scholarly journals Formulation and Quality Optimization of Effervescent Tablet of Glipizide: An Approach to Comfort Anti-Diabetic Medication

2020 ◽  
Vol 3 (2) ◽  
pp. p14
Author(s):  
Aklima Aklima ◽  
Prodip Kumar Baral ◽  
Mohammad Tohidul Amin ◽  
Tariqul Islam Emon ◽  
Mohammad Salim Hossain
Keyword(s):  
Water Soluble ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Potency Assay ◽  
Disintegration Time ◽  
Water Soluble Drug ◽  
Hausner Ratio ◽  
Diabetic Treatment ◽  
Effervescent Tablet ◽  
Poorly Water Soluble Drug

The present study is targeted to formulate and prepare effervescent tablets of Glipizide to provide more elegancy, comfortability, and improved pharmacokinetics in diabetic treatment than the conventional dosage. Three formulations (F1, F2, and F3) of the effervescent tablet of Glipizide (5mg) were formulated with different amounts and ratios of excipients. By wet granulation technique, 60 tablets for every formulation were prepared with a weight of 700mg per tablet. Then, the features of both granules and tablets were evaluated by published methods. The angle of repose, Hausner ratio, Carr's index, Loss on drying (LOD), and Moisture Content (MC) used to measure granules property successfully proved right follow ability and compressibility. In contrast, physical and drug content related investigation failed to determine the perfectness of all three formulations. Friability on the formulations was around 0.70%, indicating the expected USP limit of friability (0.5 to 1%). The mean disintegration time of the formulations was from 95s to 105s. The tablet potency assay found 95.20% for F1, 88.80% for F2, and 97.40% for F3. The dissolution pattern of the drug followed a linear relationship with time. After one and a half hours, the highest amount of 59.20% cumulative dissolution was determined for F3 that revealed its strategic improvement of the drug solubility. As Glipizide is a poorly water-soluble drug, the effervescent tablet might mitigate disintegration and dissolution-related limitations and, consequently, enhance the drug's bioavailability.

Natural Polymers in Fast Dissolving Tablets

2021 ◽  
pp. 2859-2866
Author(s):  
Ratnaparkhi M.P. ◽  
Karnawat G.R. ◽  
Andhale R.S.
Keyword(s):  
Geriatric Patients ◽  
Nutritional Supplement ◽  
Synthetic Polymers ◽  
Oral Route ◽  
Water Soluble ◽  
Natural Polymers ◽  
Disintegration Time ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Oral route is most preferable route of administration for various drugs, because it is convenient, economical, safest route. Fast dissolving tablets are popular nowadays, as they disintegrated in mouth within a few seconds without using water for swallow. Problems like Dysphagia in pediatric and geriatric patients have been overcome by formulating Fast dissolving tablet. Natural polymers are preferable because they are chemically inert, nontoxic, less expensive, biodegradable, and available easily than synthetic polymers. Natural polymers are obtained from the natural origin so they are devoid of any side effect. It is proved from the previous studies that Natural polymers are more-safe and effective than the synthetic polymers. Natural polymers improve the properties of tablet and they are used as binder, diluent, superdisintegrant, they also enhance the solubility of poorly water-soluble drug, decrease the disintegration time and provide nutritional supplement. The aim of the present article is to study various natural polymers used in fast dissolving tablets.

scholarly journals Mini-review on Natural Disintegrants in Pharmaceutical Formulations

2021 ◽  
pp. 52-56
Author(s):  
S. U. Kankanamge ◽  
A. G. K. Neranja ◽  
K. D. S. Sandarenu
Keyword(s):  
Pharmaceutical Formulations ◽  
Nutritional Supplement ◽  
Water Soluble ◽  
Aqueous Environment ◽  
Natural Polymers ◽  
Disintegration Time ◽  
Water Soluble Drug ◽  
Tablet Formulations ◽  
Potential Use ◽  
Poorly Water Soluble Drug

Disintegrants are agents which are integrated to tablets and some encapsulated formulations in order to promote the breakup of the tablet and capsule “slugs” into more small fragments in an aqueous environment which thereafter increment the available surface area and promoting a more rapid release of the drug substance.  The development of new excipients for potential use as disintegrant agent in tablet formulations continues to be of interest. This is because different disintegrant agents can be useful in promoting penetration of moisture and dispersion of the tablet matrix and disintegration of tablet has received considerable attention at present as an essential step in obtaining fast drug release. Natural polymers such as starches, gums, mucilage, and dried fruits utilized as binder, diluent, and disintegrants to increase the solubility of poorly water-soluble drug, decrease the disintegration time, and provide nutritional supplement. Natural disintegrants are safe and economical than synthetic disintegrants such as Polyvinylpyrrolidone (PVP). Therefore, in the present review, an attempt has been made to reveal the importance of the natural disintegrants in the pharmaceutical formulations.

scholarly journals Formulation of Orally Disintegrating Films as an Amorphous Solid Solution of a Poorly Water-Soluble Drug

Membranes ◽  
2020 ◽  
Vol 10 (12) ◽  
pp. 376
Author(s):  
Pattaraporn Panraksa ◽  
Pratchaya Tipduangta ◽  
Kittisak Jantanasakulwong ◽  
Pensak Jantrawut
Keyword(s):  
Mechanical Strength ◽  
Amorphous State ◽  
Strength Properties ◽  
Water Soluble ◽  
Disintegration Time ◽  
Surface Ph ◽  
X Ray ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The objective of the present study was to develop an orally disintegrating film (ODF) for a poorly water-soluble drug, phenytoin (PHT), using the cosolvent solubilization technique to achieve the amorphization of the drug, followed by the preparation of ODFs. Eleven formulations were prepared with different polymers, such as polyvinyl alcohol (PVA) and high methoxyl pectin (HMP) by the solvent casting method. The prepared films were subjected to characterization for weight variations, thickness, surface pH, disintegration time and mechanical strength properties. Then, differential scanning calorimetry, X-ray diffraction analysis and the drug release patterns of the selected films were evaluated. Among the prepared formulations, the formulation composed of 1% w/w of PVA, 0.04% w/w of sodium starch glycolate with polyethylene glycol 400, glycerin and water as cosolvents (PVA-S4) showed promising results. The physical appearance and mechanical strength properties were found to be good. The PVA-S4 film was clear and colorless with a smooth surface. The surface pH was found to be around 7.47 and the in vitro disintegration time was around 1.44 min. The drug content of the PVA-S4 film was 100.27%. X-ray diffractometry and thermal analysis confirmed the transition of phenytoin in the PVA-S4 film into a partially amorphous state during film preparation using the cosolvent solubilization approach. The resulting PVA-S4 film showed a higher dissolution rate in comparison to the film without a cosolvent. Overall, this study indicated the influence of cosolvents on enhancing the solubility of a poorly water-soluble drug and its film dissolution.

scholarly journals Formulation and development of vaginal films of poorly water soluble drug, metronidazole, using mixed solvency concept and their evaluations

2018 ◽  
Vol 8 (6) ◽  
pp. 41-48 ◽  
Author(s):  
Neha Gahlot ◽  
Rajesh Kumar Maheshwari
Keyword(s):  
Dosage Form ◽  
Research Work ◽  
Cost Effective ◽  
Stability Study ◽  
Water Soluble ◽  
High Concentration ◽  
Disintegration Time ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Aim: To deliver antibacterial therapy in an efficacious way, film dosage form has been proposed for drug delivery in vagina which can overcome bioavailability issues of poorly water soluble drugs. The present research work is aimed to explore the application of mixed solvency concept to increase solubility of poorly water soluble drug, metronidazole. Materials and Methods: Metronidazole, a slightly soluble drug in water was tried to be solubilized by employing the combination of solubilizers like niacinamide, sodium benzoate, sodium caprylate, caffeine and urea to endeavour its fast dissolving film formulations. The procured sample of drug was characterized by UV, IR and DSC studies. The formulations were evaluated for various properties of film such as thickness, folding endurance, surface pH, disintegration time and thin layer chromatography. Stability studies of vaginal films of metronidazole were performed for ten weeks at room temperature, and refrigerated conditions. Results and Discussion: It was found that 97.54% and 97.58% of drug was remaining after stability study at respective temperatures in batch F1 and 98.53% and 96.57% in batch F4.Conclusion: It was concluded that the approach of mixed solvency concept is novel, safe, cost-effective and user friendly. It also eliminates the problem of toxicity associated with high concentration of water-soluble solubilizers. So, it may be employed in dosage form development of drugs with poor solubility to overcome bioavailability issues. Keywords: Solubility, metronidazole, vaginal films, mixed solvency concept.

scholarly journals FDA-Approved Natural Polymers for Fast Dissolving Tablets

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Md Tausif Alam ◽  
Nayyar Parvez ◽  
Pramod Kumar Sharma
Keyword(s):  
Mangifera Indica ◽  
Nutritional Supplement ◽  
Oral Route ◽  
Water Soluble ◽  
Natural Polymers ◽  
Disintegration Time ◽  
Water Soluble Drug ◽  
Mango Peel ◽  
Fast Disintegrating Tablets ◽  
Poorly Water Soluble Drug

Oral route is the most preferred route for administration of different drugs because it is regarded as safest, most convenient, and economical route. Fast disintegrating tablets are very popular nowadays as they get dissolved or facilely disintegrated in mouth within few seconds of administration without the need of water. The disadvantages of conventional dosage form, especially dysphagia (arduousness in swallowing), in pediatric and geriatric patients have been overcome by fast dissolving tablets. Natural materials have advantages over synthetic ones since they are chemically inert, non-toxic, less expensive, biodegradable and widely available. Natural polymers like locust bean gum, banana powder, mango peel pectin, Mangifera indica gum, and Hibiscus rosa-sinenses mucilage ameliorate the properties of tablet and utilized as binder, diluent, and superdisintegrants increase the solubility of poorly water soluble drug, decrease the disintegration time, and provide nutritional supplement. Natural polymers are obtained from the natural origin and they are cost efficacious, nontoxic, biodegradable, eco-friendly, devoid of any side effect, renewable, and provide nutritional supplement. It is proved from the studies that natural polymers are more safe and efficacious than the synthetic polymers. The aim of the present article is to study the FDA-approved natural polymers utilized in fast dissolving tablets.

Effect of TPGS surfactant on dissolution sensitivity of a poorly water-soluble drug using high-shear wet granulation

2020 ◽  
Vol 375 ◽  
pp. 302-309
Author(s):  
Sutthilug Sotthivirat ◽  
Rishi Ramesh ◽  
Walter Wasylaschuk ◽  
Cory Bottone ◽  
Binfeng Xia ◽  
...  
Keyword(s):  
Water Soluble ◽  
Wet Granulation ◽  
High Shear ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
High Shear Wet Granulation ◽  
Poorly Water Soluble Drug

scholarly journals Impact of Superdisintegrants and Film Thickness on Disintegration Time of Strip Films Loaded With Poorly Water-Soluble Drug Microparticles

2018 ◽  
Vol 107 (8) ◽  
pp. 2107-2118 ◽  
Author(s):  
Lu Zhang ◽  
Marie Aloia ◽  
Barbara Pielecha-Safira ◽  
Honghao Lin ◽  
Prarthana Manoj Rajai ◽  
...  
Keyword(s):  
Film Thickness ◽  
Water Soluble ◽  
Disintegration Time ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

Improved Dissolution Properties of Ketoconazole through Application of Liquisolid Techniques

2015 ◽  
Vol 8 (4) ◽  
pp. 3053-3059
Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
H G Sandip
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Water Soluble ◽  
Wet Granulation ◽  
Wetting Properties ◽  
Enhanced Dissolution ◽  
Water Soluble Drug ◽  
Drug Concentrations ◽  
Water Soluble Drugs ◽  
Liquisolid Compacts

In present investigation liquisolid compact technique is investigated as a tool for enhanced dissolution of poorly water-soluble drug Ketoconazole. The liquisolid tablets were formulated with liquid medications, namely Propylene Glycol (PG) drug concentrations, 60% w/w, 70% w/w and 80% w/w. Avicel pH102 was used as a carrier material, Aerosil 200 as a coating material and Sodium starch glycollate as a super-disintegrant. Quality control tests, such as uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution tests were performed to evaluate prepared tablets. For further confirmation of results the liquisolid compacts were evaluated by XRD and FTIR studies to prove that, solubility of Ketoconazole has been increased by liquisolid compact technique. From the results obtained, it was be speculated that such systems exhibit enhanced drug release profiles due to increased wetting properties and surface of drug available for dissolution. As liquisolid compacts demonstrated significantly higher drug release rates, in PG as compared to directly compressible tablets and conventional wet granulation, we lead to conclusion that it could be a promising strategy in improving the dissolution of poor water soluble drugs and formulating immediate release solid dosage forms.  

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