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Composite disintegrant system for oral solid preparation and oral solid preparation containing composite disintegrant system

A compound disintegrant and solid preparation technology, which is applied in the direction of medical preparations containing active ingredients, medical preparations with non-active ingredients, pill delivery, etc., and can solve problems such as viscous active substances

Active Publication Date: 2018-01-19
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 a composite disintegrant system for oral solid preparations, which can rapidly disintegrate oral solid preparations and increase their dissolution rate, thereby improving bioavailability, and can especially solve the problem of strong hygroscopicity and disintegration after moisture absorption. Viscous active substances (active ingredients) that cannot be effectively disintegrated by conventional disintegrants

Method used

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  • Composite disintegrant system for oral solid preparation and oral solid preparation containing composite disintegrant system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Embodiment 1: Preparation of QR01019K

[0082] 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.

[0083] Melting point: 135-145°C.

[0084] MS / HRMS m / z: 717[M+H] + ;677[M-K] - .

[0085] 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).

[0086] H-NMR spectrum and X-ray powder diffraction spectrum are shown in figure 1 and figure 2 .

Embodiment 2

[0087] Example 2: Antihypertensive efficacy test of QR01019K on spontaneously hypertensive rats

[0088] 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

[0100] Embodiment 3: preparation and disintegration experiment of oral solid preparation

[0101] Tablets of Preparation Examples 1-11 and Comparative Examples 1-11 were respectively prepared according to the following three preparation methods, and the differences in prescription composition, tablet hardness and tablet weight of each preparation example and Comparative Examples are shown in Table 3 below.

[0102] Preparation examples 1, 7, 8 and 9, comparative examples 1, 7, 8 and 9 adopt the powder compression method: select 60 mesh sieves according to the material properties, and the material is sieved for subsequent use (in preparation example 7 and comparative example 7, active The ingredients and excipients are sieved together, and the disintegrating agent and the disintegrating agent are mixed and sieved for subsequent use; the remaining preparation examples and comparative examples are sieved separately); the active ingredients, excipients, disintegrants, There is no ...

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Abstract

The invention discloses a composite disintegrant system for an oral solid preparation. By using the system, the oral solid preparation can fast realize disintegration; and the dissolution speed can beaccelerated, so that the bioavailability is improved. Particularly, the problem that active substances (active ingredients) which have high moisture absorption performance and can become sticky afterthe moisture absorption cannot realize effective disintegration by using a conventional disintegrant can be solved. The composite disintegrant system provided by the invention contains a disintegrantand a disintegration aid. The invention further relates to an oral solid preparation containing the composite disintegrant system.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a composite disintegrant system for oral solid preparations and an oral solid preparation containing the composite disintegrant system. 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 rapi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/38A61K47/36A61K47/32A61K47/02A61K47/26A61K31/4245A61K31/497A61P9/12A61P9/04A61P3/10A61P13/12
CPCA61K31/4245A61K31/497A61P13/12A61P3/10A61K9/2018A61K9/2009A61K9/2027A61K9/2054A61K9/0007A61K9/205A61P9/12A61K9/2013A61K9/2059A61K9/2072A61K9/20
Inventor 万耀文陈永凯曾弦王朝东冯伟
Owner WUHAN LL SCI & TECH DEV
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