复旦学报(医学版)
複旦學報(醫學版)
복단학보(의학판)
JOURNAL OF FUDAN UNIVERSITY
2001年
2期
148-151
,共4页
盐酸普萘洛尔%渗透系数%离体颊黏膜渗透
鹽痠普萘洛爾%滲透繫數%離體頰黏膜滲透
염산보내락이%삼투계수%리체협점막삼투
目的探讨抗心律失常药盐酸普萘洛尔(PL·HCL)在猪口腔颊黏膜上的渗透作用及药物经口颊黏膜吸
收的影响因素。方法利用猪口腔颊黏膜分别考察了药物和黏膜促透剂甘氨胆酸钠(GC)、去氧甘氨胆酸钠
(GDC)、羟丙基-β-环糊精(HPβCD)和二甲基-β-环糊精(DMβCD)在不同浓度对黏膜预处理后该药的渗透情况,以
及pH、浓度、渗透压等理化因素对药物渗透的影响。结果GC、GDC、HPβCD、DMβCD在一定浓度时对PL·HCL
均有促透作用。药物的渗透系数P值在实验范围内随pH的升高而增大,随渗透浓度的增加而减小,而不受药
物浓度的影响。结论 PL·HCL经颊黏膜转运是被动扩散过程,受促透剂、介质pH、渗透浓度等理化性质的影
响。
目的探討抗心律失常藥鹽痠普萘洛爾(PL·HCL)在豬口腔頰黏膜上的滲透作用及藥物經口頰黏膜吸
收的影響因素。方法利用豬口腔頰黏膜分彆攷察瞭藥物和黏膜促透劑甘氨膽痠鈉(GC)、去氧甘氨膽痠鈉
(GDC)、羥丙基-β-環糊精(HPβCD)和二甲基-β-環糊精(DMβCD)在不同濃度對黏膜預處理後該藥的滲透情況,以
及pH、濃度、滲透壓等理化因素對藥物滲透的影響。結果GC、GDC、HPβCD、DMβCD在一定濃度時對PL·HCL
均有促透作用。藥物的滲透繫數P值在實驗範圍內隨pH的升高而增大,隨滲透濃度的增加而減小,而不受藥
物濃度的影響。結論 PL·HCL經頰黏膜轉運是被動擴散過程,受促透劑、介質pH、滲透濃度等理化性質的影
響。
목적탐토항심률실상약염산보내락이(PL·HCL)재저구강협점막상적삼투작용급약물경구협점막흡
수적영향인소。방법이용저구강협점막분별고찰료약물화점막촉투제감안담산납(GC)、거양감안담산납
(GDC)、간병기-β-배호정(HPβCD)화이갑기-β-배호정(DMβCD)재불동농도대점막예처리후해약적삼투정황,이
급pH、농도、삼투압등이화인소대약물삼투적영향。결과GC、GDC、HPβCD、DMβCD재일정농도시대PL·HCL
균유촉투작용。약물적삼투계수P치재실험범위내수pH적승고이증대,수삼투농도적증가이감소,이불수약
물농도적영향。결론 PL·HCL경협점막전운시피동확산과정,수촉투제、개질pH、삼투농도등이화성질적영
향。
Purpose To investigate the permeation of model drug,propranolol hydrochloride, through the
excised porcine buccal mucosa. To study the influences of various factors on the buccal absorption also
studied. Methods Using excised porcine buccal mucosa permeation test in vitro. By means of changing
the medium pH, osmotic concentration, drug concentration, the concentration of various penetration
enhancers including sodium glycodeoxycholate (GDC), sodium glycocholate (GC), dimethy1-β-cyclodextrin
(DMβCD), and hydropropyl-β-cyclodextrin(HPβCD). The permeation rates and permeability coefficients(P)
were determined and evaluated. The solubilities and apparent partition coefficients also determined in some
tests. Results The result showed that the P were increased when porcine buccal mucosae were pretreated
with every penetration enhancement of certain concentration, increased as the pH of test solution rose from
4.9 to 9.1. The P remained constant as the concentration of propranolol hydrochloride increased from 5 to
80 mg/ml, decreased with the increasing of osmotic concentration Conclusions The absorption of
propranolol hydrochloride through porcine buccal mucosa is a typical passive process, and affected by
penetration enhancers, medium pH, osmotic concentration.