Secondary-stage drug release vaginal administration preparation and preparation method thereof

A technology for vaginal administration and preparation, applied in the field of medicine, can solve the problems of limited administration time, increased production and drug costs for patients, and inability to exercise, etc., to achieve easy carrying storage and administration, increase storage validity period, and inhibit growth and reproduction Effect

Inactive Publication Date: 2019-02-01
江苏中天药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Vaginal effervescent tablets have the advantages of convenient administration and quick onset of local administration, but there are mainly the following disadvantages: (1) The administration cycle is short, the administration is frequent, and the drug adhesion is not good, so it can only be used before going to bed. Drug excipients are easy to flow out during drug administration, which affects the full play of the drug effect; (2) For some drugs with short half-lives, the frequency of drug administration will be increased, making it inconvenient to use
[0005] Although oily matrix vaginal suppository is convenient to carry and administer, it has the following disadvantages: (1) the storage conditions are harsh, and when the temperature is high, the suppository is easily softened and deformed, which affects the patient's administration and compliance; (2) oily matrix After melting, it is easy to drip from the vaginal opening, contaminating clothes
Water-soluble base vaginal suppositories are easy to carry and administer, but water-soluble bases are easy to absorb moisture, and require high environmental humidity control and water-proof performance of packaging materials during the production process, which increases product

Method used

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  • Secondary-stage drug release vaginal administration preparation and preparation method thereof
  • Secondary-stage drug release vaginal administration preparation and preparation method thereof
  • Secondary-stage drug release vaginal administration preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0035] (1) Preparation process of acid source particles and alkali source particles:

[0036] Preparation of acid source granules / alkali source granules (wet method / fluidized bed granulation): respectively take the prescribed amount of API, filler, acid source / alkali source and disintegrant, pass through a 40-60 mesh sieve 3 times, crush and remove Polymerize the agglomerated particles; then formulate the binder into a solution with a mass fraction of 5-10%, and perform fluidized bed granulation or wet granulation; the prepared particles enter the 0.4-1.2mm aperture screen instrument and equipment for consolidation During the granulation process, the water content and particle size are detected, and the final particle size is controlled to 100-500μm.

[0037] Preparation of acid source granules / alkali source granules (dry granulation): respectively take the prescribed amount of API, filler, acid source / alkali source, disintegrant, and glidant, pass through a 40-60 mesh sieve 3 time...

Example Embodiment

[0044] Example 1

[0045] The preparation process of a secondary drug release vaginal administration preparation is as follows:

[0046] Prescription 1:

[0047] Table 2 Each component in prescription 1 and its mass ratio

[0048]

[0049]

[0050] (1) Preparation of acid granules: weigh 100 g of tinidazole, 200 g of microcrystalline cellulose, 100 g of citric acid, and 20 g of sodium carboxymethyl cellulose, mix them through a 40-mesh manual sieve 3 times, and add them to the bottom of the fluidized bed; Weigh 20 g of hypromellose and add 380 mL of water to prepare a binder solution with a mass fraction of 5%. Set and adjust the fluidized bed parameters during the preparation process. The inlet air temperature is 55-60℃, and the air volume is 40-50m. 3 / h, atomization pressure 0.6-1bar, feed peristaltic pump speed 4rpm, the prepared particle size is controlled at 100-500μm, moisture control <4%, get acidic particles for use.

[0051] (2) Preparation of alkaline granules: Weigh 100g ti...

Example Embodiment

[0056] Example 2

[0057] On the basis of the prescription and process preparation in the implementation case 1, different types and dosages were screened for prescriptions, and follow-up investigations were made to see if they had an effect on adhesion performance, water absorption swelling coefficient and drug dissolution. In Example 2, high-viscosity hypromellose (M100cps) and polycarbophil were selected as the adhesive agent, and the adhesive content was selected as 5%, 10%, and 15%.

[0058] The prescription is as follows:

[0059] Table 3 Each component and its mass ratio in prescription 2-4

[0060]

[0061] The preparation process is the same as in Example 1.

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Abstract

The invention discloses a secondary-stage drug release vaginal administration preparation comprising the following components: an active ingredient immediate release granule and an active ingredient sustained release granule, wherein the active ingredient immediate release granule comprises an acid source granule and an alkali source granule, and the active ingredient sustained release granule includes a wetting agent and an adhesive. The secondary-stage drug release vaginal administration preparation mainly consists of a sustained-release part and an immediate-release part, and the immediate-release part rapidly releases part of a medicine by the principle of effervescence, and can quickly act on a local lesion of vaginal inflammation, and the slow-release part allows a slow-release skeleton to absorb water to swell to form a gel by the effects of the wetting agent, then adsorbed on the mucosa of the inner wall of the vagina to slowly release the medicine so as to achieve the functionof releasing the medicine for a long time, reducing the number of times of administration, and increasing patient compliance.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a novel controlled-release secondary drug-release preparation for vaginal administration and a preparation method thereof. Background technique [0002] Vaginitis is a common gynecological disease, manifested as vulvar and vaginal itching, burning pain, irritation and abnormal discharge. Usually the reason is that changes in the local environment of the vagina (such as acid-base balance disruption) lead to the destruction of the vagina's natural defenses, allowing certain microorganisms and pathogens to invade, and then trigger vaginal inflammation. Clinically common vaginal inflammations include: bacterial vaginosis (22% to 50%), candidal vaginitis (17% to 39%), trichomonas vaginitis (4% to 35%), senile vaginitis , Young female vaginitis. [0003] Conventional administration methods for treating vaginal inflammation include local vaginal administration in addition to oral administratio...

Claims

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Application Information

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IPC IPC(8): A61K9/26A61K47/38A61K47/12A61K47/02A61K31/4164A61P15/02A61P33/02
CPCA61K9/1611A61K9/1617A61K9/1652A61K9/2077A61K31/4164A61P15/02A61P33/02
Inventor 管运才汤晓雷
Owner 江苏中天药业有限公司
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