• 제목/요약/키워드: Propranolol.HCl

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Propranolol.HCl의 Cellulose Acetate Phthalate Microencapsulation에 관한 연구 (Microencapsulation of Propranolol.HCl with Cellulose Acetate Phthalate)

  • 구영순;김재연
    • 약학회지
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    • 제33권5호
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    • pp.312-318
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    • 1989
  • Microcapsule of Propranolol HCl with Cellulose Acetate Phthalate (CAP) by coacervation-phase separation method was studied. Encapsulation was carried out in the CAP-liquid paraffin-acetone ethanol solvent system. The optimum weight ratio for microencapsulation in the CAP-liquid paraffin-solvent system was 1.32:89.18:9.50 or 1.65:89.42:8.93. The wall thickness of microcapsules increased according to increasing of CAP concentration, but dissolution rate decreased. The dissolution of propranolol-HCl in simulated gastric and intestinal fluid test solution was completed within 3 min., but T50% of propranolol HCl from 10.0% CAP-microcapsules were 390 min. and 210 min. respectively. The released amount from 12.5% CAP-microcapsules was 41.8% within 720 min. in simulatd gastric fluid test solution and T50% of those in simulated intestinal fluid test solution was 250 min.

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알루미늄 부식에 대한 베타-차단제 억제제 효과 (Effect of β-Blocker Inhibitors on Aluminum Corrosion)

  • Fouda, A. S.;El-Ewady, G. Y.;Shalabi, K.
    • 대한화학회지
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    • 제55권2호
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    • pp.268-278
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    • 2011
  • 베타 차단제 억제제(atenolol, propranolol, timolol and nadolol)의 존재와 부존 하에서 0.1M HCl 용액에 담긴 알루미늄의 부식작용을 연구하였다. 이 연구에 무게감량, 변전위 편극, 전기화학 임피던스 분석법이 사용되었다. 억제 효과는 억제제의 농도 증가에 따라 증가하였으며, 온도가 증가함에 따라 감소하였다. 모든 억제제들은 Frumkin 등온을 따르는 알루미늄 표면에 흡착되었다. 부식반응은 전하이동과정에 의해 조절됨을 발견하였다. 억제 효과 측정을 위해 사용된 실험방법 들에 대해 조사한 결과 모두 억제효과가 우수하였다.

Witepsol 중공좌제로부터의 염산프로프라놀롤 및 인도메타신의 방출제어 (Controlled Release of Propranolol Hydrochloride and Indomethacin from Hollow Type Suppository Using Witepsol H-15)

  • 진숙영;구영순
    • 약학회지
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    • 제40권4호
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    • pp.400-410
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    • 1996
  • In oder to develop the controlled release of drugs from the suppositories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppo sitory forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The oleaginous Witepsol H-15 (WH-15) as a base, and indomethacin (IDM) of a very slightly soluble drug and propranolol-HCL (PPH) of a very soluble drug were employed as model drugs. The in vitro drug release showed that the cumulative release amount of PPH from PPH-(methylcellulose) MC-SDS and PPH-(ethylcellulose) EC-SDS hollow type suppositories reached 40% and 12% in 6 hrs,respectively. On the other hand, the drug release for a conventional suppository was 80% in 6 hrs. For the IDM suppositories,the cumulative drug release from IDM-(polyvinylpyrrolidone) PVP-SDS hollow type suppositories reached 99% in 24 hrs, whereas that from a conventional suppository reached 85%. An in vivo experiment with rabbits showed that IDM-PVP-SDS hollow type suppository delayed the absorption of IDM, significantly. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of IDM-PVP-SDS suppository were 60 min, 12.12${\mu}g$/ml and 2657${\mu}g$/ml/min, respectively. The $t_{max},\;C_{max}\;and\;AUC_{0{\to}8}$ of controlled group were 20 min, 15.49${\mu}g$/ml and 2190${\mu}g$/ml/min, respectively.

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염산 프로프라놀롤-고체 분산계-폴리비닐알코올 하이드로겔 중공좌제로부터의 약물방출 (Controlled Release of Propranolol Hydrochloride(PPH) from PPH-Solid Dispersion System-Polyvinyl Alcohol Hydrogel Hollow Type Suppository)

  • 정진훈;이정연;구영순
    • Journal of Pharmaceutical Investigation
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    • 제26권4호
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    • pp.299-308
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    • 1996
  • In order to develop the controlled release of a drug from the suppsitories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppository forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The polyvinyl alcohol(PVA) hydrogel as a base, and propranolol HCl(PPH) as a model drug were employed. In vitro drug dissolution studies showed that the dissolved amounts(%) of PPH from PPH-methylcellulose(MC)-SDS and PPH-ethylcellulose(EC)-SDS reached 100% and 63% in 4.5-hours, respectively. In the relative strength test for PVA hydrogel, PVA hydrogel became harder and more rigid when the number of freezing-thawing cycles and the ratio of PVA 2000 were increased. In vitro drug release profile revealed that the release rate(%) of PPH from PPH-EC-SDS and PPH-MC-SDS hollow type suppositories were sustained. The release amount(%) of PPH from PPH-EC-SDS hollow type suppositories was not affected by storage time, but since the use of hydrophilic MC made PPH diffuse into the hydrogel after it absorbed the water of base, the various release patterns were appeared as the storage time went by. In vivo absorption experiments with rabbits showed that PPH-EC-SDS(PPH : EC=1:3) hollow type suppository delayed the absorption of PPH, significantly. The $C_{max}$, $AUC_{0{\rightarrow}8}$ and MRT of PPH powder hollow type suppository were $196.37{\pm}5.63\;ng/ml$, 1105.26 ng/ml/min and 8.66 min, respectively. The $C_{max}$, $AUC_{0{\rightarrow}8}$ and MRT of PPH-EC-SDS(PPH : EC=1:3) were $91.30{\pm]14.14\;ng/ml$, 554.69 ng/ml/min, 235.99 min, respectively.

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서방정으로부터의 약물 용출에 대한 고분자-약물 상호작용의 영향 (Effects of Polymer-Drug Interactions on Drug Release from Sustained Release Tablets)

  • 김행자;이승진
    • Journal of Pharmaceutical Investigation
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    • 제26권2호
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    • pp.119-124
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    • 1996
  • To develop oral controlled release dosage forms, ionic interactions between polymers and drugs were evaluated. Hydroxypropylmethyl cellulose and carboxymethylene were used as model nonionic and ionic polymers, respectively. 5-fluorouracil, propranolol-HCl and sodium salicylate were selected as model nonionic, cationic and anionic, respectively. Polymer-drug mixtures were compressed into tablets and drug release kinetics from these tablets were determined. Drug release from the tablets made of the nonionic polymer was not affected by the charge of drugs, rather, was regulated by the solubility of drugs in different pH releasing media. However, drug release kinetics were significantly affected when drug-polymer ionic interactions exist. Enhanced drug release was observed from anionic drug-anionic polymer tablets due to ionic repulsion, whereas drug release was retarded in cationic drug-anionic polymer tablets owing to ionic attractive force. Therefore, the results suggested that the polymer-drug interactions are important factors in designing controlled release dosage forms.

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폴리비닐알코올 하이드로겔 좌제로부터 프로프라놀롤의 in vitro 방출과 in vivo 생체이용률간의 상관성 (Correlation between in vitro release and in vivo bioavailability of Propranolol.HCI from Poly(vinyl alcohol) Hydrogel Suppositories)

  • 김호정;구영순
    • Journal of Pharmaceutical Investigation
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    • 제28권4호
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    • pp.275-282
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    • 1998
  • In order to develop a desirable in vitro release which correlates well with in vivo bioavailability, hollow type suppository containing Propranolol HCl(PPH) powder in the cavity and conventional type suppository with dispersed PPH in the base were prepared. Polyvinyl alcohol (PVA) hydrogel as a base and PPH as a model drug were used for the preparation of suppository. The rates of drug release from the suppositories were studied by Paddle method, Muranish method, Dialysis tubing method and Rotating dialysis cell method. The release profiles from suppositories using the four different release tests were compared. After a rectal administration in rat, the mean $C_{max}$ of hollow type suppository was significantly lower than that of conventional type, but $T_{max}$, $AUC_{0{\to}12}$ and MRT of hollow type were significantly higher 1.6 times, 1.2 times and 1.9 times than those of conventional type, respectively. The computer program was used to simulate plasma concentration from in vitro released amounts of drug and in vivo pharmacokinetic parameters. Based on comparison of the simulated bioavailability from computer program with experimental bioavailability in rat we have found out in vitro release test which correlates well with in vivo bioavailability. Our results have shown the best correlation between in vitro release and in vivo bioavailability in PPH-PVA hydrogel hollow type suppository for the paddle method and conventional type suppository for the rotating dialysis cell method. In this work we propose that PPH-PVA hydrogel suppository shows in vitro-in vivo correlation. This data should help to optimize the formulation of the drug and provide a basis for quality control procedures.

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Histamine Release by Hydrochloric Acid is Mediated via Reactive Oxygen Species Generation and Phospholipase D in RBL-2H3 Mast Cells

  • Kim, Chang-Jong;Lee, Seung-Jun;Seo, Moo-Hyun;Cho, Nam-Young;Sohn, Uy-Dong;Lee, Moo-Yeol;Shin, Yong-Kyoo;Sim, Sang-Soo
    • Archives of Pharmacal Research
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    • 제25권5호
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    • pp.675-680
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    • 2002
  • In order to investigate the underlying mechanism of HCI in oesophagitis, the inflammatory response to HCI was observed in RBL-2H3 mast cells. Rat basophilic leukemia (RBL-2H3) cells were used to measure histamine release, arachidonic acid (AA) release, reactive oxygen species (ROS) and peroxynitrite generation induced by HCI. Exogenous HCl increased the level of histamine release and ROS generation in a dose dependent manner, whereas it decreased the spontaneous release of [$^3$H] M and the spontaneous production of peroxynitrite. Mepacrine (10 $\mu$M), oleyloxyethyl phosphorylcholine (10 $\mu$M) and bromoenol lactone (10 $\mu$M) did not affect both the level of histamine release and ROS generation induced by HCI. U73122 (1 $\mu$M), a specific phospholipase C (PLC) inhibitor did not have any influence on level of histamine release and ROS generation. Propranolol (200 $\mu$M), a phospholipase D (PLD) inhibitor, and neomycin (1 mM), a nonspecific PLC and PLD inhibitor, significantly inhibited both histamine release and ROS generation. Diphenyleneiodonium (10 $\mu$M), a NADPH oxidase inhibitor, and tiron (5 mM), an intracellular ROS scavenger significantly inhibited the HCI-induced histamine release and ROS generation. These findings suggest that the inflammatory responses to HCI is related to histamine release and ROS generation, and that the ROS generation by HCI may be involved in histamine release via the PLD pathway in RBL-2H3 cells.

Pharmacological Characterization of Synthetic Tetrahydroisoquinoline Alkaloids, YS 51 and YS 55, on the Cardiovascular System

  • Chang, Ki-Churl;Kang, Young-Jin;Lee, Young-Soo;Chong, Won-Seog;Choi-Yun, Hey-Sook;Lee, Duck-Hyong;Ryu, Jae-Chun
    • The Korean Journal of Physiology and Pharmacology
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    • 제2권4호
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    • pp.461-469
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    • 1998
  • Tetrahydroisoquinoline (THI) alkaloids can be considered as cyclized derivatives of simple phenylethy-lamines, and many of them, especially with 6,7-disubstitution, demonstrate relatively high affinity for catecholamines. Two -OH groups at 6 and 7 positions are supposed to be essential to exert ?${\beta}-receptor$ activities. However, it is not clear whether -OH at 6,7 substitution of THIs also shows ?${\alpha}-adrenoceptor$ activities. In the present study, we investigated whether -OH or $-OCH_3$ substitutions of 6,7 position of THIs differently affect the ?1-adrenoceptor affinity. We synthesized two 1-naphthylmethyl THI alkaloids, $1-{\beta}-naphthylmethyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline$ HBr (YS 51) and $1-{\beta}-naphthylmethyl-6, 7-dimethoxy-1,2,3,4-tetrahydroisoquinoline$ HCl (YS 55), and their pharmacological actions on ?${\alpha}_1-adrenoceptor$ were compared. YS 51 and YS 55, concentration-dependently relaxed endothelium-denuded rat thoracic aorta precontracted with phenylephrine (PE, 0.1 ${\mu}M$) in which $pEC_{50}$ were $5.89{\pm}0.21$ and $5.93{\pm}0.19$, respectively. Propranolol (30 nM) did not affect the relaxation-response curves to YS 51 and YS 55. Concentration-response curves to PE were shifted to right by the pretreatment with YS 51 or YS 55. The $pA_2$ values of YS 51 and YS 55 showed $6.05{\pm}0.24$ and $5.88{\pm}0.16$, respectively. Both probes relaxed KCl (65.4 mM)-contracted aorta and inhibited $CaCl_2-induced$ contraction of PE-stimulated endothelium- denuded rat thoracic aorta in $Ca^{2+}-free$ solutions. In isolated guinea pig papillary muscle, 1 and 10 ${\mu}M$ YS 51 increased contractile force about 4- and 8- fold over the control, respectively, along with the concentration-dependent increment of cytosolic $Ca^{2+}$ ions. While, 10 ${\mu}M$ YS 55 reduced the contractile force about 50 % over the control and lowered the cytosolic $Ca^{2+}$ level, in rat brain homogenates, YS 51 and YS 55 displaced $[^3H]prazosin$ binding competitively with Ki 0.15 and 0.12 ${\mu}M$, respectively. However, both probes were ineffective on $[^3H]nitrendipine$ binding. Therefore, it is concluded that two synthetic naphthylmethyl-THI alkaloids have considerable affinity to ?1-adrenenoceptors in rat aorta and brain.

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