In vitro dissolution of sparingly water-soluble drug dosage forms

1995 ◽  
Vol 125 (1) ◽  
pp. 99-106 ◽  
Author(s):  
Vinod P. Shah ◽  
Assad Noory ◽  
Carol Noory ◽  
Bruce McCullough ◽  
Sanford Clarke ◽  
...  
Keyword(s):  
Drug Dosage ◽  
Dosage Forms ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Water Soluble Drug

scholarly journals FORMULATION AND CHARACTERIZATION OF GASTRORETENTIVE FLOATING MICROBALLOONS OF POORLY WATER-SOLUBLE DRUG DIACEREIN

2021 ◽  
Vol 15 (5) ◽  
pp. 8-12
Author(s):  
Kajal Tomer ◽  
Dilip Kumar Gupta
Keyword(s):  
Particle Size ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Diffusion Method ◽  
Acrylic Polymer ◽  
Water Soluble Drug ◽  
Technological Advances ◽  
S 100

The drug can be released in a controlled manner using a gastro retentive dosage type. The main focus on the novel technological advances in the floating drug delivery method for gastric retention. The preparation of diacerein micro balloon is done by solvent diffusion method, using acrylic polymer like Eudragit S 100 and HPMC K4 M. The various evaluation of the prepared floating microsphere like its % yield, drug entrapment efficiency, particle size in-vitro dissolution, buoyancy, was studied. The floating microsphere was found to be spherical and range from 85 μm - 192 μm. Whereas the buoyancy in gastric mucosa between the range 30.5% -49.5%. The % yield and % entrapment efficiency were found under the range 61% - 82% and 45.1–84.1% respectively. The microsphere showed favorable in-vitro dissolution 76.8 to 94.45. The optimized formulation was found based on evaluation of floating micro-balloons, Formulation (M3E3) showed the best result as particle size 192 μm, DDE 84.1%, in vitro drug release 94.5%, and in vitro buoyancy 49.5%. all the formulations showed controlled release up to 24 hours.

Design, Optimization and Evaluation of Repaglinide Self-Nanoemulsifying Drug Delivery for Enhanced Solubility

2017 ◽  
Vol 10 (6) ◽  
pp. 3920-3928
Author(s):  
Mahalaxmi K ◽  
Sailu Ch
Keyword(s):  
Drug Delivery ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Antidiabetic Drug ◽  
Water Soluble Drug ◽  
Enhanced Solubility ◽  
Poorly Water Soluble ◽  
Capmul Mcm ◽  
Poorly Water Soluble Drug

The aim of study was to develop self-nanoemulsifying systems of poorly water-soluble drug repaglinide, which is an antidiabetic drug in the class of medications known as meglitinides. Solubility of repaglinide in oily phases and surfactants was determined to identify components of self-nanoemulsifying drug delivery system (SNEDDS). Surfactants and oil was selected based on solubility studies were further screened for their efficiency in formulation. Acrysol K 150, Kolliphor EL and Capmul MCM were selected as oil, surfactant and co-surfactant respectively. Formulation F8 was found to be optimized formulation on the basis of in vitro dissolution studies, particle size and zeta potential. The optimized formulation was then subjected to stability studies and was found to be stable after 6 months. Thus, SNEDDS were found to be influential in improving the release performance of repaglinide, indicating their potential to improve the solubility and oral bioavailability of repaglinide.  

scholarly journals FORMULATION AND EVALUATION OF SOLID SELF-EMULSIFYING DRUG DELIVERY SYSTEM OF GLICLAZIDE

2016 ◽  
Vol 8 (11) ◽  
pp. 144
Author(s):  
Suwarna R. Deshmukh ◽  
Suparna S. Bakhle ◽  
Kanchan P. Upadhye ◽  
Gouri R. Dixit
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Water Soluble Drug

Objective: Gliclazide (GCZ) is a widely prescribed anti-diabetic drug belongs to class IΙ under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. The present investigations highlight the development of solid self-emulsifying drug delivery system (solid-SEDDS) for improved oral delivery of the poorly water-soluble drug, GCZ.Methods: Various oils, surfactant and co-surfactant, were screened for their emulsification ability. Ternary phase diagrams were plotted to identify the zone of micro-emulsification. Liquid SEDDS of the drug were formulated using lemon oil as the oil phase, tween 80, as the surfactant, and labrasol, as the co-surfactant. The optimized liquid SEDDS was transformed into free-flowing powder using florite R as the adsorbent. Results: Self-emulsifying powder retained the self-emulsifying property of the liquid SEDDS. The morphology of solid-SEDDS from scanning electron microscopy studies demonstrated the presence of spherical, granular particles indicating good flowing ability. X-ray powder diffraction studies confirmed solubilization of the drug in the lipid excipients and/or transformation of a crystalline form of the drug to amorphous form. In vitro dissolution studies revealed enhanced release of the drug from solid-SEDDS as compared to plain drug and marketed formulation.Conclusion: Thus it can be concluded that solid-SEDDS, amenable for the development of solid dosage form, can be successfully developed using florite R with the potential of enhancing the solubility, dissolution rate, and bioavailability of the drug.

MICROWAVE GENERATED SOLID DISPERSION OF REPAGLINIDE WITH NOVEL NATURAL CARRIER MODIFIED GUM KONDAGOGU

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (05) ◽  
pp. 5-11
Author(s):  
Z. L Ramvallabh ◽  
◽  
B. S Baburao
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Microwave Method ◽  
Promising Alternative ◽  
Water Soluble Drug ◽  
Gum Kondagogu ◽  
Poorly Water Soluble Drug

The influence of microwave technology and modified gum kondagogu (MGK) on the in vitro dissolution rate of a poorly - water soluble drug repaglinide (RG) was studied. Solid dispersions were prepared using gum kondagogu (GK) & MGK as a carrier by microwave method. Microwave generated solid dispersions with MGK exhibited remarkable improvement in solubility and dissolution rate compared to that of pure RG. In conclusion, microwave method together with MGK as a potential carrier could be considered as simple, efficient and solvent free promising alternative method to prepare solid dispersions.

Formulation and Evaluation of Bilayer Sustained Release Tablets of Salbutamol and Theophylline

2009 ◽  
Vol 2 (3) ◽  
pp. 638-646
Author(s):  
R. Nagaraju ◽  
Rajesh Kaza
Keyword(s):  
Ethyl Cellulose ◽  
Xanthan Gum ◽  
Dosage Forms ◽  
In Vitro Dissolution ◽  
Dissolution Studies ◽  
Sustained Release Tablets ◽  
Dissolution Apparatus ◽  
Single Dosage

Salbutamol and theophylline are available in conventional dosage forms, administered four times a day, leading to saw tooth kinetics and resulting in ineffective therapy. The combination of these two drugs in a single dosage form will enhance the patient compliance and prolong bronchodilation. Various polymers, such as hydroxy propyl methylcellulose K4M (HPMC- K4M), hydroxy propyl methylcellulose K100M (HPMC- K100M), xanthan gum, ethyl cellulose and hydroxy propyl methylcellulose phthalate (HPMC-P) were studied. HPMC-P and HPMC- K4M were found to be best in controlling the release. In-vitro dissolution studies were carried out for all the bi-layered tablets developed using USP dissolution apparatus type 2 (paddle). It was found that the tablet FB15-FW3 showed 50% release of salbutamol in first hour and the remaining was released for eight hours. However, theophylline was found to be released as per the USP specifications. The IR spectrum was taken for FB15-FW3 formulation and it revealed that there is no disturbance in the principal peaks of pure drugs salbutamol and theophylline. This further confirms the integrity of pure drugs and no incompatibility of them with excipients. Also, formulation of FB15-FW3 has shown required release pattern and complies with all the evaluated parameters and comparable to the marketed formulation.

Formulation and Evaluation of Orally Disintegrating Tablets of Lamotrigine

2015 ◽  
Vol 8 (2) ◽  
pp. 2881-2888
Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
P Karade
Keyword(s):  
Drug Release ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Orally Disintegrating Tablet ◽  
Drug Content ◽  
Weight Variation ◽  
Wetting Time ◽  
Croscarmellose Sodium

The aim of this study was to design orally disintegrating tablet (ODT) of Lamotrigine. It is an Antiepileptic drug which is widely used in epilepsy. It is also used in simple and complex partial seizures and secondary generalized tonic-clonic seizures. It is poorly water soluble drug (0.46 mg/ml). Thus, an attempt was made to enhance the water solubility by complexation with β-cyclodextrin (1:1 molar ratios). The orally disintegrating tablet of lamotrigine was prepared by direct compression method using different concentration of superdisintegrants such as Sodium starch glycollate, croscarmellose sodium by sublimating agent such as camphor. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies. The prepared tablets were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The disintegration time for the complexed tablets prepared by different concentration of superdisintegrants was found to be in range of 32.54 ± 0.50 to 55.12 ± 0.57 sec and wetting time of the formulations was found to be in range of 28.47 ± 0.67 to 52.19 ± 0.72 sec. All the formulation showed almost 100 percent of drug release within 15 min. Among all the formulation F6 and F7 prepared with 18% croscarmellose sodium and camphor shows faster drug release, respectively 10 min, F6 gives good result for disintegration time, drug release, wetting time and friability. Further formulations were subjected to stability testing for 30 days at temperature of 40 ± 5 ºC/75 ± 5 %RH. Tablets showed no appreciable changes with respect to physical appearance, drug content, disintegration time and dissolution profiles. Results were statistically analyzed by one-way ANOVA at a p < 0.05. It was found that, the data at any point of time are significant at p < 0.05.

The Potential Migrated Mechanism of Water-Soluble Components in Pellets Prepared by Wet Extrusion/Spheronization: Effect of Drying Rate

2020 ◽  
Vol 17 ◽  
Author(s):  
Bingwei Wang ◽  
Jianping Liu ◽  
Zhenghua Li ◽  
Yulong Xia ◽  
Shuangshuang Zhang ◽  
...  
Keyword(s):  
Relative Humidity ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Drying Rate ◽  
Scanning Calorimetry ◽  
Drying Temperature ◽  
Wet Extrusion ◽  
Extrusion Spheronization ◽  
Soluble Components

Background: At present, there were numerous researches on the migration of components in tablets and granules, the investigation in the pharmaceutical literatrue concerning the effect of drying rate on the migration of water-soluble components of pellets was limited. Temperature and relative humidity (RH) were crucial parameters during the drying process which was an essential step in the preparation of pellets via wet extrusion/spheronization. To quantify these variables, the water loss percentage of pellets per minute was defined as drying rate. Objective: The study aimed to investigate the influence of drying rate on the migration of water-soluble components in wet pellets and the potential migrated mechanism. Methods: The pellets containing tartrazine as a water-soluble model drug and microcrystalline cellulose as a matrix former were prepared by extrusion/spheronization and dried at four different drying temperature and relative humidity. Afterward, the extent of migrated tartrazine was assessed regarding appearance, in-vitro dissolution test, Differential Scanning Calorimetry, X-Ray Powder Diffraction, Attenuated total reflectance Fourier transform infrared spectroscopy and Confocal Raman Mapping. Results: Results demonstrated that red spots of tartrazine appeared on the surface of pellets and more than 40% tartrazine were burst released within 5 minutes when pellets dried at 60℃/RH 10%. While pellets dried at 40℃/RH 80%, none of these aforementioned phenomena was observed. Conclusion: In conclusion, the faster drying rate was, the more tartrazine migrated to the exterior of pellets. Adjusting drying temperature and relative humidity appropriately could inhibit the migration of water-soluble components within wet extrusion/spheronization pellets.

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