Pharmaceutical formulation for use in hiv therapy

a technology for hiv therapy and pharmaceutical formulations, applied in the field of pharmaceutical formulations, can solve the problems of lack of bioavailability, metallic taste, and criticized soft gel formulations, and achieve the effect of reducing the chance of degradation of drug constituents

Inactive Publication Date: 2009-11-12
MATRIX LABORATORIES LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010]It is an object of the invention in its preferred form to provide an economical formulation for administration of at least one anti-retro viral drug.
[0011]It is an object of the invention in its preferred form to provide an economical formulation for administration of a plurality of anti-retro viral drugs in a single formulation.
[0012]It is an object of the invention in its preferred form to provide an economical formulation for administration of a plurality of protease inhibitors in a single formulation.
[0013]It is an object of the invention in its preferred form to provide an economical formulation for administration of Lopinavir and Ritonavir in a single formulation.
[0014]It is another object of the invention to provide a formulation which does not require use of expensive melt extrusion equipment.
[0015]It is another object of the invention to provide a formulation which does not require heating the drug constituents and thereby reduce chances of degradation of the drug constituents.

Problems solved by technology

The active substance Ritonavir [NORVIR soft gelatin capsule] is characterized by low aqueous solubility, a lack of bioavailability when given in the solid state, instability once in solution under ambient conditions and a metallic taste.
This soft gel formulation has been criticized due to stability problems and need for keeping the formulation in refrigerated condition.
The above formulation and related melt extrusion process on account of its requiring expensive extrusion machinery & use of multiple surfactants [N Vinyl pyrrolidone and Sorbitan monolaureate or polyoxyethyleneglycerol oxystearate] may not necessarily result in an economical formulation.
Also, since the disclosed process requires heating the drug constituents to high temperatures [exceeding 100° C.] it may possibly result in degradation of the drug constituents.

Method used

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  • Pharmaceutical formulation for use in hiv therapy
  • Pharmaceutical formulation for use in hiv therapy

Examples

Experimental program
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Effect test

example 1

Wet Granulation Process

[0077]

Ingredient% w / wLopinavir20.0Ritonavir5.0Poloxamer 12412.0Hypromellose (6 cps)58.0Colloidal silicon dioxide3.0Sodium stearyl fumarate2.0Dichloromethaneq.s.

[0078]Manufacturing Steps:[0079]a Lopinavir, Ritonavir and Poloxamer 124 were dissolved in dichloromethane;[0080]b. Colloidal silicon dioxide and hypromellose were sifted through a size 20 mesh;[0081]c. The mixture from step [b] was loaded into a rapid mixer granulator;[0082]d. The drug mixture of step [a] was added to the granulator and processed;[0083]e. The product was dried under vacuum at about 40° C.;[0084]f. The dry product was then milled in a multimill;[0085]g. Sodium lauryl sulfate was mixed with milled product and sifted for about 10 minutes;[0086]h. This sifted product was finally compressed into tablets.

example 2

[0087]

Ingredient% w / wLopinavir20.0Ritonavir5.0Glyceryl mono-oleate4.0Poloxamer 40763.0Colloidal silicon dioxide5.0Sodium stearyl fumarate2.0Talc1.0Methanolq.s.

[0088]Manufacturing Steps:[0089]a. Lopinavir, Ritonavir and glyceryl mono-oleate were dissolved in methanol;[0090]b. Colloidal silicon dioxide and Poloxamer 407 were sifted through a size 20 mesh;[0091]c. The mixture from step [b] was loaded into a rapid mixer granulator;[0092]d. The drug solution of step [a] was added to the granulator and processed;[0093]e. The product was dried under vacuum at about 40° C.;[0094]f. The dry product was then milled in a multimill;[0095]g. Sodium lauryl sulfate and talc was mixed with milled product and sifted for about 10 minutes;[0096]h. This sifted product was finally compressed into tablets.

example 3

[0097]

Ingredient% w / wLopinavir15.0Ritonavir3.75Glyceryl monooleate5.0Poloxamer 40715.0Hypromellose (3 cps)55.25Colloidal silicon dioxide3.0Hydrogenated cottonseed oil2.0Sodium lauryl sulfate1.0Methanolq.s.

[0098]Manufacturing Steps:[0099]a. Lopinavir, Ritonavir and glyceryl monooleate were dissolved in methanol;[0100]b. Colloidal silicon dioxide and hypromellose were sifted through a size 20 mesh;[0101]c. The mixture from step [b] was loaded into a rapid mixer granulator;[0102]d. The drug solution of step [a] was added to the granulator and processed;[0103]e. The product was dried under vacuum at about 45° C.;[0104]f. The dry product was then milled in a multimill;[0105]g. Sodium lauryl sulfate and hydrogenated cottonseed oil was mixed with milled product and sifted for about 10 minutes;[0106]h. This sifted product was finally compressed into tablets.

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Abstract

The invention discloses a formulation prepared by granulating at least one anti-retro viral drug and at least one pharmaceutically acceptable additive, using an organic solvent; milling the product; finally processing the milled product to form tablets or capsules.

Description

FIELD OF INVENTION[0001]The present invention relates to a pharmaceutical formulation and in particular to pharmaceutical formulations for use in HIV therapy. It also discloses the processes to make the same. The invention has been developed primarily for use as a formulation to be used for treatment in HIV therapy and will be described hereinafter with reference to this application. Also disclosed is an improved bottle pack for storing the formulations. However, it will be appreciated that the invention is not limited to this particular field of use.BACKGROUND OF THE INVENTION AND RELATED PRIOR ART[0002]Any discussion of the prior art throughout the specification should in no way be considered as an admission that such prior art is widely known or forms part of the common general knowledge in the field.[0003]There are multiple formulations known for use in HIV treatment therapy. The active substance Ritonavir [NORVIR soft gelatin capsule] is characterized by low aqueous solubility,...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/513A61K31/427B65D39/00
CPCA61K9/2009A61K9/2013A61K9/2027A61K9/2031A61K31/00A61K9/2054A61K2300/00A61P31/18
Inventor VELAVENI, KIRAN KUMAR NARSAIAHVERMA, SANJAY DESHRAJDIXIT, AKHILESH ASHOKDESHMUKH, ABHIJIT MUKUNDSETHI, SANJEEV MEHARCHANDMITRA, SOURAV DILIPKUMAR
Owner MATRIX LABORATORIES LTD
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