Release delayed solid oral prophylactic or pregnancy stopping pill and its use

A technology for terminating pregnancy and contraceptives, which is applied in drug delivery, drug combination, and pharmaceutical formulations, and can solve problems such as inaccurate drug dosage, adverse reactions, and effects of drug treatment

Inactive Publication Date: 2004-06-02
REGENEX PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] 2) Due to various reasons, the patient did not take the same dose of the drug according to the instructions or the doctor's advice, resulting in the actual dose of the drug being lower than the required dose, which may affect the final therapeutic effect of the drug
[0014] It can be

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Fully mix 0.75g or 1.50g levonorgestrel with 80g lactose, 5g polyvinylpyrrolidone, 10g sodium carboxymethylcellulose, 20g starch, and 50g microcrystalline cellulose and other powdery excipients, and granulate with water , dry the whole grain and press it into 1000 round tablets with a diameter of 8mm, and the content of levonorgestrel in each tablet is 0.75mg or 1.50mg. At the same time, use 88% ethanol as a solvent, prepare the special coating material containing cellulose acetate phthalate into a suspension of 10-15% solids, mix well, and coat the tablet with multiple layers . The prepared coated tablet was stirred in 750 ml of 0.1N hydrochloric acid (pH 1) for 2 hours without any disintegration or dissolution of not more than 10%. In 0.2N sodium phosphate solution (adjust the pH value to 6.8 with 1N HCl / NaOH; add 5g of sodium lauryl sulfate), the prepared coated tablet is stirred with it, and disintegration occurs in about 10 minutes , After 1 hour, take a sample a...

Embodiment 2

[0030] Use the prepared acrylic resin solution to spray a layer of the resin on the No. 3 capsule; or directly purchase the enteric-coated No. 3 capsule that has been approved by the state. Fully mix 10g of mifepristone with 70g of lactose, 10g of polyvinylpyrrolidone, 8g of sodium carboxymethyl cellulose, and 2g of magnesium stearate and other powdery excipients, granulate with water, dry the whole granules, and then fill them. In 1000 above-mentioned coated No. 3 capsules, the content of mifepristone in each capsule is 10 mg. The prepared coated capsules were stirred in 750 ml of 0.1N hydrochloric acid (pH 1) for 2 hours without any rupture or deformation. In a 0.2N sodium phosphate solution with a pH of 6.8, the prepared coated capsules were stirred and ruptured in about 15 minutes, and the contents of the drug capsules were thoroughly released in about 30 minutes, and the dissolution rate was measured by sampling after 1 hour. Or equal to 78%.

Embodiment 3

[0032] Dissolve 70 g of carboxymethylcellulose in boiling water, cool to room temperature, add 25 g of mifepristone to make a suspension aqueous solution, then slowly add aluminum sulfate aqueous solution and stir at a constant speed until a saturated coacervate is formed, filter and wash with water The soluble matter was removed, and then dried to form microspherical particles with an average particle diameter of 0.4mm. After the microspheres were coated with cellulose acetate phthalate, they were poured into 1000 No. 3 ordinary capsules. The content of mifepristone in each capsule was 25 mg, and the amount of mifepristone in every gram of microsphere particles The content is 250mg. The prepared capsule was stirred in 750ml of 0.1N hydrochloric acid (pH is 1) when the capsule dissolved and released the microsphere particles for 15 minutes, and continued to stir until 2 hours, all the particles were completely released from the capsule, but the microsphere particles No ruptur...

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Abstract

The present invention relates to the preparation form of contraceptive, and is especially one delayed dissolving orally taken solid preparation form of contraceptive or pregnancy terminating medicine. The present invention also relates to the application of the preparation form. The preparation form has one or several layers of coating or is delayed dissolving capsule, and will dissolve for absorption in neutral medium inside intestinal tract, rather than acid medium. The present invention aims at preventing inaccurate medicine dosage caused by vomiting after taking the contraceptive or pregnancy terminating medicine.

Description

technical field [0001] The invention relates to a dosage form of a contraceptive, especially a dosage form for delaying the dissolution of a solid oral contraceptive or a drug for terminating pregnancy; the invention also relates to an application of the dosage form for delaying the dissolution of a solid oral contraceptive or a drug for terminating pregnancy. Background technique [0002] There are two main types of contraceptives (excluding external contraceptives) widely used for women at present. One is derivatives of estrogen or its active or partially active mimics, such as ethinyl estradiol, ethinyl estradiol, estradiol, omexifen, etc.; the other is progesterone or its derivatives or their active or active Some active mimics, such as norethindrone, levonorgestrel, megestrol acetate, medroxyprogesterone acetate, desogestrel (Desogestrel), gestodene (Gestodene), mifepristone, 3-Keto-desogestrel, Norgestimate, Dienogest, Nomegestrol, Drospirenone Trimegestrone, etc. I...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/34A61K9/36A61K9/56A61P15/18
Inventor 卢智俊
Owner REGENEX PHARMA LTD
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