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Controlled release preparation of captopril and its preparation process

A technology of controlled-release preparations and preparations, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, drug delivery, etc., which can solve the problems of long duration and achieve the effect of eliminating missed doses

Inactive Publication Date: 2006-04-19
HANGZHOU MINSHENG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In order to solve the problem of the rapid release of captopril in the body after taking the medicine, patients must get up early in the morning to take the medicine to avoid the "morning peak phenomenon" of hypertensive patients. Captopril controlled-release preparation that can be released after 4 to 5 days after taking, and lasts for a long time, and its preparation method

Method used

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  • Controlled release preparation of captopril and its preparation process
  • Controlled release preparation of captopril and its preparation process
  • Controlled release preparation of captopril and its preparation process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1: the preparation of captopril controlled-release preparation

[0048] Prescription (per 1000 tablets):

[0049] Tablet core: Captopril 25g, starch 2.5g, HPMC K4M 22.5g, PVP K30 1g, magnesium stearate 0.5g, micropowder silica gel 0.25g;

[0050] Coating layer: mannitol 295g, HPMC K4M 85g, PVP K30 14g, magnesium stearate 4g, micropowder silica gel 2g.

[0051] Preparation:

[0052] (1) The tablet core layer is separately granulated, and 8 g of medicinal ethanol is added during the granulation process, and the tablet is compressed (Φ5mm flat flush);

[0053] (2) The coating layer is granulated separately, and 75.4 g of medicinal ethanol is added during the granulation process;

[0054] (3) Press-coated chips (Φ12mm shallow concave punch): firstly fill each die hole with 200mg of coating particles, then place the tablet core in the center of the die hole, add 200mg of coating particles, and press to form a coated chip.

[0055] Determination of in vitro rel...

Embodiment 2

[0058] Prescription (per 1000 tablets):

[0059] Tablet core: Captopril 25g, starch 2.5g, HPMC K100M 22.5g, PVP K30 1g, magnesium stearate 0.5g, SiO 2 0.25g;

[0060] Coating layer: mannitol 285g, HPMC K100M 95g, PVP K30 14g, magnesium stearate 4g, SiO 2 2g. Preparation:

[0061] (1) The core layer of the tablet is granulated separately, and 7.8 g of medicinal ethanol is added during the granulation process, and the tablet is compressed (Φ5mm flat flush);

[0062] (2) The coating layer is granulated separately, and 54 g of medicinal ethanol is added during the granulation process;

[0063] (3) Press-coated chips (Φ12mm shallow concave punch): firstly fill each die hole with 200mg of coating particles, then place the tablet core in the center of the die hole, add 200mg of coating particles, and press to form a coated chip.

[0064] Determination of in vitro release: according to "Chinese Pharmacopoeia" 2000 edition two appendix XD first method adopts the device (basket m...

Embodiment 10

[0068] Embodiment 10: the preparation of captopril controlled-release preparation

[0069] Prescription (per 1000 tablets):

[0070] Tablet core: Captopril 25g, dextrin 14.25g, HPMC K100M 10.75g, PVP K30 1g, stearic acid 0.5g, micropowder silica gel 0.25g;

[0071] Coating layer: dextran 290g, HPMC K100M 90g, PVP K3014g, stearic acid 4g, micropowder silica gel 2g.

[0072] Preparation:

[0073] (1) The tablet core layer is granulated separately, and 4g of pure water is added during the granulation process, and the tablet is pressed (Φ5mm flat flush);

[0074] (2) The coating layer is granulated separately, and 58 g of pure water is added during the granulation process;

[0075] (3) Press-coated chips (Φ12mm shallow concave punch): firstly fill each die hole with 200mg of coating particles, then place the tablet core in the center of the die hole, add 200mg of coating particles, and press to form a coated chip.

[0076] The in vitro release measurement method is the same as...

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PUM

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Abstract

The invention relates to a controlled release formulation for Captopril, a hypotensive agent, and its preparing process, wherein the retardation release time of the slow release preparation can be as long as 4-6 hours, the effect duration of the preparation can be over 18 hours.

Description

(1) Technical field [0001] The invention relates to a controlled-release preparation of antihypertensive drug captopril and a preparation method thereof. (2) Background technology [0002] Captopril, also known as Captopril, Captopril, and Captopril, is the first generation of orally effective angiotensin-converting enzyme inhibitors (ACEI). Since its publication in 1977, its antihypertensive and therapeutic effects on congestive heart failure have been recognized. Captopril is an angiotensin-converting enzyme inhibitor, which has obvious antihypertensive effects on various types of hypertension, and can improve cardiac function in patients with congestive heart failure. It is clinically applicable to various types of hypertension, especially effective for severe hypertension that is ineffective by conventional therapy. It can also be used for refractory chronic heart failure. [0003] Animal experiments have found that pulmonary vasoconstriction caused by hypoxemia is de...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/401A61K9/22A61P9/12
Inventor 骆快燕郭殿武黄安琪
Owner HANGZHOU MINSHENG PHARM CO LTD
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