGE TECHNOLOGY

2018 ◽  
Vol 11 (9) ◽  
pp. 385 ◽  
Author(s):  
Shaimaa Nazar Abd Alhammid
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Candesartan Cilexetil ◽  
Water Soluble ◽  
Production Yield ◽  
Diffusion Method ◽  
Scanning Calorimetry ◽  
Ftir Study ◽  
Loading Efficiency ◽  
Physical Mixtures

Objective: The aim of the present study is to enhance the dissolution rate of candesartan cilexetil (CC) using microsponges. Candesartan is therapeutically a potent antihypertensive agent, but it suffers a major drawback of poor oral bioavailability, which is estimated to be 15% due to its low solubility in the gastrointestinal fluids and hepatic first-pass metabolism.Methods: Eudragit-based microsponges were prepared by quasi-emulsion solvent diffusion method using different drug–polymer ratios (1:1 to 1:6), stirring speeds (250–750 rpm), and emulsifier concentrations (polyvinyl alcohol) (0.05%–0.083% w/v). Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) study for CC, physical mixtures of drug–polymer, and selected formula were investigated to estimate compatibility of CC with other used ingredients. All formulations were evaluated for particle size, production yield, and loading efficiency. The in vitro drug release study of optimized formulation was performed in phosphate buffer pH 6.8.Results: The obtained results indicated that formula F3 which contains eudragit RS100 at drug:polymer ratio (6:1) was showed the smallest particle size with higher production yield and loading efficiency. DSC and FTIR study of the physical mixtures of drug and polymer revealed no drug–polymer interaction. The results clearly confirm that the percentage of CC released at 30 min from F3, CC powder, and self-made tablet was 54%, 20.325, and 38.9%, respectively.Conclusion: Microsponges technique was considered as a promising system to enhance the solubility and dissolution rate of poor-water soluble CC.

Formulation and Evaluation of Nanosuspension Delivery System for Simvastatin

2014 ◽  
Vol 7 (2) ◽  
pp. 2459-2475 ◽  
Author(s):  
Rupali Shid L. ◽  
Shashikant N. Dhole ◽  
Nilesh Kulkarni ◽  
Santosh L. Shid L.
Keyword(s):  
Zeta Potential ◽  
Dissolution Rate ◽  
Water Soluble ◽  
In Vivo Study ◽  
Diffusion Method ◽  
Total Drug ◽  
Poloxamer 188 ◽  
Drug Content

Poor water solubility and slow dissolution rate are issues polydispersity index. The obtained results showed that for the majority of upcoming and existing biologically active  particlesize (nm) and rate of dissolution has been improved compounds. Simvastatin is poorly water-soluble drug and  when nanosuspension prepared with the higher its bioavailability is very low from its crystalline form. The  concentration of PVPK-30 with the higher concentration of purpose of the present investigation was to increase the  PVP K-30 and Poloxamer-188 and lower concentration of solubility and dissolution rate of simvastatin by the  SLS. The partical size and zeta potential of optimized preparation of nanosuspension by Emulsification Solvent  formulation was found to be 258.3 nm and 23.43. The rate Diffusion Method at laboratory scale. Prepared nanosus- of dissolution of the optimized nanosuspension was pension was evaluated for its particle size and in vitro  enhanced (90.02% in 60 min), relative to plain simvastatin dissolution study and characterized by zeta potential, (21% in 60 min), mainly due to the formation of nanosized differential scanning calorimetry (DSC) and X-Ray particles. These results indicate the suitability of 23 factorial diffractometry (XRD), motic digital microscopy, entrapment  design for preparation of simvastatin loaded efficiency, total drug content, saturated solubility study and nanosuspension significantly improved in vitro dissolution in vivo study. A 23 factorial design was employed to study  rate, and thus possibly enhance fast onset of therapeutic the effect of independent variables, amount of SLS (X1), drug effect. In vivo study shows increase in bioavailability in amount of PVPK-30 (X2) and Poloxamer-188 (X3) and  nanosuspension formulation than the plain simvastatin dependent variables are total drug content and drug. 

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