• CELLMED
• /
• 제11권1호
• /
• pp.6.1-6.7
• /
• 2021

In situ gelling devices, as they enter the body, are dosage forms in the shape of the sol but turn into gel types under physiological circumstances. Transition from sol to gel is contingent on one or a mixture of diverse stimuli, such as transition of pH control of temperature, irradiation by UV, by the occurrence of certain ions or molecules. Such characteristic features may be commonly employed in drug delivery systems for the production of bioactive molecules for continuous delivery vehicles. The technique of in situ gelling has been shown to be impactful in enhancing the potency of local or systemic drugs supplied by non-parenteral pathways, increasing their period of residence at the absorption site. Formulation efficacy is further improved with the use of mucoadhesive agents or the use of polymers with both in situ gelling properties and the ability to bind with the mucosa/mucus. The most popular and common approach in recent years has provided by the use of polymers with different in situ gelation mechanisms for synergistic action between polymers in the same formulation. In situ gelling medicine systems in recent decades have received considerable interest. Until administration, it is in a sol-zone and is able to form gels in response to various endogenous factors, for e.g elevated temperature, pH changes and ions. Such systems can be used in various ways for local or systemic supply of drugs and successfully also as vehicles for drug-induced nano- and micro-particles. In this review we will discuss about various aspects about use of these in situ gels as novel drug delivery systems.

• Mass Spectrometry Letters
• /
• 제11권4호
• /
• pp.71-76
• /
• 2020

While montelukast (ML), a cysteinyl-leukotriene type 1 receptor (CysLT1) antagonist is widely used to treat symptoms of rhinitis or asthma, its formulations are mainly limited to solid preparation due to its instability. Recently, there have been attempts to develop various ML dosage forms, and this situation increases the demand of sensitive and creditable methods to determine ML in various samples such as plasma. Thus, here, a simple and efficient method to determine ML in rat plasma using liquid-liquid extraction (LLE) and multiple reaction monitoring was presented. The mixture of DCM:EtOAc (25:75, v/v), the optimized extract solvent for LLE was found to be effective to extract ML without hydrophilic salts and proteins from the sample with limited volume. Also, the use of zafirlukast, instead of expensive ML-d6, as the internal standard makes the present method economical. The developed method was successfully validated in terms of selectivity, matrix effects (-14.8--6.9%), linearity (r230.998 within 0.5-500 ng/mL), sensitivity (the limit of detection and the lower limit of quantitation, ≤0.5 ng/mL), accuracy (88.4-100.6%), precision (3.0-13.3%), and recovery (80.8-86.3%) by following the FDA guidelines. Finally, the applicability of the validated method to pharmacokinetics (PK) studies was confirmed by the successful determination of PK parameters through it following oral administration of Singulair® granule in rats. Therefore, the present method can contribute to the development of new ML formulations through its performance to determine ML in rat plasma efficiently and sensitively.

• CELLMED
• /
• 제11권3호
• /
• pp.15.1-15.9
• /
• 2021

The chemical constitution of a drug has been accepted as an important basis for pharmacological action in Unani medicine. Various dosage forms have been developed on this concept, such as decoctions (Joshanda), infusions (Khesanda), extract (Rub / Usara), and syrup. Zarawand Mudaharaj (ZM.) / Aristolochia rotunda L. root was subjected to extraction process using Soxhlet's apparatus by using Response Surface Methodology (RSM) to design the number of random runs of the extracts with variation in the factors of temperature, the concentration of ethanol in water, time for extraction, for optimizing and maximizing the yield concentration. The data obtained, was analyzed with regression equation and ANOVA two-way summary to interpret the interaction of the factors for yield maximization. Minitab version 18 was used to design and analyze data. Validation of the optimum conditions for maximum yield of the whole extract of ZM. Root was carried out by re-run of the extract using the optimized conditions. The maximum yield percentage thus obtained using RSM was 20.87% whereas using these optimum conditions 21.35 % yield was obtained thereby validating the method. The association between the response functions and the process variables was identified by a three-factor recorded Box-Behnken design. In the present study RSM is used because itis a cheap and affordable method to optimize maximum yield percentage which may be reliably used by researchers. The study set in the surface conditions for ZM. root extraction by the Soxhlet apparatus for maximizing the yield percentage.

• Medical Lasers
• /
• 제10권1호
• /
• pp.22-30
• /
• 2021

Background and Objectives Ocular alkali burns cause severe damage to the ocular tissues and vision loss. Solcoseryl is a standardized calf blood extract that normalizes the metabolic disturbance and aids in maintaining the chemical and hormonal balance and has been used to treat burns in various tissues. This study examined the effects of Solcoseryl on a rat corneal alkali burn model. Materials and Methods Twenty rats were assigned randomly to four equal groups, including alkali burn, hyaluronic acid, Solcoseryl eyedrop, and Solcoseryl gel. A corneal alkali burn was induced by a NaOH-soaked paper disc. The treatments were given twice a day, every day. The wound area was measured after 24 and 48 hours, and the degree of neovascularization and corneal opacity were scored every week. The rats were sacrificed after three weeks for immunohistochemistry (IHC) to compare the level of inflammatory cytokines, IL-1β, IL-6, and TNF-α. The thickness of the retinal layers was compared to observe any changes in the retina. Results The use of Solcoseryl on corneal alkali burn accelerated wound healing with less neovascularization, greater opacity, and less cataract. IHC showed that the inflammation of the cornea was controlled by both the hyaluronic acid and Solcoseryl treatments. On the other hand, the inflammation had spread to the retina. When the dosage forms were compared, eyedrops were more effective on corneal inflammation, while the gel-type had a greater effect on retinal inflammation. Conclusion Solcoseryl was effective in accelerating the wound healing rate on a corneal alkali burn but could not prevent the spread of inflammation from the cornea to the retina. Eyedrops were more effective on inflammation in the cornea, and the gel was more effective in the retina.

• Journal of the Korea Academia-Industrial cooperation Society
• /
• 제17권9호
• /
• pp.228-234
• /
• 2016

The aim of this study was to develop pharmaceutical dosage forms with a bi-phasic drug using a double extrusion approach. Hot melt extrusion was performed using a co-rotating twin-screw extruder. The. 1st melt extrusion was performed using polymer with a relatively higher Tg, such as HPMC and the 2nd melt extrudate was obtained using the 1st extrudate and polymers with a lower Tg, such as HPMC-AS and PEO. In addition, the formulation with all the content in the same proportion as the double extudate was produced using single extrusion for comparison. Physical characterization was performed on the formulations employing differential scanning calorimetry (DSC). In vitro release tests were studied using a USP Type-I apparatus at $37{\pm}0.5^{\circ}C$ and 100 rpm. The similarity factor (f2) was also used to check the difference statistically. The DSC results indicated that the crystallinity of ibuprofen was changed to an amorphous state after extrusion in both double and single melt extrusion. Double melt extrudate with ibuprofen showed the desired release in acidic media (pH 1.2) in the first two hours and basic (pH 6.8) during six hours. Double melt extrudate with glimepiride showed faster release in 60 min of over 80%, whereas the single extrudate with glimepiride showed retarded release due to the interaction with HPMC. The similarity factor(f2) value was 28.5, which demonstrates that there were different drug release behavior between the double and single extrusion. Consequently, the double melt extrudated formulation was robust and gave the desired drug release pattern.

• Polymer(Korea)
• /
• 제32권4호
• /
• pp.328-333
• /
• 2008

The osmotic delivery systems are based on osmosis. The transverse diffusion of water through a porous membrane from a medium with a low osmotic pressure to a medium with a high osmotic pressure. Nifedipine tablet dosage forms of Procardia $XL^{(R)}$(Pfizer) and $Adalat^{(R)}$(Bayer) are commercialized systems of this type that push-pull osmotic tablet operates successfully in delivering water-insoluble drugs. We prepared osmotic pellet system by fluidized bed coating method, and model-drug used nifedipine. The osmotic pellet system was composed of the core material. the swelling and osmotic pressure layer, the drug coating layer, and the porous membrane. This work is performed to investigate the effect of different factors, such as composition and thickness of membrane. The osmotic pellet has been successfully prepared by fluidized bed coating technology. The drug release behavior depended on the increase of CA ratio and thickness in porous membrane. The morphology of the osmotic pellet before and after the dissolution test were observed by SEM. In conclusion, we found that the drug release of osmotic pellet depended on the composition and coating thickness of porous membrane.

• Journal of Pharmaceutical Investigation
• /
• 제25권1호
• /
• pp.9-17
• /
• 1995

To stabilize omeprazole(OMP), ethylenediamine(ED) complex of omeprazole(OMPED) was prepared by reaction between OMP and ED in methanol, and the complex formation was confirmed by the instrumental analysis, i.e., IR, DSC, EA, NMR, MS and XRD. The rates of decomposition of OMP and OMPED in aqueous solution and the shelf lives at standard temperature were measured by accelerated stability analysis. The results are summarized as follows; The mole ratio of OMP and ED in OMPED complex is 1:1, the energy of formation within OMPED might be combined between polar imidazole group of OMP with induced a dipole amine group in the readily polarizable ED molecule. At standard temperature the degradation rate constant of OMP in aqueous solution is $2.540{\times}10^{-2}\;hr^{-1}$ and the shelf life is 4.15 hrs, and in the case of OMPED the degradation rate constant is $7.986{\times}10^{-4}\;hr^{-1}$ and the shelf life is 131.96 hrs. So, the OMPED has about 31 times longer shelf life than OMP. The activation energy of OMP and OMPED are 5.23 and 18.55 kcal $mole^{-1}$ respectively. The stability of OMP is dependent chiefly on pH in the solutions and it decomposes readily in acidic medium by hydrogen ion catalized reaction but becomes stable beyond pH 9.0. In case of the ED-complex, OMPED is stable in neutral as well as in dilute acidic solutions even in pH 6, OMPED is very stable to light(UV), that is, the rate constant and shelf life of OMP are $k=1.0188{\times}10^{-2}\;day^{-1}$, $T_{90%}=4.5 \;days$, on the other hand, the those of OMPED are $k=7.138{\times}10^{-4}\;day^{-1}$, $T_{90%}=64.1\;days$, respectively. From the above results, it is thought that new dosage forms could be developed by using the OMPED as a potential OMP complex.

• Journal of Pharmaceutical Investigation
• /
• 제39권1호
• /
• pp.29-36
• /
• 2009

Since the quality of final products is significantly affected by the homogeneity of powder mixture, the powder blending process has been regarded as one of the critical pharmaceutical unit processes, especially for solid dosage forms. Accordingly, the monitoring to determine a blending process' end-point based on a faster and more accurate in-line/on-line analysis has attracted enormous attentions recently. Among various analytical tools, NIR (near-infrared) spectroscopy has been extensively studied for PAT (process analytical technology) system due to its many advantages. In this study, NIR spectroscopy was employed with an optical fiber probe for the in-line monitoring of fluid-bed blending process. The position of the probe, the ratio of binary powder mixture, the powder size differential and the back-flush period of the shaking bag were examined as principal process parameters. During the blending process of lactose and mannitol powders, NIR spectra were collected, corrected, calibrated and analyzed using MSC and PLS method, respectively. The probe position was optimized. A reasonable end-point was predicted as 1,500 seconds based on 5% RSD value. As a consequence, it was demonstrated that the blending process using a fluid-bed processor has several advantages over other methods, and the application of NIRS with an optical fiber probe as PAT system for a fluid-bed blending process could be high feasible.

• Korean Journal of Clinical Pharmacy
• /
• 제24권1호
• /
• pp.26-32
• /
• 2014

Purpose: The aim of this study was to investigate drug prescription patterns for the treatment of asthma and chronic obstructive pulmonary disease (COPD) patients in Korea. Methods: Ambulatory adult patients who were diagnosed and received treatment for the asthma (ICD-10 code J45) or COPD (ICD-10 code J44) from January 2009 to September 2011 in two independent secondary hospitals in Korea were enrolled in this study. Prescribed drug lists were generated based on the evidence-based guidelines and prescribed drug dosage forms were identified from the patient medical records and computerized drug prescription databases of the study centers. Results: Total numbers of asthma and COPD patient enrolled in this study were 2,432 and 2,615, respectively. Individual prescription-based accumulated numbers of patient were 12,021 for asthma and 16,584 for COPD. The most commonly prescribed three drugs were oral predisolone, oral formoterol and oral montelukast for asthma and oral formoterol, oral doxofylline and inhaled tiotropium for COPD. Frequencies of oral drugs were 83.4% and 63.3% while inhalers were 16.4% and 30.2%, for asthma and COPD, respectively. Conclusion: The oral treatment was prescribed more in asthma and COPD patients than inhalers. To enhance the compliance of evidence-based guidelines for these chronic airway diseases, more realistic and specific strategies to increase the use of inhalers recommended as primary treatment options for asthma and COPD would be required.

• Journal of the Korean Chemical Society
• /
• 제50권4호
• /
• pp.298-306
• /
• 2006

A rapid, simple and sensitive validated spectrophotometric methods have been described for the assay of neomycin and streptomycin either in pure form or in pharmaceutical formulations. The proposed methods were based on the oxidation of the studied drugs by a known excess of potassium permanganate in acidic medium and estimating the unreacted permanganate with amaranth dye (method A), acid orange II (method B), indigocarmine (method C), and methylene blue (method D), in the same acid medium at a suitable lmax=521, 485, 610 and 664 nm, respectively. Beers law is obeyed in the concentration range of 5-10 and 2-7 mg mL-1 for neomycin and streptomycin, respectively. The apparent molar absorptivity and sandell sensitivity values are in the range 5.47-6.20104, 2.35-2.91105 L mol-1 cm-1 and 7.57-8.59, 5.01-6.2 ng cm-2 for neomycin and streptomycin, respectively. Different variables affecting the reaction were studied and optimized. The proposed methods were applied successfully to the determination of the examined drugs either in a pure or pharmaceutical dosage forms with good accuracy and precision. No interferences were observed from excipients and the results obtained were in good agreement with those obtained using the official methods.