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Pharmaceutical preparation containing isosorbide mononitrate

A technology of isosorbide dinitrate and drugs, which is applied in the field of medicine, can solve the problems of not being able to know the types and dosages of excipients of preparation compositions, making it difficult to ensure drug safety for patients, and increasing the metabolic burden of the body, so as to avoid multi-dose drug resistance, Delays the effects of multi-dose resistance, reduction in the amount of metabolized drug

Inactive Publication Date: 2010-06-30
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since its sustained-release mechanism is a gel matrix sustained-release tablet, the drug is released through erosion and diffusion mechanisms, and its drug release rate is greatly affected by environmental factors such as eating, gastrointestinal motility, etc. After individual differences are large, it is difficult to ensure the safety of patients
[0006] Qian Yu (China Pharmaceutical Industry, Volume 16, No. 5, 2007) reported his research on Isosorbide Mononitrate Osmotic Pump Controlled Release Tablets. The dose is 50 mg, and cellulose acetate is used as a semipermeable membrane material. , 4, 6, 8, 10, and 12h in vitro release test results were 16.2%, 40.6%, 57.0%, 70.5%, 79.2%, and 91.5%, but no detailed prescription was given, and its formulation combination was unknown The type and amount of excipients
The disadvantage of this design is that the release is slow with a large dose, which increases the burden on the body's metabolism, resulting in some drug residues in the body when the drug is administered again, which is prone to drug resistance. The biggest problem with the application of isosorbide mononitrate is drug residues. The resulting drug resistance forces patients to interrupt their medication to eliminate the residual drug in the body, and their risk of disease increases greatly during the interruption of medication

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The tablet contains the following ingredients by weight percentage:

[0034] Core composition:

[0035] Isosorbide mononitrate 40g

[0036] L-Amlodipine Besylate 2.5g

[0037] Hypromellose 60g

[0038] Lactose 160g

[0039] 8% polyvinylpyrrolidone K30 ethanol solution

[0040] Magnesium stearate 3g

[0041]

[0042] Prepared into 1000 tablets

[0043] Composition of coating liquid:

[0044] Hypromellose 6cp 4g

[0045] PEG-4000 1g

[0046] Talc 1.5g

[0047] Titanium dioxide 1.5g

[0048] Ethanol / water (60 / 40) 100ml

[0049]

[0050] Coating weight gain 3%

[0051] Using conventional techniques, isosorbide mononitrate and levoamlodipine besylate are made into single-layer sustained-release tablets, and then film-coated.

Embodiment 2

[0053] The tablet contains the following ingredients by weight percentage:

[0054] Core composition:

[0055] Isosorbide mononitrate 40g

[0056] Amlodipine besylate 5g

[0057] Hypromellose 72g

[0058] Lactose 80g

[0059] Mannitol 80g

[0060] 8% polyvinylpyrrolidone K30 ethanol solution

[0061] Magnesium stearate 3g

[0062]

[0063] Prepared into 1000 tablets

[0064] Composition of coating liquid:

[0065] Hypromellose 6cp 4g

[0066] PEG-4000 1g

[0067] Talc 1.8g

[0068] Titanium dioxide 1.8g

[0069] Ethanol / water (70 / 30) 100ml

[0070]

[0071] Coating weight gain 3%

[0072] Using conventional techniques, isosorbide mononitrate and amlodipine besylate are made into single-layer sustained-release tablets, and then film-coated.

Embodiment 3

[0074] The tablet contains the following ingredients by weight percentage:

[0075] Core composition:

[0076] Isosorbide mononitrate 40g

[0077] Amlodipine maleate 10g

[0078] Hypromellose 80g

[0079] Microcrystalline cellulose 130g

[0080] 5% ethyl cellulose absolute ethanol solution

[0081] Magnesium stearate 3g

[0082]

[0083] Prepared into 1000 tablets

[0084] Composition of coating liquid:

[0085] Hypromellose 6cp 4g

[0086] PEG-2000 1g

[0087] Talc 1.5g

[0088] Titanium dioxide 1.5g

[0089] Ethanol / water (60 / 40) 100ml

[0090]

[0091] Coating weight gain 3%

[0092] Using conventional techniques, isosorbide mononitrate and amlodipine maleate are made into single-layer sustained-release tablets, and then film-coated.

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Abstract

The invention provides a pharmaceutical preparation containing isosorbide mononitrate, belonging to the technical field of medicine. The invention provides new sustained release tablets of a medicinal composition for treating hypertension, wherein, the medicinal composition for treating hypertension contains the isosorbide mononitrate, levamlodipine besylate or amlodipine, and the sustained release tablets comprise sustained release single-layered tablets, sustained release double-layered tablets, controlled release single-layered tablets and controlled release double-layered tablets. Compared with the common tablets, the sustained release tablets only need administration once a day, and have durable action, stable curative effect and small toxic or side effect.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to a medicinal preparation containing isosorbide mononitrate and amlodipine or levoamlodipine and a preparation method thereof. Background technique [0002] In people with hypertension, diastolic blood pressure (DBP) is easier to control (≤90mmHg), and systolic blood pressure (SBP) is difficult to control (≤140mmHg). In the traditional treatment of hypertension, the diastolic blood pressure is regarded as an important blood pressure control target. It seems to be incorrect now. The control of systolic blood pressure and pulse pressure is the new goal of hypertension treatment, which is the treatment of hypertension. A new breakthrough in philosophy. However, in the current clinical treatment, there is no ideal drug that has a good effect on systolic blood pressure and pulse pressure. For many hypertensive patients, diastolic blood pressure is often easy to control, while systolic blo...

Claims

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Application Information

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IPC IPC(8): A61K9/30A61K31/4422A61K31/34A61P9/12
Inventor 赵志全董方
Owner LUNAN PHARMA GROUP CORPORATION
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