表面活性劑的安全性
表(biao)面(mian)活(huo)性(xing)(xing)劑(ji)及其代謝產(chan)物(wu)在(zai)機體內引起(qi)的生物(wu)學(xue)變化(hua),亦即對機體可能造成的毒副作用包括急(ji)性(xing)(xing)毒性(xing)(xing)、亞急(ji)性(xing)(xing)毒性(xing)(xing)、慢性(xing)(xing)毒性(xing)(xing)、對生育繁殖的影響、胚(pei)胎毒性(xing)(xing)、致畸性(xing)(xing)、致突變性(xing)(xing)、致癌性(xing)(xing)、致敏性(xing)(xing)、溶(rong)血性(xing)(xing)等等。表(biao)面(mian)活(huo)性(xing)(xing)劑(ji)與人體不(bu)同(tong)部分(fen)以(yi)不(bu)同(tong)方式接觸,對上述毒副作用會提出(chu)不(bu)同(tong)的要求(qiu)。
表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)在(zai)(zai)與人(ren)體接(jie)觸的(de)(de)體系如(ru)(ru)(ru)藥物、食品(pin)、化(hua)妝品(pin)及個人(ren)衛生(sheng)用品(pin)中(zhong)的(de)(de)應(ying)用越(yue)(yue)來(lai)越(yue)(yue)廣泛(fan),隨著人(ren)類生(sheng)活(huo)(huo)(huo)水平(ping)的(de)(de)提(ti)高,人(ren)們(men)對(dui)(dui)各(ge)類與人(ren)體接(jie)觸配(pei)(pei)方(fang)中(zhong)表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)的(de)(de)毒(du)(du)副(fu)(fu)作用投入越(yue)(yue)來(lai)越(yue)(yue)多(duo)的(de)(de)關(guan)注。針對(dui)(dui)不同(tong)用途,對(dui)(dui)表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)關(guan)注的(de)(de)重(zhong)點主要集中(zhong)在(zai)(zai)對(dui)(dui)黏膜的(de)(de)刺激性(xing)(xing)(xing)(xing)(xing)、對(dui)(dui)皮膚的(de)(de)致敏性(xing)(xing)(xing)(xing)(xing)、毒(du)(du)性(xing)(xing)(xing)(xing)(xing)、遺傳(chuan)性(xing)(xing)(xing)(xing)(xing)、致癌(ai)性(xing)(xing)(xing)(xing)(xing)、致畸性(xing)(xing)(xing)(xing)(xing)和(he)(he)(he)溶血性(xing)(xing)(xing)(xing)(xing)、消化(hua)吸收性(xing)(xing)(xing)(xing)(xing)、生(sheng)物降解性(xing)(xing)(xing)(xing)(xing)等方(fang)面(mian)(mian)(mian)。例如(ru)(ru)(ru)對(dui)(dui)化(hua)妝品(pin)而言,以前選取配(pei)(pei)料的(de)(de)原(yuan)則以裝扮靚麗為主,選擇表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)只是(shi)考慮(lv)如(ru)(ru)(ru)何達到(dao)(dao)最(zui)(zui)佳(jia)的(de)(de)第一(yi)功(gong)(gong)效(xiao)或(huo)主功(gong)(gong)效(xiao),如(ru)(ru)(ru)凈洗、發(fa)(fa)(fa)泡、乳(ru)化(hua)、分散等;其次才考慮(lv)到(dao)(dao)發(fa)(fa)(fa)揮其第二功(gong)(gong)效(xiao)或(huo)輔助功(gong)(gong)效(xiao),很少或(huo)根本沒(mei)有(you)(you)考慮(lv)到(dao)(dao)表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)對(dui)(dui)皮膚、毛發(fa)(fa)(fa)等自(zi)然狀(zhuang)(zhuang)態(tai)的(de)(de)影響。現在(zai)(zai)對(dui)(dui)表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)的(de)(de)選取原(yuan)則則逐(zhu)漸(jian)趨(qu)向于在(zai)(zai)首先滿足(zu)保護皮膚、毛發(fa)(fa)(fa)的(de)(de)正常、健康(kang)狀(zhuang)(zhuang)態(tai),對(dui)(dui)人(ren)體產(chan)生(sheng)盡(jin)可能少的(de)(de)毒(du)(du)副(fu)(fu)作用的(de)(de)前提(ti)條件下,才考慮(lv)如(ru)(ru)(ru)何發(fa)(fa)(fa)揮表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)的(de)(de)最(zui)(zui)佳(jia)主功(gong)(gong)效(xiao)和(he)(he)(he)輔助功(gong)(gong)效(xiao)。這種(zhong)(zhong)發(fa)(fa)(fa)展趨(qu)勢(shi)使得表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)原(yuan)料供應(ying)商(shang)、配(pei)(pei)方(fang)師(shi)和(he)(he)(he)生(sheng)產(chan)廠商(shang)都面(mian)(mian)(mian)臨(lin)著一(yi)種(zhong)(zhong)挑戰,即如(ru)(ru)(ru)何重(zhong)新(xin)認識和(he)(he)(he)評價(jia)表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)的(de)(de)安(an)(an)全(quan)性(xing)(xing)(xing)(xing)(xing)及溫(wen)(wen)和(he)(he)(he)性(xing)(xing)(xing)(xing)(xing),向消費(fei)者提(ti)供最(zui)(zui)安(an)(an)全(quan)、最(zui)(zui)溫(wen)(wen)和(he)(he)(he)又最(zui)(zui)有(you)(you)效(xiao)的(de)(de)制品(pin)。因(yin)此,重(zhong)新(xin)評價(jia)原(yuan)有(you)(you)表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)品(pin)種(zhong)(zhong)和(he)(he)(he)新(xin)型(xing)表(biao)(biao)面(mian)(mian)(mian)活(huo)(huo)(huo)性(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)(ji)的(de)(de)安(an)(an)全(quan)性(xing)(xing)(xing)(xing)(xing)和(he)(he)(he)溫(wen)(wen)和(he)(he)(he)性(xing)(xing)(xing)(xing)(xing)是(shi)十分必(bi)要的(de)(de)。
陽離(li)子型表面活(huo)性(xing)(xing)劑(ji)常(chang)常(chang)用(yong)(yong)作消(xiao)毒(du)(du)(du)(du)殺菌(jun)劑(ji),對各類細菌(jun)、霉菌(jun)和(he)真菌(jun)有(you)較強(qiang)的殺滅作用(yong)(yong),但同時也有(you)毒(du)(du)(du)(du)副(fu)作用(yong)(yong)。它們會(hui)使中(zhong)樞(shu)神經(jing)系(xi)(xi)統和(he)呼吸系(xi)(xi)統機能下(xia)降,并使胃(wei)部充血(xue)。陰離(li)子型表面活(huo)性(xing)(xing)劑(ji)毒(du)(du)(du)(du)性(xing)(xing)較低,在通常(chang)應(ying)用(yong)(yong)濃度范圍內(nei),不會(hui)對人體造成(cheng)急(ji)性(xing)(xing)毒(du)(du)(du)(du)性(xing)(xing)傷(shang)害,但口服(fu)后會(hui)使胃(wei)腸道產生不適(shi)感,有(you)腹瀉現象。非離(li)子表面活(huo)性(xing)(xing)劑(ji)屬于低毒(du)(du)(du)(du)或無毒(du)(du)(du)(du)類,經(jing)口服(fu)無毒(du)(du)(du)(du)。其(qi)中(zhong)毒(du)(du)(du)(du)性(xing)(xing)最低的是(shi)PEG類,較次的是(shi)糖酯、AEO和(he)Span、Tween類,烷基酚聚醚(mi)類毒(du)(du)(du)(du)性(xing)(xing)偏高。
表(biao)一(yi):一(yi)些表(biao)面活性(xing)劑對(dui)黑(hei)鼠的(de)經口急性(xing)毒性(xing)

表(biao)二(er):幾種表(biao)面活性(xing)劑對水(shui)生(sheng)動物的急性(xing)毒(du)性(xing)

從表(biao)二所列數據看出,對水生(sheng)動物而言,非離子表(biao)面活性劑的毒(du)(du)性總體上高于(yu)陰(yin)離子表(biao)面活性劑的毒(du)(du)性。
亞(ya)急(ji)性(xing)(xing)和慢(man)性(xing)(xing)毒(du)性(xing)(xing)試(shi)驗(yan)(yan)一般(ban)耗時較(jiao)長,由于采用(yong)(yong)實驗(yan)(yan)動(dong)物和其(qi)它實驗(yan)(yan)條件的(de)(de)(de)差異(yi),各種(zhong)數據很難(nan)比較(jiao)。但一般(ban)認(ren)為(wei)非(fei)離子(zi)(zi)型表(biao)(biao)(biao)面活性(xing)(xing)劑(ji)的(de)(de)(de)亞(ya)急(ji)性(xing)(xing)和慢(man)性(xing)(xing)毒(du)性(xing)(xing)實驗(yan)(yan)結果均為(wei)無毒(du)類,長期服(fu)用(yong)(yong)不會(hui)造成病態反應,只(zhi)是(shi)有(you)些品(pin)種(zhong)會(hui)增加人體(ti)對脂肪、維生素或(huo)其(qi)它物質的(de)(de)(de)吸收,或(huo)在大劑(ji)量(liang)口服(fu)時引起某些臟(zang)器可(ke)逆性(xing)(xing)功能(neng)改(gai)變,因此非(fei)離子(zi)(zi)型表(biao)(biao)(biao)面活性(xing)(xing)劑(ji)可(ke)作(zuo)(zuo)為(wei)高安全性(xing)(xing)物質使(shi)用(yong)(yong)。食(shi)品(pin)中常將(jiang)非(fei)離子(zi)(zi)型表(biao)(biao)(biao)面活性(xing)(xing)劑(ji)作(zuo)(zuo)為(wei)乳(ru)(ru)化劑(ji)使(shi)用(yong)(yong),有(you)時也需要用(yong)(yong)到表(biao)(biao)(biao)面活性(xing)(xing)劑(ji)的(de)(de)(de)起泡、消泡、潤濕、分散、防(fang)(fang)結晶、防(fang)(fang)老化、防(fang)(fang)返(fan)生、保(bao)水、殺菌、抗(kang)氧化等功能(neng)。作(zuo)(zuo)為(wei)食(shi)品(pin)乳(ru)(ru)化劑(ji)使(shi)用(yong)(yong)的(de)(de)(de)表(biao)(biao)(biao)面活性(xing)(xing)劑(ji)是(shi)受到嚴(yan)格限制的(de)(de)(de),一般(ban)只(zhi)批準幾個品(pin)種(zhong)可(ke)以使(shi)用(yong)(yong),有(you)些還受到日攝入量(liang)(ADI,mg/kg)指數的(de)(de)(de)限制,即人體(ti)對某種(zhong)添加劑(ji)連(lian)續攝入,對單位(wei)重量(liang)人體(ti)不會(hui)產生侵害性(xing)(xing)影響的(de)(de)(de)最大劑(ji)量(liang)。
表三:食品乳化劑的ADI值和容許最大使用量

1.2
溶血性(xing)
藥物(wu)注(zhu)射(she)(she)液(ye)或(huo)營(ying)養注(zhu)射(she)(she)液(ye)中常用(yong)(yong)(yong)非(fei)離(li)子(zi)型(xing)(xing)表(biao)面(mian)活(huo)(huo)性(xing)劑作為增(zeng)溶(rong)(rong)(rong)(rong)(rong)劑、乳化劑或(huo)懸浮(fu)劑使用(yong)(yong)(yong),對于一次注(zhu)射(she)(she)量較大(da)的(de)(de)場合,特別(bie)是靜(jing)脈(mo)注(zhu)射(she)(she)時,表(biao)面(mian)活(huo)(huo)性(xing)劑的(de)(de)溶(rong)(rong)(rong)(rong)(rong)血(xue)性(xing)必須引起重(zhong)視。陰離(li)子(zi)型(xing)(xing)表(biao)面(mian)活(huo)(huo)性(xing)劑的(de)(de)溶(rong)(rong)(rong)(rong)(rong)血(xue)性(xing)最大(da),一般不(bu)在(zai)(zai)注(zhu)射(she)(she)液(ye)中使用(yong)(yong)(yong);陽離(li)子(zi)型(xing)(xing)的(de)(de)溶(rong)(rong)(rong)(rong)(rong)血(xue)性(xing)次之,非(fei)離(li)子(zi)型(xing)(xing)的(de)(de)溶(rong)(rong)(rong)(rong)(rong)血(xue)性(xing)最小(xiao)。在(zai)(zai)非(fei)離(li)子(zi)表(biao)面(mian)活(huo)(huo)性(xing)劑中,又以氫化蓖麻油酸PEG酯的(de)(de)溶(rong)(rong)(rong)(rong)(rong)血(xue)性(xing)作用(yong)(yong)(yong)為低,最適于靜(jing)脈(mo)注(zhu)射(she)(she),但(dan)若其(qi)中PEG聚合度加大(da),則溶(rong)(rong)(rong)(rong)(rong)血(xue)性(xing)會超過(guo)Tween類。非(fei)離(li)子(zi)型(xing)(xing)溶(rong)(rong)(rong)(rong)(rong)血(xue)性(xing)的(de)(de)排列次序(xu)為:Tween<PEG脂肪酸酯<PRG烷(wan)基酚<AEO。在(zai)(zai)Tween系列中,溶(rong)(rong)(rong)(rong)(rong)血(xue)性(xing)次序(xu)為:Tween 80
表面活性劑的溫和性
表面(mian)活(huo)性(xing)(xing)(xing)劑對(dui)人體皮(pi)膚(fu)、眼睛(jing)、毛發(fa),特(te)別是對(dui)皮(pi)膚(fu)、眼睛(jing)的(de)(de)溫和性(xing)(xing)(xing)是一(yi)個頗難定(ding)義的(de)(de)概念,截止目(mu)前(qian)為止仍(reng)然沒有統一(yi)的(de)(de)標準。表面(mian)活(huo)性(xing)(xing)(xing)劑對(dui)粘膜產生的(de)(de)刺激性(xing)(xing)(xing)或致敏性(xing)(xing)(xing)主要由三(san)個因素(su)引起:
(1)溶(rong)出性 指表面活(huo)性劑對皮(pi)膚(fu)本身的保(bao)濕成(cheng)分(fen)(如(ru)保(bao)濕因子NMF)、細(xi)胞(bao)間脂質及角質層中(zhong)游離氨(an)基(ji)酸和脂肪的溶(rong)出程(cheng)度。這些成(cheng)分(fen)的過分(fen)溶(rong)出將使皮(pi)膚(fu)油脂和表層受到破壞,皮(pi)膚(fu)保(bao)水能力下(xia)降,引起(qi)細(xi)胞(bao)成(cheng)皮(pi)屑脫(tuo)落(luo),從而造(zao)成(cheng)皮(pi)膚(fu)緊繃、刺(ci)痛(tong)或干燥(zao)感。更(geng)有(you)甚者,表面活(huo)性劑除了對細(xi)胞(bao)有(you)剝(bo)離作用外(wai),還對細(xi)胞(bao)有(you)溶(rong)解作用,如(ru)SDS就(jiu)是生物膜的很有(you)效的溶(rong)解劑。
(2)滲入性(xing)指表(biao)(biao)(biao)面活(huo)性(xing)劑(ji)經皮(pi)(pi)滲透的(de)能力,這種(zhong)作用(yong)被認為是引發皮(pi)(pi)膚各種(zhong)炎(yan)癥的(de)原因之一。表(biao)(biao)(biao)面活(huo)性(xing)劑(ji)滲入改變了皮(pi)(pi)膚的(de)原始結構狀態和(he)相鄰分子間(jian)的(de)相容性(xing),從而(er)引發接觸(chu)性(xing)皮(pi)(pi)炎(yan)、真皮(pi)(pi)皮(pi)(pi)炎(yan),造(zao)成皮(pi)(pi)膚刺(ci)激作用(yong)甚至引起過(guo)敏反應(ying),使皮(pi)(pi)膚上出(chu)現(xian)紅斑和(he)水(shui)腫現(xian)象。表(biao)(biao)(biao)面活(huo)性(xing)劑(ji)對皮(pi)(pi)膚粘膜(mo)的(de)刺(ci)激作用(yong)以陽離(li)子最(zui)甚,陰離(li)子次之,非離(li)子型(xing)(xing)和(he)兩性(xing)離(li)子型(xing)(xing)最(zui)小(xiao)。
(3)反應性 指表面活(huo)性劑對蛋(dan)白(bai)質的吸附,致使蛋(dan)白(bai)質變(bian)性以及改變(bian)皮膚pH條件(jian)等(deng)的作用。實驗表明PEG非離子類的反應性較(jiao)(jiao)低,LAS等(deng)陰離子的反應性較(jiao)(jiao)大。
2.1
評價溫和性的方法
評(ping)(ping)價表面活(huo)性劑溫(wen)和(he)(he)性的方法(fa)有多種(zhong),目前尚缺(que)少統(tong)一標準(zhun)。目前通用的溫(wen)和(he)(he)性評(ping)(ping)價方法(fa)主要(yao)分為活(huo)體(ti)試驗(in vivo test)和(he)(he)離體(ti)試驗(in vitro test)兩大(da)類。出于安全(quan)性考慮和(he)(he)滿足保護動物運(yun)動的需(xu)要(yao),目前大(da)力提倡采用離體(ti)試驗方法(fa),但大(da)部分立法(fa)仍(reng)以(yi)活(huo)體(ti)試驗結(jie)果為檢(jian)驗標準(zhun)。
2.1.1
活體實驗
(1)Draize兔(tu)(tu)(tu)皮(pi)(pi)試(shi)驗(yan)(yan)(yan)(yan) Draize兔(tu)(tu)(tu)皮(pi)(pi)試(shi)驗(yan)(yan)(yan)(yan)主要以(yi)兔(tu)(tu)(tu)皮(pi)(pi)、有時也(ye)用大白鼠(shu)或(huo)荷蘭豬皮(pi)(pi)膚作試(shi)驗(yan)(yan)(yan)(yan),以(yi)各(ge)種(zhong)濃度試(shi)樣對皮(pi)(pi)膚涂敷后觀察紅(hong)斑和(he)浮腫程度綜(zong)合給分(參見表(biao)四(si))。Draize兔(tu)(tu)(tu)皮(pi)(pi)試(shi)驗(yan)(yan)(yan)(yan)可(ke)以(yi)作為(wei)一(yi)種(zhong)獨立試(shi)驗(yan)(yan)(yan)(yan),也(ye)可(ke)以(yi)作為(wei)人(ren)(ren)體(ti)皮(pi)(pi)膚試(shi)驗(yan)(yan)(yan)(yan)的(de)(de)預備試(shi)驗(yan)(yan)(yan)(yan),一(yi)些兔(tu)(tu)(tu)皮(pi)(pi)試(shi)驗(yan)(yan)(yan)(yan)結果列于表(biao)五。活體(ti)試(shi)驗(yan)(yan)(yan)(yan)主要在(zai)人(ren)(ren)體(ti)皮(pi)(pi)膚和(he)兔(tu)(tu)(tu)皮(pi)(pi)及兔(tu)(tu)(tu)眼粘膜上進(jin)行(xing),兩種(zhong)較為(wei)常用的(de)(de)方法(fa)是(shi)Driaize兔(tu)(tu)(tu)皮(pi)(pi)試(shi)驗(yan)(yan)(yan)(yan)和(he)Draize兔(tu)(tu)(tu)眼試(shi)驗(yan)(yan)(yan)(yan)。有時也(ye)采用Duhring chamber test或(huo)Cupshaking test,即對人(ren)(ren)體(ti)前腕屈曲側(ce)部(bu)進(jin)行(xing)貼斑試(shi)驗(yan)(yan)(yan)(yan),觀察表(biao)面活性(xing)劑(ji)對人(ren)(ren)體(ti)間歇試(shi)驗(yan)(yan)(yan)(yan)引起的(de)(de)紅(hong)斑和(he)浮腫等現象。也(ye)有采用手部(bu)浸(jin)漬(zi)法(fa),即將(jiang)人(ren)(ren)手浸(jin)泡在(zai)一(yi)定(ding)濃度的(de)(de)表(biao)面活性(xing)劑(ji)溶液中(zhong)模擬搓洗動作或(huo)洗碗碟動作,一(yi)定(ding)時間后測試(shi)浸(jin)泡前后皮(pi)(pi)膚表(biao)面的(de)(de)皮(pi)(pi)脂脫落率或(huo)蛋白質溶出性(xing)。
表四:Draize試驗和RBC試驗的評價和比較

(2)Draize兔(tu)眼試(shi)驗(yan) 將0.1mL受試(shi)液作(zuo)用(yong)于白(bai)兔(tu)的角膜(mo),間隔一定時間觀察(cha)刺激結果并綜合評例(參見表(biao)5)。從表(biao)6可以看出眼粘膜(mo)對表(biao)面(mian)活(huo)性劑的耐受程度(du)也(ye)以陽離子為最低(0.5%~1.0%),陰離子型次(ci)之,對非離子表(biao)面(mian)活(huo)性劑的耐受程度(du)最高。
表五:種表面活性劑的Draize兔(tu)皮刺激指(zhi)數

表(biao)六:兔眼粘膜對幾種(zhong)表(biao)面活性劑刺激的耐(nai)受度(du)

2.1.2
離體實驗
離(li)體試驗則以體外細胞或(huo)蛋白(bai)模(mo)擬生物(wu)體,觀察(cha)表(biao)面活性劑對(dui)離(li)體蛋白(bai)或(huo)細胞的作(zuo)用,從而推斷(duan)對(dui)活體組織的作(zuo)用程度(du)。最常(chang)用的兩種離(li)體試驗方法為(wei)red blood corpuscle test(RBC test)和Zein test。
(1)RBC test 一般認為(wei)刺(ci)激性(xing)物質若(ruo)與活(huo)體蛋白質發生反應(ying),則反應(ying)首先會發生在細(xi)(xi)胞(bao)膜。RBC test即(ji)紅(hong)(hong)血(xue)(xue)球細(xi)(xi)胞(bao)試驗(yan)以(yi)離體紅(hong)(hong)血(xue)(xue)球作(zuo)(zuo)為(wei)細(xi)(xi)胞(bao)替(ti)代物進行(xing)實驗(yan),觀察各種表(biao)(biao)面活(huo)性(xing)劑對紅(hong)(hong)血(xue)(xue)球細(xi)(xi)胞(bao)的(de)作(zuo)(zuo)用情況(kuang)。該(gai)試驗(yan)中將表(biao)(biao)面活(huo)性(xing)劑對紅(hong)(hong)血(xue)(xue)球細(xi)(xi)胞(bao)的(de)溶血(xue)(xue)作(zuo)(zuo)用記作(zuo)(zuo)L值,對血(xue)(xue)紅(hong)(hong)蛋白變性(xing)作(zuo)(zuo)用記作(zuo)(zuo)D值,用L/D表(biao)(biao)征綜(zong)合指數(shu)來評(ping)價對細(xi)(xi)胞(bao)的(de)刺(ci)激作(zuo)(zuo)用。下(xia)表(biao)(biao)列出了一些(xie)常(chang)見表(biao)(biao)面活(huo)性(xing)劑的(de)RBC試驗(yan)結果。
表七:一些表面活(huo)性劑(ji)的RBC test結果

(2)Zein test Zein是(shi)一(yi)種(zhong)特定的(de)玉(yu)米蛋白質(zhi),其自(zi)身幾乎是(shi)完全(quan)不溶(rong)于(yu)水(shui)的(de)。如果zein與(yu)表面(mian)活(huo)(huo)性劑(ji)(ji)有較(jiao)大(da)的(de)相(xiang)互(hu)作用(yong),則作用(yong)后(hou)zein的(de)水(shui)溶(rong)性將(jiang)加大(da)。在Zein test中,zein用(yong)于(yu)模擬活(huo)(huo)體蛋白質(zhi)進(jin)行試(shi)驗,通過測定與(yu)表面(mian)活(huo)(huo)性劑(ji)(ji)作用(yong)前后(hou)水(shui)溶(rong)液中氮含量的(de)增大(da)決定zein溶(rong)解(jie)(jie)度的(de)變化,這(zhe)種(zhong)溶(rong)解(jie)(jie)度的(de)變化反(fan)映了表面(mian)活(huo)(huo)性劑(ji)(ji)與(yu)zein相(xiang)互(hu)作用(yong)的(de)強(qiang)弱,從而間接表征了表面(mian)活(huo)(huo)性劑(ji)(ji)對(dui)活(huo)(huo)體蛋白質(zhi)的(de)作用(yong)程度。
2.2
表面活性劑結(jie)構對溫和(he)性的影響(xiang)
由于(yu)目前尚(shang)缺少統廣的(de)法定方法評(ping)價表面(mian)活性(xing)劑的(de)刺(ci)激性(xing),因此很難排(pai)出(chu)各種具體品種溫和性(xing)的(de)大小順序,只能(neng)指出(chu)表面(mian)活性(xing)劑結構(gou)對溫和性(xing)影響(xiang)的(de)一般(ban)規律。
(1)分子大小
一些(xie)表(biao)面活性劑zeintest結(jie)果,按照(zhao)刺激(ji)性從高(gao)到低的順序(xu)排列:
1、十二(er)烷基苯(ben)磺酸鈉鹽(yan)
2、月桂(gui)醇硫酸鈉鹽
3、C12C18醇(chun)硫酸酯鈉鹽
4、仲烷基磺酸鹽
5、月桂醇硫(liu)酸酯(zhi)單乙(yi)醇胺鹽(yan)
6、月(yue)桂(gui)醇硫(liu)酸酯銨鹽(yan)
7、月桂醇硫酸(suan)酯三乙醇胺鹽
8、月桂醇醚硫酸酯鈉鹽
9、月(yue)桂醇醚
(2)硫酸酯(zhi)銨(an)鹽(yan)
10、月桂醇醚(2)硫酸酯三乙醇胺鹽(yan)
11、十(shi)二/十(shi)四醇(chun)醚(3)硫(liu)酸酯鈉(na)鹽
12、月桂醇醚磺基琥珀酸單酯二鈉鹽
13、特制月桂/油醇醚硫酸鈉/鎂混合物
14、月(yue)桂(gui)醇醚硫(liu)酸鎂鹽
15、酰胺醚硫酸鹽
16、月桂酰(xian)基多縮肽鉀鹽
小分(fen)子(zi)(zi)表面活(huo)(huo)性劑(ji)容易(yi)造成經(jing)(jing)皮(pi)滲透(tou),對皮(pi)膚刺激(ji)性大;而大分(fen)子(zi)(zi)表面活(huo)(huo)性劑(ji)不易(yi)發(fa)生本身經(jing)(jing)皮(pi)滲透(tou)問題,且由于大分(fen)子(zi)(zi)二級、三(san)級結構的(de)影響,極(ji)性基團(tuan)及(ji)疏水支鏈均不易(yi)與皮(pi)膚或(huo)毛(mao)發(fa)發(fa)生直接(jie)、強烈(lie)的(de)作(zuo)用,因而比(bi)較溫和。目前化妝品(pin)(pin)(pin)和個人衛(wei)生用品(pin)(pin)(pin)中所用的(de)表面活(huo)(huo)性劑(ji)、乳化劑(ji)有(you)向(xiang)大分(fen)子(zi)(zi)、高分(fen)子(zi)(zi)化方向(xiang)發(fa)展的(de)趨勢,或(huo)對天然(ran)高分(fen)子(zi)(zi)進行(xing)改性,如采用淀粉、多肽、水解纖維(wei)素、樹膠的(de)改性物,或(huo)采用合成高分(fen)子(zi)(zi),如用聚(ju)酰胺(an)或(huo)聚(ju)丙(bing)烯酸作(zuo)化妝品(pin)(pin)(pin)乳液的(de)乳化劑(ji)和增(zeng)稠劑(ji),收到了高效(xiao)、低刺激(ji)、具溫和性的(de)效(xiao)果。
(2)疏水基鏈(lian)長(chang)一(yi)般認為(wei)疏水基鏈(lian)越長(chang),分支化程度越小(xiao),表面活性(xing)劑(ji)對人體越溫(wen)和,這一(yi)點已經得到眾多事(shi)實證明(ming)。但目前也發(fa)現存在(zai)例外,如(ru)P&G開發(fa)AGS(烷基甘(gan)油(you)醚(mi)磺酸鹽)時發(fa)現,并不是長(chang)鏈(lian)烷基的衍(yan)生物,而是八碳(tan)烷基的衍(yan)生物刺激性(xing)最低,起(qi)泡(pao)性(xing)亦好。
(3)分子內引入(ru)PEG基團(tuan)
PEG型(xing)非(fei)離子表(biao)(biao)面(mian)活(huo)性(xing)(xing)劑無論在對皮膚粘(zhan)膜或(huo)眼粘(zhan)膜的(de)(de)刺激性(xing)(xing)方面(mian)都表(biao)(biao)現得比陰、陽離子型(xing)表(biao)(biao)面(mian)活(huo)性(xing)(xing)劑的(de)(de)低。增大分(fen)子中PEG長度,刺激性(xing)(xing)會進一步(bu)降低,既使(shi)是在離子型(xing)表(biao)(biao)面(mian)活(huo)性(xing)(xing)劑中引(yin)入(ru)PEG鏈,形成所謂摻合(he)型(xing)(hybrid)表(biao)(biao)面(mian)活(huo)性(xing)(xing)劑,也會增大分(fen)子的(de)(de)溫(wen)和性(xing)(xing),SDS中引(yin)入(ru)PEG鍵形成AES便是一個很好的(de)(de)例證(zheng)。分(fen)子中引(yin)入(ru)甘油(you)或(huo)其它多元醇(chun)也會收到(dao)與引(yin)入(ru)PEG鏈相同(tong)的(de)(de)結果。
(4)表面(mian)活性劑結構與皮膚的(de)相似性
本身結構(gou)比較復雜(za),與(yu)皮(pi)(pi)(pi)膚(fu)(fu)結構(gou)具(ju)有(you)(you)一(yi)定相似(si)性(xing)(xing)(xing)(xing)(xing)(xing)或相近(jin)性(xing)(xing)(xing)(xing)(xing)(xing)的(de)(de)(de)(de)表面(mian)(mian)活(huo)(huo)性(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)對(dui)皮(pi)(pi)(pi)膚(fu)(fu)比較溫(wen)和(he)(he)。因此(ci)目前化妝(zhuang)品(pin)和(he)(he)個人(ren)衛生用(yong)品(pin)中(zhong)新開發(fa)的(de)(de)(de)(de)一(yi)些溫(wen)和(he)(he)型(xing)(xing)表面(mian)(mian)活(huo)(huo)性(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)都(dou)具(ju)有(you)(you)比較復雜(za)的(de)(de)(de)(de)結構(gou),不再是長鏈烷基與(yu)親水基的(de)(de)(de)(de)簡單結合體(ti),而是多分(fen)(fen)子縮(suo)合物(wu)型(xing)(xing)。如Witco推出SBCS(Disodium PEG-5 Laurylcitrate Sulfosuccinate),將(jiang)檸檬酸(suan)(suan)酯與(yu)磺基琥(hu)珀(po)酸(suan)(suan)酯的(de)(de)(de)(de)結構(gou)合二為一(yi),據(ju)稱具(ju)有(you)(you)很低的(de)(de)(de)(de)皮(pi)(pi)(pi)膚(fu)(fu)刺激(ji)(ji)性(xing)(xing)(xing)(xing)(xing)(xing)和(he)(he)很好(hao)的(de)(de)(de)(de)應用(yong)性(xing)(xing)(xing)(xing)(xing)(xing)能(neng)。此(ci)外,分(fen)(fen)子中(zhong)引(yin)入(ru)酰(xian)胺鍵或引(yin)入(ru)水解(jie)蛋白、氨基酸(suan)(suan)結構(gou)等,增加了表面(mian)(mian)活(huo)(huo)性(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)分(fen)(fen)子與(yu)皮(pi)(pi)(pi)膚(fu)(fu)組織的(de)(de)(de)(de)相似(si)性(xing)(xing)(xing)(xing)(xing)(xing),亦有(you)(you)助(zhu)于(yu)增加表面(mian)(mian)活(huo)(huo)性(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)的(de)(de)(de)(de)溫(wen)和(he)(he)性(xing)(xing)(xing)(xing)(xing)(xing),如改(gai)(gai)性(xing)(xing)(xing)(xing)(xing)(xing)皂(zao)(zao)AM(N-酰(xian)基甲(jia)基牛黃酸(suan)(suan)鈉)、酰(xian)基丙(bing)基甜菜堿、油酰(xian)多肽等。如將(jiang)醇醚磺基琥(hu)珀(po)酸(suan)(suan)酯鈉鹽(yan)改(gai)(gai)成(cheng)醇酰(xian)胺磺基琥(hu)珀(po)酸(suan)(suan)酯鈉鹽(yan),其對(dui)皮(pi)(pi)(pi)膚(fu)(fu)和(he)(he)眼睛粘膜的(de)(de)(de)(de)刺激(ji)(ji)性(xing)(xing)(xing)(xing)(xing)(xing)均小于(yu)前者,且兩者都(dou)比AES低。急性(xing)(xing)(xing)(xing)(xing)(xing)毒(du)性(xing)(xing)(xing)(xing)(xing)(xing)試(shi)驗表明LD50由(you)前者的(de)(de)(de)(de)12000mg/kg提高到約20000mg/kg。酰(xian)基β-丙(bing)氨酸(suan)(suan)的(de)(de)(de)(de)鉀鹽(yan)或銨鹽(yan),水溶性(xing)(xing)(xing)(xing)(xing)(xing)很好(hao),又(you)具(ju)有(you)(you)羧酸(suan)(suan)根的(de)(de)(de)(de)柔(rou)和(he)(he)結構(gou),作為香波(bo)配(pei)料使用(yong)時,與(yu)水中(zhong)的(de)(de)(de)(de)鈣、鎂(mei)離(li)子形成(cheng)的(de)(de)(de)(de)鈣、鎂(mei)改(gai)(gai)性(xing)(xing)(xing)(xing)(xing)(xing)皂(zao)(zao),能(neng)在頭發(fa)周圍形成(cheng)潤滑性(xing)(xing)(xing)(xing)(xing)(xing)好(hao)的(de)(de)(de)(de)層狀晶體(ti),使頭發(fa)得(de)到溫(wen)和(he)(he)調理和(he)(he)保(bao)護(hu),不會產生一(yi)般皂(zao)(zao)垢帶來的(de)(de)(de)(de)僵(jiang)硬、發(fa)澀(se)感。
(5)離子(zi)基團的極性
離(li)子(zi)(zi)基(ji)(ji)(ji)團(tuan)(tuan)的(de)(de)(de)(de)極(ji)性(xing)愈小,對皮(pi)膚(fu)(fu)、毛發愈溫(wen)和。在SDS結構中(zhong)引入(ru)PEG基(ji)(ji)(ji)團(tuan)(tuan)形(xing)成的(de)(de)(de)(de)AES已大(da)大(da)降低(di)了(le)對皮(pi)膚(fu)(fu)、毛發的(de)(de)(de)(de)脫脂力;如(ru)果(guo)進一步將(jiang)磺(huang)酸(suan)(suan)根改(gai)(gai)變(bian)(bian)為羧酸(suan)(suan)根,形(xing)成ECH(烷(wan)基(ji)(ji)(ji)醚醋酸(suan)(suan)鹽(yan)),則形(xing)成更溫(wen)和的(de)(de)(de)(de)一類(lei)表(biao)面(mian)活性(xing)劑乳化劑。更換離(li)子(zi)(zi)化基(ji)(ji)(ji)團(tuan)(tuan)的(de)(de)(de)(de)反(fan)離(li)子(zi)(zi)種類(lei),即改(gai)(gai)變(bian)(bian)離(li)子(zi)(zi)基(ji)(ji)(ji)團(tuan)(tuan)在水(shui)溶液中(zhong)的(de)(de)(de)(de)離(li)子(zi)(zi)化度也有助于(yu)改(gai)(gai)變(bian)(bian)表(biao)面(mian)活性(xing)劑分(fen)子(zi)(zi)的(de)(de)(de)(de)溫(wen)和性(xing)。如(ru)將(jiang)AES中(zhong)的(de)(de)(de)(de)鈉離(li)子(zi)(zi)改(gai)(gai)變(bian)(bian)為銨離(li)子(zi)(zi),有助于(yu)減小分(fen)子(zi)(zi)的(de)(de)(de)(de)離(li)子(zi)(zi)化度,因而AES銨鹽(yan)的(de)(de)(de)(de)溫(wen)和性(xing)增大(da),可作為香波(bo)和浴波(bo)的(de)(de)(de)(de)主(zhu)表(biao)面(mian)活性(xing)劑。如(ru)將(jiang)AES中(zhong)鈉離(li)子(zi)(zi)改(gai)(gai)變(bian)(bian)為鎂等(deng)二價離(li)子(zi)(zi),則可大(da)大(da)增加頭(tou)發洗滌后(hou)的(de)(de)(de)(de)平滑(hua)性(xing)和柔(rou)和性(xing)。少量脂肪酸(suan)(suan)鈣、鎂皂與大(da)量鈉皂混合,可賦(fu)予(yu)皮(pi)膚(fu)(fu)浴后(hou)的(de)(de)(de)(de)光(guang)滑(hua)、潔凈、爽(shuang)快感(gan),這(zhe)是強親水(shui)性(xing)基(ji)(ji)(ji)團(tuan)(tuan)磺(huang)酸(suan)(suan)根、硫酸(suan)(suan)根所不具備的(de)(de)(de)(de)。
2.3
配伍性和(he)溫和(he)性
開發結構特殊的新表面活性劑品種,追求溫和性是一件耗時費資、永無止境的事,利用表面活性劑的復配協合性,或對原有表面活性劑品種進行工藝、化學結構方面的改進是提高產品溫和性的另一條途徑。
(1)表(biao)(biao)面(mian)(mian)活性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)的(de)(de)(de)純(chun)化(hua)許多(duo)表(biao)(biao)面(mian)(mian)活性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)的(de)(de)(de)純(chun)品經檢測(ce)都是(shi)(shi)刺激性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)低、溫(wen)和(he)(he)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)高(gao)的(de)(de)(de)品種(zhong)(zhong),但(dan)工(gong)(gong)(gong)業(ye)產品中由于原(yuan)(yuan)料、工(gong)(gong)(gong)藝、副反應(ying)等(deng)(deng)(deng)眾多(duo)原(yuan)(yuan)因(yin),會在產品中帶進一些(xie)雜質(zhi),如未(wei)反應(ying)原(yuan)(yuan)料、副產物、有(you)毒有(you)色物質(zhi)等(deng)(deng)(deng),限制(zhi)了這些(xie)表(biao)(biao)面(mian)(mian)活性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)作為高(gao)品質(zhi)、溫(wen)和(he)(he)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)品種(zhong)(zhong)在化(hua)妝品和(he)(he)個人衛生用(yong)品中的(de)(de)(de)應(ying)用(yong)。最(zui)為典(dian)型的(de)(de)(de)例子是(shi)(shi)磺基(ji)琥珀酸單(dan)酯二鈉鹽品種(zhong)(zhong),在溫(wen)和(he)(he)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)排(pai)列次(ci)序中它甚至名列咪唑(zuo)啉(lin)和(he)(he)甜菜堿(jian)兩(liang)(liang)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)表(biao)(biao)面(mian)(mian)活性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)之前。但(dan)具有(you)諷刺意味的(de)(de)(de)是(shi)(shi)其工(gong)(gong)(gong)業(ye)產品對皮膚(fu)的(de)(de)(de)刺激性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)頗大,不(bu)適于作為溫(wen)和(he)(he)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)表(biao)(biao)面(mian)(mian)活性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)使用(yong)。另一個例子是(shi)(shi)甜菜堿(jian)型兩(liang)(liang)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)表(biao)(biao)面(mian)(mian)活性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)其溫(wen)和(he)(he)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)排(pai)名亦名列前矛,但(dan)工(gong)(gong)(gong)業(ye)品中由于含游離胺(an)和(he)(he)過(guo)量氯乙酸鈉等(deng)(deng)(deng)而帶來刺激性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)。目(mu)前已(yi)有(you)許多(duo)工(gong)(gong)(gong)作集(ji)中在對原(yuan)(yuan)有(you)優秀溫(wen)和(he)(he)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)表(biao)(biao)面(mian)(mian)活性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)品種(zhong)(zhong)的(de)(de)(de)工(gong)(gong)(gong)藝優化(hua)和(he)(he)產品純(chun)化(hua),以還其溫(wen)和(he)(he)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)的(de)(de)(de)本業(ye)面(mian)(mian)目(mu)。由RHONE-POULENC制(zhi)備的(de)(de)(de)高(gao)純(chun)無刺激咪唑(zuo)啉(lin)兩(liang)(liang)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)表(biao)(biao)面(mian)(mian)活性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji),我們實驗(yan)室制(zhi)備的(de)(de)(de)晶體甜菜堿(jian)兩(liang)(liang)性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)表(biao)(biao)面(mian)(mian)活性(xing)(xing)(xing)(xing)(xing)(xing)(xing)(xing)劑(ji)(ji)、BALLESTRA用(yong)刮膜干(gan)燥法脫除二氧六五制(zhi)備的(de)(de)(de)AES等(deng)(deng)(deng)都是(shi)(shi)這樣的(de)(de)(de)品種(zhong)(zhong)。
(2)表(biao)面活性劑復配
幾種常(chang)用(yong)大宗(zong)表(biao)(biao)面(mian)(mian)(mian)(mian)活(huo)性(xing)劑(ji)(ji)(ji)產(chan)品,如(ru)LAS、AES、SDS等存(cun)在著較為(wei)嚴(yan)重的(de)(de)(de)(de)刺(ci)激性(xing)問(wen)(wen)題,除了對其化學結構和(he)生產(chan)工藝作(zuo)(zuo)出(chu)改(gai)進外,還可(ke)(ke)以與(yu)(yu)一(yi)(yi)些溫(wen)(wen)和(he)性(xing)好的(de)(de)(de)(de)表(biao)(biao)面(mian)(mian)(mian)(mian)活(huo)性(xing)劑(ji)(ji)(ji)復(fu)(fu)(fu)(fu)配(pei)(pei)(pei)(pei),利用(yong)表(biao)(biao)面(mian)(mian)(mian)(mian)活(huo)性(xing)劑(ji)(ji)(ji)復(fu)(fu)(fu)(fu)配(pei)(pei)(pei)(pei)體(ti)系(xi)在刺(ci)激性(xing)方(fang)面(mian)(mian)(mian)(mian)的(de)(de)(de)(de)協合效應,增加復(fu)(fu)(fu)(fu)配(pei)(pei)(pei)(pei)體(ti)系(xi)的(de)(de)(de)(de)溫(wen)(wen)和(he)性(xing),使低(di)檔原(yuan)料(liao)升(sheng)級(ji)。這一(yi)(yi)方(fang)面(mian)(mian)(mian)(mian)也已(yi)經作(zuo)(zuo)出(chu)了許多(duo)(duo)有益(yi)的(de)(de)(de)(de)嘗試,如(ru)將酰(xian)(xian)胺型(xing)(xing)磺(huang)基(ji)琥珀(po)酸鈉鹽與(yu)(yu)AES按3:1復(fu)(fu)(fu)(fu)配(pei)(pei)(pei)(pei)時刺(ci)激性(xing)降(jiang)(jiang)(jiang)到(dao)比(bi)兩性(xing)表(biao)(biao)面(mian)(mian)(mian)(mian)活(huo)性(xing)劑(ji)(ji)(ji)更低(di)的(de)(de)(de)(de)水平(ping),可(ke)(ke)以用(yong)于配(pei)(pei)(pei)(pei)制兒(er)童(tong)香波和(he)高檔低(di)刺(ci)激香波。再如(ru)在LAS,AES/烷(wan)醇酰(xian)(xian)胺常(chang)用(yong)餐(can)具(ju)洗滌劑(ji)(ji)(ji)復(fu)(fu)(fu)(fu)配(pei)(pei)(pei)(pei)體(ti)系(xi)中配(pei)(pei)(pei)(pei)入少量APG(烷(wan)基(ji)葡糖苷(gan)(gan)),便(bian)可(ke)(ke)使配(pei)(pei)(pei)(pei)方(fang)的(de)(de)(de)(de)刺(ci)激性(xing)下(xia)降(jiang)(jiang)(jiang)一(yi)(yi)個等級(ji),達到(dao)基(ji)本無(wu)刺(ci)激的(de)(de)(de)(de)水平(ping)。25%烷(wan)基(ji)多(duo)(duo)苷(gan)(gan)與(yu)(yu)75%AES復(fu)(fu)(fu)(fu)配(pei)(pei)(pei)(pei),可(ke)(ke)使AES的(de)(de)(de)(de)刺(ci)激性(xing)降(jiang)(jiang)(jiang)低(di)70%以上。當然復(fu)(fu)(fu)(fu)配(pei)(pei)(pei)(pei)體(ti)系(xi)也有局限(xian)性(xing),特別是對目前流(liu)行的(de)(de)(de)(de)濃縮(suo)型(xing)(xing)配(pei)(pei)(pei)(pei)方(fang),其中使用(yong)大量的(de)(de)(de)(de)表(biao)(biao)面(mian)(mian)(mian)(mian)活(huo)性(xing)劑(ji)(ji)(ji),此時靠復(fu)(fu)(fu)(fu)配(pei)(pei)(pei)(pei)不(bu)可(ke)(ke)能從(cong)根本上解(jie)決溫(wen)(wen)和(he)性(xing)問(wen)(wen)題,只有使用(yong)性(xing)能溫(wen)(wen)和(he)的(de)(de)(de)(de)主(zhu)表(biao)(biao)面(mian)(mian)(mian)(mian)活(huo)性(xing)劑(ji)(ji)(ji)才能從(cong)根本上解(jie)決問(wen)(wen)題。因此,開發新型(xing)(xing)溫(wen)(wen)和(he)性(xing)表(biao)(biao)面(mian)(mian)(mian)(mian)活(huo)性(xing)劑(ji)(ji)(ji)和(he)利用(yong)已(yi)有表(biao)(biao)面(mian)(mian)(mian)(mian)活(huo)性(xing)劑(ji)(ji)(ji)復(fu)(fu)(fu)(fu)配(pei)(pei)(pei)(pei)是提(ti)高產(chan)品溫(wen)(wen)和(he)性(xing)的(de)(de)(de)(de)兩個方(fang)面(mian)(mian)(mian)(mian),相輔相成(cheng),缺一(yi)(yi)不(bu)可(ke)(ke)。
表面活性劑的選取原則
3.1
藥物
(1)配伍變化和禁忌
選擇藥物中使用的表(biao)面(mian)活(huo)(huo)性(xing)(xing)劑首(shou)先必須掌握表(biao)面(mian)活(huo)(huo)性(xing)(xing)劑與藥物的配伍變化和禁忌(ji)知(zhi)識(shi),所選表(biao)面(mian)活(huo)(huo)性(xing)(xing)劑只能(neng)對(dui)藥物起增效(xiao)作用或(huo)與之不(bu)(bu)發生相互作用,不(bu)(bu)得(de)使藥物減效(xiao)或(huo)失效(xiao),即(ji)不(bu)(bu)得(de)影響藥劑的穩定(ding)(ding)性(xing)(xing),如晶型改(gai)變、分散穩定(ding)(ding)性(xing)(xing)、水解、氧(yang)化穩定(ding)(ding)性(xing)(xing)等。
(2)口服藥物
口服(fu)藥物(wu)(wu)如丸、片、乳液(ye)制劑等(deng)中使用(yong)的(de)(de)表面(mian)活性(xing)劑首(shou)先(xian)得滿足食品乳化劑的(de)(de)ADI指(zhi)標(biao),并從動物(wu)(wu)經口急性(xing)毒性(xing)小的(de)(de)陰離子(zi)(zi)或非離子(zi)(zi)品種中挑(tiao)選(參(can)見(jian)表1),常(chang)常(chang)選用(yong)蔗(zhe)糖(tang)酯和吐(tu)溫(wen)類(lei)產品。此外還得綜合考慮對人體胃腸(chang)的(de)(de)刺激作用(yong)、代謝作用(yong)等(deng)因(yin)素。
(3)注射(she)類藥物(wu)
注射類(lei)針(zhen)劑(ji)特別(bie)是靜脈注射針(zhen)劑(ji)中(zhong)使用(yong)的(de)表(biao)面活性(xing)劑(ji)須注意溶血(xue)性(xing)次序,優先選(xuan)擇溶血(xue)作用(yong)小(xiao)的(de)非離子型表(biao)面活性(xing)劑(ji)如Tween類(lei)產品或氫化(hua)蓖(bi)麻(ma)油(you)酸(suan)PEG酯等,同時考(kao)慮(lv)致(zhi)變性(xing)因素。
(4)外用(yong)藥物
外用軟膏、藥水(shui)、栓劑(ji)、膜劑(ji)、氣霧劑(ji)中使(shi)用的表面活性劑(ji)主要(yao)對皮膚和粘膜刺激(ji)性和致敏性要(yao)求高,盡量采用無刺激(ji)作用或(huo)有輕(qing)刺激(ji)作用的品(pin)種如磺基琥珀酸酯或(huo)APG等(deng)。使(shi)用SDS、SEO等(deng)也(ye)時(shi)有報道,但(dan)一般均需經(jing)臨床試驗證(zheng)明無明顯(xian)刺激(ji)性和致敏性方(fang)可采用。
(5)主要功(gong)能
在保證(zheng)滿(man)足配伍變化和(he)禁忌要(yao)(yao)求,并無安全性(xing)和(he)溫和(he)性(xing)之虞的前提(ti)下,應(ying)盡量選擇合適(shi)的表面活性(xing)劑(ji)結構類(lei)型及鏈長(chang),以滿(man)足增(zeng)溶、分散(san)、乳(ru)化、潤(run)濕等不同應(ying)用要(yao)(yao)求,使表面活性(xing)劑(ji)發揮最(zui)佳主要(yao)(yao)功能(neng)作用。
3.2
餐具洗滌劑






