MEGGLE Excipients & Technology Direct Compression Expertise

MEGGLE Excipients & Technology are specialists in the lactose-based excipients required to support direct compression (DC) tableting and processing.

MEGGLE offers a wide range of lactose-based compounds that meet all the different requirements for ideal direct compression forms. Its industry-leading comprehensive pharmaceutical excipient portfolio covers solid dosage forms from tablets, capsules, and sachets to powder formulations and dry powder inhalation.

MEGGLE’s direct compression lactose offering extend beyond products, manufacture and supply to technical expertise, process and development consultancy.

Direct Compression challenges

Direct Compression is the most accessible form of tablet production, involving the fewest process stages and quickest production.

Choice of ideal direct compression excipient is defined by a range of factors, including:

• Need for “DC excipients” particle engineered to ensure correct flow and compression characteristic
• Consideration of active ingredient dosage levels (low and high)
• Compatibility with other ingredients with a ‘classic’ direct compression powder mixture usually containing a binder and a lubricant and sometimes a disintegrant and glidant as well

The selection of pharmaceutical excipients for direct compression is more critical than that for granulation in general, or wet granulation in particular. Few traditional excipients combine the functional characteristics, specifically powder flow and compactibility, required for robust direct compression. This makes modifying traditional excipients a necessity.

MEGGLE direct compression excipients

MEGGLE offers a broad range of different lactose-based excipients suitable for direct compression. These products are offered under a range of brand: including Tablettose®, FlowLac®, Cellactose®, MicroceLac®, StarLac®, CombiLac® and RetaLac®, covering three main categories:

• Agglomerated lactose
• Spray-dried lactose
• Co-processed excipients

Direct compression products:

Agglomerated lactose

MEGGLE’s Tablettose® range is manufactured using a continuous spray agglomeration process, where water is used as agglomerating fluid and is sprayed onto fluidized milled lactose particles, creating bonds to form agglomerated lactose.

Tablettose® is purpose-designed for Direct-Compression, combining the flowability of coarse lactose crystals and the high compressibility of milled lactose.

Featuring a broad range of particle size distributions, Tablettose® offers a range of benefits including very good flowability and compactibility, low hygroscopicity, excellent stability, superior blending characteristics and rapid disintegration, it thus supports a wide range of useful applications, including low-dose DC formulations, capsule and sachet filling, effervescent tablets, artificial sweeteners and orally disintegrating tablets.

Spray dried lactose

FlowLac® is produced by spray-drying a fine milled alpha-lactose monohydrate suspension. When lactose is spray-dried, the rapid water evaporation causes amorphous lactose to form. Most commercially available, spray-dried lactose products contain 10 to 15 % amorphous lactose at the time of manufacture, depending on the solids content and process conditions.

Due to the spray-drying process, FlowLac® has a spherical shape, consisting of small alpha-lactose monohydrate crystals bound by amorphous lactose. This provides excellent flow-ability and extraordinary compact-ability compared with other lactose grades.

Other benefits include low hygroscopicity, high stability and fast disintegration times.

The amorphous content and high stability allows achievement of superior DC tableting properties and also supports low to medium dose DC formulations, formulations with poorly flowing APIs, capsule and sachet filling

Co-processed lactose and cellulose

Alpha-lactose monohydrate and cellulose powder are functional excipients used in oral solid dosage forms. Both are naturally derived and well-established for use in the pharmaceutical industry.

In an effort to create synergistic functional performance, such as improved compactability and mixing characteristics, MEGGLE has used co-spray drying to integrate alpha-lactose monohydrate and cellulose powder into a monoparticulate system.

Cellactose® 80 was developed to provide the flow and compaction properties necessary for direct compression tableting, comprising 75 % alpha-lactose monohydrate and 25 % powdered cellulose, both maintaining their individual chemical identities.
While designed for direct compression tableting, Cellactose® 80 can be used in other formulation applications such as dry granulation and capsule filling. In comparison with a corresponding physical blend of the individual components, Cellactose® 80 provides improved compactability, superior flowability, and increased adherence capacity, which reduces segregation tendencies typical of simple powder blends and make it ideal for low-dose formulations.

Alpha-lactose monohydrate and microcrystalline cellulose

MicroceLac® 100 provides the flow and compaction properties desired for direct compression tableting, combining 75 % alpha-lactose monohydrate and 25% microcrystalline cellulose (MCC), both maintaining their individual chemical identities.

To develop synergistic functional performance, such as increased compact-ability and powder flow, alpha-lactose monohydrate and microcrystalline cellulose were co-spray-dried, creating a mono-particulate system having two compaction mechanisms, brittle fracture and plastic deformation, within individual particles.

MicroceLac® 100 is designed for direct compression and may be applied to other formulation development approaches such as dry granulation and capsule filling. In comparison to a physical blend of the individual components, MicroceLac® 100 provides enhanced compaction and superior flowability to improve blending and mitigate API content variability. Superior blending characteristics make MicroceLac® 100 ideal for low-dose formulations where API content uniformity is critical, while excellent compaction properties help increase tablet hardness, making it well-suited for high-dose formulations as well.

Alpha-lactose monohydrate and maize starch

Alpha-lactose monohydrate and maize starch (corn starch) are functional excipients used in oral solid dosage forms. Both are naturally derived and well established in the pharmaceutical industry. Lactose is frequently used as a diluent or direct compression binder. Starch can be used as a binder for wet or dry applications, disintegrant, and diluent.

StarLac® combines 85 % alpha-lactose monohydrate and 15 % native maize starch to provide the compaction and lubricant insensitivity characteristics desired for direct compression, and the hydration properties desired for rapid API release. Additionally, StarLac®’s flowability is superior compared to a physical blend of the individual components in equivalent ratio.

StarLac® is designed for direct compression and may be used in other formulation development approaches. In comparison to a physical blend of the individual components, StarLac® provides superior flow, improved compaction, decreased lubricant sensitivity, and hardness-independent tablet disintegration. Its brittle and plastic deformation characteristics support a range of dry granulation formulations.

StarLac® possesses a narrow particle size distribution (PSD) that supports homogenous powder blend preparation, essential for achieving good tablet quality.

Co-processed hypromellose lactose for direct compression

MEGGLE’s co-processed lactose RetaLac® is the first hypromellose/lactose-based, co-processed excipient specifically designed for DC and dry granulation of modified release formulations.

RetaLac® is a binary composition but monoparticulate in structure, having hypromellose and lactose in each particle. It is characterized by superior functional performance such as improved flow and blend-ability. Additionally, due to its monoparticulate structure, RetaLac® possesses both plastic and brittle fracture deformation characteristics, enhancing compactability in DC compared to traditional wet granulated and physical admixtures of the parent ingredients.

It is particularly useful in supporting the modified release applications that form an important development strategy for the global pharmaceutical industry, particularly in extending the life-cycle of products nearing patent expiration or improving efficacy through more structured active pharmaceutical ingredient (API) release profiles, cost effective product manufacture, and improved patient compliance.

Co-processed lactose, microcrystalline cellulose and starch

MEGGLE’s high-functionality excipient, CombiLac® is specifically designed to ease oral solid dosage form development and manufacture, consisting of 70 % alpha-lactose monohydrate, 20 % microcrystalline cellulose (MCC) and 10 % white, native corn starch, each conforming with Ph.Eur., USP-NF, and JP compendial requirements. These three individual components are integrated into an inseparable monoparticulate structure.

CombiLac® shows improved compaction properties compared to an equivalent admixture of individual ingredients, providing robust tablets with minimal friability. It assures rapid, hardness-independent tablet disintegration for effective API release, and features powder flow characteristics necessary to enhance dosage form weight uniformity and throughput in DC.

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