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Oral solid preparation for treating hypertension and related diseases

A technology for solid preparations and high blood pressure, which is applied in cardiovascular system diseases, metabolic diseases, urinary system diseases, etc., and can solve problems such as viscous active substances, difficult preparations, and poor fluidity of prescriptions.

Active Publication Date: 2019-02-12
WUHAN LL SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The invention provides an oral solid preparation for the treatment of hypertension and related diseases, which has better disintegration performance and dissolution rate, thereby improving bioavailability, and can especially solve the problem of strong hygroscopicity and becoming sticky after moisture absorption Problems existing in the active substance (active ingredient) cannot be effectively disintegrated by using conventional prescriptions and processes, and the poor fluidity of the prescription leads to difficulties in preparation, etc.

Method used

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  • Oral solid preparation for treating hypertension and related diseases
  • Oral solid preparation for treating hypertension and related diseases
  • Oral solid preparation for treating hypertension and related diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Embodiment 1: Preparation of QR01019K

[0084] Dissolve QR01019 (1.0g) in dichloromethane (5ml), stir at room temperature to form a solution, add potassium phthalimide (0.27g) to the solution, keep it warm for 4 hours, cool to -50°C, filter, The solid obtained by spin-drying the solvent is amorphous QR01019K.

[0085] Melting point: 135-145°C.

[0086] MS / HRMS m / z: 717[M+H] + ;677[M-K] - .

[0087] 1 H-NMR (400MHz, DMSO-d 6 )δ: 1.44(t, 3H), 1.46(t, 3H), 2.38(s, 3H), 2.41(s, 3H), 2.44(s, 3H), 4.64(q, 2H), 5.29(d, 1H ), 5.32(d, 1H), 5.52(d, 1H), 5.56(d, 1H), 6.86(q, 1H), 6.90(d, 2H), 7.18(m, 2H), 7.22(d, 2H) , 7.33 (m, 1H), 7.36 (m, 1H), 7.46 (d, 1H), 7.52 (dd, 1H), 7.75 (d, 1H).

[0088] H-NMR spectrum and X-ray powder diffraction spectrum are shown in figure 1 with figure 2 .

Embodiment 2

[0089] Example 2: Antihypertensive efficacy test of QR01019K on spontaneously hypertensive rats

[0090] Spontaneously hypertensive rats aged 12 weeks (hereinafter referred to as SHR, purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.) were anesthetized by intraperitoneal injection of 2.5% sodium pentobarbital. The blood pressure sensing catheter was inserted into the abdominal aorta, the implant was fixed on the abdominal wall, and the postoperative daily care was performed after suturing. Animals whose systolic blood pressure exceeded 160mm Hg were selected into groups, with 8 animals in each group, 3 groups in total. The control group was given 0.5% sodium carboxymethylcellulose (hereinafter referred to as CMC-Na); the OR01019 group and the QR01019K group were dissolved in 0.5% CMC-Na, and the dosage was based on the effective dose of 1 mg / kg azilsartan. The drug volume is 4mL / kg, all administered by intragastric administration, with the systolic...

Embodiment 3

[0102] Embodiment 3: Preparation of oral solid preparation

[0103] Prepare the tablet of Preparation Example 1-8 according to the following preparation process, and the prescription is shown in Table 3 below.

[0104] Preparation:

[0105] (1) Preparation of adhesive: Dissolve the adhesive with pure water to obtain the corresponding aqueous solution for later use; take the pH regulator, add purified water above 80°C to dissolve completely, and cool to room temperature to obtain monosodium fumarate aqueous solution ; Mix the binder aqueous solution with the monosodium fumarate solution, and stir evenly to obtain the binder mixed solution.

[0106] (2) Granulation: take the active ingredient and excipients and mix them through a 40-mesh sieve, then pour them into a fluidized bed granulator, spray the prepared binder mixed solution, granulate the mixture, and Dry in a bed granulator, and pass the obtained granules through a 30-mesh sieve for granulation.

[0107] (3) Tablet c...

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Abstract

The invention provides an oral solid preparation for treating hypertension and related diseases. The preparation is prepared from an active ingredient, a pH regulator, an excipient, a disintegrant, afiller, a lubricant, and an adhesive. The solid preparation has good disintegration performance and dissolution rate, and improves bioavailability, and can especially solve the problems that the active substances (active ingredients) with strong hygroscopicity become sticky after moisture absorption, which are not effectively disintegrated by using conventional prescriptions and processes, and have poor formulation fluidity leading difficulties in preparation. The invention also provides a preparation method and application of the oral solid preparation.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an oral solid preparation and its application. Background technique [0002] In general, the absorption rate of oral solid preparations depends on the dissolution (release) speed of the active substance (active ingredient) from the solid preparation, and the dissolution (release) speed of the active ingredient often depends on the disintegration speed of the solid preparation, so basically It can be considered that the disintegration rate of the oral solid dosage form is the determining step for the absorption rate of the active ingredient by the body. Most disintegrants have good water absorption and swelling properties. The role of disintegrants in oral solid preparations is to eliminate or destroy the bonding force caused by adhesives or high compression, so that they can be rapidly broken in the dissolution medium. into fine granular substances, so that the active ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/36A61K47/38A61K47/32A61K47/02A61K47/12A61K31/4245A61K31/497A61P9/00A61P9/12A61P9/04A61P3/10A61P13/12
CPCA61K9/2009A61K9/2013A61K9/2027A61K9/205A61K9/2054A61K9/2059A61K9/2095A61K31/4245A61K31/497
Inventor 程卫胡晓婧胡柳陈永凯冯伟王朝东
Owner WUHAN LL SCI & TECH DEV
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