Pharmaceutical composition for application to mucosa
a technology of pharmaceutical composition and mucosa, which is applied in the direction of inorganic non-active ingredients, immunological disorders, metabolism disorders, etc., can solve the problems of inability to transport an adequate amount of drugs into the blood, inability to retain adequate amounts of drugs at the tissue, and inability to achieve the method of using an absorption enhancer. , to achieve the effect of enhancing drug absorption through the mucosa, high permeability to the blood, and marked efficiency
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example 1
[0038] Fluorescein composition Nos. 1 to 10 for application to the mucosa comprising the components described in the following Table 1 were prepared. For each pharmaceutical preparation, osmotic pressure was measured using the Micro-Osmometer Model 3MO from Advance Instruments, Inc. The result is shown in Table 1.
[0039] One hundred μl each of the compositions 1 to 10 for application to the nasal mucosa was sprayed to the unilateral nasal cavity of rabbits (Japanese White, male, weighing 3 kg) using a commercially available suspension device. At 5, 10, 15, 30, 60, and 120 minutes after the administration, 0.5 ml of the blood was taken from the ear vein and the plasma level of fluorescein was determined by HPLC. From the time-concentration curve till 120 minutes after the spraying, AUC0-120min was determined and bioavailability (B.A.) for the intravenous injection was calculated. The mean values of three rabbits are shown in Table 1.
TABLE 1OsmoticCompositionpressureB.A.No.Compositi...
example 2
[0041] 5-Carboxy fluorescein composition Nos. 17 to 18 for application to the mucosa comprising the components described in the following Table 3 were prepared. For each pharmaceutical preparation, osmotic pressure was measured using the Micro-Osmometer Model 3MO from Advance Instruments, Inc. The result is shown in Table 3. Bioavailability (B.A.) of the compositions 17 to 18 determined by the method described in Working example 1 is also shown in Table 3.
TABLE 3OsmoticCompositionpressureB.A.No.Composition(mOsm)(%)175-carboxy fluorescein: 0.1% w / w652Crystalline cellulose carmellosesodium: 1.7% w / wPolysorbate 80: 0.1% w / wBenzalkonium chloride: 0.03% w / w185-carboxy fluorescein: 0.1% w / w3047Crystalline cellulose carmellosesodium: 1.7% w / wPolysorbate 80: 0.1% w / wBenzalkonium chloride: 0.03% w / wGlucose: 0.4% w / w
example 3
[0043] Salmon calcitonin composition Nos. 23 to 24 for application to the mucosa comprising the components described in the following Table 5 were prepared. For each pharmaceutical preparation, osmotic pressure was measured using the Micro-Osmometer Model 3MO from Advance Instruments, Inc. The result is shown in Table 5. Bioavailability (B.A.) of the compositions 23 to 24 determined by the method described in working example 1 is also shown in Table 5.
TABLE 5OsmoticCompositionpressureB.A.No.Composition(mOsm)(%)23Salmon calcitonin: 0.008% w / w1052Crystalline cellulose carmellosesodium: 1.7% w / wPolysorbate 80: 0.1% w / wBenzalkonium chloride: 0.03% w / w24Salmon calcitonin: 0.008% w / w3047Crystalline cellulose carmellosesodium: 1.7% w / wPolysorbate 80: 0.1% w / wBenzalkonium chloride: 0.03% w / wGlucose: 0.4% w / w
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