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<title>Research Triangle Pharmaceuticals - RTP</title>
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<H2>RTP<BR>
Research Triangle Pharmaceuticals</H2>
<ADDRESS>4364 S. Alston Ave. Durham NC 27713<BR>
tel: (919) 361-2277 fax: (919) 361-2290</ADDRESS>
<A NAME="TOC">Table of Contents</A>
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<LI><A HREF="#PROFILE">Company Profile</A></LI>
<LI><A HREF="people.html">People at RTP</A></LI>
<LI><A HREF="#MICRO">MicroCrystal</LI>
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<LI><A HREF="#MICRO1">Technology Profile</A></LI>
<LI><A HREF="#MICRO2">Advantages of MicroCrystals Technology</A></LI>
<LI><A HREF="#MICRO3">MicroCrystal Technology vs. Liposomes</A></LI>
<LI><A HREF="#MICRO4">Oral Availability</A></LI>
<LI><A HREF="#MICRO5">Payload Capacity</A></LI>
<LI><A HREF="#MICRO6">Sustained Release</A></LI>
<LI><A HREF="#MICRO7">Immediate Release</A></LI>
<LI><A HREF="#MICRO8">Toxicity</A></LI>
<LI><A HREF="#MICRO9">Marketing Exclusivity</A></LI>
<LI><A HREF="#MICRO10">Conclusion</A></LI>
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<H3><A NAME="PROFILE">Company Profile</A></H3>
RTP is a technology development company.  The primary business focus of RTP is to acquire, develop, and out-license novel pharmaceutical products and technologies that offer significant medical and health care benefits.  Among other innovations, the <A HREF=""#MICRO"">MicroCrystal(TM)</A> drug delivery system for water-insoluble drugs is RTP's flagship technology.
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<H3><A NAME="MICRO">MicroCrystal</A></H3>
<H4><A NAME="MICRO1">Technology Profile</A></H4>
MicroCrystal(TM) technology consists of encapsulation of a water-insoluble pharmaceutical agent in natural or semi-synthetic phospholipids. The final product is a very fine aqueous suspension of submicron-sized (0.3 to 1.0 micron) phospholipid-coated drug -- MicroCrystals. The components used in MicroCrystal technology are biocompatible and are classified by the U.S. Food and Drug Administration (FDA) as Generally Recognized As Safe. Both liquid and lyophilized dosage forms are available.
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The concept of using phospholipids for drug delivery has intrigued scientists for decades. After years of research, RTP has successfully devised a lipid-based drug delivery system for oral, parenteral, or topical administration of hydrophobic compounds.
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<H4><A NAME="MICRO2">Advantages of MicroCrystal Technology</A></H4>
The MicroCrystal drug delivery system offer many advantages over other drug drug delivery systems. These advantages ranges from payload capacity to marketing exclusivity. RTP is committed to the MicroCrystal drug delivery system.
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<H4><A NAME="MICRO3">MicroCrystal Technology vs. Liposomes</A></H4>
Unlike liposomes, which are primarily meant to entrap water-soluble agents, MicroCrystal formulations are ideal for water-insoluble drugs. 
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<LI>MicroCrystal(TM)</LI>
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<LI>Inner core is hydrophobic</LI>
<LI>Lipid chains point inward</LI>
<LI>High payload</LI>
<LI>Extended shelf life</LI>
<LI>Less expensive to manufacture</LI>
<LI>Not retained by the RES</LI>
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<LI>Liposomes</LI>
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<LI>Inner core is hydrophilic</LI>
<LI>Phosphate groups point inward</LI>
<LI>Relatively low payload capacity</LI>
<LI>Limited shelf life</LI>
<LI>Relatively expensive to manufacture</LI>
<LI>Retained by RES</LI>
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The goal of a drug delivery system is to provide a patient-friendly formulation that is capable of delivering medically relevant amounts of drug. The versatility and reliability of the MicroCrystal technology provide many advantages over formulations that employ organic solvents and detergents to achieve adequate drug payloads.
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<H4><A NAME="MICRO4">Oral Availability</A></H4>
Improvement if oral availability using MicroCrystal technology has been demonstrated in dog and rat models with various drugs that are known to have poor oral availability. For example, MicroCrystal-formulated acyclovir in a cross-over study with sonicated bulk suspensions. In animal models, the bioavailability of acyclovir increased by 76%, and the bioavailablity of cefuroxime increased by 385%.
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<H4><A NAME="MICRO5">Payload Capacity</A></H4>
MicroCrystal technology produces high concentrations (up to 200 mg/mL) of physiologically compatible oral and parenteral formulations. MicroCrystal formulations may be lyophilized for subsequent reconstitution, pressed into tablets, or filled into capsules.
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<H4><A NAME="MICRO6">Sustained Release</A></H4>
Intramuscular and subcutaneous injections of MicroCrystal formulations provide a tissue-compatible, sustained release lasting 12 to 96 hours. The slow release pattern results from encapsulation of the raw drug with phospholipids. Additional advantages of MicrCrystal sustained release include consistent blood levels of drug and high tissue compatibility.
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<H4><A NAME="MICRO7">Immediate Release</A></H4>
MicroCrystal technology delivers immediate release of drug through intravenous dosing. The rapid dilution of MicroCrystals improves the binding process of drug to plasma proteins. 
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<H4><A NAME="MICRO8">Toxicity</A></H4>
Pilot intravenous toxicity sudies in rats show that the dose-dependent toxicity profiles of MicroCrystal formulations are identical to those seen with drugs that are not formulated using MicroCrystal technology. Additionally, in an acute toxicity study in rabbits (Draize Test), MicroCrystal-formulated drugs failed to produce significant irritation. These results indicate that no additional toxic effects are produced by the components of the MicroCrystal formulations.
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<H4><A NAME="MICRO9">Marketing Exclusivity</A></H4>
Through extensive U.S. and internationally issued and pending patents, MicroCrystal techology offers a patentable drug delivery system. For drugs approaching off-patent status, MicroCrystal technology offers a potential patent-extension strategy. MicroCrystal formulations can be commercially manufactured using currently available equipment and excipients.
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<H4><A NAME="MICRO10">Conclusion</A></H4>
Versatility and reliability are essential elements of successful drug delivery systems. The MicroCrystal drug delivery system offers the following advantages:
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<LI>applicable to all dosing routes</LI>
<LI>reduces toxicity of parenteral formulations by eliminating the need for organic solvents or extreme pH</LI>
<LI>improved oral bioavailability offers the opportunity to convert parenteral-only formulations to oral formulations</LI>
<LI>may lower the required oral dose for drugs that are poorly absorbed</LI>
<LI>enables the commercialization of otherwise therapeutically effective drugs whose development has been halted due to difficulties in formulation or lack of appropriate bioavailability</LI>
<LI>the manufacturing process is relatively simple and is readily amenable to commercial scale production</LI>
<LI>extensive patent protection offers a unique product-line extension strategy</LI>
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Call Research Triangle Pharmaceuticals to learn if the MicroCrystal drug delivery system is the solution to your formulation challenge. Additional information is available upon your request.
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Research Triangle Pharmaceuticals
<ADDRESS>4364 S. Alston Ave. Durham NC 27713<BR>
tel: (919) 361-2277 fax: (919) 361-2290</ADDRESS>
WebletMaster David Hopp <EM>dhopp@mail.cato.com</EM>
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