• Journal of Pharmaceutical Investigation
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• 제20권2호
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• pp.65-71
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• 1990

Some studies reported physicochemical factors of drugs affecting solubility and dissolution rate. However, few have been reported about pharmaceutical application of crystal forms (habits). Therefore, using acetylsalicylic acid and phenacetin as model substances, we monitored the effects of crystal forms on the dissolution rates.

• Journal of Pharmaceutical Investigation
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• 제5권4호
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• pp.7-16
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• 1975

The drug release property from the coated tablets which contain 291mg of acetylsalicylic acid were estimated from comparison of the blood level and the urinary excretions after oral ingestion of coated tablets and noncoated tablet in human. The coating materials are 2-methyl-5-vinylpyridine-methylacrylic acid copolymer(MPM), dimethyl aminoethyl methacrylate methyl methacrylate copolymer(EE), polyvinyl acetal diethyl aminoacetate(AEA), and shellac. Each of 7 subjects ingested 873mg of acetylsaliylic acid. All tablets are coated approximately $3.5{\pm}0.5%(w/w)$ per tablet with each of the coating materials and met K.P.II. standard for potency and disintegration time. The availability was decreased in the following order:MPM coated tablets>EE coated tablets>AEA coated tablets>> shellac coated tablets.

• The Korean Journal of Pain
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• 제37권2호
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• pp.141-150
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• 2024

Background: Stingless bee propolis is a popular traditional folk medicine and has been employed since ancient times. This study aimed to evaluate the antinociceptive activities of the chemical constituents of aqueous propolis extract (APE) collected by Trigona thoracica in a nociceptive model in mice. Methods: The identification of chemical constituents of APE was performed using high-performance liquid chromatography (HPLC). Ninety-six male Swiss mice were administered APE (400 mg/kg, 1,000 mg/kg, and 2,000 mg/kg) before developing nociceptive pain models. Then, the antinociceptive properties of each APE dose were evaluated in acetic acid-induced abdominal constriction, hot plate test, and formalin-induced paw licking test. Administration of normal saline, acetylsalicylic acid (ASA, 100 mg/kg, orally), and morphine (5 mg/kg, intraperitoneally) were used for the experiments. Results: HPLC revealed that the APE from Trigona thoracica contained p-coumaric acid (R² = 0.999) and caffeic acid (R² = 0.998). Although all APE dosages showed inhibition of acetic acid-induced abdominal constriction, only 2,000 mg/kg was comparable to the result of ASA (68.7% vs. 73.3%, respectively). In the hot plate test, only 2,000 mg/kg of APE increased the latency time significantly compared to the control. In the formalin test, the durations of paw licking were significantly reduced at early and late phases in all APE groups with a decrease from 45.1% to 53.3%. Conclusions: APE from Trigona thoracica, containing p-coumaric acid and caffeic acid, exhibited antinociceptive effects, which supports its potential use in targeting the prevention or reversal of central and peripheral sensitization that may produce clinical pain conditions.

• Archives of Pharmacal Research
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• 제10권1호
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• pp.29-35
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• 1987

The effect of drug addition on the bovine serum albumin (BSA)-edible dye complex was studied by spectrophotometric method. The edible dyes tested were amranth, erythrosine, tatrazine and sunset yellow. The moles of bound dye per protein mole and free energies for edible dyes bounded were determined at pH 7.4. The values of free energy change by the addition of drughs to BSA-edible dye were ranged fro -6, 260 to 08030 cal/mole. In the wide range of edible dye concentration (0.3-$7{\times}10^{-5}$$^{-5}$ M), acetylsalicylic acid (ASA) showed pattern of displacement different from that of dye. It was assumed that ASA has different binding mechanisms from edible dye.

• Journal of Pharmaceutical Investigation
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• 제2권2호
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• pp.5-17
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• 1972

It was reported that cyclodextrin has a distinctive ability to form inclusion compound with a wide variety of compounds. The authors studied the stability of acetylsalicylic acid in cyclodextrin solution. From the results of this experiment, the decomposition of Aspirin in cyclodextrin solution was progressed according to the pseudofirt order reaction and its degradation rate constant was decreased and the thermodynamic activation energy of the degradation of aspirin was accetrated with the increase of cyclodextrin Conclusively, it was considered that cyclodextrin increased the stability of aspirin in aqueous solution by its inclusion compound formation.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.123-123
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• 1993

Acetylsalicylic acid (aspirin)와 인삼의 항산화 성분인 maltol의 축합반응으로 합성된 신물질 Aspalatene이 저용량: 장기 복용시 항산화활성과 더불어 지혈시간 연장효과가 탁월함을 보고 한 바 있다. Aspalatone은 aspirin과는 달리, 장기 복용시에도 위궤양 유발 작용이 거의 나타나지 않으므로 말초순환개선제로서의 개발이 기대된다. 본 연구에서는 Aspalatone의 항혈전작용을 in vivo, ex vivo 및 in vitro에서 연구하였다. Mouse thromboembolism test를 이용한 in vivo실험에서 Aspalatone은 aspirin과 유사하게 collagen에 의한 치사를 유의적으로 감소시켰으며 ADP에 의한 치사에는 영향을 미치지 않았다. 또한 10일간의 장기 투여 실험에서는 저용량에서 영향을 미치지 않았다. 또한 10일간의 장기 투여 실험에서는 저용량에서 항혈전 작용을 나타내며 투여 중단 4일 후에도 약효가 유지되는 것을 밝혔다. 이는 Aspalatone이 aspirin과 같이 cycloosygenase에 작용하여 항혈전 작용을 나타냄을 강력히 시사하고 있다.

• Biomolecules & Therapeutics
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• 제8권4호
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• pp.332-337
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• 2000

Physicochemical properties of aspalatone (acetylsalicylic acid maltol ester, AM), which has been recently found to have an antithrombotic effect, were studied in terms of solubility, dissolution, partition coefficient (Pc) and stability. The solubility of AM at 37$^{\circ}C$ was about 1.2 mg/ml and the P$_{c}$ value for n-octanol/water and chloroform/water was 11.4 and 382.6, respectively. Dissolution rates of AM at pH 1.2 and 6.8 were more than 80% within 30 min. The degradation of AM followed apparent first-order kinetics, and was dependent on temperature, pH and ionic strength. From the pH-rate profile, the optimal pH was found to be at around 4.0. Half-lives at pH 1.2 and 6.8 were 33.5 and 44.4 hr, respectively. The degradation rate of AM at pH 1.2 was somewhat faster than that of aspirin, but at pH 7.0, the degradation rate of AM was slower than that of aspirin.n.

• Journal of Korean Neurosurgical Society
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• 제46권3호
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• pp.277-280
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• 2009

Posterior cranial fossa subdural hematomas and extension of the subdural hematoma to the cerebellopontine angle is rarely seen and the concurrent development of acute peripheral facial palsy and the management strategy have not previously been reported in this pathology because of its rarity. We present this case to emphasize that minor head trauma may lead to a posterior cranial fossa hematoma extending to the cerebellopontine angle and cause peripheral facial palsy in patients using aspirin (acetylsalicylic acid). In addition, partial evacuation and waiting for the resorption of the hematoma may help to prevent damage to the 7th and 8th cranial nerves.

• Journal of Pharmaceutical Investigation
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• 제30권4호
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• pp.267-271
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• 2000

The effect of cyclodextrins on the solubility and stability of aspalatone (acetylsalicylic acid maltol ester, AM, CAS 147249-33-0), which has been recently found to have an antithrombotic effect, was investigated. The addition of ${\beta}-cyclodextrin\;({\beta}-CD),\;dimethyl-{\beta}-cyclodextrin\;(DMCD)\;or\;2-hydroxypropyl-{\beta}-cyclodextrin\;(HPCD)$ to the aqueous solution increased the solubility of AM concentration-dependently. From the phase solubility diagram, stability constants for $AM-{\beta}-CD$, -DMCD or -HPCD complexes were calculated to be 43.1, 78.3 and $53.0\;M^{-1}$. The addition of ${\beta}-CD$, DMCD or HPCD to AM solution retarded the degradation rate of AM in the acidic region. However, ${\beta}-CD$ and HPCD rather acted as an accelerator of degradation in the neutral and alkaline regions. DMCD had a stabilizing effect at all pHs studied.

• 생약학회지
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• 제5권3호
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• pp.179-184
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• 1974

Experiments were carried out to evaluate the anti-inflammatory activity of Caragana chamlagu $L_{AMARCK}$ roots, which was known to be effective as antineuralgic, antirheumatic and antiarthritic, etc. in the folk cures of this country. The ether extract of the root has shown significant effects against the rat paw edema induced by 1% carrageenin and its potency was comparable with acetylsalicylic acid, a anti-inflammatory drug, when given orally in 5% acacia gum suspension. The ethanol and hexane extracts, on the other hand, stimulated the formation of rat paw edema under the same experimentation.