SOLUBILITY ENHANCEMENT, FORMULATION DEVELOPMENT AND EVALUATION OF IMMEDIATE RELEASE TABLET OF ANTIHYPERTENSIVE DRUG TADALAFIL

The objective of the study was to enhance the solubility and dissolution rate of Tadalafil using hydrophilic carriers such as PVP K-30, Poloxamer 188, Sodium starch glycolate and compatibility study of Tadalafil with different polymers by FTIR. Characterization of solid dispersion-FTIR, DSC and phase solubility analysis was study to improve the oral bioavailability. Formulation and evaluation of immediate release tablets prepare from solubility enhanced Tadalafil. Among the various approaches Solvent evaporation has gained good acceptance in recent years in the industry for enhancing the solubility and dissolution rate of poorly soluble drugs. Poloxamer 188 used as polymer as it is good solubilizing agent. As per the phase solubility studies, a 32 factorial study were used to prepare the immediate release tablet and evaluated for the interactions and in vitro drug release. Sodium Starch Glycolate and PVP used as superdisintegrants. The solubility of tadalafil in selected ratios containing tadalafil and Poloxamer 188 solid dispersion prepared by solvent evaporation was determined. From the various ratios 1:0.5 was resulted in a much higher enhancement (9.75folds). Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) studies conducted, explain overall drug and excipients compatibility. More than 90% of tadalafil was released from IR tablet within 30 min. There is enhancement of the solubility rate if tadalafil by solid dispersion with Poloxamer 188 prepared by solvent evaporation method. The compatibility studies of the drug and polymers showed that there was no incompatibility between them. Wet granulation method showed that, the desired flow properties for the compression into tablets. Tablets were prepared using wet granulation method resulted into simple, cheap, more suitable method for the manufacturing immediate release dosage form.

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

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2011.4.3.6 ◽

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.

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Formulation, Development and Evaluation of Bilayer Tablet of Flurbiprofen

International Journal of Scientific Research in Science and Technology ◽

10.32628/ijsrst196130 ◽

2019 ◽

pp. 246-251

Author(s):

Nitin A Gaikwad ◽

Indrjeet V Mane ◽

Manohar D Kengar ◽

Ranjeet S Jadhav

Keyword(s):

Immediate Release ◽

Wet Granulation ◽

Content Uniformity ◽

Formulation Development ◽

Sodium Starch Glycolate ◽

Bilayer Tablets ◽

Bilayer Tablet ◽

Weight Variation ◽

Initial Release ◽

Higuchi Model

In the Study of Formulation of Bilayer Tablet of Flurbiprofen the Following Materials Using sodium starch glycolate as immediate release and HPMC K15 in different ratios as release retardant materials using a wet granulation method. All tablets exhibited good physical properties with Respect to appearance, content uniformity, hardness, weight variation and Invitro dissolution data show at increasing proportions Of sodium starch glycolate for immediate release whereas HPMC K15sustaineddrugreleaserate. The bilayer tablets showed an initial release of drug In about1hr, then sustaining the release for 12h, The kinetic analysis of dissolution data showed that release was observe din these tablets. When data was fitted to the Higuchi model. Bilayer tablets of flurbiprofen can be successfully formulated Using sodium starch glycolate and HPMC K15 in different ratios as release retardant materials employing a wet granulation method.

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Improvement of Solubility and Dissolution of Rilpivirine Solid Dispersions by Solvent Evaporation Technique and Novel Carriers

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.4.5 ◽

2018 ◽

Vol 11 (4) ◽

pp. 4177-4184

Author(s):

Bhikshapathi D. V. R. N. ◽

Vishwa M

Keyword(s):

Drug Release ◽

Dissolution Rate ◽

Solid Dispersion ◽

Drug Carrier ◽

Solid Dispersions ◽

Immediate Release ◽

Solvent Evaporation ◽

Onset Of Action ◽

Enhanced Solubility ◽

Evaporation Technique

Rilpivirine benzonitrile is a pharmaceutical drug used for the treatment of HIV infection it is characterized with poor solubility that limits its absorption and dissolution rate, which delays onset of action. In the present study, immediate release solid dispersion of antiretroviral Rilpivirine was formulated by solvent evaporation technique. Eighteen solid dispersions were prepared with 1:1:1, 1:2:1 and 1:3:1 ratios of drug: carrier: surfactant. There was significant improvement in the rate of drug release from all 18 solid dispersions and the formulation (SE12) comprising Rilpivirine: Kolliwax GMS II: SLS in 1:3:1 by solvent evaporation process has shown enhanced solubility about 30 folds and significant improvement in the rate of drug release. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of Rilpivirine has been converted into an amorphous form from crystalline within the solid dispersion formulation. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of Rilpivirine.

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Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.6.7 ◽

2018 ◽

Vol 11 (6) ◽

pp. 4337-4348

Author(s):

Bhikshapathi D. V. R. N. ◽

Srinivas I

Keyword(s):

Central Composite Design ◽

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Solvent Evaporation ◽

Release Mechanism ◽

Solvent Evaporation Method ◽

Onset Of Action ◽

Evaporation Method ◽

Central Composite

Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.

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Rosuvastatin cocrystals: an attempt to modulate physicochemical parameters

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-021-00213-7 ◽

2021 ◽

Vol 7 (1) ◽

Author(s):

Venkata Deepthi Vemuri ◽

Srinivas Lankalapalli

Keyword(s):

Physicochemical Properties ◽

Dissolution Rate ◽

Functional Groups ◽

Preliminary Investigation ◽

Scale Up ◽

Solvent Evaporation ◽

Molar Ratio ◽

The Novel ◽

Formulation Development ◽

Hydrogen Bond Interaction

Abstract Background The meager physicochemical properties like low solubility and low dissolution rate of rosuvastatin calcium remain as an obstruction for formulation development. In the present work, we explore the evolution of rosuvastatin cocrystal, which may offer the synergetic physico-chemical properties of the drug. Cocrystal crafting depends on two possible intermolecular interactions; heteromeric and the homomeric selection of compounds with complementary functional groups are contemplated as a possible cause of supramolecular synthons in cocrystal formation. Specifically, cocrystals of rosuvastatin with l-asparagine and l-glutamine with molar ratio (1:1) were fabricated by using slow solvent evaporation and slow evaporation techniques. Novel cocrystals of rosuvastatin-asparagine (RSC-C) and rosuvastatin-glutamine (RSC-G) cocrystals obtained by slow solvent evaporation were utilized for preliminary investigation and further scale-up was done by using the solvent evaporation technique. Results The novel cocrystals showed a new characteristic of powder X-ray diffraction, thermograms of differential scanning calorimetry, 1H liquid FT-NMR spectra, and scanning electron microscopy. These results signify the establishment of intermolecular interaction within the cocrystals. In both the novel cocrystals, rosuvastatin was determined to be engaged in the hydrogen bond interaction with the complementary functional groups of l-asparagine and l-glutamine. Compared with the pure rosuvastatin, RSC-C and RSC-G cocrystal showed 2.17-fold and 1.60-fold improved solubility respectively. The dissolution test showed that the RSC-C and RSC-G cocrystal exhibited 1.97-fold and 1.94-fold higher dissolution rate than the pure rosuvastatin in pH6.8 phosphate buffer respectively. Conclusion Modulation in the chemical environment, improvement in the solubility, and dissolution rate demonstrated the benefit of co-crystallization to improve the physicochemical properties of the drug. Graphical abstract

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

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2018v10i1.21179 ◽

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.

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

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11ispl4.4370 ◽

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.

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Formulation and Optimization of Immediate Release Cajanus Cajan Starch-Based Tablets Containing Metronidazole

Oriental Journal of Physical Sciences ◽

10.13005/ojps05.01-02.05 ◽

2020 ◽

Vol 5 (1-2) ◽

pp. 16-19

Author(s):

Ahmed Abdalla Bakheit Abdelgader ◽

Daud Baraka Abdallah ◽

Elnazeer I. Hamedelniel ◽

Hiba Atif Mutwakil Gafar ◽

Mohammed Abdelrahman Mohammed

Keyword(s):

Cajanus Cajan ◽

Immediate Release ◽

Wet Granulation ◽

Maize Starch ◽

Disintegration Time ◽

Sodium Starch Glycolate ◽

Upper Level ◽

High Level ◽

Starch Paste ◽

Tablet Dosage

Starch is found almost in all organs of plants as a carbohydrate reserve. It is considered one of the most commonly used pharmaceutical additives, mainly in tablet dosage forms; it used as a tablet binder when incorporated through the wet granulation process or as a disintegrant. Cajanus cajan has a high level of carbohydrate, which makes it another potential choice as a source for starch. This study aims to investigate and optimize the effect of Cajanus cajan starch concentrations as well as wet massing granulation time on physicochemical properties of metronidazole tablets. The hardness, friability percentage, and disintegration time of prepared tablets were determined, and the central composite design was employed in the optimization process. Then the tablets of optimized batch were compared against those tablets in which maize starch and sodium starch glycolate were used instead of Cajanus cajan starch. The results indicated that metronidazole tablets containing the upper level of starch paste (Cajanus cajan and/or maize starch paste) exhibited better percentage friability, hardness, and disintegration time than those formulated with lower levels and those without starch paste. The study showed that experimental design is a useful technique for optimizing Cajanus cajan starch-based tablets, which enabled a better understanding of how different variables could affect the responses. In addition, the study demonstrated that incorporation of Cajanus cajan starch in tablets formulation led to improvement of its physical properties compared to the formulations of maize starch and sodium starch glycolate respectively.

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