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Solid Pharmaceutical Dosage Formulation

a technology of pharmaceutical dosage and solid dosage, which is applied in the field of pharmaceutical dosage formulations, can solve the problems of reducing the amount of pi in each gelatin capsule, affecting the effect of drug load, and difficult formulation of pi, so as to reduce the burden of pi on hiv patients, increase the drug load in these formulations, and achieve effective therapeutic effects

Inactive Publication Date: 2008-12-04
ABBVIE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The undissolved PI formulation reduces pill burden, eliminates refrigeration needs, and provides consistent therapeutic benefits with reduced adverse events and variability in blood levels, enhancing treatment efficacy and convenience.

Problems solved by technology

PIs are poorly soluble and are very difficult to formulate.
The fill solutions required to dissolve the PI often contain excipients that cause discomfort or irritate the gastrointestinal system.
Furthermore, only a limited amount of the PI can be dissolved in these dosage forms which therefore limits the amount of the PI loaded in each gelatin capsule.
Such treatment regimens are further complicated by the fact that some of the dosage forms (including some PI's) require refrigerated storage conditions to prevent degradation of the active ingredients.
For subjects residing in economically challenged or developing countries where refrigerators are not as common in households, such storage conditions represent a particularly challenging dilemma.
In turn, this can lead to unwanted adverse events in those patients experiencing high blood levels of the drug or rendering the treatment less effective or ineffective in those patients experiencing low blood levels of the drug.
Unfortunately, many patients do not always adhere to this routine due to the complexity of their treatment regimens or otherwise.
Often patients will take the medication on an empty stomach that leads to low bioavailability of the drug, and perhaps ineffective treatment.

Method used

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  • Solid Pharmaceutical Dosage Formulation
  • Solid Pharmaceutical Dosage Formulation
  • Solid Pharmaceutical Dosage Formulation

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0068]

ComponentWeight %Weight %Weight %Ritonavir 18-22.54.174.17Lopinavirin total16.6716.67Copovidone (N-65-75 71.1670.12vinylpyrrolidone / vinylacetate copolymer60:40)Span 20 (Sorbitan4-107.05.02monolaurate)Cremophor RH400-10—3.02(polyoxyethylene-glyceroloxystearate)Colloidal silica0-3 1.01.0

[0069]Copovidone (N-vinyl pyrrolidone / vinyl acetate copolymer 60:40) was mixed with ritonavir (4.17 parts by weight), lopinavir (16.67 parts by weight) and colloidal silica (1.0 part by weight). The powdery mixture was then fed into a twin-screw extruder (screw diameter 18 mm) at a rate of 2.0 kg / h and a melt temperature of 133° C. The clear, fully transparent melt was fed to a calender with two counter-rotating rollers having mutually matching cavities on their surfaces. Tablets of 1080 mg were thus obtained. DSC and WAXS analysis did not reveal any evidence of crystalline drug material in the formulation.

[0070]The bioavailability of the formulation was assessed using beagle dogs (mixed sexes, w...

example 2

[0072]

ComponentWeight %Weight %Ritonavir  18-22.520.8Lopinavir——Copovidone (N-vinyl60-7563.15pyrrolidone / vinyl acetatecopolymer 60:40)Span 20 (Sorbitan 5-15—monolaurate)in totalCremophor RH4010.00(polyoxyethyleneglyceroloxystearate)PEG 60000-85.00Colloidal silica0-31.04

[0073]The above composition is processed by melt extrusion. The resulting extrudate can be used as such or milled and compressed into tablets, preferably by the use of suitable tabletting aids such as sodium stearyl fumarate, colloidal silica, lactose, isomalt, calcium silicate, and magnesium stearate, cellulose or calcium hydrogenphosphate.

example 3

[0074]

ComponentWeight %Ritonavir4.16Lopinavir16.67Copovidone (N-vinyl pyrrolidone / vinyl78.17acetate copolymer 60:40)Colloidal silica1.0

[0075]Copovidone (N-vinyl pyrrolidone / vinyl acetate copolymer 60:40; 78.17 parts by weight) was mixed with ritonavir (4.16 parts by weight), lopinavir (16.67 parts by weight) and colloidal silica (1.0 part by weight). The powdery mixture was then fed into a twin-screw extruder (screw diameter 18 mm) at a rate of 2.0 kg / h and a melt temperature of 133° C. The clear, fully transparent melt was fed to a calender with two counter-rotating rollers having mutually matching cavities on their surfaces. Tablets of 1080 mg were thus obtained. DSC and WAXS analysis did not reveal any evidence of crystalline drug material in the formulation.

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Abstract

The present invention provides a pharmaceutical dosage formulation, and more particularly, a pharmaceutical dosage formulation comprising an HIV protease inhibitor.

Description

[0001]This application is a continuation of U.S. patent application Ser. No. 11 / 064,467 filed on Feb. 23, 2005, which is incorporated herein by reference in its entirety. This application is also a continuation-in-part of U.S. patent application Ser. No. 10 / 925,442 filed on Aug. 25, 2004, which claims priority to U.S. Provisional Patent Application Ser. No. 60 / 498,412 filed on Aug. 28, 2003.FIELD OF THE INVENTION[0002]The present invention relates to a pharmaceutical dosage formulation, and more particularly, relates to a pharmaceutical dosage formulation comprising an HIV protease inhibitor.BACKGROUND OF THE INVENTION[0003]Millions of people around the world are suffering from HIV / AIDS, and millions more are likely to become infected each year. Many medications are currently available for the treatment of HIV / AIDS including HTV protease inhibitors (PIs), nucleoside / nucleotide reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs). Most...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/00A61K31/513A61K31/427A61K9/16A61K9/20
CPCA61K9/1617A61K9/1635A61K47/32A61K9/1694A61K9/2009A61K9/2013A61K9/2018A61K9/2027A61K9/2031A61K9/204A61K9/2077A61K9/2095A61K9/2866A61K31/00A61K31/426A61K31/427A61K31/513A61K2300/00A61P31/18A61K9/28
Inventor ROSENBERG, JOERGREINHOLD, ULRICHLIEPOLD, BERNDBERNDL, GUNTHERBREITENBACH, JORGALANI, LAMAN L.GHOSH, SOUMOJEET
Owner ABBVIE INC