Valsartan and hydrochlorothiazide compound preparation and preparation process thereof

A preparation technology of hydrochlorothiazide, which is applied in the field of pharmaceutical preparations, can solve the problems of low bioavailability, increased degradation products, and low dissolution rate in vitro, and achieve the effects of improving dissolution rate and solubility, improving stability, and good miscibility

Active Publication Date: 2021-06-29
上海耀大生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, since both valsartan and hydrochlorothiazide are insoluble in water, they have the disadvantages of slow dissolution rate, low dissolution rate in vitro, and low bioavailability, which have a great impact on the absorption of drugs
In addition, valsartan is sensitive to water, absorbs moisture, increases moisture, increases degradation products, and has poor chemical stability. Valsartan hydrochlorothiazide tablets have very important practical significance

Method used

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  • Valsartan and hydrochlorothiazide compound preparation and preparation process thereof
  • Valsartan and hydrochlorothiazide compound preparation and preparation process thereof
  • Valsartan and hydrochlorothiazide compound preparation and preparation process thereof

Examples

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Embodiment 1

[0069] This embodiment provides a preparation process for a valsartan-hydrochlorothiazide compound preparation, comprising the following steps:

[0070] (1) Raw material pretreatment: the main drug valsartan and hydrochlorothiazide are respectively carried out to micronized pretreatment by jet mill;

[0071] (2) Excipient pretreatment: Povidone K30, poloxamer, sulfobutyl ether-β-cyclodextrin, low-substituted hypromellose, sodium lauryl sulfate, microcrystalline cellulose PH102 , crospovidone XL, magnesium stearate and colloidal silicon dioxide are passed through a 40-mesh sieve, and set aside;

[0072] (3) Preparation of dispersion: mix 35 parts of povidone K30, 62 parts of polyethylene glycol, 35 parts of mannitol, 4 parts of poloxamer, 5 parts of citric acid and 83 parts of valsartan and place under high pressure In the reactor, the temperature of the system in the autoclave was raised to 40°C; the supercritical CO 2 Send in the autoclave, control the pressure in the kettl...

Embodiment 2

[0088] This embodiment provides a preparation process for a valsartan-hydrochlorothiazide compound preparation, comprising the following steps:

[0089] (1) Raw material pretreatment: the main drug valsartan and hydrochlorothiazide are respectively carried out to micronized pretreatment by jet mill;

[0090] (2) Excipient pretreatment: Povidone K30, poloxamer, sulfobutyl ether-β-cyclodextrin, low-substituted hypromellose, sodium lauryl sulfate, microcrystalline cellulose PH102 , crospovidone XL, magnesium stearate and colloidal silicon dioxide are passed through a 40-mesh sieve, and set aside;

[0091] (3) Preparation of dispersion: mix 38 parts of povidone K30, 66 parts of polyethylene glycol, 45 parts of mannitol, 8 parts of poloxamer, 6 parts of citric acid and 90 parts of valsartan and place under high pressure In the reactor, the temperature of the system in the autoclave was raised to 40°C; the supercritical CO 2 Send in the autoclave, control the pressure in the kettl...

Embodiment 3

[0107] This embodiment provides a preparation process for a valsartan-hydrochlorothiazide compound preparation, comprising the following steps:

[0108] (1) Raw material pretreatment: the main drug valsartan and hydrochlorothiazide are respectively carried out to micronized pretreatment by jet mill;

[0109] (2) Excipient pretreatment: Povidone K30, poloxamer, sulfobutyl ether-β-cyclodextrin, low-substituted hypromellose, sodium lauryl sulfate, microcrystalline cellulose PH102 , crospovidone XL, magnesium stearate and colloidal silicon dioxide are passed through a 40-mesh sieve, and set aside;

[0110] (3) Preparation of dispersion: mix 40 parts of povidone K30, 65 parts of polyethylene glycol, 42 parts of mannitol, 6 parts of poloxamer, 6 parts of citric acid and 88 parts of valsartan and place under high pressure In the reactor, the temperature of the system in the autoclave was raised to 40°C; the supercritical CO 2 Send in the autoclave, control the pressure in the kettl...

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Abstract

The invention discloses a valsartan and hydrochlorothiazide compound preparation and a preparation process thereof. The preparation process comprises the following steps: pretreating raw materials; pretreating auxiliary materials; preparing dispersion: dispersing valsartan on the surface of the carrier by adopting a supercritical fluid impregnation technology; preparing inclusion compound: carrying out inclusion on hydrochlorothiazide by adopting sulfobutyl ether-beta-cyclodextrin; preparing pre-coated particles: conducting top spraying granulation on the hydrochlorothiazide inclusion compound through a composite adhesive; premixing: mixing the valsartan solid dispersion, the auxiliary materials and the hydrochlorothiazide pre-coated particles; distributing materials: dividing the premixed powder into two parts; respectively carrying out dry granulation on the two parts of premixed powder; mixing totally; tabletting; and coating to obtain the product. The compound preparation with good bioavailability and drug stability is prepared by combining a supercritical impregnation technology, a secondary inclusion technology and a different oil pressure powder granulation technology, the production cost is low, and the process is simple and easy to implement.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a valsartan-hydrochlorothiazide compound preparation and a preparation process thereof. Background technique [0002] Valsartan-hydrochlorothiazide compound preparation is a safe and orally effective antihypertensive drug widely used in clinic. Valsartan is an orally effective and specific angiotensin II (AT1) receptor antagonist that selectively acts on AT1 receptor subtypes, blocking the binding of Ang II to AT1 receptors (its specificity The effect of antagonizing the AT1 receptor is about 20,000 times greater than that of the AT2 receptor), thereby inhibiting vasoconstriction and the release of aldosterone, resulting in a hypotensive effect. Hydrochlorothiazide is a thiazide diuretic that directly increases the secretion of sodium ions and chloride ions by affecting the reabsorption of electrolytes by the renal tubules, resulting in increased urine output and decre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/549A61K9/30A61J3/06A61P9/12A61K31/41
CPCA61K31/41A61K31/549A61K47/6951A61P9/12A61K9/2081A61K9/282A61K9/2095A61J3/06Y02P20/54
Inventor 顾珽李小清蒋雅红李玉柱张健王兰杰白国燕周双凤郁波韩国玉范颖颖
Owner 上海耀大生物科技有限公司
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