Ultrasound Effect on Swelling Properties and Drug Release Behaviors of Spray-Dried Tapioca Starch Tablets

2013 ◽  
Vol 747 ◽  
pp. 131-134
Author(s):  
Somkamon Manchun ◽  
Sontaya Limmatvapirat ◽  
Pornsak Sriamornsak

Modified starches have been widely used as an excipient in matrix tablets to control drug release. A new processing method for the production of modified starch, high power ultrasonic treatment (400 W), was applied to native tapioca starch. The spray drying technique was used after modification (i.e., by ultrasonic or heat treatment). Matrix tablets were then prepared by direct compression using theophylline as a model drug. The effect of starch modification on swelling, erosion and in vitro drug release behaviors of compressed matrices was investigated in 0.1 N HCl or phosphate buffer (pH 6.8). The matrix tablets of modified tapioca starch formed a continuous gel layer while in contact with the aqueous medium undergoing a combination of swelling and erosion. The ultrasound-treated starch swelled and eroded less than the native starch and heat-treated starch, thus the drug release from matrix tablets using ultrasound-treated starch was slower. For these results, it can be concluded that the ultrasound-treated starch was a promising excipient for controlled drug release.

2014 ◽  
Vol 16 (2) ◽  
pp. 398-406 ◽  
Author(s):  
Uroš Klančar ◽  
Saša Baumgartner ◽  
Igor Legen ◽  
Polona Smrdel ◽  
Nataša Jeraj Kampuš ◽  
...  

Materials ◽  
2019 ◽  
Vol 12 (21) ◽  
pp. 3634 ◽  
Author(s):  
Luciano C. B. Lima ◽  
Caio C. Coelho ◽  
Fabrícia C. Silva ◽  
Andréia B. Meneguin ◽  
Hernane S. Barud ◽  
...  

Inorganic matrices and biopolymers have been widely used in pharmaceutical fields. They show properties such as biocompatibility, incorporation capacity, and controlled drug release, which can become more attractive if they are combined to form hybrid materials. This work proposes the synthesis of new drug delivery systems (DDS) based on magnesium phyllosilicate (Talc) obtained by the sol–gel route method, the biopolymer chitosan (Ch), and the inorganic-organic hybrid formed between this matrix (Talc + Ch), obtained using glutaraldehyde as a crosslink agent, and to study their incorporation/release capacity of amiloride as a model drug. The systems were characterized by X-ray diffraction (XRD), Therma analysis TG/DTG, and Fourier-transform infrared spectroscopy (FTIR) that supported the DDS’s formation. The hybrid showed a better drug incorporation capacity compared to the precursors, with a loading of 55.74, 49.53, and 4.71 mg g−1 for Talc + Ch, Talc, and Ch, respectively. The release assays were performed on a Hanson Research SR-8 Plus dissolver using apparatus I (basket), set to guarantee the sink conditions. The in vitro release tests showed a prolongation of the release rates of this drug for at least 4 h. This result proposes that the systems implies the slow and gradual release of the active substance, favoring the maintenance of the plasma concentration within a therapeutic window.


2012 ◽  
Vol 90 (7) ◽  
pp. 600-607 ◽  
Author(s):  
Li Xu ◽  
Lidong Shao ◽  
Minqi Hu ◽  
Lin Chen ◽  
Yunmei Bi

A new third-generation thermoresponsive amphiphilic dendron consisting of a hydrophobic poly(benzyl ether) dendritic core and hydrophilic oligo(ethylene glycol) peripheries was synthesized by an efficient convergent approach. Its structure was confirmed by 1H NMR, 13C NMR, IR, GPC, MALDI-TOF MS, and elemental analysis. Turbidity and dynamic light scattering (DLS) measurements demonstrated that the dendron showed a reversible temperature-dependent phase-transition behavior in aqueous solution and its lower critical solution temperature (LCST) was lower than that of the corresponding second-generation dendron, indicating the dependence of LCSTs on the generation of dendrons. Fluorescent spectroscopy and TEM studies revealed that the dendron would self-assemble into nanospherical micelles with a very low critical micelle concentration (CMC) in water. The core-shell structure of the micelles was proved by 1H NMR analyses of the micelles in D2O. The drug-loading capacity of the dendron micelles is about 29 wt % for podophyllotoxin (POD) used as a model drug, and in vitro release tests showed a desired thermoresponsive drug-release behavior. These results indicate that the dendron is promising as stimuli-responsive material for biomedical applications.


Author(s):  
Surender Verma ◽  
S. Singh ◽  
D. Mishra ◽  
Atul Gupta ◽  
Rakesh Sharma

The objective of present study was to develop colon targeted drug delivery using bacterially triggered approach through oral route. Valdecoxib (COX-2 inhibitor) was chosen as a model drug in order to target it to colon which may prove useful in inflammatory bowel disease and related disorders. Matrix tablets of Valdecoxib were prepared by wet granulation technique utilizing different ratio of Guar gum and Sodium starch glycholate. The prepared matrix tablets were evaluated for uniformity of weight, uniformity of content, hardness and in vitro dissolution study in simulated gastric and intestinal fluid (Phosphate Buffer pH-1.2, pH-6.8 and pH-7.4), followed by Dissolution study in bio-relevant dissolution media Phosphate Buffer (pH-6.8) containing rat caecal content. The results revealed that the formulated batch had released lesser quantity of drug at pH 1.2 and pH 7.4 in 2 hors whereas in biorelevent dissolution media containing rat caecal content it released significantly higher amount of drug which was also significantly higher than the dissolution media of same pH without caecal content (microflora) and it was concluded that guar gum can be used as a potential carrier for targeting drugs to colon.


Author(s):  
Bhikshapathi D. V. R. N. ◽  
Haarika B ◽  
Jyothi Sri S ◽  
K Abbulu

The purpose of present investigation was to develop floating matrix tablets of gemifloxacin mesylate, which after oral administration could prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. Tablets containing drug, various viscosity grades of hydroxypropyl methylcellulose such as HPMC K4M and HPMC K15M as matrix forming agent, Sodium bicarbonate as gas-forming agent and different additives were tested for their usefulness in formulating gastric floating tablets by direct compression method. The physical parameters, in vitro buoyancy, release characteristics and in vivo radiographic study were investigated in this study. The gemifloxacin mesylate floating tablets were prepared using HPMC K4M polymer giving more sustained drug release than the tablet containing HPMC K15M. All these formulations showed floating lag time of 30 to 47 sec and total floating time more than 12 h. The drug release was decreased when polymer concentration increases and gas generating agent decreases. Formulation that contains maximum concen-tration of both HPMC K15M and sodium bicarbonate (F9) showing sufficiently sustained with 99.2% of drug release at 12 h. The drug release from optimized formulation follows Higuchi model that indicates the diffusion controlled release. The best formulation (F9) was selected based on in vitro characteristics and used in vivo radiographic studies by incorporating barium sulphate as a radio-opaque agent and the tablet remained in the stomach for about 6 h.   


Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.


2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.


2020 ◽  
Vol 10 (3) ◽  
pp. 237-249
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma

Introduction: Hydrodynamically balanced system (HBS) possesses prolonged and continuous delivery of the drug to the gastrointestinal tract which improves the rate and extent of medications that have a narrow absorption window. The objective of this work was to develop a Hydrodynamically Balanced System (HBS) of Metoprolol Succinate (MS) as a model drug for sustained stomach specific delivery. Materials and Methods: Experimental batches were designed according to 3(2) Taguchi factorial design. A total of 9 batches were prepared for batch size 100 capsules each. Formulations were prepared by physically blending MS with polymers followed by encapsulation into hard gelatin capsule shell of size 0. Polymers used were Low Molecular Weight Chitosan (LMWCH), Crushed Puffed Rice (CPR), and Hydroxypropyl Methylcellulose K15 M (HPMC K15M). Two factors used were buoyancy time (Y1) and time taken for 60% drug release (T60%; Y2). Results: The drug excipient interaction studies were performed by the thermal analysis method which depicts that no drug excipient interaction occurs. In vitro buoyancy studies and drug release studies revealed the efficacy of HBS to remain gastro retentive for a prolonged period and concurrently sustained the release of MS in highly acidic medium. All formulations followed zero-order kinetics. Conclusion: Developed HBS of MS with hydrogel-forming polymers could be an ideal delivery system for sustained stomach specific delivery and would be useful for the cardiac patients where the prolonged therapeutic action is required.


2021 ◽  
pp. 096703352098235
Author(s):  
Tomomi Takaku ◽  
Yusuke Hattori ◽  
Tetsuo Sasaki ◽  
Tomoaki Sakamoto ◽  
Makoto Otsuka

The effect of grinding on the pharmaceutical properties of matrix tablets consisting of ground glutinous rice starch (GRS) and theophylline (TH) was predicted by near infrared (NIR) spectroscopy. Ground GRS samples were prepared by grinding GRS in a planetary ball mill for 0-120 min, measured by X-ray diffractometry (XRD) and NIR, and then evaluated for crystallinity (%XRD) based on XRD profiles. Tablets containing TH (5 w/w%), ground GRS (94 w/w%), and magnesium stearate (1 w/w%) were formed by compression. Gel-forming and drug-release processes of the tablets were measured using a dissolution instrument with X-ray computed tomography (XCT). Swelling ratio (SWE) and mean drug-release time (MDT) were evaluated based on XCT and drug-release profiles, respectively. Calibration models for predicting percent %XRD, MDT, and SWE were constructed based on the NIR of ground GRS using partial least-squares. The results indicated the possibility of controlling the pharmaceutical properties of matrix tablets by altering the pre-gelatinization of GRS based on changes in their NIR spectra during the milling process.


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