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Method of treating hypertension

a pulmonary hypertension and hypertension technology, applied in the direction of pharmaceutical delivery mechanism, organic active ingredients, dispersed delivery, etc., can solve the problems of increased pulmonary vascular resistance and pulmonary arterial pressure, right-side heart failure, and associated pah with significant morbidity and mortality

Inactive Publication Date: 2018-12-06
CIPLA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes methods for treating pulmonary hypertension, specifically by using the drug cinitapride or its derivatives. The treatment can help to reduce or eliminate symptoms associated with the condition. The patent also includes compositions containing cinitapride or its derivatives for the treatment of hypertension. The technical effect of the patent is to provide a new treatment option for pulmonary hypertension that can help to improve symptoms in patients with the condition.

Problems solved by technology

Pulmonary arterial hypertension (PAH), one of the five types of pulmonary hypertension (PH), is a life-threatening disease characterized by pulmonary vascular remodeling that leads to increased pulmonary vascular resistance and pulmonary arterial pressure, most often resulting in right-side heart failure.
PAH is associated with significant morbidity and mortality.
In PAH, progressive narrowing of the pulmonary arterial bed results from an imbalance of vasoactive mediators, including prostacyclin, nitric oxide, and endothelin-1.
This leads to an increased right ventricular afterload, right heart failure, and premature death.
The molecular mechanism underlying PAH pathophysiology is not known yet, but it is believed that the endothelial dysfunction results in a decrease in the synthesis of endothelium-derived vasodilators such as nitric oxide and prostacyclin.
Moreover, stimulation of the synthesis of vasoconstrictors such as thromboxane and vascular endothelial growth factor (VEGF) results in a severe vasoconstriction and smooth muscle and adventitial hypertrophy characteristic of patients with PAH.
However, penetrance is low, carriers have a 20% lifetime risk of developing pulmonary hypertension.
Despite a certain success achieved in recent years, many patients with PAH are not adequately managed with existing therapies.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Arterial Hypertension Efficacy Model: Monocrotaline Rat

[0072]The studies were conducted for hemodynamic evaluation of cinitpride in anesthetized sprague dawley rats treated with monocrotaline (“MCT”) to induce pulmonary arterial hypertension. Sildenafil was used as an internal control to compare the effects of cinitapride.

[0073]The effects of cinitapride were evaluated in rats with monocrotaline induced pulmonary arterial hypertension using sildenafil as standard care treatment. Male Sprague-Dawley rats were orally administered vehicle cinitapride (0.3 or 0.9 mg / kg total daily dose, divided into a BID regimen given every day for 28 days starting on Day 1), or sildenafil (30 mg / kg, administered twice daily) (n=10 in each group). Rats received a single injection of monocrotaline (60 mg / kg, s.c.) on Study Day 1. On the twenty-eighth day following monocrotaline dosing, the rats were anesthetized with ketamine / xylazine for terminal monitoring of pulmonary and systemic arterial pressures ...

example 2

or Formulating the Cinitapride Composition According to the Invention

[0099]1. Prepare the binder solution by dissolving Povidone in purified water.[0100]2. Sift Cinitapride, Microcrystalline cellulose, Lactose, Corn Starch and Hypromellose through specified mesh sieve.[0101]3. Load the sifted materials of step 2 in a rapid mixer granulator and dry mix.[0102]4. Granulate the dry mix by using the binder of step 1.[0103]5. Dry and size the granules obtained in step 4.[0104]6. Blend the dried sized granules with presifted Colloidal silicon dioxide and talc followed by lubrication with presifted magnesium stearate in asuitable blender.[0105]7. Compress the lubricated blend into tablets using suitable tooling[0106]8. Prepare the film coating solutioin by dispersing the opadry dry mix in purified water.[0107]9. Coat the compressed tablets obtained in step 7 with the film coating dispersion prepared in step 8.

example 3

tical Composition Prepared Using the Process in Example 2

[0108]

Sr. NoIngredientsQty (mg / tab)1.Cinitapride0.1-50  2.Microcrystalline cellulose75-2003.Lactose75-2004.Povidone4-165.Corn Starch10-45 6.Purified waterQs7.Hypromellose (HPMC K4M / K15 M / K100 M)150-750 8.Colloidal silicon dioxide1-6 9.Talc3-1210.Magnesium Stearate3-1211Ready mix opadry5-1012Purified waterQs

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Abstract

Disclosed herein are compositions and methods for the treatment of pulmonary hypertension, including pulmonary arterial hypertension. The methods include administering to a patient in need thereof an effective amount of cinitapride or derivative thereof. The compositions include an effective amount of cinitapride or derivative thereof, in some instances combined with one or more additional agents for the treatment of pulmonary hypertension.

Description

CROSS REFERENCE TO RELATED APPLICATION[0001]This application claims the benefit of Indian Application IN 201621027225, filed on Aug. 9, 2016, the contents of which are incorporated herein in its entirety.FIELD OF THE INVENTION[0002]The present invention relates to a method of treatment of pulmonary hypertension, including pulmonary arterial hypertension, by administering cinitapride either alone or optionally in combination with one or more other agents. The present invention also pertains to compositions and kits useful for the treatment of pulmonary arterial hypertension in humans containing cinitapride or derivative thereof, alone or in combination with one or more drugs.BACKGROUND[0003]Pulmonary arterial hypertension (PAH), one of the five types of pulmonary hypertension (PH), is a life-threatening disease characterized by pulmonary vascular remodeling that leads to increased pulmonary vascular resistance and pulmonary arterial pressure, most often resulting in right-side heart ...

Claims

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Application Information

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IPC IPC(8): A61K31/4468A61K45/06
CPCA61K45/06A61K2300/00A61K31/4468A61K9/0095A61K47/26A61K47/38A61K47/20A61K9/0019A61K9/2054A61K9/2009A61K9/2013A61K9/2018A61K9/2059A61K9/2027
Inventor MALHOTRA, GEENAJOSHI, KALPANAGHOSALKAR, JEEVAN
Owner CIPLA LTD