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.

Inactive Publication Date: 2012-09-12
LYKA LABS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The patent does not address the use of nasal administration of synthetic alternatives such as levonorgestrel

Method used

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Examples

Experimental program
Comparison scheme
Effect test

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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PUM

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Abstract

The present invention discloses an emergency contraceptive formulation for nasal and / or pulmonary administration comprising of levonorgestrel optionally in combination with ethylestradiol. The said formulation can be in form of solution, suspension or carrier based systems selected from microemulsion and liposomes.

Description

field of invention [0001] The present invention relates to the field of drug delivery. In particular, the invention relates to nasal and / or pulmonary routes of administration of emergency contraceptives comprising synthetic progesterone or synthetic estrogen or a combination of both. Background of the invention [0002] Birth control, more commonly known as "contraception," is one or more acts, devices, sexual practices, or subsequent drug regimens intended to prevent or reduce the likelihood of pregnancy or childbirth. Birth control includes about three methods, namely, prevention of fertilization of an egg or "contraception"; prevention of implantation of an embryo, or abortifacient and chemical or surgically induced abortion of an embryo or fetus. [0003] The history of birth control begins with the discovery of the relationship between sexual intercourse and pregnancy. Traditionally, the method of interruption or withdrawal or extraction of sexual intercourse to avoi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/127A61K9/14A61K9/19A61K31/565
CPCA61K9/0043A61K9/0073A61K9/0075A61K9/1075A61K9/127A61K9/146A61K9/19A61K31/565A61K47/32A61K47/36A61P15/18
Inventor A·R·米斯拉N·I·刚德海M·R·巴加捷B·B·沙阿R·S·萨满特
Owner LYKA LABS LTD
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