Kim, Jun-Young;Seo, Eun-Su;Park, Dae-Soon;Park, Kwang-Min;Kang, Seong-Wook;Lee, Chang-Hyung;Kim, Seong-Hum
Fibers and Polymers
/
제4권3호
/
pp.107-113
/
2003
The branched polypropylene (b-PP) was prepared by melt blending process with initiator, antioxidant, and functional monomers to improve the melt strength through the melt grafting. The melt flow index (MFI) of the b-PP was increased with increasing the initiator content. On the introduction of the alkylamine as the branching agents the MFI of the b-PP was increased, while that of the b-PP with the pentaerythritol triacrylate (PT) was decreased. It may be caused by the chain scission of the i-PP backbone due to the reduced thermal stability of the i-PP on the melt blending. The MFI of the b-PP without the antioxidant was increased due to the chain scission occurred during the melt processing, while on the introduction of the antioxidant, the MFI of the b-PP was decreased. The crystallization temperature of the b-PP was higher than that of PP, which was attributed to the branched chain structure. It was found that the PT was the most effective functional monomers for enhancing the melt properties of the b-PP.
Cardiovascular diseases prevail among modern societies and underdeveloped countries, and a high mortality rate has also been reported by the World Health Organization affecting millions of people worldwide. Hyperactive platelets are the major culprits in thrombotic disorders. A group of drugs is available to deal with such platelet-related disorders; however, sometimes, side effects and complications caused by these drugs outweigh their benefits. Ginseng and its nutraceuticals have been reported to reduce the impact of thrombotic conditions and improve cardiovascular health by antiplatelet mechanisms. This review provides (1) a comprehensive insight into the available pharmacological options from ginseng and ginsenosides (saponin and nonsaponin fractions) for platelet-originated cardiovascular disorders; (2) a discussion on the impact of specific functional groups on the modulation of platelet functions and how structural modifications among ginsenosides affect platelet activation, which may further provide a basis for drug design, optimization, and the development of ginsenoside scaffolds as pharmacological antiplatelet agents; (3) an insight into the synergistic effects of ginsenosides on platelet functions; and (4) a perspective on future research and the development of ginseng and ginsenosides as super nutraceuticals.
Glibenclamide is a second generation sulfonylurea that is orally active as a hypoglycemic drug. It exists as a crystalline powder which is sparingly soluble in water. It was investigated that the potential of glibenclamide to exhibit polymorphism. Three polymorphic modifications (form 1, form 2 and form 3) and three pseudopolymorphic modifications (form 4, form 5 and form 6) were obtained by crystallization from different organic solvents. The isolated crystal forms were characterized by differential scanning calorimetry(DSC), thermogravimetric analysis(TGA) and X-ray crystallography powder diffraction studies. Form 1 was the most stable and melt at $175.4^{\circ}C$. Form 2 was metastable and melt at $151.0^{\circ}C$. Form 3 was a new polymorphic modification because it was different from form 1 and form 2 in X-ray crystallography powder diffraction data. Form 4 was a 1 : 7(toluene : glibenclamide) toluene solvate; form 5 was a 1 : 5(toluene : glibenclamide) toluene solvate; form 6 was a 3 : 8(pentanol : glibenclamide) pentanol solvate. All forms were stable in 3-month storage under 0% or 100% humidity condition. The dissolution rate of form 4 was highest; those of form 2, form 3, form 1, form 5 and form 6 followed.
The patient, 62-years-old woman, had a constant dull pain in the right mandible and an intermittent spontaneous burning sensation of the mouth. The pain began 6 months ago. About 5 years ago, a trauma in her right mandible which was so severe that kept her in the hospital for 2 days. This was followed by mouth opening disturbance with pain for about 2 years. However, she did not have a treatment for the temporomandibular disorder symptoms. After then, she experienced the trigeminal neuralgia characterized by an electrical pain which lasted about 30 minutes in her right face and head when touching the skin or hair. After taking a year course treatment of trigeminal neuralgia, the symptom disappeared. The pain was a constant dull pain and a intermittent burning pain which are contradictory. And the pain responded to various modalities such as physical therapy, anti-inflammatory drug, carbamazepine, and amitriptyline, among which carbamazepine was most effective. The diagnosis was clinically made as an atypical trigeminal neuralgia. The term 'atypical' is used when there is something unknown and the problem is not identified. It is thought that an atypical pain may be approached in the perspective of chronic pain, neuropathic pain, and myofascial pain, the mchanisms of which are poorly understood. As the knowledge of pain physiology improves, there needs to be modification and re-evaluation. Pain disorders must be classified on the basis of an understanding of the underlying mechanism and etiology.
Dementia is a clinical syndrome characterized by a cluster of symptoms and signs that manifest as difficulties in cognitive functions such as memory, psychological and psychiatric changes, and impairments in activities of daily living. As a result of worldwide trends of population aging, dementia has had a huge impact on public health in almost all countries. Disease modification therapies for dementia have not yet been developed. However, pharmacotherapy is essential in patients with dementia to combat delays in their cognitive and functional decline. In this article, we review the current pharmacotherapy for dementia. Three acetylcholinesterase inhibitors-donepezil, rivastigmine, galantamine-and memantine are the only medications that have been approved for the treatment of dementia. We present the indications, dose recommendations, side effects, and criteria for National Health Insurance coverage in Korea of these medications for dementia treatment. Although the Ministry of Food and Drug Safety in Korea has not approved any medications for managing the behavioral and psychological symptoms of dementia, some antipsychotics and antidepressants have been studied and used clinically for those purposes. Clinicians may consider vitamin E, Ginkgo biloba extract, choline alfoscerate, or omega-3 fatty acids as additional treatment options. Non-steroid anti-inflammatory drugs, estrogen hormone therapy, and statins are not generally recommended for dementia treatment. We believe that our findings will aid clinicians in the treatment of patients with cognitive decline.
Panax ginseng Meyer is a traditional Chinese medicine that is widely used as tonic in Asia. The main pharmacologically active components of ginseng are the dammarane-type ginsenosides, which have been shown to have anti-cancer, anti-inflammatory, immunoregulatory, neuroprotective, and metabolic regulatory activities. Moreover, some of ginsenosides (eg, Rh2 and Rg3) have been developed into nutraceuticals. However, the utilization of ginsenosides in clinic is restrictive due to poor permeability in cells and low bioavailability in human body. Obviously, the dammarane skeleton and glycosyls of ginsenosides are responsible for these limitations. Therefore, improving the oral bioavailability of ginsenosides has become a pressing issue. Here, based on the structures of ginsenosides, we summarized the understanding of the factors affecting the oral bioavailability of ginsenosides, introduced the methods to enhance the oral bioavailability and proposed the future perspectives on improving the oral bioavailability of ginsenosides.
The prevalence of obesity in children and adolescents is increasing worldwide. Obesity in children and adolescents not only increases the risk of transitioning to obesity in adulthood but also increases the risk of cardiometabolic diseases such as high blood glucose, high blood pressure, dyslipidemia, fatty liver, and hyperinsulinemia during childhood. The goal of treating obesity in children and adolescents is not to focus on weight loss but to help children reach a healthy weight while maintaining normal growth appropriate for their age and sex. To achieve this goal, regular physical activity and exercise, dietary modification, improvement of obesity-prone environmental factors, and behavioral changes are required for a healthy lifestyle. If appropriate weight control is not achieved through lifestyle modifications, pharmacotherapy may be considered for adolescents with severe obesity aged 12 and above. Recent clinical trials have reported the efficacy and safety of pharmacotherapy in severely obese adolescents. Currently, two medications can be prescribed in Korea for patients with obesity aged 12 and above: Orlistat and Liraglutide. However, despite effective weight control through drug treatment, body weight may increase again after treatment discontinuation. Therefore, it is crucial to evaluate adherence to health behaviors during visits and continue to educate on lifestyle modifications, even during pharmacotherapy, to minimize weight regain.
It has been known that retinoids are intrinsically of critical importance for control of premalignant epithelial cell differentiation. In the absence of retinoids, normal cellular differentiation and growth does not occur in epithelia such as those of trachea and bronchi. Furthermore, it was also reported that retinoid deficiency enhanced susceptibility to chemical carcinogenesis in the respiratory system, in the bladder, and in the colon of the experimental animal. In 1974, Bollag examined the effects of synthetic retinoids in prevention of development of cancer and demonstrated synthetic retinoids to have more favorable therapeutic index than retinoic acid for causing regression of skin papilloma in mice. Therefore, it was assumed that this anticarcinogenic effect of vitamin A derivatives could be due to modification of the metabolism of the carcinogenic polycyclic hydrocarbon, which must first be activated to exert their effect. Hill and Shih reported that vitamin A compounds and analogs had inhibitory effect on drug metabolizing enzyme from liver and lung tissue of mouse and hamster. Lucy suggested that the chemoprevention effect of vitamin A derivatives is due to reaction with molecular oxygen, and it is possible that inhibition of hydroxybenzpyrene formation is a result of this property. On the other hand, butylated hydroxytoluene which is a potent antioxidant strongly inhibited the formation of mammary tumor induced by dimethylbenranthracene. Also, it was observed that this antioxidant inhibited cancer induction in rats by N-2-fluo-renylacetamide. The purpose of this experiment was to investigate the effect of vitamin A derivatives such as retinoic acid and retinoid on drug-metabolizing enzyme and to determine whether riboflavin tetrabutylate or vitamin E could prevent of modify any changes induced by vitamin A delivatives in the rats. The results obtained were as followings. 1) Body weight was significantly reduced by retinoic acid, but not by retinoid. 2) Retinoic acid markedly increased liver weight while retincid showed no effect on liver weight. Treatment of riboflavin tetrabutylate did not affect retinoic acid-induced change in both body weight and liver weight. 3) Both retinoic acid and retinoid remarkably decreased the activity of aminopyrine demethylase. Pretreatment of riboflavin tetrabutylate, however, prevented inhibitory effect of retinoic acid on the enzyme activity. 4) No significant effect of vitamin E on aminopyrine demethylase was observed in both groups treated with retinoic acid and retinoid.
Liposome as a carrier of topotecan (TPT), a promising anticancer drug, has been reported in attempt to improve the stability and antitumor activity of TPT. However, the biodistr ibution pattern of TPT liposome in vivo and PEG-modified liposome containing TPT have not been studied systemically. In this paper, the in vitro stability and in vivo biodistribution behavior of several liposomes containing TPT with different lipid compositions and PEG-modification were studied. Compared with the 'fluid' liposome (S-Lip) composed of soybean phosphatidylcholine (SPC), the 'solid' liposome (H-Lip) composed of hydrogenated soybean phosphatidylcholine HSPC decreased the leaking efficiency of TPT from liposome and enhanced the stability of liposome in fetal bovine serum (FBS) or human blood plasma (HBP). The results of biodistribution studies in S$_{180}$ tumor-bearing mice showed that liposomal encapsulation increased the concentrations of total TPT and the ratio of lactone form in plasma. Compared with free TPT, S-Lip and H-Lip resulted in 5- and 19- fold increase in the area under the curve (AUC$_{0\rightarrow\propto}$), respectively. PEG- modified H-Lip (H-PEG) showed 3.7-fold increase in AUC$_{0\rightarrow\propto}$ compared with H-Lip, but there was no significant increase in t$_{1/2}$ and AUC$_{0\rightarrow\propto}$ for PEG-modified S-Lip (S-PEG) compared with S-Lip. Moreover, the liposomal encapsulation changed the biodistribution behavior, and H-Lip and H-PEG dramatically increased the accumulation of TPT in tumor, and the relative tumor uptake ratios were 3.4 and 4.3 compared with free drug, respectively. There was also a marked increase in the distribution of TPT in lung when the drug was encapsulated into H-Lip and H-PEG. Moreover, H-PEG decreased the accumulation of TPT in bore marrow compared with unmodified H-Lip. All these results indicated that the membrane fluidity of liposome has an important effect on in vitro stability and in vivo biodistribution pattern of liposomes containing TPT, and PEG-modified 'solid' liposome may be an efficient carrier of TPT.
Enterobiasis is common helminthic infections found in man. But control of this disease is still troublesome because of its difficulty in the d diagnosis and prevention of infection. Considering the difficulty of accurate diagnosis of pinworm infection, which is very common and somewhat pathogenic, reevaluation of cellotape anal swab method for the diagnosis of enterobiasis was performed. A total of 147 children ranging the ages of 1-12 years in 3 orphanages in the suburbs of Seoul, Korea was subjected for this study. Repeated cellotape anal swabs were carried out against 70 children, 7 times for 3 days interval, in the morning 6am. Finally 10 mg/kg body weight pyrantel pamoates were given to all children including egg negative cases and whole stools of 3 following successive days were collected for the confirmation of residual worm ourden at the time of treatment. Cellotape anal swabs were also performed to another 77 children at 6am, 3pm, 9pm, twice for 3 days interval. The resultant findings were summarized as follows; 1) While the each time average detection rate of Enterobius egg was 28.8% in this study group, the accumulative detection rate up to 7th examination was 62.8%. The accumulative detection rate rose continuously up to 6th examination. 2) After administration of pyrantel pamoate 10 mg/kg body weight, final infection rate was increased to 72.9% by adding worm positive cases who didn't show any evidence of infection in the cellotape anal swabs. 3) Although pinworms were detected in 35 among 70 children treated, 7 cases (20%) of them were egg negative cases in 7 consecutive cellotape anal swabs. 4) Pinworms were expelleded in 14 (87.5%) among 16 children whose swab result was positive in the last examination which was done concurrently with drug administration. 5) Estimated infection rate calculated by best asymptotically normal estimate of Neuman from Moriya's modification revealed 71.5% similar to 72.9% of present results. 6) The result of anal swab performed at 6am was higher than that of 3pm or 8pm. In conclusion, cellotape anal swab method for Enterobius vermicularis infection was considered as method having relatively high positive accuracy. However to gain the reliable infection rate, at least 6 examination is required in the group with 25-30% infection rate by single swab. Moriya's modification of Neuman could be used efficiently in the mass control of this diease for the estimation of true infection rate of E. vermicularis in the sampled population.
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