Application of an oily gel formed by hydrogenated soybean phospholipids as a percutaneous absorption-type ointment base. 1994

T Henmi, and M Fujii, and K Kikuchi, and N Yamanobe, and M Matsumoto
Showa College of Pharmaceutical Sciences, Tokyo, Japan.

We investigated the possibility of developing an oily gel formed by hydrogenated soybean phospholipids (HSL) as a percutaneous absorption-type ointment base. Liquid paraffin (LP) was used as the oil, and indomethacin (IM), ketoprofen (KP), flurbiprofen (FP) and ibuprofen (IP) were used as model drugs. IM did not dissolve in LP, but solubilized when heated with HSL at a concentration of about 1% with 15% HSL at 95 degrees C. IM gel was thus prepared as follows: IM and HSL were mixed, added into LP, capped tightly, heated in a water bath and cooled. The consistency of the gel increased with increasing IM concentration, indicating some kind of interaction between IM and HSL. The release of IM from the IM gel was faster than that from a preparation in which IM was mixed in gel at room temperature (Gel + IM). The release rate of IM from IM gel was proportional to IM concentrations up to 1%, but became constant above that. Permeation of IM through hairless rat abdominal skin from IM gel was higher than that from the Gel + IM. The permeation rate was proportional to IM concentrations in the range of 0.1 to 0.5% in 15% HSL gel. KP and FP also solubilized in gel when subjected to the same procedure as IM, and their release and permeation increased when they were formulated as gels. However, no evident improvement of permeation was observed in the case of IP, which had high LP solubility. It was suggested that HSL showed no enhancing effect, but solubilized IM, KP or FP, leading to high permeation from the gel. After 3 months' storage, the permeation rate did not change for 0.5% IM in 15% HSL gel, but decreased for 1% IM in 15% HSL gel. This indicates that in the case of 1% IM in 15% HSL gel, IM is in a supersaturated state immediately after preparation and then recrystallizes with time.

UI MeSH Term Description Entries
D008297 Male Males
D009823 Ointment Bases Various mixtures of fats, waxes, animal and plant oils and solid and liquid hydrocarbons; vehicles for medicinal substances intended for external application; there are four classes: hydrocarbon base, absorption base, water-removable base and water-soluble base; several are also emollients. Bases, Ointment
D010743 Phospholipids Lipids containing one or more phosphate groups, particularly those derived from either glycerol (phosphoglycerides see GLYCEROPHOSPHOLIPIDS) or sphingosine (SPHINGOLIPIDS). They are polar lipids that are of great importance for the structure and function of cell membranes and are the most abundant of membrane lipids, although not stored in large amounts in the system. Phosphatides,Phospholipid
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000894 Anti-Inflammatory Agents, Non-Steroidal Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects. Analgesics, Anti-Inflammatory,Aspirin-Like Agent,Aspirin-Like Agents,NSAID,Non-Steroidal Anti-Inflammatory Agent,Non-Steroidal Anti-Inflammatory Agents,Nonsteroidal Anti-Inflammatory Agent,Anti Inflammatory Agents, Nonsteroidal,Antiinflammatory Agents, Non Steroidal,Antiinflammatory Agents, Nonsteroidal,NSAIDs,Nonsteroidal Anti-Inflammatory Agents,Agent, Aspirin-Like,Agent, Non-Steroidal Anti-Inflammatory,Agent, Nonsteroidal Anti-Inflammatory,Anti-Inflammatory Agent, Non-Steroidal,Anti-Inflammatory Agent, Nonsteroidal,Anti-Inflammatory Analgesics,Aspirin Like Agent,Aspirin Like Agents,Non Steroidal Anti Inflammatory Agent,Non Steroidal Anti Inflammatory Agents,Nonsteroidal Anti Inflammatory Agent,Nonsteroidal Anti Inflammatory Agents,Nonsteroidal Antiinflammatory Agents
D012869 Skin Absorption Uptake of substances through the SKIN. Absorption, Skin,Intracutaneous Absorption,Intradermal Absorption,Percutaneous Absorption,Transcutaneous Absorption,Transdermal Absorption,Absorption, Intracutaneous,Absorption, Intradermal,Absorption, Percutaneous,Absorption, Transcutaneous,Absorption, Transdermal,Absorptions, Intracutaneous,Absorptions, Intradermal,Absorptions, Percutaneous,Absorptions, Skin,Absorptions, Transcutaneous,Absorptions, Transdermal,Intracutaneous Absorptions,Intradermal Absorptions,Percutaneous Absorptions,Skin Absorptions,Transcutaneous Absorptions,Transdermal Absorptions
D013025 Glycine max An annual legume. The SEEDS of this plant are edible and used to produce a variety of SOY FOODS. Soy Beans,Soybeans,Bean, Soy,Beans, Soy,Soy Bean,Soybean
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D066298 In Vitro Techniques Methods to study reactions or processes taking place in an artificial environment outside the living organism. In Vitro Test,In Vitro Testing,In Vitro Tests,In Vitro as Topic,In Vitro,In Vitro Technique,In Vitro Testings,Technique, In Vitro,Techniques, In Vitro,Test, In Vitro,Testing, In Vitro,Testings, In Vitro,Tests, In Vitro,Vitro Testing, In

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