scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF GASTRO-RETENTIVE DOSAGE FORM OF ATAZANAVIR SULPHATE

2018 ◽  
Vol 10 (1) ◽  
pp. 60
Author(s):  
Hemant Kumar Jain ◽  
Madhuri Taware
Keyword(s):  
Solid Dispersion ◽  
Dosage Form ◽  
In Vitro Release ◽  
Hplc Method ◽  
Phase Solubility ◽  
Dissolution Profile ◽  
Formulation Development ◽  
Peg 6000 ◽  
Phase Solubility Study ◽  
Gastro Retentive

Objective: To improve dissolution properties of atazanavir sulphate by preparing gastro-retentive granules by solid dispersion method and development of RP-HPLC method for estimation of this drug.Methods: Estimation of atazanavir sulphate was done using high performance liquid chromatography (HPLC) on inertsil column (5 µm, 250x4, 6 mm) with a mobile phase consists of methanol: water (91:9 v/v), at 0.5 ml/min flow rate and 249 nm UV detection. The method was validated as per ICH guidelines. Selection of the carrier for gastro-retentive formulation was based on phase solubility study of the drug. Solid dispersions of gastro-retentive granules of different composition of drug and carrier, were prepared by the kneading, heating and solvent evaporation. A 32factorial design was applied to optimize the gastro-retentive formulation. The amounts of polyethylene glycol 6000 (PEG 6000) (X1) and hydroxypropyl methyl cellulose (HPMC) (X2) were selected as independent variables and in vitro-release at 5, 9 h and total floating time was selected as dependent variables. Results: HPLC method was found to be linear in a concentration range of 10-60 μg/ml of the drug (r2= 0.999). The low value of % RSD in precision study indicates reproducibility of the method. The low value of LOD and LOQ suggests the sensitivity of the method. The solubility enhancement study of drug with various carriers followed descending order of solubility [Gelucire 44/14>PEG 6000>polyvinyl pyrrilidone (PVP)]. Highest % cumulative release was observed for the heating method at drug polymer (PEG 6000) ratio 1:5. Hence, this ratio has been selected for preparation of solid dispersion. From comparison of dissolution profile of formulated batches, formulation F4 [containing PEG6000 (1.6 g) and HPMC (200 mg)] showed promising dissolution parameters with desired floating properties.Conclusion: Results obtained by validation studies suggested that the developed HPLC method is simple, accurate, precise and can be used for routine analysis of atazanavir sulphate formulation. Results of evaluation of prepared batches indicate that batch F4 is a promising formulation for gastro-retentive dosage form of drug. 

scholarly journals “FORMULATION DEVELOPMENT AND SOLUBILITY ENHANCEMENT OF ROSUVASTATIN CALCIUM BY USING HYDROPHILIC POLYMERS AND SOLID DISPERSION METHOD”

2021 ◽  
pp. 50-55
Author(s):  
LOVEPREET KAUR ◽  
TARANJIT KAUR ◽  
AMAR PAL SINGH ◽  
AJEET PAL SINGH
Keyword(s):  
Solid Dispersion ◽  
Dosage Form ◽  
Hydrophilic Polymers ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Formulation Development ◽  
Dispersion Method ◽  
Particle Size Reduction ◽  
Acacia Gum ◽  
Rosuvastatin Calcium

Objective: Preparation of Rosuvastatin Calcium by Using Hydrophilic Polymers and Solid Dispersion Method, Rosuvastatin calcium is a Dyslipidaemic agent, which act as a selective competitive inhibitor of HMG CoA educates enzyme and is used in the treatment of hyperlipidemia. Methods: In the present work, Solid Dispersion was prepared by kneading method to increase the solubility of Rosuvastatin Calcium. Results: Solid dispersions were evaluated by determining percentage yield, drug content, solubility, Scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), DSC and in vitro dissolution profile. The prepared solid dispersion are formulated into capsule dosage form and characterized by various parameters i.e. weight variation, content uniformity, disintegration and dissolution. The evaluated parameters of capsule dosage form increase in solubility and dissolution rate of the pure drug. Conclusion: These are various techniques to enhance the solubility of the drug, such as particle size reduction, use of surfactants, solid dispersion etc. Carriers are the major players in these formulations, e. g. Hydroxypropylmethylcellulose, ethylcellulose, Carbopol, Acacia Gum etc. Carbopol and Acacia Gum is one of the most efficient polymers work as a carrier for these drugs to enhance solubility.

Formulation and Evaluation of Immediate Release Bilayer Tablets of Telmisartan and Hydrochlorothiazide

2011 ◽  
Vol 4 (3) ◽  
pp. 1477-1483
Author(s):  
Natarajan R ◽  
N Patel ◽  
Rajendran N N ◽  
M Rangapriya
Keyword(s):  
Antihypertensive Drugs ◽  
In Vitro Release ◽  
Immediate Release ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Dissolution Profile ◽  
Formulation Development ◽  
Sodium Starch Glycolate ◽  
Bilayer Tablets

The main goal of this study was to develop a stable formulation of antihypertensive drugs telmisartan and hydrochlorothiazide as an immediate-release bilayer tablet and to evaluate the dissolution profile in comparison with a reference product. The formulation development work was initiated with wet granulation. Telmisartan was converted to its sodium salt by dissolving in aqueous solution of sodium hydroxide to improve solubility and drug release. Lactose monohydrate and microcrystalline cellulose were used as diluents. Starch paste is prepared in purified water and was used as the binder. Sodium starch glycolate is added as a disintegrating agent. Magnesium stearate was used as the lubricant. The prepared granules were compressed into a double-layer compression machine. The tablets thus formulated with higher proportion of sodium starch glycolate showed satisfactory physical parameters, and it was found to be stable and in vitro release studies are showed that formulation (F-T5H5) was 101.11% and 99.89% respectively. The formulation T5H5 is further selected and compared with the release profile of the innovator product, and was found to be similar (f2 factor) to that of the marketed product. The results suggest the feasibility of developing bilayer tablets consisting of telmisartan and hydrochlorothiazide for the convenience of patients with hypertension.  

scholarly journals Solid Dispersion and Inclusion Complex for Solubility Enhancement of Rifabutine: A Comparative Study

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1772-1778
Author(s):  
Jyoti Maithani ◽  
Ranjit Singh ◽  
Sanjay Singh ◽  
Kapil Kalra
Keyword(s):  
Inclusion Complex ◽  
Solid Dispersion ◽  
Amorphous Structure ◽  
Solvent Evaporation ◽  
Physical Mixture ◽  
Complex Method ◽  
Physicochemical Interaction ◽  
Dissolution Profile ◽  
Formulation Development ◽  
Peg 4000

Improvement in the solubility of a hydrophobic drug has a significant role in formulation development. The target of this study was the use of solid dispersion and inclusion complex method to enhance and to compare the watery solubility and dissolution qualities of Rifabutin. Various strategies in various proportions have been used in the preparation of the consideration complex with ß-cyclodextrin (ß-CD) and Hydroxypropyl-ß-cyclodextrin (HPß-CD) and found that the better-improved solubility has been seen in kneading technique (AK1) in comparison to the physical mixture method and solvent evaporation method. Various techniques were applied in the preparation of the solid dispersion of Mannitol and polyethene glycol (PEG) 4000. They observed that solvent evaporation (CS4) had shown the better improvement of solubility when compared with the physical mixture method and kneading method. As the two methodologies were analysed, it was observed that the inclusion complex technique was far better as it caused a noteworthy enhancement in dissolution profile (99.23±0.25). The drug content was calculated (99.15±0.14) and % inclusion yield was calculated (99.5 %), which was found to be maximum with the kneading technique (AK1). The characterization FTIR and SEM of the complexes shows that the drug had an amorphous structure. The amorphous structure of a drug has higher dissolution potential than the crystalline structure of the drug. The IR Spectroscopy and Scanning electron microscopy (SEM) were done to check their impact on dissolution behaviour and any if there was any physicochemical interaction between the carrier and the drug.

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

2012 ◽  
Vol 1 (12) ◽  
pp. 423-430 ◽  
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

scholarly journals Dissolution Enhancement of Flurbiprofen by Solid Dispersion Adsorbate Technique

2021 ◽  
Vol 69 (2) ◽  
Author(s):  
Sohansinh S. Vaghela ◽  
Samkit M. Shah ◽  
Sanjesh G. Rathi ◽  
Shrenik K. Shah
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Dissolution Enhancement ◽  
Phase Solubility ◽  
Fusion Method ◽  
Poloxamer 188 ◽  
X Ray ◽  
Solubility Study ◽  
Phase Solubility Study

Flurbiprofen solid dispersion Adsorbate (SDA) has been prepared using PEG 4000 and Poloxamer 188 as carrier and Neusilin as adsorbent material. The SDA of Flurbiprofen was prepared by using Fusion method in various drugs to carrier ratios. The phase solubility study concludes that both polymers have ability to improve the aqueous solubility of flurbiprofen. Pure API Flurbiprofen and final formulation samples of SDA are characterized by FTIR, DSC and X-ray diffraction spectroscopy. X-ray powder diffraction and DSC study indicated that the drug was present in amorphous form. FTIR study revealed that the characteristic peaks in spectra of pure Flurbiprofen are also present in spectra of SDA’s. Drug found compatible with the excipients. The highest improvement in solubility and in-vitro drug release were observed in solid dispersion prepared with Poloxamer 188 (F14) by fusion method. The increased dissolution rate of drug from solid dispersion adsorbates may be due to surface tension lowering effect of polymer to the medium and increased wettability and dispersibility of drug. Hence, F14 Solid dispersion adsorbates with the Poloxamer carrier in 1:2 ratio considered as most satisfactory among all solid dispersion adsorbates.

scholarly journals Stability Indicating Liquid Chromatographic Method for Estimation of Trihexyphenidyl Hydrochloride and Risperidone in Tablet Formulation: Development and Validation Consideration

2014 ◽  
Vol 2014 ◽  
pp. 1-5 ◽  
Author(s):  
Patel Bhaumik ◽  
Gopani Mehul ◽  
Vikani Kartik ◽  
Patel Rashmin ◽  
Patel Mrunali
Keyword(s):  
High Performance ◽  
Dosage Form ◽  
High Performance Liquid Chromatographic ◽  
Hplc Method ◽  
Calibration Plot ◽  
Simultaneous Estimation ◽  
Formulation Development ◽  
Rp Hplc ◽  
Tablet Dosage ◽  
Liquid Chromatographic

This paper describes validated reverse phase high-performance liquid chromatographic (RP-HPLC) method for simultaneous estimation of trihexyphenidyl hydrochloride (THP) and risperidone (RSP) in the pure powder form and in combined tablet dosage form. The HPLC separation was achieved on a core shell C18 (100 mm length × 4.6 mm, 2.6 μm particle size) using methanol : ammonium acetate buffer 1% (85 : 15 v/v; pH-6.5) as mobile phase and delivered at flow rate of 0.8 mL/min. The calibration plot showed good linear relationship with r2 = 0.997 ± 0.001 for THP and r2 = 0.998 ± 0.001 for RSP in concentration range of 50–175 μg/mL and 50–175 μg/mL, respectively. LOD and LOQ were found to be 0.40 and 1.29 μg/mL for THP and 1.24 and 3.92 μg/mL for RSP. Assay of THP and RSP was found to be 100.16 ± 0.03% and 99.83 ± 0.02%, respectively. THP and RSP were subjected to different stress conditions (acidic, basic, oxidative, thermal, and photolytic degradation). The degraded product peaks were well resolved from the pure drug peak. The method was successfully validated as per the ICH guidelines. The developed RP-HPLC method was successfully applied for the estimation of THP and RSP in tablet dosage form.

scholarly journals Formulation Development to Enhance the Solubility of Metoclopramide Base Drug by Solid Dispersion and Evaluation of Transdermal Film

2018 ◽  
Vol 8 (6) ◽  
pp. 183-191
Author(s):  
Goutam Mukhopadhyay ◽  
Rahul Mukhopadhyay ◽  
Ankita Mukhopadhyay ◽  
Shymodip Kundu ◽  
Banerjee Shreya ◽  
...  
Keyword(s):  
Melting Point ◽  
Controlled Release ◽  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Formulation Development ◽  
Dissolution Study ◽  
Phase Solubility Study ◽  
Metoclopramide Hydrochloride ◽  
Pvp K30

Aims & Objectives: The present work deals with the modification of controlled release dosage form of poorly water soluble drug (Metoclopramide hydrochloride) in order to improve the bioavailability and to control drug release for a longer period of time by the aid of solid dispersion. Methods: Various binary combination of MET-solid dispersion was prepared with different carriers such as HPβCD, PVP K30 and PLX-188 by solvent evaporation technique and then the aqueous solubility, dissolution study and phase solubility study was performed. DSC analysis is performed to carry out for metoclopramide loaded solid dispersion, physical mixture & also for pure drug to analyze the crystalline and amorphous nature of compounds. Results and Discussion:  The saturation solubility of Metoclopramide with various carriers at different pH was performed and found that in pH 5.5 (solubility is 5553.2µg/ml), pH 6.8 (3363.3µ/ml), pH 7.4 (1367.3µg/ml) at 37oC. In dissolution study of solid dispersion (5:1) of different carriers in DDW, the Cumulative % dissolution is found in the order of PVP K30>PLX-Met>HPβCD-Met & in pH 7.4, in the order of PLX-Met>PVP K30>HPβCD-Met. DSC thermogram of Metoclopramide base showed a sharp endothermic peak at its melting point (147oC) which exhibits in crystalline form complying with that of Metoclopramide hydrochloride form, melting point was found to be 850C.  In the ex-vivo study of several transdermal patches, patch C [SD of MET: HPβCD (1:5)] showed the controlled release and permeation of drug. Conclusion: Poor solubility of new chemical entities being a well known problem for past few decades despite the imbalance between significant research efforts & few successful marketed formulations, the solid dispersion proves to hold a key position among all the various formulation strategies to enhance the aqueous solubility & dissolution rate and thereby the bioavailability of  poorly aqueous solubility of drug. Keywords: Bioavailability,DSC, Metoclopramide hydrochloride, solid dispersion, HPβCD,

Design of Experiment Approach to Assess The Effect Of Formulation Variables On Extrusion And Spheronization Of Telmisartan And Cilostazol Loaded Pellets And Its Pharmacokinetic Study

2021 ◽  
Vol 16 ◽  
Author(s):  
Kalpana Patel ◽  
Prutha Godhani ◽  
Hemangini Patel ◽  
Vaishali Thakkar ◽  
Tejal Gandhi ◽  
...  
Keyword(s):  
Inclusion Complex ◽  
Solid Dispersion ◽  
Pharmacokinetic Study ◽  
Class Ii ◽  
Phase Solubility ◽  
Solubility Study ◽  
Drug Content ◽  
Bcs Class Ii ◽  
Apparent Solubility ◽  
Phase Solubility Study

Background: Solubility is an important parameter that affects availability of drug in systemic circulation. Drugs having poor solubility belonging to BCS class II eventually results in lower dissolution and bioavailability. Hence, improvement of solubility is a challenging task. Hence the present work focusses on using solid dispersion and inclusion complex approach for both telmisartan and cilostazol belonging to BCS Class II drugs. Objective: The present study was carried out to improve apparent solubility of telmisartan and cilostazol (BCS-Class II drugs) and optimization as pellets along with its pharmacokinetic study. Methods: Phase solubility study was carried out to screen the excipients such as, PVPK30, PVA, HPMC E5 and β-CD. Solvent evaporation method was adopted to prepare the solid dispersions and inclusion complex of both the drugs. Pellets were optimized by extrusion spheronization method using 32 factorial design and characterized by morphology, drug content, DSC, FTIR, XRD, SEM, in-vitro studies and drug content study Results: Phase solubility study showed improved apparent solubility of telmisartan with HPMC E5 (1:3) by solid dispersion and cilostazol with β-CD (1:3) using inclusion complexation method. Drug characterization did not reveal any incompatibility. Formulation was optimized on the basis of acceptable pellet properties, including acceptable spherical shape and micromeritics properties. The percent friability of all batches was found to be less than 1%. The optimized pellets of both drugs prepared with micro crystalline cellulose provided desirable maximum release with acceptable release profile. Conclusion: The formulated pellets when studied in vivo showed superior pharmacokinetic profile. The drawback associated with apparent solubility and bioavailability of both drugs can thus be alleviated by use of novel pellet formulation.

scholarly journals Formulation Development and In vitro Evaluation of Combination Product of Glyburide and Metformin Hydrochloride Tablet

2015 ◽  
Vol 16 (2) ◽  
pp. 195-203
Author(s):  
Mohammed Motaher Hossain Chowdhury ◽  
Abedah Nawreen ◽  
Md Sohel Rana
Keyword(s):  
In Vitro Release ◽  
Angle Of Repose ◽  
Metformin Hydrochloride ◽  
Physical Parameters ◽  
Dissolution Profile ◽  
Combination Product ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Compressibility Index

This study was attempted to formulate a combination product of Glyburide and Metformin Hydrochloride Tablets USP 2.5mg/500mg and to evaluate their physico-chemical properties. Wet granulation method was adopted for preparation of tablet using different excipients namely Microcrystalline cellulose, Povidone K-30, Copovidone, Croscarmellose sodium and Sodium stearyl fumerate in six different formulations (F1-F-6). The granules for tabletting were evaluated for angle of repose, bulk density, tapped density, compressibility index and drug content etc. The tablets were subjected to thickness, hardness, friability, disintegration and in vitro release studies. The results of physical parameters of tablets showed that there were capping, hardness and friability problems in formulation F-1, F-2 and F-3. Granules of formula F-4, F-5 and F-6 showed satisfactory flow properties, compressibility index and the physical parameters of tablets from these three formulations gave optimum result in comparison to innovator's brand. Disintegration time of these three formulations (7-8 min) was found similar with innovator's brand (6.30-7.30 min). Assay of formula F-6 of glyburide (97.97%) and Metformin Hydrochloride (100.2%) met the USP specification (90%-110%). It was also found that dissolution profile of Glyburide depends on particle size of Glyburide powder. When micronized and non micronized grade of Glyburide was used in a ratio of 3:1 (F-6) it gave similar dissolution profile as innovator's brand where the similarity factor (f2) was calculated as 59. On the other hand, dissolution profile of Metformin hydrochloride was found similar in all the three formulations (F-4, F-5, F-6) with reference to innovator having all f2 values above 50. Formulation F-6 possessed good stability in accelerated condition for 6 months study. By comparing the dissolution profiles with the innovator's drug glucovance® tablet, it was revealed that the formulation F-6 exhibit similar drug release profile for both Glyburide and Metformin Hydrochloride. DOI: http://dx.doi.org/10.3329/bpj.v16i2.22304 Bangladesh Pharmaceutical Journal 16(2): 195-203, 2013

scholarly journals Dissolution Profile of Ibuprofen Solid Dispersion Prepared with Cellulosic Polymers and Sugar by Fusion Method

1970 ◽  
Vol 4 (1) ◽  
pp. 31-37 ◽  
Author(s):  
Nadia Saffoon ◽  
Yeakuty Marzan Jhanker ◽  
Naz Hasan Huda
Keyword(s):  
Solid Dispersion ◽  
Dosage Form ◽  
Solid Dispersions ◽  
Dissolution Profile ◽  
Fusion Method ◽  
Method Evaluation ◽  
Dissolution Studies ◽  
Dissolution Properties ◽  
Rate Of Dissolution ◽  
Cellulosic Polymers

The purpose of this study was to prepare and characterize solid dispersions of the NSAID Ibuprofen with HPMC, HPC, icing sugar, dextrose, mannitol and lactose with the intention of improving its dissolution properties. The solid dispersions were prepared by the fusion method. Evaluation of the properties of the dispersions was performed using dissolution studies. The results obtained showed that the rate of dissolution of Ibuprofen was considerably improved when formulated in solid dispersions with HPMC and HPC. Solid dispersions with icing sugar, dextrose, mannitol and lactose showed drug retarding capability which may trigger more research in the intension of exploiting this feature to prepare sustained release dosage form.   Key words: Ibuprofen; Solid dispersion; Fusion method; Dissolution rate. DOI: http://dx.doi.org/10.3329/sjps.v4i1.8864 SJPS 2011; 4(1): 31-37

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