Biomedical subjects

Thaned Pongjanyakul

Publications and source records attributed to Thaned Pongjanyakul.

11 recordsLinked to original sources

PubMed2006

Alginate-magnesium aluminum silicate films: effect of plasticizers on film properties, drug permeation and drug release from coated tablets.

The effect of hydrophilic plasticizers, namely glycerin and polyethylene glycol 400 (PEG400), on physicochemical properties of sodium alginate-magnesium aluminum silicate (SA-MAS) microcomposite films was characterized and application of the films for controlling drug release from tablets was evaluated as well. The plasticizers could possibly interact with SA or MAS by formation of hydrogen bonding, as revealed using FTIR spectroscopy. PXRD studies presented that glycerin or PEG400 could intercalate into the silicate layers of MAS and higher crystallinity of the films with PEG400 was obtained. This led to a different thermal behavior of the films. Glycerin gave more flexibility of the films than PEG400. Incorporation of plasticizers into the films did not affect water uptake in acid medium, but increasing an erosion of the films because of the leaching of the plasticizers. Water vapor permeability of the films decreased with increasing amount of plasticizers in the range of 10-30% (w/w). Diffusion coefficient (D) of acetaminophen (ACT) across the films in acid medium increased with addition of the plasticizers because the leaching of plasticizers could reduce tortuosity of aqueous pore channels of the films. The tablets coated with plasticized films had a quite smooth surface without defect as shown by SEM. The ACT release profiles from the coated tablets showed a zero-order release kinetic with drug diffusion mechanism across in situ insoluble composite films in acid medium, and coating film swelling and erosion mechanism in pH 6.8 phosphate buffer. Moreover, neither the release rate nor the release pattern of the ACT coated tablets was obviously changed. The findings show that glycerin or PEG400 could improve physicochemical properties of the SA-MAS films and the plasticized films could control the drug release from tablets in gastro-intestinal condition.

Acetaminophen↗

PubMed2006

Xanthan-alginate composite gel beads: molecular interaction and in vitro characterization.

Xanthan gum (XG), a trisaccharide branched polymer, was applied to reinforce calcium alginate beads in this study. Composite beads consisting of XG and sodium alginate (SA) were prepared using ionotropic gelation method. Diclofenac calcium-alginate (DCA) beads incorporated with different amounts of XG were produced as well. Molecular interaction between SA and XG in the composite beads and the XG-DCA beads was investigated using FTIR spectroscopy. Physical properties of the XG-DCA beads such as entrapment efficiency of diclofenac sodium (DS), thermal property, water uptake, swelling and DS release in various media were examined. XG could form intermolecular hydrogen bonding with SA in the composite beads with or without DS. Differential scanning calorimetric study indicated that XG did not affect thermal property of the DCA beads. The DS entrapment efficiency of the DCA beads increased with increasing amount of XG added. The XG-DCA beads showed higher water uptake and swelling in pH 6.8 phosphate buffer and distilled water than the DCA beads. A longer lag time and a higher DS release rate of the XG-DCA beads in pH 6.8 phosphate buffer were found. In contrast, the 0.3%XG-DCA beads could retard the drug release in distilled water because interaction between XG and SA gave higher tortuosity of the bead matrix. However, higher content of XG in the DCA beads increased the release rate of DS. This can be attributed to erosion of small aggregates of XG on the surface of the DCA beads. This finding suggested that XG could modulate physicochemical properties and drug release of the DCA beads, which based on the existence of molecular interaction between XG and SA.

Alginates↗

PubMed2006

Modulation of drug release from glyceryl palmitostearate-alginate beads via heat treatment.

Diclofenac calcium alginate (DCA) beads containing glyceryl palmitostearate (GPS) were prepared by ionotropic gelation method. The effect of GPS amount and heat treatment on characteristics of the DCA beads was investigated. Incorporation of GPS into the DCA beads increased particle size and entrapment efficiency of diclofenac sodium (DS), but decreased water uptake in distilled water, and DS release rate. The heat treatment caused the DCA beads to be irregular shape particles and to possess higher water uptake. A slower release rate of DS in distilled water was found because of interaction of DS and alginate polymer matrix, and a restriction of water sorption into the inside region of the beads, which caused by the shrinkage of the beads after heating. However, the heat treatment did not affect particle shape and water uptake in distilled water of the 3%GPS-DCA beads. Differential scanning calorimetric study showed that GPS in the DCA beads was resolidified to different polymorph after cooling. Furthermore, the micro-Raman spectra indicated the existence of DS in the GPS matrix particles in the beads due to the partition of DS into the melted GPS during heat treatment. This led to a decrease in release rate of DS in pH 6.8 phosphate buffer and a change in DS release pattern in distilled water. Thus, not only the calcium alginate matrix, but also the resolidified GPS matrix in the alginate beads controlled the DS release from the 3%GPS-DCA beads with heat treatment.

Alginates↗

PubMed2005

Investigation of novel alginate-magnesium aluminum silicate microcomposite films for modified-release tablets.

Physicochemical properties of sodium alginate-magnesium aluminum silicate (SA-MAS) composite films were investigated and a potential as a film former of SA-MAS dispersion for modifying drug release from tablets was evaluated as well. Interaction between SA and MAS in the composite films was revealed using FTIR spectroscopy. Thermal behavior of the composite films was changed due to the complexation of SA and MAS. Powder X-ray diffractometry data suggested that a higher crystallinity of the composite film and a phase-separated microcomposite were formed. The composite films in the ratios of 1:0.5 and 1:1 showed the increases of tensile strength and percentage of elongation when compared with SA films. Water vapor permeability of the composite films tended to increase with increasing ratio of MAS. The decreases in water uptake and drug permeability in 0.1 M HCl were found in the composite films. A positive charge drug, propranolol HCl, provided a higher affinity on the composite films than a weakly acidic nonelectrolyte, acetaminophen, resulting in a longer lag time and a higher partition coefficient depending on the content of MAS in the composite films. This was due to the complex formation of propranolol HCl and MAS. Using SEM, the tablets coated with SA-MAS dispersion had a smooth surface, while those with SA dispersion showed a pinholing on the surface, resulting in a faster drug release. The drug release profiles of the tablets could be modified by coating with the composite film at different coating levels. This finding suggests that MAS could improve physicochemical properties of the SA films, leading to a novel coating material of the SA-MAS dispersion for modifying drug release from tablets.

Absorption↗

PubMed2005

Effect of polysulfonate resins and direct compression fillers on multiple-unit sustained-release dextromethorphan resinate tablets.

The purpose of this work was to investigate the effect of different polysulfonate resins and direct compression fillers on physical properties of multiple-unit sustained-release dextromethorphan (DMP) tablets. DMP resinates were formed by a complexation of DMP and strong cation exchange resins, Dowex 50 W and Amberlite IRP69. The tablets consisted of the DMP resinates and direct compression fillers, such as microcrystalline cellulose (MCC), dicalcium phosphate dihydrate (DCP), and spray-dried rice starch (SDRS). Physical properties of tablets, such as hardness, disintegration time, and in vitro release, were investigated. A good performance of the tablets was obtained when MCC or SDRS was used. The use of rod-like and plate-like particles of Amberlite IRP69 caused a statistical decrease in tablet hardness, whereas good tablet hardness was obtained when spherical particle of Dowex 50 W was used. The plastic deformation of the fillers, such as MCC and SDRS, caused a little change in the release of DMP. A higher release rate constant was found in the tablets containing DCP and Dowex 50 W, indicating the fracture of the resinates under compression, which was attributable to the fragmentation of DCP. However, the release of DMP from the tablets using Amberlite IRP69 was not significantly changed because of the higher degree of cross-linking of the resinates, which exhibited more resistance to deformation under compression. In conclusion, the properties of polysulfonate resin, such as particle shape and degree of cross-linking, and the deformation under compaction of fillers affect the physical properties and the drug release of the resinate tablets.

Compressive Strength↗

PubMed2005

Formulation development and stability testing of oral morphine solution utilizing preformulation approach.

PURPOSE: Prefomulation approach utilizing the fractional-ordered randomized blocked design was employed for the formulation development and stability testing of morphine solution. METHODS: Factors expecting to affect the stability of morphine were evaluated, i.e., vehicle, antioxidant, chelating agent, and pH of the solution. Eight formulations of a possible 16 were prepared according to the block design. The stability of the preparations was tested after 35 days of storage. The data of preformulation study were used for formulation development. RESULTS: The presence of glycerin and ethylenediamine-tetraacetic acid in the formulation, and the pH of the solution adjusted to 4, stabilized morphine. The concentration of morphine decreased drastically in the formulations containing sodium metabisulfite, and those pH adjusted to 6. After 35 days, only 65% of morphine was found in the formulation containing sodium metabisulfite and pH adjusted to 6. The results of preformulation study were used for preparing oral morphine preparations. Samples were kept in amber glass bottles and stored at 4 degrees C and 25 degrees C/75% RH for 13 months. No precipitation of the four formulations was detected. Only a decrease of odor and a small increase of pH value of the preparations (< 0.3 units) were observed. More than 97% of morphine remained in all samples. The samples were free from microbial contamination. CONCLUSION: Stable morphine solution formulations can be achieved with the utilization of the preformulation approach. They were stable more than 13 months when stored at 4 degrees C and 25 degrees C/75% RH.

Administration, Oral↗

PubMed2005

Molecular interaction in alginate beads reinforced with sodium starch glycolate or magnesium aluminum silicate, and their physical characteristics.

Diclofenac calcium-alginate (DCA) beads were reinforced with different amounts of sodium starch glycolate (SSG) or magnesium aluminum silicate (MAS) and were prepared using ionotropic gelation method. Complex formation of sodium alginate (SA) and SSG or MAS in calcium-alginate beads was revealed using FTIR spectroscopy. Differential scanning calorimetric study indicated that diclofenac sodium (DS) in amorphous form was dispersed in the matrix of DCA beads. The thermal behavior of SSG-DCA and MAS-DCA beads was similar to the control bead. Both additives can improve the entrapment efficiency of DCA beads. The swelling and water uptake of the beads depended on the properties of incorporated additives. The SSG-DCA beads showed a higher water uptake and swelling than MAS-DCA beads. Moreover, the swelling of the beads showed a good correlation with the square root of time. The release kinetic of the beads in pH 6.8 phosphate buffer was swelling controlled mechanism, while that in distilled water followed Higuchi's model. The slower release rate and the longer lag time in pH 6.8 phosphate buffer was obtained from the SSG-DCA and MAS-DCA beads because of complex formation between SA and SSG or MAS. However, SSG in the beads could increase the release of DS from the beads in distilled water because it acted as a channeling agent. In contrast, MAS retarded the release of DS from the beads in distilled water due to the stronger matrix formation.

Alginates↗

PubMed2005

Influence of magnesium aluminium silicate on rheological, release and permeation characteristics of diclofenac sodium aqueous gels in-vitro.

The effect of magnesium aluminium silicate (MAS) on rheological, release and permeation characteristics of diclofenac sodium (DS) aqueous gels was investigated. DS aqueous gels were prepared using various gelling agents, such as 15% w/w poloxamer 407 (PM407), 1% w/w hydroxypropylmethylcellulose (HPMC), and 1% w/w high and low viscosity grades of sodium alginate (HV-SA and LV-SA, respectively). Different amounts of MAS (0.5, 1.0 and 1.5% w/w) were incorporated into the DS gels. Incorporation of MAS into the DS gels prepared using SA or PM407 caused a statistical increase in viscosity (P<0.05) and a shift from Newtonian flow to pseudoplastic flow with thixotropic property. The DS release rates of these composite gels were significantly decreased (P<0.05) when compared with the control gels. This was due to an interaction between MAS and PM407 or SA, and adsorption of DS onto MAS particles. Moreover, a longer lag time and no change in DS permeation flux were found when MAS was added to the gels. The findings suggest that the rheological characteristics of gels prepared using PM407 or SA could be improved by incorporating MAS. However, the use of MAS could retard the DS release and extend the lag time of DS permeation.

Alginates↗

PubMed2004

Melted glyceryl palmitostearate (GPS) pellets for protein delivery.

Lysozyme was incorporated into glyceryl palmitostearate (GPS) pellets by compression and melting at loadings of 2, 5 and 10% (w/w). Released lysozyme from both compressed and melted pellets showed good retention of enzymatic activity (>80% active). The percentage lysozyme recovered during in vitro release experiments, over 120 h, was significantly lower from the melted pellets (<15%) compared with compressed pellets (71-85%). Scanning electron microscopy suggested this difference in release was due to differences in porosity of the compressed and melted pellets. Inclusion of hydrophilic components, PEG 4000 and Gelucire 50/13, in the melted matrices increased the percentage of lysozyme released in vitro. Lysozyme released from GPS/PEG 4000 matrices showed good retention of enzymatic activity (>88% active) while that from GPS/Gelucire 50/13 showed reduced activity (68 and 51% active). PEG 4000 was not completely miscible with GPS at the concentrations studied and heterogenous systems resulted. At a loading of 20-35% (w/w) PEG 4000 in GPS greater than 80% of the incorporated lysozyme was released, indicating the likely achievement of interconnecting hydrophilic channels throughout the GPS matrix. In conclusion, melted GPS demonstrated potential as a matrix for the controlled release of proteins and release rates could be modified by inclusion of hydrophilic components.

Diglycerides↗

PubMed2003

Acrylic matrix type nicotine transdermal patches: in vitro evaluations and batch-to-batch uniformity.

Nicotine transdermal patches (NTPs) were fabricated using an acrylic pressure sensitive adhesive emulsion to form a transparent matrix film. An automated thin layer chromatography (TLC) plate scraper was used to control the thickness of the cast nicotine matrix film. The in vitro release behavior and permeation of nicotine across abdominal human epidermis (HE) from the NTPs was studied using United States Pharmacopeia (USP) dissolution apparatus 5 (paddle over disk) and modified Franz-diffusion cell, respectively. The release of nicotine from the NTPs showed a good linear correlation with the square root of time (R2 > 0.99). This indicated a matrix diffusion controlled-release mechanism. The surface morphology of the matrix of the NTP was uniform and nonporous before and after release, indicating that the dried adhesive nicotine matrix was a homogeneous single-phase film. Neither the nicotine content in the range 4.70-8.41% w/w nor the film thicknesses of the NTPs affected the apparent diffusion coefficient of nicotine in the acrylic matrix. A good relationship between the amount of nicotine permeated across the HE and the square root of time was also observed with R2 > 0.98. This study also showed that the NTPs provided a good delivery system with more than 65% of the nicotine delivery being controlled by the device. Moreover, the release of nicotine from six production batches met the criteria of USP 24. This finding presented a good potential of this method for upscaling to industrial manufacturing.

Acrylic Resins↗

PubMed2002

Shed king cobra and cobra skins as model membranes for in-vitro nicotine permeation studies.

Shed king cobra skin (SKCS) and shed cobra skin (SCS) were investigated for use as barrier membranes, including some pre-hydration factors, for in-vitro nicotine permeation. Inter-specimen variations in nicotine fluxes using shed snake skin were compared with those using human epidermis. Nicotine in the form of 1% w/v aqueous buffer solution at pH 5 and transdermal patches (dose 14 mg day(-1)) were used. The nicotine fluxes across the shed snake skin were not significantly affected (P > 0.05) by temperature and duration of hydration pre-treatment. Scanning electron micrographs of SKCS and SCS revealed a remarkable difference in surface morphology, but the nicotine fluxes using both shed skins were not significantly different (P > 0.05). When compared with the results obtained using human epidermis, there were similarities in fluxes and permeation profiles of nicotine. Using nicotine solution, the nicotine permeation profiles of all membranes followed zero order kinetics. The amount of nicotine permeated provided good linearity with the square root of time over 24 h (R(2) > 0.98) when using nicotine patches. The nicotine fluxes using SKCS and SCS had less inter-specimen variation than those using human epidermis. The results suggest a potential use for SKCS or SCS as barrier membranes for in-vitro nicotine permeation studies.

Animals↗