Emergency contraceptive
A technology for emergency contraception and pulmonary drug delivery, which is used in drug combination, drug delivery, and pharmaceutical formulations to achieve good compliance.
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Examples
Embodiment 1
[0056] Liposomes:
[0057] Numbering raw material composition 1 Levonorgestrel and / or ethyl estradiol 1:1 or 1 2 Drugs: HSPC: DSPG: Cholesterol 1:12:1:1 (molar ratio) 3 α-tocopherol Equivalent to 1% of lecithin 4 Chloroform:Methanol (as solvent) 1:2 5 Double distilled water (as a hydration medium) 1ml / 20 mg solid content
[0058] Liposome preparation process:
[0059] Thin film hydration method:
[0060] (a) Lecithin, cholesterol, α-tocopherol (equivalent to 1% by weight of lecithin) and levonorgestrel and / or ethyl estradiol were dissolved in chloroform:formaldehyde in a round bottom flask {1 :2} in the mixture;
[0061] (b) Dry the solution from step (a) by rotating the round bottom flask at 120 rpm under vacuum at 30 °C, followed by drying under a nitrogen blanket for 20 min until a smooth, uniform and dry film is formed;
[0062] (c) hydrating the film formed in step (b) by double-distilled water at the glass trans...
Embodiment 2
[0073] Solution:
[0074] Numbering raw material composition 1 Levonorgestrel and / or ethyl estradiol 0.5-1% 2 Propylene Glycol 5-10% 3 polyethylene glycol 400 10-15% 4 ethanol up to 5% 5 Akola up to 1% 6 Chitosan acetate 0.5%-1% 7 double distilled water until 100%
[0075] making process:
[0076] (a) Disperse accurately weighed chitosan powder in 0.01% acetic acid;
[0077] (b) using a magnetic stirrer to stir the dispersion in step (a) until a clear solution is obtained;
[0078] (c) freezing the solution of step (b) overnight to remove entrapped air;
[0079] (d) adjust the final concentration of chitosan to 1% mass volume ratio;
[0080] (e) Accurately weigh and disperse levonorgestrel and / or ethyl estradiol in double distilled water, or alternatively use the levonorgestrel and / or ethyl estradiol lipid of Example 1 plastid;
[0081] (f) sonicating the solution of step (e) for 1 hour to obtain partic...
Embodiment 3
[0088] powder:
[0089] Numbering raw material composition 1 Microemulsified drug / drug encapsulated in liposome (Example 1) 0.5-1% 2 HPMC 1% 3 Grind lactose 400 or medicinal lactose 325 until 100%
[0090] making process:
[0091] (a) centrifugation of the optimal batch of liposomes prepared according to Example 1 to form microparticles;
[0092] (b) hydrating the microparticles of step (a) with a desired amount of sucrose-containing hydration medium to obtain different lipid:sucrose mass ratios to form a suspension;
[0093] (c) The suspension from step (b) was frozen overnight at -40°C and dried under negative substitution pressure for 24 hours to obtain porous masses;
[0094] (d) mixing ground lactose 400 (lactose) or medicinal lactose 325 (trehalose) and HPMC with the porous block of step (c) to form a powder;
[0095] (e) sieve the powder of step (d) through #200 and #240 sieves;
[0096](f) Capsules (type '2') of the individua...
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