Absorption enhancers suppositories

Lindmark, T., et al. 1997. Mechanism of absorption enhancement in humans after rectal administration of ampicillin in suppositories containing sodium caprate. Pharm Res 14 930. 

An important issue that has been recognized recently concerns the potential adverse effect of absorption enhancers on the rectal mucosa, as shown in rats after a single application [61,62], Safety evaluation of the applicability of absorption enhancers is imperative. In clinical application, medium-chain fatty acids such as sodium caprate are used only for suppositories containing antibiotics [36],... 

Watanabe, Y., et al. 1992. Absorption enhancement of polypeptide drugs by cyclodextrins. I. Enhanced rectal absorption of insulin from hollow-type suppositories containing insulin and cyclodextrins in rabbits. Chem Pharm Bull 40 3042. 

CyDs are known to be able to solubilize lipophilic drugs as well as lipophilic absorption enhancers, leading to the improvement of the enhancer s efficiency. There are some reports on the use of CyDs as a candidate for a coenhancer. For example, Yanagi et al. [35] reported that CyDs may promote the potency of absorption enhancers in rectum of rabbits. Inclusion complex of decanoic acid (CIO), an absorption enhancer, with a-CyD was prepared as an additive of cefmetazole sodium suppository and rectally administered to rabbits. Plasma concentration and area under the curve (AUC) of cefmetazole sodium after rectal administration of a suppository containing ClO-a-CyD complex to rabbits increased more significantly than those with no additive. 

Matsumoto, Y., et al. 1989. Rectal absorption enhancement of gentamicin in rabbits from hollow type suppositories by sodium salicylate or sodium caprylate. Drug Des Deliv 4 247. 

Despite the fact that many such absorption-enhancing agents have been tried in mucosal delivery as well as in nasal delivery, only sodium caprate used in rectal suppositories of antibiotics has gained regulatory approval as an additive with absorption-enhancement activity.f Because most other compounds are not approved for mucosal application in the Pharmaco-peiae in many countries, specialized attention must be paid to putting these additives into practical use. For example, bile salts have been recognized as safe and... 

Lecithins are also used in suppository bases, to reduce the brittleness of suppositories, and have been investigated for their absorption-enhancing properties in an intranasal insulin formulation. Lecithins are also commonly used as a component of enteral and parenteral nutrition formulations. 

Uses Emulsifier, bodying agent, emollient, lubricant, vise, modifier for pharmaceuticals (clinical nutrition, coating, delivery/absorption enhancement, dermatological emulsion, infant formulas, nutritional/sports supplements, suppositories, tablets) emollient, emulsifier, lubricant, vise, modifier for cosmetics (creams/lotions, mascara, foundation, sun care preps.) Properties Lovibond R4.0 max. bead insol. in water sol. in oil elevated temps. m.p. 57-62 C HLB 3-4 acid no. 3.0 iodine no. 5.0 nonionic... 

Chem. Descrip. Polyglyceryl mixed veg. fatty acid esters conforms to hydrogenated veg. oil NF CAS 68334-28-1 EINECS/ELINCS 269-820-6 Uses Food emulsifier, crystal inhibitor in veg. oils lubricant in pharmaceuticals (clinical nutrition, coating, delivety/absorption enhancement, dermatologicals, infant formulas, nutritional/sports supplements, suppositories) lubricant in cosmetics (creams/lotions, sun care preps.) Regulatory FDA 21 CFR 172.854(c)... 

Many studies have been published on the use of various enhancers for the rectal absorption. They increase the absorption of an active substance by enhancing the membrane permeation, rather than increasing the solubility. Published examples of absorption enhancers are capric acid and sodium caprate, lauric acid and sodium laurate, sodium salicylate and sodium cholate. These enhancers however give an unpredictable and strongly variable improvement of the biological availability [5b]. Nevertheless they sometimes lead to a licensed medicine sodium caprate is already in use in a suppository product available in Japan [7]. 

Uses Coemulsifier, penetrant, stabilizer, thickener for pharmaceutical topical emulsions, cosmetics, veterinary preps. excipienL bioavailability enhancer for oral use (hard shell capsule) absorption enhancer for penetration of active drugs through the skin (creams, lotions), rectal and vaginal suppositories Features Hydrophilic amphiphilic... 

Takahashi, H., et al. 1997. The enhancing mechanism of capric acid (CIO) from a suppository on rectal drug absorption through a paracellular pathway. Biol Pharm Bull 20 446. 

Iwaoku, R., et al. 1982. Enhanced absorption of phenobarbital from suppositories containing phenobarbital-(3-cyclodextrin inclusion complex. Chem Pharm Bull 30 1416. 

Arima, H., et al. 1992. Enhanced rectal absorption and reduced local irritation of the antiinflammatory drug ethyl 4-biphenylylacetate in rats by complexation with water-soluble (3-cyclodextrin derivatives and formulation as oleaginous suppository. J Pharm Sci 81 1119. 

Uekama, K., et al. 1995. Modification of rectal absorption of morphine from hollow-type suppositories with a combination of a-cyclodextrin and viscosity-enhancing polysaccharide. 

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