Effect of water-soluble additives on drug release from silicone rubber matrices. II. Sustained release of prednisolone from non-swelling devices

1986 ◽  
Vol 30 (1) ◽  
pp. 1-7 ◽  
Author(s):  
G. Di Colo ◽  
V. Carelli ◽  
E. Nannipieri ◽  
M.F. Serafini ◽  
D. Vitale
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Silicone Rubber ◽  
Water Soluble ◽  
Effect Of Water

scholarly journals High-Amylose Sodium Carboxymethyl Starch Matrices: Development and Characterization of Tramadol Hydrochloride Sustained-Release Tablets for Oral Administration

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Teresa Nabais ◽  
Grégoire Leclair
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Corn Starch ◽  
Water Soluble ◽  
Hydroxyl Groups ◽  
Sustained Drug Release ◽  
Tramadol Hydrochloride ◽  
Carboxymethyl Starch ◽  
High Amylose ◽  
Sodium Carboxymethyl Starch

Substituted amylose (SA) polymers were produced from high-amylose corn starch by etherification of its hydroxyl groups with chloroacetate. Amorphous high-amylose sodium carboxymethyl starch (HASCA), the resulting SA polymer, was spray-dried to obtain an excipient (SD HASCA) with optimal binding and sustained-release (SR) properties. Tablets containing different percentages of SD HASCA and tramadol hydrochloride were produced by direct compression and evaluated for dissolution. Once-daily and twice-daily SD HASCA tablets containing two common dosages of tramadol hydrochloride (100 mg and 200 mg), a freely water-soluble drug, were successfully developed. These SR formulations presented high crushing forces, which facilitate further tablet processing and handling. When exposed to both a pH gradient simulating the pH variations through the gastrointestinal tract and a 40% ethanol medium, a very rigid gel formed progressively at the surface of the tablets providing controlled drug-release properties. These properties indicated that SD HASCA was a promising and robust excipient for oral, sustained drug-release, which may possibly minimize the likelihood of dose dumping and consequent adverse effects, even in the case of coadministration with alcohol.

Development and Evaluation of Sustained Release Matrix Tablets of Tramadol Hydrochloride

1970 ◽  
Vol 9 (4) ◽  
pp. 3364-3371
Author(s):  
Ganesh Basarkar ◽  
Vijay Suryawanshi ◽  
Dinesh Hire
Keyword(s):  
Calcium Phosphate ◽  
Drug Release ◽  
Sustained Release ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix System ◽  
Tramadol Hydrochloride ◽  
Sustained Release Formulation

The objective of the present study was to control the release of freely water soluble Tramadol hydrochloride over a prolonged period of time by embedding the drug into novel wax matrix system. The matrix granules were prepared by melt granulation technique. The need for the administration two to four times a day when larger dose are required can decrease patient compliance. Sustained release formulation that would maintain plasma levels for 24 hrs for once daily dosing of Tramadol hydrochloride was prepared. The compatibility of the drug and wax examined using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared Spectrophotometer (FTIR). The effect of wax concentration (5 to 35%) and channeling agents (Avicel PH-101 and Di-calcium phosphate) on the in vitro drug release at 24 hrs. was studied.  Results of DSC confirmed drug-wax compatibility. Increasing the wax concentration resulted in a significant retardation of drug release. The drug release study revealed that the optimized formulation (F6) 30% novel wax sustained drug release for 24hrs. At the same wax concentration, drug release from tablets decreased with Di-calcium phosphate and increased with Avicel PH 101. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. A hydrophobic matrix system is thus useful technique for prolonging the drug release of freely water soluble drugs such as Tramadol hydrochloride

Formulation Development and Evaluation of Sustained Release Matrix Tablets of Guaiphenesin

2016 ◽  
Vol 9 (3) ◽  
pp. 3312-3316
Author(s):  
Ganesh D. Basarkar ◽  
Ketan H. Shah ◽  
Madhuri B. Sonawane
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Rice Bran ◽  
Half Life ◽  
Water Soluble ◽  
Matrix Tablet ◽  
Formulation Development ◽  
Sustained Release Formulation ◽  
Rice Bran Wax ◽  
Melt Granulation

In this study we sought to formulate and evaluate sustained release matrix tablet of guaiphenesin by melt granulation technology. The sustained release tablets were prepared by melt granulation technique using rice bran wax as a drug retardant and dibasic calcium phosphate (DCP) as a channelling agent. Guaiphenesin is an expectorant and has a short plasma half-life of one hour. Because of high frequency of administration and short biological half-life, guaiphenesin was considered as model drug. Sustained release formulation that would maintain plasma levels for 12 hours is sufficient for twice daily dosing of guaiphenesin. The compatibility of drug and wax was examined by differential scanning calorimetry (DSC). The effect of waxes at different (drug: wax) concentrations on the release profile of drug from matrix formulation were studied. Drug release was studied at pH 1.2 for 2 hour and pH 6.8 for 10 hours. A significant retardation in the drug release was observed by increasing the wax concentration. The drug release study revealed that wax concentration of 30% to be optimum. Dissolution study showed 99% drug release within 12 hrs. Kinetic modelling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. These results suggest that the rice bran wax has good release retardant property for highly water-soluble drug such as guaiphenesin.

Reverse micelles-in-microspheres with sustained release of water-soluble combretastatin A4 phosphate for S180 tumor treatment

2016 ◽  
Vol 4 (4) ◽  
pp. 760-767 ◽  
Author(s):  
Liping wu ◽  
Liyan Qiu
Keyword(s):  
Cancer Therapy ◽  
Drug Release ◽  
Sustained Release ◽  
Reverse Micelles ◽  
Encapsulation Efficiency ◽  
Water Soluble ◽  
Tumor Treatment ◽  
Sustained Drug Release ◽  
Unique Type ◽  
Combretastatin A4

CA4P-loaded microspheres (CA4P-MS) composed of PELA reverse micelles (CA4P-RM) and PLGA with a sea-island structure were prepared. This unique type of construction can greatly improve the encapsulation efficiency of water-soluble CA4P and provide sustained drug release and action for cancer therapy.

scholarly journals Evaluation of formulation and effects of process parameters on drug release and mechanical properties of tramadol hydrocloride sustained release matrix tablets

2015 ◽  
Vol 69 (5) ◽  
pp. 503-510 ◽  
Author(s):  
Nenad Nikolic ◽  
Djordje Medarevic ◽  
Svetlana Ibric ◽  
Zorica Djuric
Keyword(s):  
Mechanical Properties ◽  
Tensile Strength ◽  
Drug Release ◽  
Sustained Release ◽  
Process Parameters ◽  
Water Soluble ◽  
Matrix Tablets ◽  
High Dose ◽  
Compression Pressure ◽  
Water Soluble Drug

This study investigates using of high molecular weight polyethylene oxide (PEO WSR Coagulant) for the preparation of sustained release matrix tablets containing high dose, highly water soluble drug, tramadol HCl. Proportion of PEO polymer, type of insoluble filler, proportion of tramadol HCl, amount of drug in tablet, tablet diameter and compression pressure were recognized as critical formulation and process parameters and their influence on drug release and tablet mechanical properties was evaluated. Percentages of tramadol HCl released after 30 and 240 minutes were selected for evaluation of drug release, while tensile strength was used as indicator of tablet mechanical properties. Only proportion of tramadol HCl exhibits statistically significant effect on percentages of tramadol HCl released after 30 and 240 minutes, with higher, wherein increasing of the tramadol HCl proportion increased its release rate among the evaluated variables in selected ranges. All of the investigated factors exhibit statistically significant effect on tablets tensile strength, with the largest influence of filler type. Tablets prepared with highly compressible filler (microcrystalline celullose) exhibit higher tensile strength and therefore better mechanical properties to those prepared with partially pregelatinised starch (Strach 1500).

Effects of release modifier on Carvedilol release from Kollidon SR based matrix

2012 ◽  
Vol 1 (8) ◽  
pp. 186 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Microcrystalline Cellulose ◽  
Matrix Tablets ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Weight Variation ◽  
The Matrix ◽  
Tablet Formulations

<p>Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.</p><p>DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.11095">http://dx.doi.org/10.3329/icpj.v1i8.11095</a></p> <p>International Current Pharmaceutical Journal 2012, 1(8): 186-192</p>

Sign in / Sign up

Export Citation Format

Share Document