Oral preparation capable of dosing fertility-controlling drugs by positioning at small intestine and production method thereof

A technology for contraceptives and oral preparations, applied in pharmaceutical formulations, drug combinations, drug delivery, etc., can solve problems such as inaccurate drug dosage, drug overdose, and increase in adverse reactions, and achieve the effect of ensuring the effectiveness of drugs and ensuring effective doses

Inactive Publication Date: 2009-12-09
北京华禧联合科技发展有限公司
View PDF1 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] (1) The supplementary dose is the entire dose in a single dose, and only part of the dose is lost by vomiting, which leads to actual drug overdose and increased adverse reactions
[0020] (2) Some patients did not take the medicine again, and as a result, the dosage of the medicine was insufficient due to vomiting, resulting in the final contraceptive failure
[0022] There is still no better method or special drug for preventing or treating oral contraceptives that cause vomiting. A

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Oral preparation capable of dosing fertility-controlling drugs by positioning at small intestine and production method thereof
  • Oral preparation capable of dosing fertility-controlling drugs by positioning at small intestine and production method thereof
  • Oral preparation capable of dosing fertility-controlling drugs by positioning at small intestine and production method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Drospirenone Ethinylestradiol Enteric-Coated Tablets

[0034]

[0035] Mix the above materials, add water to granulate, dry, granulate, and press into 1000 round tablets with a diameter of 8 mm, each containing 0.03 mg of ethinyl estradiol and 3 mg of drospirenone.

[0036] At the same time, 85% ethanol is used as a solvent, and a 10-15% suspension is prepared with a special coating material containing cellulose acetate phthalate, and after mixing, a layer is coated on the prepared tablet. The coated tablet made was stirred in 750ml of 0.1N hydrochloric acid (PH1) for 2 hours, without any disintegration or dissolution was not more than 10%; in 0.2N sodium phosphate solution (adjusted with 1N HCL / NaOH PH to 6.8; add 5g sodium lauryl sulfate), the prepared coated tablet was stirred therein, and disintegrated completely in about 10 minutes, and the dissolution rates of ethinyl estradiol and drospirenone were respectively greater than 80% by sampling after 1 hour. %.

Embodiment 2

[0038] Mifepristone enteric-coated tablets / capsules

[0039]

[0040] (1) Mix the above materials, add water to granulate, dry, granulate, and press into 1000 tablets, each containing 25 mg of mifepristone.

[0041] At the same time, 80% ethanol is used as a solvent, and a 10-15% suspension is prepared with a special coating material containing cellulose acetate phthalate, and after mixing, a layer is coated on the prepared tablet.

[0042] or

[0043] (2) Mix the above materials, add water to granulate, dry, and pour the whole grain into enteric-coated No. 3 capsules approved by the state. Each capsule contains 25 mg of mifepristone.

[0044] (3) The coated tablet or capsule made above was stirred in 0.1N hydrochloric acid (PH1) of 750ml for 2 hours, without any disintegration or dissolution being no more than 10%; in 0.2N sodium phosphate solution ( Use 1N HCL / NaOH to adjust the pH to 6.8; add 5g sodium lauryl sulfate), and stir the prepared coated tablet or capsule wit...

Embodiment 3

[0046] Compound Levonorgestrel Enteric-Coated Tablets

[0047]

[0048]

[0049] Mix the above materials, add water to granulate, dry, granulate, and press into 1000 round tablets with a diameter of 8 mm, each containing 0.15 mg of ethinyl estradiol and 0.03 mg of levonorgestrel.

[0050]At the same time, 85% ethanol is used as a solvent, and a 10-15% suspension is prepared with a special coating material containing cellulose acetate phthalate, and after mixing, a layer is coated on the prepared tablet. The coated tablet made was stirred in 750ml of 0.1N hydrochloric acid (PH1) for 2 hours without any disintegration or dissolution was not more than 10%; in 0.2N sodium phosphate solution (adjusted with 1N HCL / NaOH PH to 6.8; add 5g sodium lauryl sulfate), and the prepared coated tablet was stirred therein, and disintegrated completely in about 10 minutes, and after 1 hour, the dissolution rates of ethinyl estradiol and levonorgestrel were sampled and measured respectively...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention provides an oral preparation capable of dosing fertility-controlling drugs by positioning at small intestine and a production method thereof. The fertility-controlling drug positioning at small intestine is prepared by wrapping one or plural layers of coatings on solid oral fertility-controlling drug preparation or directly using slow-release capsules so as to enable the preparation not to dissolve in gastric acid but dissolve at the small intestine part where the acidity is nearly neutral, thus causing the drugs to release and to be absorbed in the intestine, successfully avoiding the circumstances of vomiting owing to gastricsolubility of oral fertility-controlling drugs and inaccurate drug dosage whivh results in failure of fertility-controlling.

Description

technical field [0001] The present invention provides a kind of oral preparation capable of small intestine localized administration of contraceptive medicine. The dosage form is coated with one or more layers of coatings on the outer layer of solid oral contraceptive preparation or directly uses delayed-dissolving capsules, so that the dosage form can be dissolved in gastric acid. It does not dissolve, but dissolves in the small intestine where the acidity is close to neutral, so that the drug starts to be released and absorbed in the intestine, and can successfully prevent the vomiting often caused by oral contraceptives due to gastric dissolution, as well as the inaccurate dosage of the drug due to vomiting, Eventual contraceptive failure. The invention also relates to a preparation method of the oral preparation of the contraceptive medicine for small intestine localized administration. Background technique [0002] Oral contraceptives are one of the most widely used me...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/30A61K9/26A61K9/24A61K9/48A61K31/569A61K31/567A61K31/5575A61K31/585A61K47/38A61K47/32A61K47/36A61P15/18
Inventor 王建航谢晓东毕华
Owner 北京华禧联合科技发展有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap