DEVELOPMENT AND EVALUATION OF LAMOTRIGINE SOYA LECITHIN SOLID DISPERSION: IN VITRO AND PHARMACODYNAMIC INVESTIGATION

Objective: Epilepsy is a common neurodegenerative disorder characterized by spontaneous and repeated attacks of convulsions. It requires immediate pharmacotherapy to prevent its progression to status epilepticus. However, most of the anticonvulsant drugs are poorly water-soluble and demonstrate the delayed onset of action. Thus there is a need to improve its solubility for the better pharmaceutical profile. The objective of the present investigation was to enhance the solubility of lamotrigine incorporating soya lecithin as a phospholipid carrier by solid dispersion technique Methods: Solid dispersions of lamotrigine were prepared with soya lecithin by the solvent method. The effect of concentration of phospholipid and solvents on aqueous solubility and dissolution profile of lamotrigine was analyzed. Results: Ethanol increased lamotrigine solubility with soya lecithin in ratio 5:1. X-ray diffraction and scanning electron micrograph indicated a smaller crystallite size of lamotrigine with fairly uniform size distribution in the lamotrigine-soya lecithin solid dispersion. The resultant solid dispersion also significantly delayed the onset of clonic convulsion (875.8 s) as compared to control (85.5 s) and offered complete protection (100%) against the pentylenetetrazole induced seizures in the rat as compared to control (33.33%). Also, solid dispersion with maximum drug content (77.68%) and dissolution rate (91.40%) was formulated as an orodispersible tablet and characterized for its pharmaceutical properties. Conclusion: It can be concluded that the solid dispersion of lamotrigine incorporated with soya lecithin demonstrated enhanced solubility and dissolution rate may have potential clinical application.

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Assessment of dissolution profile of Pantoprazole tablets available in Bangladesh

Stamford Journal of Pharmaceutical Sciences ◽

10.3329/sjps.v4i2.10441 ◽

2012 ◽

Vol 4 (2) ◽

pp. 58-62

Author(s):

Aparajita Malakar ◽

Bishwajit Bokshi ◽

Utpal Kumar Karmakar

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Water Soluble ◽

Dissolution Profile ◽

Coating Materials ◽

Volatile Solvents ◽

Kneading Method ◽

Enhanced Solubility ◽

Materials Used ◽

Liquisolid Compacts

The aim of the present study was to increase the solubility of a poorly water soluble BCS class II drug, valsartan. Liquisolid technology and solid dispersion by kneading method were techniques used to improve the solubility of the drug by using non-volatile solvents and some hydrophilic carriers. Liquisolid compacts were prepared by dissolving the drug in suitable non volatile solvents. The various non volatile solvents used were PG, PEG, and glycerine. The carrier coating materials play an important role in improving the solubility of the drug. The dissolution rate of the drug was increased by using propylene glycol as non-volatile solvent at 20:1 ratio of carrier to coating material. Solid dispersion by kneading method were another attempt to improve solubility the various carrier materials used were PVP K 30, PEG 6000 and mannitol, these carriers are used in various ratios to improve its solubility. The dissolution rate of drug using solid dispersion kneading method with mannitol was increased at 1:3 ratio. The DSC and FTIR studies revealed no drug excipients interactions, whereas XRD revealed the reduced crystalinity of drug, which showed enhanced solubility. From the results it was concluded that the liquisolid compacts enhanced the solubility of valsartan in comparison to traditional solid dispersion method.DOI: http://dx.doi.org/10.3329/sjps.v4i2.10441 S. J. Pharm. Sci. 4(2) 2011: 58-62

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

Journal of Pharmaceutical and Biological Sciences ◽

10.18231/j.jpbs.2021.018 ◽

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.

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Enhancing dissolution profile of diazepam using hydrophilic polymers by solid dispersion technique

International Current Pharmaceutical Journal ◽

10.3329/icpj.v1i12.12453 ◽

2012 ◽

Vol 1 (12) ◽

pp. 423-430 ◽

Cited By ~ 3

Author(s):

Md. Sariful Islam Howlader ◽

Jayanta Kishor Chakrabarty ◽

Khandokar Sadique Faisal ◽

Uttom Kumar ◽

Md. Raihan Sarkar ◽

...

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Water Soluble ◽

Distilled Water ◽

Dissolution Profile ◽

Peg 6000 ◽

Solvent Method ◽

Pure Drug ◽

Dispersion Technique

The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug by a solid dispersion technique, in order to investigate the effect of these polymers on release mechanism from solid dispersions. Diazepam was used as a model drug to evaluate its release characteristics from different matrices. Solid dispersions were prepared by using polyethylene glycol 6000 (PEG-6000), HPMC, HPC and Poloxamer in different drug-to-carrier ratios (1:2, 1:4, 1:6, 1:8, 1:10). The solid dispersions were prepared by solvent method. The pure drug and solid dispersions were characterized by in vitro dissolution study. Distilled water was used as dissolution media, 1000 ml of distilled water was used as dissolution medium in each dissolution basket at a temperature of 37°C and a paddle speed of 100 rpm. The very slow dissolution rate was observed for pure Diazepam and the dispersion of the drug in the polymers considerably enhanced the dissolution rate. This can be attributed to improved wettability and dispersibility, as well as decrease of the crystalline and increase of the amorphous fraction of the drug. SEM (Scanning Electron microscope) studies shows that the solid dispersion having a uniform dispersion. Solid dispersions prepared with PEG-6000, Poloxamer showed the highest improvement in wettability and dissolution rate of Diazepam. Solid dispersion containing polymer prepared with solvent method showed significant improvement in the release profile as compared to pure drug, Diazepam.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12453 International Current Pharmaceutical Journal 2012, 1(12): 423-430

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

Universal Journal of Pharmaceutical Research ◽

10.22270/ujpr.v4i1.240 ◽

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.

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Formulation and In-Vitro Evaluation of Meloxicam Solid Dispersion using Natural Polymers.

Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) ◽

10.31351/vol30iss1pp169-178 ◽

2021 ◽

Vol 30 (1) ◽

pp. 169-178

Author(s):

Hiba Radhi ALhassani ◽

Eman B. H. Al-Khedairy

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Water Solubility ◽

Oral Absorption ◽

Chemical Interaction ◽

Water Soluble ◽

Natural Polymers ◽

Drug Content ◽

Percentage Yield

Meloxicam (MLX) is non-steroidal anti -inflammatory, poorly water soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Solid dispersion (SD) is an effective technique for enhancing the solubility and dissolution rate of such drug. The present study aims to enhance the solubility and the dissolution rate of MLX by SD technique by solvent evaporation method using sodium alginate (SA), hyaluronic acid (HA), collagen and xyloglucan (XG) as gastro-protective hydrophilic natural polymers. Twelve formulas were prepared in different drug: polymer ratios and evaluated for their, percentage yield, drug content, water solubility, dissolution, crystal lattice using powder X-ray diffraction (PXRD) and studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-polymer interaction. All the prepared showed improvement of drug solubility except that prepared with HA. The best result was obtained with formula SD1 (MLX: SA 1:1) that showed a high percentage yield (97), high drug content (97.4±0.05) and increase in solubility compared to solubility of pure MLX with improved dissolution rate. the PXRD study revealed the conversion of the drug to amorphous form without chemical interaction according to FTIR results

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

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i50a33417 ◽

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.

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Enhancement of dissolution rate of Olmesartan medoxomil using urea as carrier by different solid dispersion techniques

International Journal of Research in Pharmaceutical Sciences and Technology ◽

10.33974/ijrpst.v1i1.35 ◽

2018 ◽

Vol 1 (1) ◽

pp. 36-42

Author(s):

B Sangameswaran ◽

M Gomathi

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Olmesartan Medoxomil ◽

Angle Of Repose ◽

In Vitro Dissolution ◽

Dissolution Profile ◽

Poor Solubility ◽

Co Precipitation

The poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T fluid often leads to insufficient bioavailability. As per Biopharmaceutical Classification System (BCS), Olmesartan belongs to the class-II category having poor solubility and high permeability. Since only dissolved drug can pass the gastrointestinal membrane, the proper solubility of the drug is ultimately desired. Its oral bioavailability is 26%. Hence, an attempt was made to enhance its solubility by formulating solid dispersions using different techniques viz., Melting, Kneading, Co-precipitation, Solvent evaporation and Physical mixing etc., Drug and carrier (Urea) in different ratios like 1: 1, 1: 2, 1: 3 and 1:4 were used for formulating solid dispersions. The compatibility of the drug with the carrier was checked by FTIR studies, these results revealed that there was no interaction between them. The angle of repose, bulk density, tapped density; Carr’s index and Hausner ratio were calculated for the micrometric characterization of all the solid dispersions. The drug content was found to be high and uniform in all formulations. The prepared Solid dispersion SEM4 (1:4) showed minimal wetting time of 13 seconds compared with the other formulations. In vitro dissolution, release studies in Phosphate buffer pH of 6.8 revealed that the prepared solid dispersions showed faster drug release compared with the pure drug. The in vitro dissolution profile showed ascendency on increasing the carrier concentration

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Preparation and comparative evaluation of liquisolid compacts and solid dispersions of Valsartan

Stamford Journal of Pharmaceutical Sciences ◽

10.3329/sjps.v4i2.10440 ◽

2012 ◽

Vol 4 (2) ◽

pp. 48-57

Author(s):

PK Lakshmi ◽

Ch Srinivas ◽

B Kalpana

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Water Soluble ◽

Coating Materials ◽

Volatile Solvents ◽

Kneading Method ◽

Enhanced Solubility ◽

Materials Used ◽

Liquisolid Compacts

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Solid Dispersion by Fluidized Bed Processing: A Platform for Enhancement of Dissolution Rate of Simvastatin Poorly Water-Soluble Drug

Journal of Pharmaceutical Research International ◽

10.9734/jpri/2021/v33i42a32381 ◽

2021 ◽

pp. 32-43

Author(s):

Rajendra K. Surawase ◽

Kamalkishor G. Baheti

Keyword(s):

Dissolution Rate ◽

Fluidized Bed ◽

Solid Dispersion ◽

Zero Order ◽

Water Soluble ◽

In Vitro Dissolution ◽

Dissolution Profile ◽

Poorly Water Soluble Drugs ◽

Water Soluble Drugs ◽

Poorly Water Soluble

Aim: The aim of this study was to study the solubility and dissolution kinetics of poorly water-soluble drugs simvastatin from its solid dispersion with different carriers by using fluidized bed processing technique. Methods: The effect of different surfactants such as Gelucire® 44/14, PVP- K30 and Poloxamer- 188 on solid dispersion dissolution and solubility of simvastatin was investigated. Solid dispersion is formed using various techniques with polymeric carrier to potentially enhance the solubility and dissolution rate such as fluidized bed processing, it will extend drug absorption, therefore the objectives were to make a comparative evaluation among different solid dispersions. Results: The simvastatin solid dispersion prepared by fluidized bed processing significantly enhanced in vitro dissolution and solubility relative to that of the unprocessed form. The dissolution profiles were correlated using various mathematical models such as Zero order, first order, Higuchi and Hixon Crowell model and the Zero order kinetics model gave better correlation results than the other models. Conclusion: Dissolution profile of simvastatin was significantly improved via complexation with Gelucire 44/14 as compared with the pure drug and other carriers using FBP processing is a highly effective strategy for enhancing the solubility and dissolution of poorly water-soluble drugs.

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DEVELOPMENT OF SOLID DISPERSION TABLET OF CARVEDILOL TO IMPROVE SOLUBILITY

INDIAN DRUGS ◽

10.53879/id.53.01.10330 ◽

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.

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