• 약학회지
• /
• 제14권1_2호
• /
• pp.28-35
• /
• 1970

The absorption of Aminopyrine from the small intestine of a rat in combination with antihistamic agent, Diphenhydramine, Pheniramine, Tripelennamine and Diphenhydramine respectively, was examined. Through the rat small intestine canal, a definite quantity of a sample solution comprising 0.5 mM of Aminopyrine and 0.1 mM of each antihistamic agent in phosphate buffer solution (pH=7.4) was perfused through the rat small intestine at rate 5 ml per minute. The samples of the circulating solution were taken out after 5 minutes of the perfusion to give initial concentration and every 30 minutes for 3 hours. The amount of residual Aminopyrine in the solution was determined photometrically at 720 m.mu. by using 0.4% potassium ferricyanate solution and 1% ferric nitrate in 0.1N nitric solution. The mixed compounds of Aminopyrine with antihistamic agent, such as Aminopyrine with Diphehydramine, Aminopyrine with Pheniramine, Aminopyrine with Tripelennamine and Aminopyrine with Chloropheniramine showed more increased absorption than Aminopyrine alone. the absorption rate constants and apparent permeability coefficients of the mixed compounds were shown in detail.

• Journal of Pharmaceutical Investigation
• /
• 제10권1호
• /
• pp.4-12
• /
• 1980

The studies of the compounding analgestic antipyretics were examined by the converted Koster's method (mice) and the converted Mac Donald's method (mice) induced on the three assumption crossover test. And the following results were found. 1. The same effect of the writhing inhibition in this compounding antipyretic dosage by it's oral administration is as follows. Aminopyrine 100mg/kg. (standard), aminopyrine 50mg/kg compounding with chlorpheniramine maleate 2mg/kg., compounding with diphenhydramine hydrochloride 8mg/kg., compounding with atropine sulfate 0.2mg/kg., or compounding with scopolamine hydrobromide 0.2mg/kg. And aspirin80mg/kg., Salicylamide 90mg/kg., sulpyrine 60mg/kg., or phenacetin 70mg/kg. compounding with the same dosage of the adjutants above. 2. The elevation-rate of the reaction threshold in this compounding antipyretic dosage by it's oral administration calculate as follows. When the elevation-rate (ER) of aminopyrine (100mg./kg.) is 1.00 (Standard), ER of aminopyrine (50mg./kg.) compounding with chlorpheniramine maleate (2mg./kg.) calculated 1.42, aspirin (80.mg./kg.) compounding with diphenhydramine hydrochloride (80mg./kg.) calculated 1.18, salicylamide (90mg./kg.) compounding with chlorpheniramine maleate (2mg./kg.) calculated 1.15, sulpyrine (60mg./kg.) compounding with chlorpheniramine maleate(2mg./kg.) calculated 1.28, and ER phenacetin (70mg./kg.) compounding with chlorpheniramine maleate (2mg./kg.) calculated 1.19.

• 약학회지
• /
• 제24권2호
• /
• pp.111-116
• /
• 1980

희첨 Siegesbeckiae Herba 의 축추물(수성및 알콜성)을 가토의 정맥내에 투여할때 일과성이 긴 하나 현저한 혈압강하작용이 나타나며 이들의 혈압강하작용은 atropoine이나 diphenhydramine에 의하여 유의성인 억제가 이루어짐을 저자들은 발표한바 있다. 그러나 벨라도나 알칼로이드가 개및 고양이에서는 심전 증가를 일으키거나 가토에서는 그렇지를 못하는것처럼 동물의 종에 따라 약물의 반응이 상이한 경우가 있다. 따라서 이 희첨의 실용성 여부를 정확히 파악하기 위한 실험의 한 방법으로서 실험 동물의 종차에 따른 혈압강하작용및 그 기전에 있어서 차이점의 유무를 확인하고저 비교적 작용강도가 큰 비의 에탄올 엑기스로 개및 닭을 이용하여 이번 실험을 시행하였다.

• 생약학회지
• /
• 제7권3호
• /
• pp.215-220
• /
• 1976

1. Nepetae Herba water extract (NHW) produced a fall of blood pressure in the rabbit. 2. The depressor effect of NHW was inhibited by atropine, but was not affected by propranolol, hexamethonium and diphenhydramine. 3. NHW showed pressor response in the rabbit treated with atropine. 4. The pressor response in the atropine treated rabbit was inhibited by phentolamine and guanethidine.

• 약학회지
• /
• 제37권2호
• /
• pp.119-123
• /
• 1993

A spectrophotomertic method is proposed for the determination of antihistamines. The method is based on solvent extraction of the ion pair formed between antihistamines and colored picric acid into chloroform. The binding state of antihistamines-picric acid complexes were presumed by IR and $^{1}$H-NMR spectra as intermolecular hydrogen bonding. This method was applicable to the determination of antihistamines in the pharamaceutical preparations.

• 대한약리학회지
• /
• 제22권1호
• /
• pp.34-44
• /
• 1986

본 실험실에서는 한국 특산인 매자나무 (Berberis koreana Palibin)의 뿌리에서 majarine(isoquinoline alkaloid)을 분리하여 여러 가지의 약리작용을 검토한 바 있다. 현재는 majarine의 화학적 구조를 변화시켜 그 유도체의 약리작용을 검색하고 있으며, 그 중 majarine의 isoquinoline ring에 치환되어 있는 두 methoxy group 중 하나를 hydroxy기로 치환된 majarol을 합성하였다. Majarol을 흰쥐 정맥내로 투여하여 혈압 및 심박동수의 변화와 epinephrine, phentolamine, isoproterenol, propranolol, atropine, diphenhydramine과 hexamethonium 등에 대한 약물 상호작용을 관찰하였으며 또 적출 개구리 심장에 대한 작용을 관찰하여 다음과 같은 성적을 얻었다. Majarine을 저용량(0.5-2 mg/kg)에서 용량의존적으로 현저하고 일시적인 혈압 강하와 약간의 심박동수 감소를 나타냈으며, 고용량(>5mg/kg)에서는 이차적으로 지속적인 혈압강하와 심박동수 감소를 나타냈다. 일시적인 혈압강하작용은 atropine sulfate, diphenhydramine과 hexamethonium에 의해 억제되지 않았고, epinephrine의 혈압 상승작용은 majarol의 전처치로 현저하게 차단되었으며, majarol 투여시 나타나는 지속적인 혈압 강하는 심박동수 감소에 수반되어 나타났고 이는 propranolol에 의해 억제되지 않았으며, isoproterenol의 positive chronotropic effect는 majarol 전처치로 차단되지 않았다. majarol은 저용량에서 적출개구리 심장의 수축기 장력을 증가시켰으며 고용량에서는 개구리 적출심장에 대해 억제적으로 작용하였다. 이러한 결과로 보아 majarol의 일시적이고 현저한 혈압강하작용은 ${\alpha}$-adrenoceptor 차단작용에 의한 것으로 사료되고, 이차적으로 나타나는 지속적인 혈압강하작용은 심박동수의 감소와 동시에 나타나는 것으로 보아 심장에 대한 작용인 것으로 추정되며, majarol의 심장에 대한 작용을 ${\beta}$-adrenoceptor에 대한 작용보다는 심근에 대한 직접적인 작용인 것으로 추정된다.

• 약학회지
• /
• 제17권2호
• /
• pp.103-110
• /
• 1973

In this study the effect of alcohol extract of atractlis (AAE) on the blood pressure of the rabbit was investigated. The results of the experiment are as follows. AAE elicited hypotension with doses ranging from 3 to 30 mg/kg, i.v., exhibiting a linear dose-relationship. This effect of AAE was abolished by atropine and potentiated by physostigmine, while not affected by diphenhydramine, hexamethonium, propranolol and cyproheptadine. AAE did not influence the pressor responses to norepinephrine and the depressor to isoproterenol. The above results indicate that AAE produced the hypotension by stimulating the parasympathetic nervous system related to acetylcholine.

• Journal of Pharmaceutical Investigation
• /
• 제1권1호
• /
• pp.30-33
• /
• 1971

Comparative studies were made on the analgesic effect of salicylamide, used individually and combined with parasympatholytics (propantheline and atropine) and antihistaminics (tripelennamine, diphenhydramine) as regards the analgesic effect (in thermal contact method) were examined by its oral administration with each combined drug to mouse (three assumption cross-over test), and the following effects were found. 1. The increasing order of the parasympatholytics to the analgesic effect of salicylamide is as follows: propantheline>atropine. 2. The increasing order of the antihistaminics to the analgesic effect of salicylamide is as follows: chlorpheniramine>diphenhdramine>tri pelennamine. In the ratio '1 : 1' salicylamide to parasympatholytics and antihistaminics, the analgesic effect of salicylamide was more increase than the other ratio in this study.

• 약학회지
• /
• 제21권1호
• /
• pp.17-25
• /
• 1977

Intravenous injection of Mori Radicis Cortex Water Extract (MWE) regularly caused the does-related, lowering of blood pressure in the rabbits anesthetized with urethane, and then did not show the cumulative effect and the tachyphylaxis. The hypotensive effects of MWE were inhibited by atropine, chlorisodamine, phentolamine and bethanidine, while not altered by diphenhydramine, propranolol and cyproheptadine. Atropine after chlorisondamine did not alter the effect of MWE. MWE potentiated the pressor effect of nore-pinephrine, but did not carotid occlusion was inhibited by previous administration of MWE. It is conclude that MWE elicits hypotensive action in the rabbit by the centrally induced cholinergic effect and the inhibitation of responses to sypathetic adrenergic nerve activation.

• 생약학회지
• /
• 제7권2호
• /
• pp.99-109
• /
• 1976

Scolopendra corpus has been used as anticonvulsants and antispasmodics in the oriental medicine. It was previously shown that water extract of Scolopendra corpus had an inhibitory action on ileum in mouse. To investigate the anticonvulsant and antispasmodic activity of Scolopendra corpus, pharmacological studies have been carried out with the water extract of Scolopendra subspinipes mutilans $L.\;K_{OCH}$, which is widely distributed in Korea. 1. The extract depressed convulsions induced by picrotoxin and strychnine. 2. Sedative and antipyretic analgesic action were observed. 3. In mouse and rabbit, tone of intestinal smooth muscle was suppressed with the treatment of the extract and intestinal contraction induced by $BaCl_2$ was also inhibited, suggesting that the extract has a papaverine-like effect. Whereas, in guinea pig, intestinal and tracheal smooth muscle were stimulated, and the effect was antagonized by pre-and after-treatment of diphenhydramine, suggesting that the extract has a histamine-like effect. 4.Flow rate was increased when hind-limb of Toad was perfused with saline containing the extract, but returned to normal within 10 min. Hypotensive effect was observed in rabbit and the effect was abolished by vagotomy.